Title of Invention	NOVEL, ARYLSULFONAMIDE COMPOUNDS FOR THE TREATMENT OF OBESITY, TYPE II DIABETES AND CNS-DISORDERS
Abstract	The present invention relates to substituted bis-arylsulfonarnide and arylsulfonarnide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

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NOVEL, ARYLSULFONAMIDE COMPOUNDS FOR THE TREATMENT OF OBESITY, TYPE II DIABETES AND CNS-DISORDERS RELATED APPLICATIONS This application claims priority to Swedish application number 0101660-9, filed on May 11, 2001, U.S. provisional application number 60/294,102, filed on May 29, 2001, and U.S. provisional application number 60/294,132, filed on May 29, 2001, the contents of which are incorporated herein by reference. TECHNICAL FIELD The present invention relates to substituted bis-ai7lsulfonamide and arylsulfonamide compounds, to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the cential nei-vous system. BACKGROUND ART Obesity is a condition characterized by an increase in body fat content resulting in excess body weight above accepted norms. Obesity is the most important nutritional disorder in the western world and represents a major health problem in all industrialized countries. This disorder leads to increased mortality due to increased incidences of diseases such as cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes. Searching for compounds, which reduce body weight has been going on for many decades. One line of research has been activation of serotonergic systems, either by direct activation of serotonin receptor subtjpes or by inhibiting serotonin reuptake. The exact receptor subt>pc profile required is however not known. Serotonin (5-hydrox>tr>ptamine or 5-HT), a key transmitter of the peripheral and central nervous system, modulates a wide range of physiological and pathological functions, including anxiet}', sleep regulation* aggression, feeding and depression. Multiple serotonin receptor subt>pc5 have been identified and cloned. One of these, the S-HT^ receptor, was cloned by several groups in 1993 (Ruat, M. et al. (1993) Biochem. Biophys. Res. Comniun.193: 268-276; Sebben, M. et al. (1994) NeuroReport 5: 2553-2557). This receptor is positively coupled to adenylyl cyclase and displays affinity for antidepressants such as clozapine. Recently, the effect of 5-HT5 antagonist and 5-HT6 antisense oligonucleotides to reduce food intake in rats has been reported (Bentley, J.C, et al. (1999) Br J Pharmac. Suppl. 126, P66; Bentley, J.C. et al. (1997) J. Psychophamiacol. Suppl. A64, 255). Compounds with enhanced affinity and selectivity for the S-HT^ receptor have been identified, e.g. in WO 00/34242 and by Isaac, M. et al. (2000) 6'Bicyclopiperazinyl-l-aiylsulfonylindoles and 6-Bicyclopiperidinyl-l-aiylsulfonylwdoles derivatives as novel, potent and selective 5-HTe receptor antagonists. Bioorganic & Medicinal Chemistry Letters 10: 1719-1721. DISCLOSURE OF THE INVENTION It has surprisingly been found that the compounds of formula (I) and (II) show affinity for the S-HT^ receptor as antagonists at a low nanomolar range. Compounds according to the invention and their pharmaceutically acceptable salts have 5-HT6 receptor antagonist activity and are believed to be of potential use in the tieatment or prophylaxis o] obesity and type II diabetes, as well as in the treatment or prophylaxis of disorders of the central nervous system such as an?liety, depression, panic attacks, memory disorders, sleep disorders, binge disorders, migiaine, anorexia, bulimia, obsessive compulsive disorders, psychoses, Alzheimer's disMSg, Parlcinson's disease, Huntington's chorea and/or schizophrenia, drug abuse, Attention Deficit Hyperactive Disorders (ADHD). Defmitions Unless othcn^'ise stated or indicated, the following definitions shall apply throughoi the specification and the appended claims: The term "Cj.^ alkyF' denotes a straight or branched alkyl group having from 1 to 6 carbon atoms. Examples of said lower alkyl include methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec-butyl, t-butyl and stiaight- and branched-chain pentyl and hexyl. The temi "C1.5 alkoxy" denotes a straight or branched alkoxy group having from 1 to 6 carbon atoms. Examples of said lower alkoxy include methoxy, ethoxy, n-propoxy, iso-propoxy, n-butoxy, iso-butoxy, sec-butoxy, t-butoxy and straight- and branched-chain pentoxy and hexoxy. The term "halogen" shall mean fluorine, chlorine, bromine or iodine. The terms "C4.6 cycloalkyl" and "C3.7 cycloalkyl" denote a cyclic alkyl group having a ring size from C4 to Q or from C3 to C7, respectively. Examples of said cycloalkyl include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, methylcyclohexyl and cycloheptyl. Compounds of Formula I In a first aspect, this invention provides a compound of the general formula (I) R* and R3 are independently (a)H (b)C1-6alkyl, (c)C1-6alkoxy, (d) straight or branched C1-6 hydroxyalkyi, (e) sti'aight or branched C1-6 alkylhalides; or (f) a group Ar; AT is (a) phenyl, (b) 1-naphthyl, (c) 2-naphthyI, (d) benzyl, (e) cinnamoyl, (f) a 5 to 7-membered, partially or completely saturated, heterocyclic ring containing 1 to 4 heteroatoms, selected from oxygen, nitrogen and sulfur, or (g) a bicyclic ring system consisting of two heterocyclic rings as defined under (Q, or a bicyclic ring system consisting of one benzene ring and one heterocyclic ring as defined under (f); alternatively, R* and R3 are linked to form a gioup (CH2)20, (CH2)40, or (CH2)3.5 in formula (lb); optionally, the group Ar is substituted with (a) y, or (b) a 5 to 7-membered, partially or completely saturated, heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; Yis (a)H. (b) halogen. (c) C1-6 alkyl. (d) CF3, (e) hydroxy, (f) C1-6alkoxy, (g)Ci.4alkeny]; (h) phenyl; (i) phenoxy, g) benzyloxy, (k) benzoyl, (I) OCF3, (m) CN, (n) straight or branched C|.6 hydroxyalkyl, (0) straight or branched Ci-g alkylhalides, (p) NHa, (q) NHR*. (r) NR'^R3 (s) NO2, (t) -CONR'^R'. (u) NHSO2R*, (v) NR'*C0R(x) S02NR'^R(Z)-C(=0)R', (k) -C02R3 or (l) S(0)nR*; wherein n is 0,1, 2 or 3; R3 and R** are independently: (a)-S02R', (b)H. (c) C1-6alkyl, (d)C1-C3alkcnyl, (e)C1-C3alk)lar>'l, (f) Ar as defined above for R3 (g)-C(=0)R3 (h) -C(0)NR*R3 (i) -C(S)NR3R', (j) -CO2R'; (k) -C(S)R3 (1) stiaight or branched C1.6 hydroxyalkyl, or (m) straight or branched C\.6 alkylhalides; alternatively, R and R are linked to fonn a group (CH2)20, (CH2)40, or (CH2)3.5 in formula (la); R3 is selected from the group consisting of the following chemical groups: R3 and R3 are independently (a)H. (b)Ci-6aikyl, (c) C3.7 cycloalkyl, or (d) Ar, as defined above in R*; alternatively, R3 and R3 arc linked to form a group (CH2)20, (CH2)40 or (CH2)3.5; (a) H, or (b) C1-6alkyl. i Preferred compounds of the general formula (I) are those wherein: Xis Sin N-R' R—N , °~S . (la) (lb) R'is (e) a group Ar; or (0 C1-6 alkyl Aris (a) phenyl, (b) I-naphthyl, (c) 2-naphthyl, or (f) a 5 to 7-membered, partially or completely saturated, heterocyclic ring containing 1 to 4 heteroatoms, selected from oxygen, nitrogen and sulfur; the group Ar is substituted with Y, wherein Y is (a) H. (b) halogen, (c) C1-6alkyl, (d) CF,, (OCualkoxy, (g)C1-4alkenyl; (h) phenyl; (I) OCF3, or (n) straight or branched d-e hydroxyalkyl; R' and R' are indipendently (a)H (b) CI-3 alkyl, in particular methyl or ethyl (c) -S02R3 or (d) are linked to form a gioup (CH2)40 R3 is selected from the group consisting of the following chemical groups: wherein R is (a) H, or (b) C\s alkyl, in particular methyl. R6 and R3 are independently (a) H. (b) C1-6alkyl, (c) C3.7 cycIoaIk>I, or (d)Ar. N-[2-[ethyI(phenylsulfonyl)amino]"4-(4-methyI-I-piperazinyl)phenyl]benzenesulfonamide hydrochloride 3-fluoro-N-[2-{[(3-f]uorophenyl)sulfonyl]ainino}-4-(4-methyl-l- piperazinyl)phenyl]benzenesulfonamide hydrochloride Is}.|4-(4-niethyl-l-piperazinyl)-2-[(S-quinolinylsulfonyl)amino]phenyl}-S- quinolinesulfonamide hydrochloride hydrochloride 4-methyl-N- {4-(4-methyl-1 -piperazinyl)-2-[(methylsulfonyl)aniino]phenyl}benzenesulfonamide hydrochloride N-(4-(l-piperazinyl)-2-[(phenylsulfonyl)amino]phenyl)-l-naphthalenesulfonamide hydrochloride N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyI)phenyl]-8-quinolinesulfonamide hydrochloride 2-methyl-N-[2-[(phenylsulfonyl)amino]-4-(]-piperazinyl)phenyl]benzenesulfonamide hydrochloride 4-butoxy-N-[2-[(phenylsulfonyl)amino]-4-(l-piperaziny])phenyl]benzenesulfonamide hydrochloride 5-fluoro-2-methyl-N-[2-[(phenylsulfonyi)amino]-4-(l- piperazinyl)phenyl]benzenesulfonamide hydrochloride 2-methoxy-4-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l- piperazinyl)phenyl]benzenesulfonamide hydrochloride N-{4-(l,4-diazepan-I-yI)-2-[(phenylsulfonyI)amino]phenyl}benzenesulfonamide hydrochloride N-{5-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]phenyl}-N-eihylbenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-I-yl)-2-[(phenylsulfonyl)arnino]phenyl}-2-naphthalenesulfonamide hydrochloride N-{4-(l,4-dia2epan-I-yl)-2-[methyl(phenylsulfonyl)amino]phenyl}benzenesulfonamide hydrochloride N-{4-(l,4-diazcpan-l-yl)-2-[(methylsulfonyl)amino]phenyl}-l-naphthalcnesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl>2-[(meihylsulfonyl)amino]phcnyl}-2-naphthaleriesulforuirnide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[methyl(methylsulfonyl)amino]phenyl} -1 -naphthalenesul fonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfony])amino]phenyl}-8-quinolinesu]fonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(phenylsulfonyl)amino]phenyl} -2,4,6- triniethylbenzenesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(phenylsulfonyl)amino]phenyl} -4-methylbenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]phenyl}-2-methylbenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]pheny]}-5-fluoro-2-methylbenzenesulfonamide hydrochloride N- {5-( 1,4-diazepan-1 -yl)-2-[methyl(phenylsulfonyl)amino]phenyl} -4-methylbenzenesulfonamide hydrochloride 3-amino-4-(l,4-diazepan-l-yl)-N-(2-methoxyphenyl)benzenesulfonamide hydrochloride 3-amino-N-(3-chlorophenyl)-4-(l ,4-diazepan-1 -yDbenzenesulfonamide hydrochloride 3-aniino-N-(2-chlorophenyl)-4-(l,4-diazepan-l-yl)benzenesulfonamide hydrochloride 3-amino-4-(4-methyl-l ,4-diazepan-l-yl)-N-phenylbenzenesulfonamide hydrochloride 3-amino-N-(2-methoxyphenyl)-4-(l-piperazinyl)benzenesulfonamide hydrochloride 2-[ 1,4]Diazepan-1 -yl-5-(3,4-dihydro-1 H-isoquinoline-2-siilfonyl)-aniline dihydrochloride hydrochloride 3-Amino-2-chloro-N-naphthalen-I-yl-4-piperazin-l-yl-benzenesulfonamide, hydrochloride hydrochloride Compounds of the Formula II In a further aspect, the invention provides a compound having the general fonrula (II) or a pharmaceutically acceptable salt thereof, wherein R', R'-and R" are H; or two of R', R'^ and R'" are H; and the remaining of R3 R'^ and R'* is (a) -NHz. (b) -NHR6, (C)-NRV, (d) -N(CO)R3 (e) -N(CS)R3 or (0 -NO2; R'° and R" is a group R3 or R' as defined for Formula I; (a) homopiperazine, (b) melhylhomopipcrazine or (c) a group R3as defined for Formula I, wherein R3 is as defined for Formula I; Y is as defined for Formula I. Prcfcncd compounds of the general formula (II) arc those wherein: Depending on the process conditions the end products of the Formula I are obtained either in neutral or salt form. Both the free base and the salts of these end products are within the scope of the indention. Acid addition salts of the new compounds may in a manner kno^ii perse be transformed into the free base using basic agents such as alkali or by ion exchange. The free base obtained may also form salts with organic or inorganic acids. In the preparation of acid addition salts, preferably such acids are used which form suitably therapeutically acceptable salts. Examples of such acids are hydrohalogen acids, sulfuric acid, phosphoric acid, nitric acid, aliphatic, alicyclic, aromatic or heterocyclic carboxyl or sulfonic acids, such as fonnic acid, acetic acid, propionic acid, succinic acid, glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, ascorbic acid, maleic acid, hydroxjTiialeic acid, pyruvic acid, p-hydroxybensoic acid, embonic acid, methanesulfoinc acid, ethanesulfonic acid, hydroxyethanesulfonic acid, halogenbensenesulfonic acid, loluenesulfonic acid, mandelic acid or naphthalenesulfonic acid. Throughout the specification and the appended claims, a given chemical formula or name shall encompass all stereo and optical isomers and racemates thereof where such isomers exist. All diasiereomeric forms possible (pure enantiomers, tautomers, racemic mixtures and unequal mixtures of two enantiomers) are within the scope of the invention. Such compounds can also occur as cis- or trans-, £"- or Z- double bond isomer forms. All isomeric foiTns are contemplated. Pharntaceutical formulations Phannaceutical fonnulations are usually prepared by mixing the active substance, or a pharmaceutically acceptable salt thereof, with conventional pharmaceutical excipients. The formulations can be further prepared by known methods such as granulation, compression, microencapsulation, spray coating, ^ic, Tliis invention relates to a method of treating obesity or type 11 diabetes. The method includes administering to a mammal subject (e.g., human) in need thereof an effective amount of one or more compounds of the fonnula (I) or the formula (II) above. Also winthin the scope of this invention is a method for modulating (e.g., inhibiting) 5-HT6 receptor activity. The method includes administering to a mammal in need thereof an eflectivc amount of a compound of the formula (I) or the formula (II) above. "An effective amount" refers to an amount of a compound which confers a therapeutic effect on the treated subject. The therapeutic effect may be objective (i.e., measurable by some test or marker) or subjective (i.e., subject gives an indication of or feels an effect). For clinical use, the compounds of the invention are formulated into pharmaceutical formulations for oral, rectal, parenteral or other mode of administration. Usually the amount of active compounds is between 0.1-95% by weight of the preparation, preferably between 0.2-20% by weight in preparations for parenteral use and preferably between 1 and 50% by weight in preparations for oral administration. The typical daily dose of the active substance varies within a wide range and will depend on various factors such as for example the individual requirement of each patient and the route of administration. In general, oral and parenteral dosages will be in the range of 5 to 1000 mg per day of active substance, preferably 50 to 150 mg per day. The specific examples below are to be construed as merely illustrative, and not limitative of the remainder of the disclosure in any way whatsoever. Without further elaboration, it is believed that one skilled in the art can, based on the description herein, utilize the present invention to its fullest extent. All publications cited herein are hereby incorporated by reference in their entirety. EXAMPLES In the following examples, the stincture of the prepared compounds were confirmed by standard spectroscopic methods and elemental analysis and/or high resolution MS. The NMR data were obtained on a JEOL JNM-EX 270, a Bruker 400 DPX or a Bruker DRX 500 spectrometer. IR spectra were obtained on a Perkin Elmer SPECTRUM 1000 FT-IR spectrometer. High resolution MS were obtained on a Micromass LCT spectrometer. Elemental analysis was pcrtbrmed by Mikro Kemi AB Uppsala Sweden. Melting points, when given, were obtained on a Buchi or a Gallenkamp melting point apparatus and are uncorrected. Synthesis according to Scheme 1, Method 2 (R = Boc) INTERMEDIATE 1 SjTithesis of N-EthyI-5-fluoro-2-nitroaniIine. A suspension of 2,4-difluoro-l-nitrobenzene (0.50 g, 0.003 mmol), ethylamine hydrochloride (0.49 g, 0.006 mmol), K:C03 (1.66 g, 0.012 mmol) in acetonitrile (30 mL) was stined at room temperature for 16 hours and then filtered. The filtrate was concentrated and dissolved in small amount of CHCI3 Purification by column chromatography on silica using pentane/diethyl ether 95:5 as eluent gave 0.45 g of a yellow solid. 'H NMR (CDCI3) 6 S.23-8.18 (m, IH). 8.08 (br s, IH), 6.49-6.45 (m, IH), 6.38-6.32 (m, IH), 3.34-3.27 (m, 2H), 1.38 (tr, J = 7.22 Hz, 3H); '^CNMR (CDCI3) 5 167.55 (d, JCF= 255.6 Hz), 147.4 (d, JCF= 12.9 Hz), 129.91 (d, JcF= 12.9 Hz), 128.71 (br s), 103.73 (d, JCF= 24.8 Hz), 99.14 (d, JCF= 27.6 Hz), 37.88, 14.05; MS (posESI) m/z = found 184.0653, calc 184.064S. Anal. (C,2H,jN402) C,H,N. INTERMADIATE 2 Synthesis of N-Ethyl-2-nitro-5-(l-piperazinyl)aniline. A suspension of N-etliyl-5-fluoro-2-nitroaniline (1.5 g, 8.12 mmol), piperazine (0.979 g, 11.37 mmol), K2CO3 (3.36 g, 24.3 mmol) in DMF (40 mL) was heated in a microwave oven for 1 min at 100 W. The reaction mixture was allowed to cool and then heated for another minute at lOOw. This procedure was repeated 5 times. The suspension was filtered and then concentrated. The crude oil was purified via flash chromatogiaphy on silica using CHCh/MeOH/NHj 9:1.0.4% as eluent to give 1.53 g (75%) of a yellow solid. 'H NMR (CDCI3) 6 8.30 (br s, 1H), 8.0S-8.04 (m, IH), 6.25-6.20 (m. IH), 5.88-5.86 (m, 1H),3.39-3.28 (m, 6H), 3.03-2.97 (m. 4H), 1.37 (tr, J=7.2 Hz, 3H); "C NMR INTERMEDUTE 3 Synthesis of tert-Butyl 4-(3-(ethylamino)-4-nitrophenyl]-l-piperazinecarboxylate, To a solution ofN-ethyl-2-nitro-5-(l-piperazinyl)aniline (1.020 g, 4.075 mmol), and NaOH (0.39 g, 2.45 mmol) in THF:H20 (64 mL, 1:1) was added a solution of di-tertbutyl-dicarbonate (2.67 g, 12.2 mmol) in 5 mL THF. The solution was stined at room temperature for 16 hours. The mixture was neutralized with 1 N HCl. The volatiles were removed under vacuum to yield 1.4 g of crude material (98%). *H NMR (CDCI3) 6 8.28 (brs, IH), 8.13-8.09 (m, IH), 6.27-6.22 (m, IH), 6.05-6.02 (m, IH), 3.67-3.61 (m, 4H), 3.45-3.3S (m, 4H), 3.35-3.27 (m, 2H), 1.50 (s, 9H); MS (posESI) m/z = found 350.1951, calc 350.1954. INTERMEDIATE 4 Synthesis of tert-Butyl 4-(4-amino^3-(ethylamino)pbenyl]-l-piperazinecarboxylate. To a solution of teit-butyl 4-[3-(ethylamino)-4-nitrophenyl]-l-piperazinecarboxylate (1.028 g, 2.93 mmol) in 40 mL EtOH:THF (4:1) solvent system was added Raney-Ni (1 mL of a EtOH suspension) followed by addition hydrazine hydrate (0.734 g, 14.67 mmol). The mixture was stirred vigorously for 3 houi-s and then filtered through a Celite pad pR3treated with water. The filtrate was concentrated and then purified by column chromatography on silica using CHCb/MeOH/NHs 9:1:0.4% as eluent to give 0.877 g (93%) of a red oil. The oil was used immediately in the next reaction. HPLC purity >90 %; MS (posEI) m/z = 320 (M^; Method 1, Scheme 1: General for sulfonylation (Rl = Me) INTERMEDIATE 5 Synthesis of N-ethyl-5-(4-methyM-piperazinyl)-2-nitroaniline (Method L Scheme 1) N-cthyl-5*(4-methyl-l-piperazinyl)-2-nitroaniline was prepared from 2,4-difluoro-l-nitrobcnzcnc and methylpiperazine using the same method described for N-cthyl-2-nitro-5-(l-pipcrazinyl)aniline and was obtained as yellow solid (99 %). 'H NMR (CEKTb) 6 8.30 (br s, IH). 8.08-8.04 (m. IH), 6.25-6.20(m, IH), 5.89-5.86(m. IH), 3.45-3.39 (m.4H), 3.35-3.25 (m, 2H), 2.56-2.50 (m. 4H), 2.35 (s, 3H), 1.37 (tr. J=7.2 Hz, 3)); "C NMR 6 (CDCI3) 155.92, 147.72, 128.99, 124.19, 104.30, 94.37, 54.78,47.05, 46.25, 37.73, 14.43; MS (posESI) m/z = found 264.1575, calc 264.1586. Anal. (C13H20N4O2.O.5 H2O) C, H, O. INTERMEDIATE 6 Synthesis of N-2-EthyM-(4-methyI-l-piperazinyI)-l,2-ben2enediamin€ (Method 1, Scheme 1) N-EthyI-5-(4-methyI-l-piperazinyl)-2-nitroaniline was reduced with Raney-Ni as described previously for the synthesis of tert-butyl 4-[4-amino-3-(ethylamino)phenyl]-l-piperazinecarboxylate to give N-2-ethyl-4-(4-methyl-l-piperazinyl)"l,2-bcnzenediamine (yield >90%) as a red oil. The product is very sensitive to oxidation and was therefore used immediately in the next reaction step. HPLC purity >90 %; MS (posEI) m/z = 234 (M""); EXAMPLE 1 N-(2-{Ethyl((3-fluorophenyl)sulfonyl]amino}-4-(4-metbyl-l-piperaziuyl)phenylj-3-fluorobenzenesulfonamide hydrochloride (Method 1, Scheme 1) To a solution of amine N-2-ethyl-4-(4-methyl-l-piperazinyl)-l,2-benzenediamine (0.200 g, O.S53 mmol) and pyridine (0.48 mL. 5.97 mmol) in CH2CI: (S mL) was added a solution of 3-fluorobenzenesuIfonyl chloride (249 mg, 1.28 mmol) in CH2CI2 (2 mL). The mixture was stirred at room temperature for 16 hours. CH2CI2 (10 mL) was added and the mixture was washed with saturated aqueous NaHCOj, The organic layer was dried over Na2S04, filtered and concentrated. Purification by column chromatography (AI2O3, ElOAc/MeOH 9.5:0.5) gave two products. The first fraction contained 110 mg of N-[2-{ethyl[(3-fluorophenyl)sulfonyI]amino} -4-(4-methyl-1 -piperazinyl)phenyI]-3-fluorobenzencsulfonamide hydrochloride. The second fraction contained 100 mg of N-[2-(cihylamino)-4-(4-methyl-l-piperazinyl)phenyl]-3-fluorobenzenesulfonamide hydrochloride. Both products were converted to the HCI-salts. N-[2-{cthyl[(3-fluorophcnyl)sulfonyl]amino}-4-(4-mcthyl-I-pipcrazinyl)phenyl]-3-nuorobcnzcnesulfonamidc hydrochloride: 'H NMR (DMS0-5) 5 IL14 (br s, IH), 927 (s, IH), 7,75-7.35 (m, 8H). 7.1S-7.I5 Sm, IH), 6.95-6.90 (m, IH), 6.07-6.04 (m, IH). 3.47-3.30 (m, 4H), 3.05-2.85 (m, 4H), 2.73 8d, J=4.7 Hz), 0.72 (tr, J=7.2Hz); '^C NMR (CU3UU) 5 162.65 (d, JcF=5.5 Hz), 160.68 (d, JCF=4.6 HZ), 146.61, 142.52 (d, JCF=7.4 HZ), 139.04 (d, JcF=6.4Hz), 131.58(131.63, 131.28, 128.67, 124.25, 123.14, 122.89, 120.56 (d, JCF=21 HZ), 120.05 (d,JcF=21 HZ), 116.52, 115.64,114.80 (d, JCF=25HZ), 113.97 (d, JCF=25 HZ), 51.8S, 45.82, 44.84, 41.79, 12.31; Ms (posES-FIA) m/z = 551 (M+H) EXAMPLE 2 N-(2-lethyl(phenyisulfonyl)ainino)-4-(4-methji-l-piperazinyl)phenyl]-benzenesulfonaniide hydrochloride (Scheme 1, Method 1) N-[2-[ethyl(phenylsulfonyl)aniino]-4-(4-methyl-l-piperazinyl)phenyI] benzenesulfonamide hydrochloride was prepared as described in Scheme 1. Sulfonylation from N-2-ethyl-4-(4-melhyl-l-piperazinyl)-l,2-benzenediamine and phenylsulfonyl chloride was perfonned as described in Method 1. Purification by chromatography (Si02, chloroform:methanol:NH3 9:1:0.4%) followed by trituration with MeOH gave 68 mg (15% yield) of the free base which was converted to its HCl-salt. MS (posES-FIA) m/z = found: 514.1700, calc: 514.1708; Anal. (C25H30N4O4S2.2HCI) C, H, N. EXAMPLE 3 3-Fluoro-N-(2-{((3-nuorophenyI)sulfonyljamino}-4-(4-methyI-l-piperaz]oyl)phenyl]benzenesulfonamide hydrochloride (Scheme 3) Synthesis of 2-AminO'5-(4-methyl'l'piperazinyl)aniline. A mixture of 2-nitro-3-chloroaniline (4.47g, 25.9 mmol), methylpiperazine (3.1 g, 31 mmol) and K2CO3 (5.4Ig, 39 mmol) in acetonitrile was stirred at 70 °C for 48 h. The mixture was filtered and purified by column chromatography (SiOz, CH2Cl2/MeOH/Hepiane/NH3 4:1:5 x 0.2 %) to give 1.6 g of product (unreacted starting material was isolated): 'H-NMR 6 7.66-7.45 (m, 5H), 6.78 (d, IH), 6.62 (d, JH), 6.50 (dd, IH), 3.39-3.35 (m, 4H), 3.02-2.99 (m. 4H); MS (posES-FiA) m/z 333.0 (M* + H). The product (1.06 g, 4.49 mmol) was dissolved in EtOH:THF (4:1). Rancy-Ni and hydrazine (1.12 mL, 22 mmol) were added. The reaction was stirred at room temperature for 3 h until the yellow color disappeared. Filtration through wet Cdite pad, folJowcd by removal of the solvent afforded 0.802 g of 2-amino-5-(4'mcthyM- piperazinyl)aniline which was used without further purification in the next step. 3-Fluorobenzenesulfonyl chloride (0.133 g, 0.68 mmol) was added to a solution of 2-amino-5-(4-methyl-l-piperazinyI)aniIine (O.I4]g, 0.68 mmol) and pyridine (514 mL, 6.39 mmol) in CH2CI2. After 1 h the mixture was washed with aq NaHCOs (10 %), dried (MgS04) and the solvent was removed. Purification by chromatography (Si02, CHaCh/methanoI/heptane, 4; 1:5) gave 3-fluoro-N-[2-amino-4-(4-methyl-1 -piperazinyl)-phenyl]benzenesulfonamide (0.140 g, 57 %). MS (posES-FIA) m/z = found: 365.2, calcd: 364.14; Anal. (C17H22CIFN4O2S 3H:0) C, H, N, S. The reaction produced a small amount of bis-sulfonylated compound 3-fluoro-N-[2-{[(3-fluorophenyl)sulfonyl]amino}-4-(4-methyl-l-piperazinyl)-phenyl]benzenesulfonamide (0.010 g, 3 %). The products were tiansformed into their HCl-salt before analysis; MS (posES-FIA) m/z = found. 523.5, calcd: 522.12. Anal, (C23H25CIF2N4O4S2) C, H, N, S. EXAMPLE 4 rsf,|4«(4.inethyl-l-piperazinyl)-2-|(8-quinolinylsulfonyl)aminolpheny|}-8-quinoiinesulfonamide bydrocbioride (Scheme 3) 8-Quinolinesulfonyl chloride (0.185 g, O.SI mmol) was added to a solution of 2-amino-5-(4-methyJ-l-pipera2inyl)aniline (0.16S g, 0.81 mmol) and pyridine (514 mL, 6.39 mmol) in CH2CI2. After 1 h at room temperature the mixture was washed with aq NaHCOj (10 %), dried (MgSO^) and the solvent was removed. Purification by chromatography (Si02, CH2Cl2/MeOH/heptane, 4:1:5) gave N-2-amino-4-(4-methyM-piperazinyl)-]-phenyl-8" quinolinesulfonamide (0.110 g, 35 %). MS (posES-FIA) m/z = found: 384.2, calcd 383.48; %); Anal. (C,9H22CIN502S 3H2O) C, H, N, S and a small amount of the bis-sulfonylated N-{4-(4-methyl-l-piperazinyl)-2-[(S-quinolinylsulfonj'l)amino]phenyl}-8-quinolinesulfonamide (0.070 g, 15 %). The product was converted to HCl salt before analysis; MS (posES-FIA) ni/= « found: 589.6, calcd: 588.16; Anal. (CwH:i,ClN^04S:2H2O) C, H, N. Synthesis according to Scheme 2 Scheme 2, Method 3: General Rl - Me INTERMEDIATE 7 Synthesis of N-(5-fluoro-2-nitrophenyl)benzenesulfonainide (Scheme 2, Method 3) Benzenesulfonamide (3.14 g, 20 mmol) was dissolved in DMF (100 niL) and NaH (60% in oil, 40 mmol, 1.60 g) was added. The reaction was stin'cd until the gas evolution ceased. 2,4-Difluoronitrobenzene (18 mmol, 2.9 g, 2 mL) was added and the reaction mixture was stirred over night at 35°C. The reaction mixture was poured into HCl (IM aq, 100 mL) and extracted with toluene (25 mL x 5). The organic phase was dried (MgS04) and concentrated and re-crystallized from EtOH to give a first crop of 3.75 g of a yellow solid. A second crop of 0.20 g was collected from the EtOH remains. Yield 3.95 g, 13.3 mmol (74%). MS (posES-FL\) m/z = found: 296; Calc: 296,0. INTERMEDL^TE 8 Synthesis of N-(5-(4-methyI-l-piperazinyF)-2-n!irophenyIIben2enesuIfonamide (Scheme 2, Method 3) N-(5-fluoro-2-nitrophenyl)benzenesulfonamide (2 x 0.50 g, 1.688 mmol) was ti-eated with N-methyl-piperazine (2 x 4.65 g, 45.6 mmol) and put in two pyrex tubes and sealed. Each tube was put in a Lab Well MW-10 microwave oven for 2 min at 50W. The reaction mixtures were combined and poured into 0.5 M NaOH (aq) and extracted with CH2CI2, dried (MgS04) and concentrated to give 0.99 g, (2.63 mmol) in 78% yield as a yellow solid. Anal (Ci7 H20 N4 O4 S) C, H, N. S; MS (posES-FL\) m/z = found: 377.4; Calcd: 376.12, EXAMPLE 5 N-I2-Chloro-4-({4-(4-niethyI-l-piperazinyI)-2-|(phenylsulfonyl)aniinoI-aoilino}sulfonyi)phenyl]acetainide hydrochloride (Scheme 2, Method 3) N-[5-(4-McthyI-l-pipcrazinyl)-2-nitrophenyl]bcnzenesulfonamidc (0.600 g, 1.59 mmol) was dissolved in THF (20 mL) followed by the addition of Rancy-Ni (0.322 g, in cthanol) and hydrazine hydrate (0.100 g, 2.0 mmol). The reaction mixture was stirred for Ih, filtered through Cehte and concentrated. The residue was dissolved in pyridine (12 mL) and divided in 12 equal parts. To one part was added 3-cloro-4-N-acetamido-benzenesulfonylchloride (52 mg, 0.20 mmol). The reaction mixture was stirred over night, poured into petroleum ether to foim a precipitate that was collected by centrifugation. The precipitate purified by column chromatography (SiOz, CH^Ch/MeOH 95:5 to 9:1). The pure product was dissolved in MeOH and treated with HCl/diethyl ether to give 9.6 mg, (12% yield). MS (posES-FIA) m/z = found: 57S.4; Calcd: 577.12. EXAMPLE 6 3,4-Dimethoxy-N-{4-(4-metbyI-l-piperazinyl)-2-I(pbenylsulfonyl)-amino]pbenyI}beDzenesulfonamide hydrochloride (Scheme 2, Method 3) N-[5-(4-Methyl-l-piperazinyI)-2-nitrophenyl]ben2enesulfonamide (0.600 g, 1.59 mmol) was dissolved in THF (20 mL) followed by the addition of Raney-Ni (0.322 g, in ethanol) and hydrazine hydrate (0.100 g, 2,0 mmol). The reaction mixture was stin-ed for Ih, filtered through Celite and concentrated. The residue was dissolved in pyridine (12 mL) and dix'ided in 12 equal parts. To one part was added 3,4-dimethoxy-bensenesulfonylchloride (47 mg, 0.20 mmol). The reaction mixture was stirred overnight, poured into petroleum ether to fomi a precipitate that was collected by centrifugation. The precipitate was purified by column chromatography (SiO:, CHiCWMcOU 95:5 to 9:1). The pure product was dissolved in MeOH and treated with HCl/diethyl ether to give 34.5 mg, (45% yield). MS (posES-FL\) m/z = found: 547.4; Calcd: 546.16. EXAMPLE 7 3-Methoxy-4-methyl-N-{4-(4-mctbyI-l-pipera2inyl)-2-I(phenylsulfonyl)-amiDolphenyl}benzenesuiroDamide bydrocbloride (Scheme 2, Method 3) N-[5-(4-Mclhyl-1 -pipera2inyl)-2-nitrophenyI]ben2encsulfonamide (0.600 g, 1.59 mmol) was dissolved in THF (20 mL) followed by the addition of Rancy-Ni (0.322 g, in ethanol) and hydrazine hydrate (0.100 g, 2.0 mmol). The reaction mixture was stirred for Ih, filtered through Celite and concentrated. The residue was dissolved in pyridine (12 mL) and divided in 12 equal parts. To one part was added 2-niethoxy-4-methyl. benzenesulfonylchloride (44 mg, 0.20 nimol). The reaction mixture was stirred overnight, poured into petroleum ether to form a precipitate that was collected by centriftigation. TTie precipitate was purified by purified by column chromatogi-aphy (Si025 CH2Cl2/MeOH 95:5 to 9; 1). The pure product was dissolved in MeOH and treated with HCl/diethyl ether to give 21 mg, ( 28% yield). MS (posES-FIA) ?n/z = found: 530.1635; Calcd: 530.1658. INTERMEDIATE 9 Synthesis of N-(5-nuoro-2-nitrophenyl)methanesuIfonamide (Scheme 2, Method 3) Methylsulfonamide (2.421 g, 25.4 mmol) was dissolved in DMF (100 mL) and NaH (60% in oil, 1.00 g, 25 mmol) was added. The reaction stiixed for 1 h and added to a stirred solution of 2,4-difluoronitrobenzene (4.372 g, 27.5 mmol) in DMF (20 mL). The reaction mixture was stiired for 2h, poured into a mixture (1:1) of brine and IM HCl, and extracted with toluene. The organic phase was dried (MgSOa), and concentrated to give a solid that was cr}'Stanized from toluene / petroleum ether. The flask tipped over and some material was lost, to give 1.32 g, 5.64 mmol in 22% yield. MS (posES-FIA) w/z = found: 234; Calcd: 234.01; Anal (Ci H7 FN: O4 S), C, H, N, S. INTERMADIATE 10 Synthesis of N-(5-(4-niethyl-l-piperazinyI)-2-nitrophenyl]"methanesuifonamide (Scheme 2, Method 3). N-(5-fluoro-2-nitrophenyl)methanesulfonamide (1.33 g, 5.68 mmol) was dissolved in DMF (10 mL) and N-methylpiperazine (2.00 g, 20 mmol) was added. The reaction mixture was stirred at 20°C for Ih, and then heated with a heat gun for 5 min to reach boiling of DMF (1 SO'^C), then left stirring for another hour. The reaction mixture was then f>oured into brine and extracted with toluene (10 mL x 2). EtOAc (20 mL x 2) and CH2CI2 (20 mL x 2), NaHCOs was then added to the water phase and then the water phase was extracted with CH2CI2 (20 mL X 2). The organic phases were combined and dried (MgSOa) and concentrated to give a semi solid. EtOH was added and left over night and then filtered off to give 1.503 g (4.78 mmol) in 84 % yield. MS (posES-FlA) m/z = found: 315; Calc M=314.10; Anal (Ci2 Hi8 N4 O4 S). C, H, N, S. EXAMPLE 8 4-Metbyl-N"{4-(4-inethyl-l-piperazinyl)-2-((naethyIsulfonyl)amino]-pbeDyl}benzenesulfoDan]ide hydrochloride (Scheme 2, Method 3) N-[5-(4-methyM-piperazinyl)-2-nitrophenyl]-methanesulfonamide (0.45 g, 1.43 nimol) was dissolved in THF (10 nnL) followed by the addition of Raney-Ni (0.15 g in ethanol) and hydrazine hydrate (78 mg, 1.56 mmol). The reaction was stiiTed for lb. Another aliquot of hydrazine hydrate (20 i^L) was added and the reaction stined for another hour, filtered through Celite and concentrated to give 0.42 g that was used to the next step without further purification. The material was dissolved in DMF (10 mL) and divided into 3 equal parts. To one part was added p-toluene sulfonyl chloride (0.095 g, 0.5 mmol) and the reaction was stirred for 1 h and poured into a mixture of petroleum ether/acetone (30 mL/10 mL) to give a precipitate. Additional product was found in the solution and added to the precipitate. The product was isolated by chromatography (SiOz, CHaCb/MeOH 9:1) to give 0.063 g, ( 28% yield). MS (posES-FLM m/z = found: 38.1393; Calcd: 438.1395. EXAMPLE 9 3,4-Dimetho\'y-N-{4-('*-niethyM-piperazinyl)-2-[(niethylsuIfonyI)amino]-pbeDyljbeDzenesulfoDamide hydrochloride (Scheme 2, Method 3) N-[5-(4-methyl-l-piperazinyl)-2-nitrophenyl]-methanesulfonamide (0.45 g, 1.43 mmol) was dissolved in THF (10 mL) and Raney-Ni (0.15 g in ethanol) was added followed by hydrazine hydrate (78 mg, 1.56 mmol) and the reaction was stirred for lb. Additional hydrazine hydrate (20 ^iL) was added and the reaction stirred for another hour, filtered through Celite and concentrated to give 0.42 g of product that was used without further purification. The material was dissolved in DMF (10 mL) and divided into 3 equal parts. To one part was added 3,4 dimethox>'bensenesuIfonylchloride (O.I 18 g, 0.5 mmol) and the reaction was stirred for 1 h, poured into a mixture of petroleum ether/acetone (30 mUlO mL) to form a precipitate. Additional product was found in the solution and was added to the precipitate. The product was isolated by chromatography (Si02, CH2Cl2/MeOH 9:1) to give 0.064 g, (26% yield). MS (posES-FIA) m/? = found: 484.1436; Calcd: 484.1450. EXAMPLE 10 3-Cyano-N-{4-(4-methyM-piperazinyl)-2-[(methylsuIfonyI)aminoj" phenyi}benzenesulfoDamide hydrochloride (Scheme 2« Method 3) N-[5-(4-methyI-l-piperazinyl)-2-ninopheny!]-methanesulfonamide (0.45 g, 1.43 mmol) was dissolved in THF (10 mL) and Rayney-Ni (0.15 g in ethanol) was added followed by hydrazine hydrate (78 mg, 1.56 nimol) and the reaction was stirred for Ih. Additional hydrazine hydrate (20 ^L) was added and the reaction stirred for another hour, filtered through Celite and concentrated to give 0.42 g of product that was used without further purifications. The material was dissolved in DMF (10 mL) and divided into 3 equal parts. To one part was added 3-cyanobenzenesulfonylchloride (0.101 g, 0.5 mmol) and the reaction was stirred for 1 h. poured into a mixture of petroleum ether/acetone (30 niL/lO mL) to form a precipitate. Additional product was found in the solution and was combined to the precipitate. The product was isolated by chromatography (SiO:, CHaCh/NieOH 9:1) to give 0.0301g, (13% yield). MS (posES-FL\) m/z = found: 449.1177; Calcd: 449.1191. Scheme 2, Method 4: General Rl = H N-(2-amino-5-(4-boc-l-pipera2inyI)-phenyl)-benzenesuIfonaniide A mixture of N-(2-nitro-3-fluorophenyl)"benzenesulfonamide (4.68 g, 15,7 mmol), Boc-piperazine (3.5 g, IS.9 mmol) and K2CO3 (3.S g, 27.8 mmol) in DMF was stirred at 70°C for 24h, The mixture was filtered and purified by column chromatography (Si02, CH2Cl2/MeOH/heptane/NH3 4:1:5:0.2 %) to give 2,0 g of desired product. *H-NMR 5 7.9S (d, IH), 7.89-7,84 (m, 2H), 7.63-7.50 (m, 3H), 7.00 (d, IH), 6.68 (dd, IH), 3.59-3.45 (m, 8H), 1.49 (s, 9H); MS (posES-FIA) ni/z = found: 485.0 (M* + Na*), The product (L85 g, 4.00 mmol) was dissolved in ElOH:THF (4:1) followed by addition of Rancy-Ni and hydrazine (1.0 mL, 20 mmol). The reaction was stirred at room temperature for 3 h until the yellow color disappeared. Filtration through wet Cclitc, followed by removal of the solvent -40- afforded 1.26 g of N-(2-amino-5-(4-tert-butoxycarbonyl-l-piperazinyl)-phenyl)-benzenesulfonamide which was used without further purification. To a solution of N-{2-amino-5-(4-^butyloxyca^bonyl-piperazinyl)-phenyl}benzenesulfona^lide(79 nig, 0.1S4mmoI) and pyridine (131 p.L, 1.6nimol) in CH2CI2 (7 niL) and different sulfonylchlorides (0.239 mmol) was added. After 2 h at room temperature the solvent was removed. Purification by chi'omatography (Si02. CH2Cl2/MeOH/heptane, 4:1:15) followed by Boc-deprotection which was achieved by dissolving the residue in small amount of MeOH and adding HCl/ether. The mixture was left at room temperature for 0.5 h after which the solvent was removed. Re-crystallization (MeOH/ether) afforded the final products respectively. EXAMPLE 11 fij-|4.(l-PiperaziDyl)-2-|(phenylsulfonyl)amino]phenyl}-l-iiaphthalenesuironamide hydrochloride (Scheme 2, Method 4) N- {4-( I -Piperazinyl)-2-[(phenylsulfonyl)amino]phenyl} -1 -naphthalenesulfonamide was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)-phenyl} benzenesulfonamide and 1-naphthalenesulfonylchloride (54 mg, 0.239 mmol) according to general method 3 to give 40 mg of a purple solid. MS (posES-FL\) m/z = Found: 523.2; Calcd 523.14; *H NMR 5 8.83-8.59 (m, IH). 8.10 (d, IH), 8.02-7.97 (m, IH), 7.90 (d, IH), 7.74-7.38 (m, 8H), 6.69-6.65 (m, IH), 6.39-6.34 (m, 2H), 3.35-3.14 (m, 8H). EXAMPLE 12 5-(DlmethyIamino)-N-{4-(I-piperazinyl)-2-[(phenyIsulfonyl)aniinolphenyl}-l-naphthalenesulfonamide hydrochloride (Scheme 2, Method 4) 5-(Dimcthylamino)-N-{4-(l-piperazinyl)-2-{(phcnylsulfonyl)amino]phcnyl}-l-naphthalenesulfonamide was synthesized from N-(2-amino-5-(4-/-butyloxycarbonyl-pipcrazinyl)- phenyl}benzenesulfonamide and dansylchloride (64 mg, 0.239 mmol) according to general method 3 to give 60 mg of a purple solid. MS (posES-FlA) m/z ■= Found: 5663; Calcd: 566.18; *H NMR 6 8.84 (d, IH), 8.60 (d, IH), 8.08 (d, 2HX 7.84-7.47 (m, 7H), 6.70 (d, IH), 6.56-6,53 (m, IH), 6.41-6.37 (m, IH), 3.46 (s, 6H), 3.25-3.12 (m, SH). EXAMPLE 13 N-[2-((Phenylsulfonyl)arainol-4-(l-piperazinyl)phenylI-8-quinolinesulfonainide hydrochloride (Scheme 2, Method 4) N-[2-[(PhenylsulfonyI)amino]-4-(l-piperazinyl)phenyl]-S-quinolinesulfonamide was synthesized from N-{2-amino-5-(4-;-butyloxycarbonyl-piperazinyl)- phenyl}ben2enesiilfonamide and 8-quinolinesulfonylchIoride (54 mg, 0.239 mmol) according to general method 3 to give 50 mg of a purple solid. MS (posES-FIA) m/z = Found: 524.2; Calcd: 524.13; *H NMR 5 9.34 (dd, IH), 8.79 (dd, IH), 8.37 (dd, IH), 8.25 (dd, IH), 7.92 (dd, IH), 7.73 (t, IH), 7.57-7,40 (m, 5H), 7.17 (d, IH), 6.71 (dd, IH), 6.14 (d, IH), 3.23-3.0S (m, 8H). EXAMPLE 14 2,4,6-Trimethyi-N-(2-I(phenyIsulfonyI)amino]-4-(l-piperaziDyOpheQyljbenzenesulfonamide hydrochloride (Scheme 2, Method 4) 2,4,6-Trimethyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl}benzenesulfonamide and 2-mesitylenesulfonylchloride (52 mg, 0.239 mmol) according to general method 3 to give 50 mg of a purple solid. MS (posES-FIA) m/z = Found: 515.3; Calcd 515.17; 'H-NMR 5 7.74 (d, 2H); 7.63-7.46 (m, 3H). 6.92 (s, 2H), 6.74-6.55 (m, 3H). 3.27-3.20 (m, SH), 2.35 (s, 6H), 2.25 (s, 3H). EXAMPLE 15 4-Metbyl-N*(2-|(pbeDylsulfonyl)amino|-4-(l-piperaziDyl)pbenyl] benzenesuironamide hydrochloride (Scheme 2, Method 4) 4-Methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl]ben2enesulfonamide was synthesized froinN-{2-aniino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl}benzenesulfonamide and p-toluenesulfonylchloride (46 mg, 0.239 mmol) according to general method 3 to give 70 mg of a purple solid. MS (posES-FIA) m/2 = Found: 487.2; Calcd: 4S7.14; *H-NMR 5 7.73-7.45 (m, 7H), 7.26 (d, 2H), 6.74 (s, IH), 6.62-6.60 (ni, 2H),, 3.69 (app t, 2H), 3.39 (app t, 2H), 3.29-3.74 (m, 4H), 2.38 (s, 3H). EXAMPLE 16 N-(2-({I(E)-2-Phenylethenyl)sulfonyl}amino)-5-(l-piperazinyl)phenyl] benzeaesulfonaniide hydrochloride (Scheme 2, Method 4) N-[2-( {[(E)-2-PhenylethenyI]su]fonyl} aniino)-5-( 1 -pipera2inyl)phenyl] benzenesulfonamide was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl}benzenesulfonamide and P-styrenesulfonylchloride (48 mg. 0.239 mmol according to general method 3 to give before Boc-deprotection 160 mg of a purple solid. MS (posES-FIA) m/z = Found: 499.2; Calcd 499.14; 'H-NMR 5 8.26 (d, IH). 8.04 (d, IH), 7.75-7.38 (m,8H), 7.22 (d, lH,y= 15.4 Hz), 7.16 (d, lH),6.97(d, lH),y= 15.4 Hz), 6.78 (dd, IH). 6.68 (d, IH), 3.68 (app t, 2H), 3.39 (app t, 2H), 3.28-3.21 (m, 4H). EXAMPLE 17 2,5-Dimethoxy-N-[2-[(phenyIsuIfonyI)amino]-4-(l-piperazinyI)pbenyll benzenesulfonamide hydrochloride (Scheme 2, Method 4) 2,5-Dimethoxy-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide was s}Tiihesized from of N-{2-amino-5-(4-/-butyloxycart)onyl-pipcrazinyl)- phenyl}benzenesulfonamide and 2,5-dimcthoxybenzencsulfonylchloridc (57 mg, 0-239 mmol) according to general method 3 to give 60 mg of a puq>lc solid. MS (posES-FIA) m/z -= Found: 533.1; Calcd: 533.14; 'H-NMR 5 7.68-7.48 (m, 5H), 7.16-7.05 (m, 4H). 6.69 (dd, IH), 6.42 (d, 1H), 4.03 (s, 3H), 3,69 (s, 3H), 3.26-3,10 (m, 8H). EXAMPLE 18 2-IVIethyl-N-[2-I(phenylsulfon)i)aminol-4-(l-piperazinyl)phenyI] benzenesulfonamide hydrochloride (Scheme 2, Method 4) 2-Methyl-N-[2-[(phenylsulfonyI)amino]-4-(l-piperazinyOphenyljbenzenesulfonamide was synthesized fi*omN-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl)benzenesulfonamide and o-toluenesuifonylchloride (46 mg, 0.239 mmol) according to general method 3 to give before Boc-deprotection 160 mg of a puiple solid. MS (posES-FIA) m/z = Found: 4S7.1; Calcd 487,14; *H-NMR 5 7.74-7.16 (m, 8H), 6.78-6.52 (m, 4H), 3.27-3.16 (m, 8H), 2.58 (s, 3H). EXAMPLE 19 2,4-Difluoro-N-(2-((phenylsuIfonyI)aminol-4-(l-piperazinyl)phenyll benzenesulfonamide hydrochloride (Scheme 2, Method 4) 2,4-Difluoro-N-[2-[(phenylsulfonyl)aniino]-4-(l-piperazinyl)phenyl] benzenesulfonamide was synthesized fiom N-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl}benzenesulfonamide and 2,4-difluorobenzenesulfonylchloride (94 mg, 0.455 mmol) according to general method 3 to give before Boc-deprotection 160 mg of a purple solid. MS (posES-FL\) m/z = Found: 509.1; Calcd 509.11; 'H-NMR 5 77.71-7.46 (m, 6H), 7.25-7.17 (m, IH), 7.03-6.96 (m, 2H), 6.72 (dd, IH), 6.44 (d, IH), 3.20-3.16 EXAMPLE 20 4-Buto\'y-N*[2-[(phenyI.sulfonyl)aminoj-4-(I-piperazinyl)phenylJ benzenesulfonamide hydrochloride (Scheme 2, Method 4) 4-Butoxy-N-(2-[(phcnylsulfonyl)amino]-4-(l-pipcrazinyOphenyiJbcnzcncsuIfonamidc was synthesized from N-{2-amino-5-(4-r-butyloxycarbonyl-piperazinyl)- phenyl} benzenesulfonamide and 4-n-butox>'benzenesuIfonylchloride (59 mg, 0.239 mmol) according to general method 3 to give 70 mg of a puiple solid. MS (posES-FlA) m/z = Found: 545.2; Calcd 545.18; *H-NMR5 7.73-7.45 (m, 7H), 6.95-6.91 (m, 2H), 6.72-6.70 (m, IH), 4.00 (t, 2H), 3.29-3.24 (m, 8H), 1.79-1.70 (m, 2H), 1.55-1.43 (m, 2H), 0.97 (t, 3H). EXAMPLE 21 3,5-Dimethy!-N-(2-((phenylsulfonyI)amino]-4-(l-piperazinyl)phen}il-4-isoxazolesulfonamide hydrochloride (Scheme 2, Method 4) 3,5-Dimethyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl]-4-isoxazolesulfonamide was synthesized froniN-{2-amino-5-(4-r-butyloxycarbonyl-piperazinyl)-phenyI}benzenesulfonamide and 3,5-dimethyIisoxazolesulfonylchloride (47 mg, 0.239 mmol) according to general method 3 to give 70 mg of a purple solid. MS (posES-FlA) m/z = Found: 492.1; Calcd 492.13; 'H-NMR 5 7.72-7.47 (m, 5H), 6.98 (d, IH), 6.80 (dd, lH),6.50(d, IH), 3.28-3.22 (m,8H), 2.22 (s,3H), 2.11 (s, 3H). EXAMPLE 22 5-FIuoro-2-methyl-N-(2-((phenyIsulfonyl)amiDo]-4-(l-piperazinyI)phenyIIbenzene-sulfonamide (Scheme 2, Method 4) 5-Fluoro-2-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)-phenyl]benzenesulfonamide was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl" piperazinyl)- phenyl }benzenesulfonamide and 5-fluoro-2-methylbenzenesuIfonylchloride (50 mg, 0.239 mmol) according to general method 3 to give 60 mg of a puiple solid. MS (posES-FIA) m/z = Found: 505.2; Calcd 505.13; ^H-NMR 5 7.73-7.17 (m, 8H), 6.83 (d, IH), 6.6S (dd, IH), 6.50 (dd, IH), 3.27-3.17 (m, SH), 2.55 EXAMPLE 23 4--N-(2-f(pbeoylsuironyl)amioo|--Hl-piperazinyl)pbenyi]-benzeDesulfooamide hydrochloride (Scheme 2« Method 4) 4-(MethylsuIfonyl)-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)-phenyl]benzenesulfonamide was synthesized from N-{2-amino-5-(4-Nbutyloxycarbonyl-piperazinyl)- phenyljbenzenesulfonamide and 4-methylsulfonylbenzenesulfonylchloride (61 mg, 0.455 mrnol) according to general method 3 to give 70 mg of a piuple solid. MS (posES-FIA) m/2 = Found: 551.2; Calcd: 551.10. EXAMPLE 24 2-(Methylsulfonyl)-N-[2-|(pheDylsulfonyl)amino]-4-(l-piperazinyl)phenyIl benzenesulfonamide hydrochloride (Scheme 2, Method 4) 2-(MethyIsulfony])-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl]benzenesulfonamide was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl}benzenesulfonamide and 2- methylsiilfonylbenzenesulfonylchloride (61 mg, 0.239 mmol) according to general method 3 to give 70 mg of a purple solid. MS (posES-FIA) m/z = Found: 551.2; Calcd: 551.10; 'H-NMR 5 8.36-7.46 (m,9H), 6.95 (d, lH),6.68(dd, lH),6.46(d, IH), 3.47 (s, 3HX 3.28-3.17 (m, SH). EXAMPLE 25 2-Methoxy-4-methyl-N-(2-((phenylsulfonyl)aminoI-4-(l-piperazinyl)phenyl] benzenesulfonamide hydrochloride (Scheme 2, Method 4) 2-Methoxy-4-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)ph€nyl] benzenesulfonamide was sjnthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-piperazinyl)- phenyl)benzenesulfonamide and 2-methoxy-4-methylbenzcnesulfonyIchloride (53 mg, 0.239 mmol) according to general method 3 to give 80 mg of a purple solid. MS (posES-FIA) m/z = Found: 517.2; Calcd 517.15; 'H NMR 5 7.67-7,37 (m, 6H), 7,10-7.04 (m, 2H), 6,97-6.74 (m, 2H), 6.30 (d, IH), 4.06 (s, 3H), 3,26-3.09 (m, 8H), 2.37 (s, 3H). EXAMPLE 26 4-Methoxy-2-methyI-N-(2-((phenylsulfonyI)am!noJ-4-(l-piperazinyl)phenylJ benzenesulfonainide hydrochloride (Scheme 2, Method 4) 4-Methoxy-2-niethyI-N-[2-[(phenylsulfonyl)aTnino]-4-(l-piperazinyl)phenyl] benzenesulfonamide was synthesized fiom N-{2-amino-5-(4-Nbutyloxycarbonyl-piperazinyl)- phenyl}benzenesulfonamide and 2-methy]-4- trifluoromethoxybenzenesulfonylchloride (53 mg, 0.455 mmol) according to general method 3 to give before Boc-deprotection 70 mg of a purple solid. MS (posES-FIA) m/z = Found: 571.2; Calcd 571.12; *H NMR 6 773-7.09 (m, 8H), 6.S6 (d, lH),6.69(dd, lH),6.48(d, IH), 3.29-3.17 (m,SH), 2.62 (s,3H). EXAMPLE 27 N-{4-(bomopiperazinyl)-2-((phenylsulfonyI)amiDo]pbenyl}benzenesulfonafnide hydrochloride (Scheme 1, Method 2) Benzenesulfonyl chloride (0.088 g, 0.50 nimol) was added to a solution of 2-amino-5«(4./-butyloxycarbonyl-homopiperazin-l-yl)aniline (0.153 g, 0.50 mmol) and pyridine (514 mL, 6.39 mmol) in DCM. After I h at r.t. the mixture was washed with NaHCOs (10 %) dried (MgSOa) and the solvent was removed. Purification by column chromatography (CHiCb/MeOH/heptane, 4:1:15) gave a mixture of N-{2-amino-4-[4-r-butyloxycarbonyl-homopiperazin-l-yl-]phenyl}benzenesuIfonamide and of the bis-sulphonylated N-{4-[4-r-butyloxycarbonyl] homopiperazinyl)-2-[(phenylsulfonyl)amino]phenyl}benzenesulfonamide (0.150 g, 86 %). Boc-deprotection was achieved by dissolving the mixture in MeOH and adding HCl/ether. The mixture was let at r.i. for 0.5 h. Purification by preparative HPLC gave N-{4-(homopiperazinyI)-2-[(phenylsulfonyl)amino]phenyl} benzenesulfonamide hydrochloride; Anal. (C2,H27CIN404S:) C H, N, S ; M+ 4S7.4 Calcd 486.14. AndN-{4-(homopipcrazinyl)-2-[(phcnylsuIfonyl)amino3phenyl}benzcnesulfonamide hydrochloride: Anal. (CTHZJCIN^O^S) C, H, N, S ; M+ 347.5 Calcd 346.15. EXAMPLE 28 N-(4-(l,4-diazepan-l-yl)-2-{j(3-fluorophenyl)sulfonyl)animo} pbeDyl)-3-fluorobenzenesulfoDamide hydrochloride (Scheme 1, Method 2) The compound was prepared from 2-amino-5-(4-/-butyloxycarbonyl-l-homopiperazinyl)aniline and 3-flourobenzenesulfonyl chloride. Purification by column clu'omatography (CH2Cl2/MeOH/heptane, 4:1:15) gave a mixture of N-{2-amino-4-(4-^ butyloxycarbony^homopipe^a2in-l-y]-]phenyI}3-fluorobenzenesulfonamideandN-{4-[4-/-butyloxycarbonyl] homopiperazinyl)-2-[(3-flourophenylsulfonyl)amino]phenyl}-3-fluorobenzenesulfonamide (0.180 g, 73 %). Boc-deprotection was achieved by dissolving the mixture in small amount of MeOH and adding HCl/ether. The mixture was let at r.t. for 0.5 h. Purification by preparative HPLC gave N-(4-(l,4-diazepan-l-yI)-2-{[(3-fluorophenyl)sulfonyl]amino}phenyl)-3-fluorobenzenesulfonamide hydrochloride Anal. (C23H27CIN4O4S2) C, H, N, S.; M-H 524.4 Calcd 522.12. EXAMPLE 29 ]SI-{4-(l,4-diazepaD-l-yI)-2-[etbyl(phenylsulforiyl)amino]phenyI}benzeDesulfonainide hydrochloride (Scheme 1, Method 2) A solution of benzenesulfonyl chloride (0.579 mL, 4.53 mmol) in DCM (2.0 mL) was added to tert-butyl 4-[4-amino-3-(ethylamino)phenyl]-l,4-diazepane-l-carboxylate (0.605 g, 1.81 mmol), and pjTidine (1.02 mL, 12.67 mmol) in DCM (8.0 mL). The mixture was stirred at room temperature for 16 hours and then concentrated. The crude intermediate was purified by column chromatography on silica using CHCl3/10% MeOH + 0.4% NH3. Deprotection using HCI-ether/EtOAc gave 0.365 g of the crude product as a HCI-salt. Purification on a reversed phase preperative HPLC gave 94 mg of the product as an acetic acid salt which was converted to the HCl salt and recr>'stallized from MeOH/Ether: yield 64 mg. *H NMR (DMS0-rf6) 5 9.05 (br s, 2H), 8.66 (s, IH), 7.89-7.85 (m, 2H), 7.75-7.55 (m, 8H), 7.07 (app d, J=9.1 Hz, IH), 6.71-6.66 (m, IH), 5.70 (app d, J=3.2 Hz, IH). 3.50-3.32 Method 4 (Scheme 2) Diverse sulfonylchlorides were added to a solution ofN-{2-aniino-5-(4-r-butyloxycarboTxyl-l,4-diazepan-l-yl)- phenyl}ben2enesulfonamide and pyridine (135 \xL, 1.7 mmol) in DCM (7mL),. After 1 h at r.t, the solvent was removed. Purification by column chromatography (CH^Ch/MeOH/Heptane, 4:1:15) followed by Boc-deprotection which was achieved by dissolving the residue in small amount of MeOH and adding HCl/ether. The mixture was left at r.t. for 0.5 h after which the solvent was removed. Recrystallization (MeOH/ether) afforded the final product. EXAMPLE 30 N-{5-(lj4-diazepan-l-y!)-2-((inethyIsulfonyl)aminolphenyI}ben2enesulfoiiqmide (Scheme 2, Method 4) N-{5-(l,4-dia2epan-l-yl)-2-[(methylsulfonyl)amino]phenyl}ben2enesulfonamide was synthesized fiom N-{2-amino-5-(4-^butyloxycarbonyl-1,4-diazepan-1 -yl)-phenyl}benzenesu!fonamide (0.075 g, 0.16 mmol) and , methanesulfonyl chloride (0.017 mL, 0.22 mmole) to give 41.6 mg of a light purple solid; Anal. (C24H27CIN4O3S x I.3H2O) C, H, N, S.; M+ 425.4 Calcd 425.12. EXAMPLE 31 N-{5-(I,4-diazepan-l-yI)-2-((ethy!sulfonyI)amino]phenyl}benzenesulfonamide hydrochloride (Scheme 2, Method 4) N-{5-(l,4-diazepan-l-yl)-2-[(ethylsulfonyl)amino]phenyl}benzenesulfonamide hydrochloride was s>'nthesized from N-(2-amino-5-(4-r-butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl}benzenesulfonamide (0.085 g, 0.19 mmol) and ethanesulfonyl chloride (0.032 ^L, 0.25 mmol) to give 29.1 mg of a light purple solid; Anal. (C24H:7CIN403S x O.75H2O) C, H, N, S.; M+ 439.4 Calcd 439.14. EXAMPLE 32 N-{4-(l,4-diazepan-l-yl)-2-|(phenyIsulfonyl)amino)phenyl}ll,r-biphenyI]-4-suironaniide hydrochloride (Scheme 2, Method 4) N-(4.(i ^4-diazepan-l-yl)-2-[(phenyisulfonyI)amino]phenyl} [I, I '-biphenyI]-4-sulfonamide hydrochloride was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl}benzenesulfonamide (0.081 g, 0.18 mmol) and , 1,1 '-biphenyl-4-sulfonyl chloride (0.059 g, 0.24 mmol) to give 42.9 mg of a light purple solid; Anal. (C2.H27CIN4O3S) C, H,N, S.; M+ 563.5 Calcd 563.17. EXAMPLE 33 N-(2,l^-benzoxadiazoM-yl)-4-(l,4-diazepan-l-yI)-2-|(phenylsuIfonyl)amino]benzenesuIfonamide hydrochloride (Scheme 2, Method 4) N-(2,1,3-benzoxadiazol-4-yl)-4-( 1,4-diazepan-1 -yl)-2-[(phenylsulfonyl)amino]benzenesulfonamide hydrochloride was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl}benzenesulfonamide (0.072 g, 0.16 mmol) and 2,l,3-benzoxadiazol-4-yl sulfonyl chloride (0.072 g, 0.21 mmol) to give 3S-0 mgofa light puiple solid; M+1 537.2 Calcd 537.15; ^HNMR5 8.21 (d, lH),7.80(d, IH), 7.68-7.46 (m, 6H), 6.92 (d, IH), 6.49 (dd, IH), 6.12 (d, IH), 3.57 (app t, 2H), 3.34 (app t, 2H), 3.17 (app t, 2H), 3.11 (app t, 2H), 2.03-1.95 (m, 2H). EXAMPLE 34 N-{4-(l,4-diazepan-l-yI)-2-[(pbeDylsulfoDyl)amino|phenyl}-2-naphthalenesulfoDaraide hydrochloride (Scheme 2, Method 4) N-{4-(1^4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]phenyl}-2-naphthalenesulfonamide hydrochloride was synthesized from N-{2-amino-5-(4-/-but>'Ioxycarbonyl-l,4-diazepan-I-yl)- phenyl}benzenesulfonamide (0.084 g, 0.19 mmol) and , 2-naphtylsulfonyl chloride (0.055 mL, 0.24 mmol) to give 67.8 mg of a light puqplc solid; Anal. (C24HrClN40,S) C, H, N. S; M+ 529.2 Calcd 529.12. EXAMPLE 35 N-{4-(l,4-diazepaD-l-yl)-2-[(metbylsulfonyl)amino]phenyl}beDzenesulfoDaniide hydrochloride (Scheme 2, Method 4) Benzenesulfonylchloride (0.233 g, l.S mmol) was added to a solution ofN-{5-(4-t-butyloxycarbonyl-l,4-diazepan-l-yl)-2-amino]phenyl}methanesulfonamide (0.540 g, 1.4 mmol) and pjoidine (0.995 mL, 12.6 mmol) in DCM (40 mL) After 2 h at rt the solvent was removed. Purification by column chromatography (DCM/MeOH/heptane 4:1:5) gave 580 mg (79 %) of a light purple solid. Boc-deprotection was carried out by dissolving the compound in small amount of MeOH and adding HCl/ether. The solvent was removed and the product was recrystrallized fiom MeOH/ether. M+1 425.2 Calcd 425.12 EXAMPLE 36 N-{4-(l,4-diazepan-l-yl)-2-(methyl(methylsulfonyl)amino|phenyI}benzenesulfonaraide hydrochloride (Scheme 2, Method 4) Mel (45 ^L, 0.72 mmol) was added to a mixture of N-{4-(4-t-butyloxycaI^>onyl-l,4-dia2epan-l-y^)-2-[(methylsulfonyl)amino]phenyl}benzenesulfonamide (0.189 g, 0.36 mmol) and K2CO3 (0.124, 0.90 mmol) in acetone (25 mL). Tlie mixture was stirred at r.t, for 2 h, filtered and the solvent was removed. Columnchromatography (DCM/MeOH/Heptane 4:1:15) gave 110 mg ofN-{4-(4-t-butyloxycarbonyll,4-diazepan-l-yl)-2-[methyl(methylsulfonyl)amino]-phenyl}benzenesulfonamide and 20 mg of N-{4-(4-t-butyloxycarbonyl l,4-diazepan-l-yl)-2-[(methylsulfonyl)amino]phenyl)-N-methyI-benzenesulfonamide. Boc-deprotection was carried out by dissolving the compounds in small amount of MeOH and adding HCl/ether. The solvent was removed and the products were recrystrallized fi-om MeOH/ether. N-{4-(l,4-diazepan-l-yl)-2- [methyl(methylsulfonyI)amino]phenyl}benzenesulfonamide hydrochloride M+1 439.2 Calcd 439.14. EXAMPLE 37 N-{4-(l,4-diazepan-l-yl)-2-((methyIsuIfonyI)aininolphenyl}-N-raetbylbenzenesulfoDamide hydrochloride (Scheme 2, Method 4) Mel (45 nL, 0.72 mmol) was added to a mixture of N-{4-(4-t-butyIoxyca^bonyM,4-diazepan■■l-yl)-2-[(methylsuIfonyI)amino]phenyl}benzenesulfonanlide (0.189 g, 0.36 nimcl) and K2CO3 (0.124, 0.90 mmol) in acetone (25 mL). The mixture was stirred at r.t. for 2 h, filtered and the solvent was removed. Purification by column chromatography (DCM/MeOH/Heptane 4:1:15) gave 110 mg of N-{4-(4-t-butyloxycarbonyll,4-diazepan-l-y])-2-[methyl(niethylsulfonyl)amino]phenyl}benzenesulfonamide and 20 mgofN-{4-(4-t-butyloxycarbonyl 1,4-diazepan-1 -yl)-2-[(methylsulfonyl)amino]phenyl} -N-methyl benzenesulfonamide. Boc-deprotection was carried out by dissolving the compounds in small amount of MeOH and adding HCl/ether. The solvent was removed and the products were recrystrallized from MeOH/ether. N-{4-(l,4-diazepan-l-yl)-2-[(methylsulfonyl)amino]-phenyl}-N-methylbenzenesulfonamide hydrochloride M+1 439.2 Calcd 439.14. EXAMPLE 38 N-{4-(l,4-diazepan-l-yl)-2-[methyl(pbenylsulfonyl)amino]phenyl} benzenesulfonamide hydrochloride (Scheme 2, Method 4) Mel (45 fiL, 0.72 mmol) was added to a mixture of N-{4-(4-t-butyloxycarbonyl-l,4-diazepan-l-yl)-2-((phenyIsulfonyl)amino]phenyl}ben2enesuIfonamide (0.1S9 g, 0.36 mmol) and K2CO3 (0.124, 0.90 mmol) in acetone (25 mL). The mixture was stirred at r.t. for 2 h, filtered and the solvent was removed. Purification by column chromatography (DCM/MeOH/heptane 4:1:15) gave N-{4-(4-t-butyloxycarbonyl-l,4-dia2epan-l-yl)-2-[methyI(phenylsulfony!)-amino3phenyl} benzenesulfonamide as a colourless oil. Boc-deprotection was earned out by dissolving the compound in small amount of MeOH and adding HCl/cthcr. The solvent was removed and the residue was recrystrallized from MeOH/cther to give 62.7 mg of product M+I 501.3 Calcd 501.16. Scheme 3 Tea solution ofN-{2-3mino-5-(4-r-butyIoxycarbonyl-1,4-diazcpan-l-yl)- phenyl} methanesulfonamide (134 mg, 0.35 mmol) and pyridine (250 ^L, 3.14 mmole) in DCM (7mL), the sulfonylchloride (0.455 mmol) was added. After 2 h at r.t. the solvent was removed. Purification by column chromatography (CH^Cb/MeOH/Heptane, 4:1:15) followed by Boc-deprotection which was achieved by dissolving the residue in small amount of MeOH and adding HCl/ether. The mixture was left at r.t. for 0.5 h after which the solvent was removed. Recrystallization (MeOH/ether) afforded the final product. EXAMPLE 39 N*{4-(l,4-diazepan-]-yl)-2-[(methylsuironyl)amiDo]pbeuyl}-l-naphtbalenesul-fonaniide hydrochloride (Scheme 3) The compound was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl}methanesulfonamide and 1-naplhalenesufonylchloride (103 mg, 0.455 mmol) to give before Boc-deprotection 150 mg of a purple solid. M+1 475.1 Calcd 474.14. EXAMPLE 40 IV-{4-(l,4-diazepan-l'yI)-2-|(methyIsulfonyI)amino]phenyI}-2-naphtbalenesul-fonaniide hydrochloride (Scheme 3) The compound was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl} methanesulfonamide and 2-napthalenesufonylchloride (103 mg, 0.455 mmol) to give before Boc-deprotection 120 mg of a purple solid. M+1 475.1 Calcd 474.14. EXAMPLE 41 fj.(4^],4-diazepan-l*yl)-2-((inethylsuironyl)amiDo)pbenyI} fonamide bydrocbloride (Scheme 3) The compound was s>'nthesi2ed from N-{2-amino-5-(4-/-butyIoxycarbonyI-l,4-diazcpan-1-yl)- phenyl} methanesulfonamide and 4-fluorobcn2cnesuironylchloridc (89 mg. 0.455 mmol) to give before Boc-deprotection 170 mg of a purple solid. M+1 443.1 Calcd 443.11. EXAMPLE 42 N-{4-(l,4-diazepan-l-yl)-2-I(methyIsulfonyI)aminoJphenyl}-4-nitrobenzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized fiom N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl}methanesulfonamide and 4-nitroben2enesulfonylchloride (101 mg, 0.455 mmol) according to general method 3 to give before Boc-deprotection 118 mg of a puiple solid. M+1 470.1 Calcd 470.11. EXAMPLE 43 N-{4-(l,4-dia2epan-l-yl)-2-((methylsulfonyl)amino]phenyl}-3-(tnfluoromethyI)-benzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from N-{2-amino-5-(4-/-butylo\ycart>onyl-l,4-diazepan-1-yI)- phenyl} methanesulfonamide and 3-trifluoromethylbenzenesulfonylchloride (111 mg. 0.455 mmol) to give before Boc-deprotection 145 mg of a purple solid. M+1 493.1 Calcd 493.11. EXAMPLE 44 N-{4-(l,4-diazepan-l-yl)-2-((methylsulfonyl)aminolphenyl}-2-methylbenzenesu!-fonaniide hydrochloride (Scheme 3) The compound was synthesized from N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl}methanesulfonamide and o-toluenesulfonylchloride (87 mg, 0.455 mmol) to give before Boc-deprotection 175 mg of a purple solid. M+1 439.2 Calcd 438.14. EXAMPLE 45 N-{4-(l,4-diazepan-l-yl)-2-((methylsulfonyI)amino|pbenyl}-4-(trinuoromethoxy)-benzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from N-{2-amino-5-(4-r-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyI}niethanesulfonamide and 4-trifluoromethoxybenzenesulfonylchlonde (119 mg, 0.455 mmol) give 140 mg as a purple solid. M+1 509.1 Calcd 509.11. EXAMPLE 46 IV-(4«(l,4-diazepan"l-yl)-2-((methylsulfonyl)aniinolphenyl}-3,5-dimethyM-isoxazolesulfonamide hydrochloride (Scheme 3) The compound was synthesized from N-{2-amino-5-(4-r-butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl) methanesulfonamide and 3,5-dimethylisoxazole-4-sulfonylchloride (89 mg, 0.455 mmol) 3 to give 120 mg of as purple solid. M+1 444.2 Calcd 444.13. EXAMPLE 47 N-{4-(l,4-diazepan-l-yl)-2-((methyIsulfonyl)aminoJpheuyl}-3-metboxybenzene-sulfonamide hydrochloride (Scheme 3) The compound was synthesized from N-(2-amino-5-(4-/-butyIoxycarbonyl-l,4-diazepan-1-yl)- phenyl}methanesulfonamide and S-methoxybenzenesulfonj'lchloride (94 mg, 0.455 mmol) to give 160 mg as a purple solid. M+1 455.2 Calcd 455.13. INTERMEDL^TE 11 tert-ButyI4-{4-{|(4-methylphenyl)sulfonylJamino}-3-((methyIsulfonyI)amino|phenyl}-l,4-dia2epane-l-carboxylate (scheme 2, Method 4) /e/7-ButyI 4-{4-nitTO-3-[(melhyIsulfonyl)amino]phenyl}-l,4-diazepane-I-carboxylate (I g, 2.4 mmol) was dissolved in THF (20 mL) and methanol (2 mL). Rancy nickd (0.2 g) was added followed by hydrazine hydrate (0.2 mL). Nitrogen was evolved and the mixture stirred for 1 hour. The reaction was shov\Ti to be incomplete by tic (CH:Cl2. MeOH 9:1) so a further 0.1 mL of hydrazine hydrate was added. After a further hour, the reaction mixture was absorbed onto a bed of silica gel and eluted with CH2Cl2:MeOH:NH40H (9:1:0.01 150 mL). The solvent was removed by evaporation, toluene (100 mL) was added and evaporated to remove any water and hydrazine. The cmde amine (0. 9 g) was dissolved in acetonitrile (20 mL). To this solution under nitrogen was added dimethylaminopyridine (0.32 g) and toluenesulfonyl chloride (0.51 g) and the mixture stiixed for 3 hours. The solution was poured into water (100 mL) and extracted with ethyl acetate (30 mL). The organic extract was washed with water, dried over MgSOa and evaporated to give 0.83 g of crude product which was purified by flash chromatography (EtOAciPetrol 1:1). Yield 0.53 g (41%) 'HNMR{400 MHz, CDCh) 6 1.38, 1.40 (2s, 9 H), 1.91 {m,J= 6.11 Hz, 2 H), 2.44 (s, 3 H), 3.03, 3.05 (2s, 3H), 3.16-3.33(m, 2H),3.46-3.57(m,6H), 6.02(s, 1 H),6.21 (ab, 7= 9.03 Hz, 1 H), 6.30 (ab, 7= 9.03 Hz, 1 H), 6.97 (d, 7 = 2.69 Hz, 1 H), 7.27 (ab, J= 8.55 Hz, 2 H), 7.33, 7.36 (2s, 1 H), 7.57 (ab, /= S.06 Hz, 2 H); MS (ESI+) for C24H34N4O6S2 m/z 561.1800 (M+)* (Calculated 561.1817). EXAMPLE 48 N-{4-(l,4-diazepan-l-yI)-2-|(methylsulfonyl)amino]phenyl}-4-metfaylbenzenesulfonamide hydrochloride (PHA 516123A) /e/-/-Butyl 4-{4-{[(4-niethylphenyl)sulfonyl]amino}-3-[(methylsulfonyl)amino]phenyl}-l,4-diazepane-l-carboxylate (0.5 g) was dissolved in methanol (15 mL). A solution of HCl in ethyl acetate (IN, 25 mL) was added and the mixture stirred for 2 hours. Ether (200 mL) was added and the mixture stined for 3 hours to allow full precipitation. The product was collected by filtration, washed with ether and dried. Yield 0.43 g (98%) 'H NMR (400 MHz. DMSO-^d) 5 2.03 (m, 2 H), 2.36 (s, 3 H), 2.9 (s, 3 H), 3.02-3.09 (br m, 2 H), 3.11-3.19 (br m, 2 H), 3.41 (br t,J= 7.08 Hz, 2 H), 3.63 (br m, 2 H), 6.46 (d ab, y = 2.8 Hz, 8.8Hz, 1 H), 6.62 (ab, J= 8.8 Hz, 1 H), 6.71 (d, y= 2.S Hz, 1 H), 7.36 (ab, y= 8.3 Hz, 2 H), 7.58 (ab, J= 8.3 Hz, 2 H), S.39 (s, 1 H), 9.2 (br, 2 H), 9.S (s, 1 H); MS (ESI+) for C19H27N4O4S2 m/z 439.148 (M+H)* (Calculated 439.1474). INTERMEDIATE 12 N-ethy!-N-(5-fluoro-2-nitrophenyl)methanesulfonamide (Scheme 2, Method 4) N-ethyl-methanesulfonamide (Mijs et ai J.Chem.Soc.Chem.Com. 1972 p412) (5 g 40.6 mmol) was added to a suspension of sodium hydride (1.9 g, 55% in mineral oil) in anhydrous DMF (100 mL) under nitrogen. The mixture was warmed to 55°C for one hour and 2,4-difluoronitrobenzene (4.4 mL) was added dropwise. The reaction was stin*ed at 60°C overnight, poured into water (500 mL) and the product exti-acted into CH2CI2 (5 x lOOmL). The organic exti-acts were washed with water, dried over MgSOa and evaporated to give an oily product. Tlie remaining DMF was removed by tritvuation with petrol. The crude product was purified by flash chromatography (ethyl acetate:petrol 1:1) to yield the desired product which was recrystallised fiom ethanol. Yield 3.5g (33%). Calculated N % 10,68 C % 41,22 S% 12,23 H% 4,23; Found N% 10,68 C% 41,39 S% 12,22 H%4,17. INTERMEDIATE 13 tert-But>'l 4-{3-(elhyl(methylsiilfonyl)aniinoj-4-nitrophenyl}-l,4-dia2epane*l-carboxylate (Scheme 2, Method 4) N-Ethyl-N-(5-fluoro-2-nitrophenyl)methanesulfonamide (3.2 g, 12.2 mmol), tert-bulyl i-homopiperazinecarboxylate (2.5 g) and potassium carbonate (2 g) were lieated together in DMSO at 50 °C for 5 hours. The solution was allowed to cool and poured into 500 mL of water. The solid product was collected by filtration, washed with water and dii^d. The product was purified by flash chromatogi*aphy (ethyl acetate:petrol 1:1). Yield 2.6g (48%) 'H NMR (400 MHz, CDCI3) 5 1.16 (l, y= 7.33 Hz, 3 H), 1.39 (s, 9 H), 2.0 (br, 2 H), 2.99 (s, 3 H), 3.2 (br, 2 H), 3.54-3.75 (br, S H), 6.65 (br d, 7= 9.3 Hz, 1 H), 6.67 (d, 7= 2.93 Hz, 1 H), 8.1 (d, y = 9.3 Hz, 1 H); MS (ESI+) for C19H30N4O6S m/z 442 (M^). Preparation ofN'{4'(l,4'diazepau-I-yl)-2'[ethyl(methyl5ulfonyl)ammo]phenyl}- sulfouamides lcrt-ButyI4-{3-[cthyI(mcthyIsulfonyl)amino]-4-nitrophenyl}-l,4-diazcpane-l- carboxylatc (2.5 g, 5.7 mmol) was dissolved in THF (50 mL) and methanol (5 mL). Rancy nickel (0.5 g) was added followed by hydrazine hydrate (0.5 mL). Nitrogen wasncvolvcd and the mixture stirred for 1 hour. The reaction mi.xturc was absorbed onto a bed of silica gel and eluted with CH2Cl2:MeOH:NH40H (9:1:0.01 200 mL). The solvent was removed by evaporation, toluene (200 mL) was added and evaporated to remove any water and hydrazine. The crude amine (2.15 g) was dissolved in acetonitrile (50 mL) with dimethylaminopyridine (O.S g). This solution was divided into three portions. To each portion was added a sulfonyl chloride (2.2 mmol) and the mixtures were stirred overnight at 40°C. The reactions were worked up by adding to water (150 mL), exti*acting the product into ethyl acetate, washing with water, drying over MgS04 and evaporating. Each of the crude boc protected products was purified by flash chromatography (ethyl acetate:petrol 1:1). They were then deprotected directly by dissolving in methanol (10 mL), adding a solution of HCl in ethyl acetate (IN, 50 mL) and stirring for 2 hours. The products were precipitated with ether (500 mL), collected by filtration and dried under vacuum. The products obtained were: EXAMPLE 49 N-{4-(l,4-diazepan-l-yI)-2-(ethyI(methylsu!fonyI)-amiaolphenyl}-4-methylbenzenesulfonamide hydrochloride (Scheme 2, Method 4) Was obtained from toluene sulfonyl chloride: Yield 0.36 g 'H NMR (400 MHz, DMSO-i/d) 6 0.79 (t, 7 = 7.0S Hz, 3 H), 2.04 (m, 2 H), 2.37 (s, 3 H), 3.07 (s, 3 H), 3.02-3.12 (hr, 2 H), 3.12-3.20 (br, 2 H), 3.45 (l,J= 5.85 Hz, 2 H), 3.50 (q, J = 7.5 Hz, 2 H), 3.67 (br, 2 H), 6.65-6.73 (m, 2 H), 6.94 (d, 7 = 9.03 Hz, 1 H), 7.38 (ab, / = 8.5 Hz, 2 H), 7.70 (ab, / = 8.06 Hz, 2 H), S.52 (s, 1 H), 9.2 (br s, 2 H) MS (ES1+) for C21H30N4O4S2 m/z 466.1722 M^ (Calc 466.1708). EXAMPLE 50 p4-{4.(l,4-diazepan-l-yl)-2-|ethyl-(metbylsulfonyi)-amino]pbeDyl}-3,4-dimethoxybenzenesulfonamide hydrochloride (Scheme 2, Method 4) Was obtained from 3,4-dimeihoxyben2encsulfonyl chloride: Yield 0.43 g 'H NMR (400 MHz, DMSO-rf^) 6 0.81 (t, 7 = 7.08 Hz, 3 H), 2.05 (m, 2 H), 3.08 (s, 3 H), 3.03-3.11 (br, 2 H), 3.11-3.19 (br. 2 H). 3.45 (t,y« 6.10 Hz, 2 H), 3.52 (q, J= 7.0S Hz, 2 H). 3.68 (br t, y = 5.13 Hz, 2 H), 3.77 (s, 3 H), 3.81 (s, 3 H), 6.66-6.74 (m, 2 H), 6.97 (d, 7= 8.79 Hz, 1 H), 7.09 (d, J= 8.55 Hz, 1 H), 7.33-7.4 (m, 2 H), 8.49 (s, 1 H), 9.3 (br s, 2 H) MS (ESI+) for C22H32N4O6S2 m/i 512.1759 M^ (Calc 512.1763). EXAMPLE 51 N-{4-(l,4-diazepan-l-ji)-2-(ethyl(methyl-sulfonyl)amino)phenyI}-8-quinolinesulfonamide hydrochloride (ScheDie 2, Method 4) Was obtained from 8-quinoline sulfonyl chloride: Yield 0.46 g 'H NMR (400 MHz, DMSO-rffi) 8 0.17 (t, 7= 7.08 Hz, 3 H), 2.06 (m, 2 H), 2.93 (s, 3 H), 3.0-3.2 (m, 6 H), 3.47 (t, J= 5.86 Hz, 2 H), 3.70 (t, J= 5.12 Hz, 2 H), 6.59 (m, 1 H), 6.77 (d m, J = 9 Hz, 1 H), 7.31 (d, 7= 9 Hz, 1 H), 7.65-7.75 (m, 2 H), 8.24 (d, 7= 7.32 Hz, 1 H), 8.29 (d, 7= 9.5 Hz, 1 H), 8.55 (dd, 7= 8.55, 1.71 Hz, 1 H), 9 (br, 1 H), 9.09 (dd. 7= 4.16, 1.71 Hz, 1 H), 9.3 (br, 2 H); MS (ESI+) for C23H29N5O4S: m/z 503.1667 M* (Calc 503.1661). INTERMEDL\TE 14 N-(5-nuoro-2-nitropheiiyI)methanesulfonainide (Scheme 2, Method 4) 2,4-di-Nitrobenzene (5.5mL, 50mmol), methanesulfonamide (4.75g, 50mmol) and potassium carbonate (lOg) were stirred together in DMSO (lOOmL) at SO°C overnight. Water (300i"nL) was added followed by hydrochloric acid (IN, 300mL). The solid product was collected by filtration, washed with water and dried. Yield 9.57g (82%) 'H NMR (400 MHz, CDCI3) 5 3.2 (s, 3 H), 6.92 (m, 1 H), 7.64 (dd, 7= 10.5, 2.7 Hz, 1 H), 8.34 (dd,7= 9.5, 5.6 Hz, 1 H), 10.0 (brs, 1 H); MS (ES1+) for C7H7FN2O4S m/z 234 M*. INTERMEDIATE 15 N- N-(5-fluoro-2-nltrophenyl)methancsulfonamidc compound (5g, 21mmo1), methyl iodide (3mL) and potassium carbonate (lOg) were stirred together in DMSO (lOOmL) at sec overnight. The reaction was not complete and a further ImL of methyl iodide was added. After a further 24 hours at 80°C, water (lOOOmL) was added. The solution was " decanted from a small amount of sticky residue. The product crystallized out from the aqueous solution (48 hours) and was collected by filtration, washed with water and dried. Yield 3.3g (63%); ^H NMR (400 MHz, CDCI3) 5 3.04 (s, 3 H), 3.30 (s, 3 H), 7.20 (m, 1 H), 7.31 (dd,y= 8.54, 2.68 Hz, 1 H), 8.0 (dd, J= 9.3, 5.6 Hz, 1 H); MS (ESI+) for C8H9FN2O4S m/z 248 M^. INTERMEDIATE 16 tert-Butyl-4"{3-|methyl(methylsulfonyl)aminol-4'nitrophenyl}-l54-diazepane-l-carboxylate (Scheme 2, Method 4) N-(5-Fluoro-2-nitrophenyl)-N"methyImethanesulfonamide (3.1 g, 12.5 mmol), terl-butyl 1-homopiperazinecarboxylate (2.5 g) and potassium carbonate (2 g) were healed together in DMSO (50 mL) at SO °C ovemight. The solution was allowed to cool and poured into 500 mL of water. The solid product was collected by filtration, washed with water and dried. Yield 4.6 g (86%); 'H NMR (400 MHz, CDri3) 6 1.41 (s, 9 H), 2.0 (brs, 2 H), 3.01 (s, 3 H), 3.28 (s, 3 H), 3.3-3.8 (br, 8 H), 6.64 (d, J- 8.1 Hz, I H), 6.74 (d, 7- 4.8 Hz, 1 H), 8.09 (d,y=8.1 Hz, 1 H); MS (ESI+) for CisH2sN40tS m/z 428.1709 (M^(calc. 428.1730). Preparation ofN-{4-(l,4'diazepan-l-yl)-2-[methyl(methyhulfonyl)a}nino]phenyl}-sulfonamides iert-Butyl-4-{3-[methyl(methylsulfonynamino]-4-nitrophenyl}-l,4-diazepane-l-carboxylate (2.5 g, 5.7 mmol) was dissolved in THF (50 mL) and methanol (5 mL). Raney nickel (0.5 g) was added followed by hydrazine hydrate (0.5 mL), Nitrogen was evolved and die mixture stirred for 1 hour. The reaction mixture was absorbed onto a bed of silica gel and eluted with CH2Ch:MeOH:NH40H (9:1:0.01 200 mL). The solvent was removed by evaporation, toluene (200 mL) was added and evaporated to remove any water and hydrazine. The crude amine (2.36 g) was dissolved in acctonitrilc (50 mL) with dimcthylaminop>Tidinc (0.8 g). This solution was divided into six portions. To three of these portions was added a sulfonyl chloride (I.l mmol) and the mixtures were stirred ovemight at 40**C The reactions were worked up by adding ethyl acetate (50 mL), washing with brine and water, drying over MgS04 and evaporating. Each of the crude hoc protected products was purified by flash chromatography (ethyl acetate:petrol 2:1). They were then deprotected directly by dissolving in methanol (10 mL), adding a solution ofHCl in ethyl acetate (IN, 50 mL) and stirring for 2 hours. The products were precipitated with ether (500 mL), collected by filtration and dried under vacuum. The products obtained were: EXAMPLE 52 N-{4-(l,4-dia2epan-l-yl)-2-(niethyl(methyIsulfonyI)-aminolphenyI}-4-metbylbenzeDesulfonamide hydrochloride (Scheme 2, Method 4) Was obtained from toluene sulfonyl chloride: Yield 0.18g 'HNMR (400 MHz, DMSO-c?tf) 5 2.04 (br m, 2 H), 2.36 (s, 3 H), 2.72 (s, 3 H), 3.05 (s, 3 H), 3.1-3.4 (m, 4 H), 3.46 (t,y= 6.34 Hz, 2 H), 3.70 (t, J= 4.8S Hz, 2 H), 6.69 (d,y= 2.7 Hz, 1 H),6.72(s, 1 H), 6.95 (d,y= 8.78 Hz, 1 H), 7.36 (ab,y= 8.54 Hz, 2 H), 7.57 (ab,J= 8.54 Hz, 2 H), 8.39 (s, 1 H), 9.24 (brs, 2 H); MS (ESI+) for C20H23N4O4S2 m/z 452.1545 M* (Calc. 452.1552). EXAMPLE 53 N-{4-(l,4-dia2epan-l-yl)-2-|methyl-(methyl-sulfonyI)amino)phenyl}-naphthaIene-2-sulfonaniide hydrochloride (Scheme 2, Method 4) Was obtained from 2-naphthalenesulfonyl chloride: Yield 0.09g 'H NMR (400 MHz, DMSO-af EXAMPLE 54 N-{4-(l,4-diazepan-l-yl)-2-(methyl(methylsulfonyl)aminolphenyl}-S-(2-pyridinyl)-2-tbiopbenesulfonamide hydrochloride (Scheme 2, Method 4) Was obtained from 5-(2-pyridinyl)thiophene-2-sulfonyl chloride: Yield 0.12 g 'H NMR (400 MHz, DMS0-d6) 5 2,05 (br m, 2 H), 2.90 (s, 3 H), 3.07 (s, 3 H), 3.1-3.4 (m, 4 H), 3.4S (t,y= 6.1 Hz, 2 H), 3.71 (m, 2 H), 6.75 (dd, J= 9.0, 2.7 Hz, 1 H), 6.78 (s, 1 H), 7.03 (d, J= 8.8 Hz, 1 H), 7,39 (dd, 7 = 7.6, 4.2 Hz, 1 H), 7.50 (d, /= 4.2 Hz, 1 H), 7.84 (d, J= 3.9 Hz, 1 H), 7.91 (td, y = 7.6, 1.7 Hz, 1 H), S.03 (d, 7- 7.S Hz, 1 H), 8.56 (d, 7= 4.9 Hz, 1 H), 8.S1 (s, 1 H), 9.3 (br, 2 H); MS (ESI+) for C22H27N5O4S3 m/z 521.1200 M^ (Calc. 521.1225). Scheme 3 To a solution of N-{2-aniino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl} benzenesulfonamide (92.5 mg, 0.207 mmol) and pyridine (131 p-L, 1.6 mmol) in DCM (7 mL), the sulfonylchloride (0.27 mmol) was added. After 2 h at r.t. the solvent was removed. Purification by columnchromatogiaphy (CH2Cl2/MeOH/Heptane, 4:1:15) followed by Boc- . deprotection which was achieved by dissolving the residue in small amount of MeOH and adding HCl/ether. The mixture was left at r.t. for 0.5 h after which the solvent was removed. Recrystallization (MeOH/ether) afforded the final product. EXAMPLE 55 N*(4-(l,4"diazepan-l-yl)-2-|(phenylsulfonyl)amino]phenyl}-l-naphthalenesulfonamlde hydrochloride (Scheme 3) The compound was synthesized ft-om of N-{2-amino-5-(4-^butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl} benzenesulfonamide and l-naphthalenesulfonylchloride (61 mg, 0.27 mmol) to give 56 mg as puiple solid. M+1 537.2 Calcd 537.15; *HNMR 5 8,67-8.64 (m, IH), S.10(d, IH), 8.02-7.98 (m, lH),7.89(dd, IH), 7.77-7.38 (m, 8H), 6.46 (d, lH),6.26(d, IH), 6.14 (dd, IH), 3.54 (app t, 2H), 3,36-3.31 (m, 2H), 3.17 (app t, 2H), 2.05-1.96 (m, 2H). EXAMPLE 56 IV-{4-(l,4-diazepan-l-yl)-2-((phenyIsulfonyI)aminoJphenyl}-5-(dimethylaniino)-l-naphthalenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from ofN-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yl)- henyl}benzenesuIfonamide and dansylchloride (73 mg, 0.27 mmol) to give 51 mg AS purple solid. M+1 580.3 Calcd 580.20; ^HNMR 5 8.86 (d, IH), 8.62 (d, IH), 8.08-7.46 (m, 9H), 6.64 (d, IH), 6.32 (dd, IH), 6.14 (d, IH), 3.53 (app t, 2H), 3.45 (s, 6H), 3.16-3.06 (m,4H), 2.03-1.95 (m,2H). EXAMPLE 57 N-{4-(l,4-diazepan-l-yI)-2-((phenylsulfonyl)amino]phenyl}-8-quinolinesuIfonaniide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl jbenzenesulfonamide and 8-quinolinesulfonylchloride (61 mg, 0.27 mmol) to give 34 mg of a puiple solid. M+1 538.2 Calcd 538.15. EXAMPLE 5S N-{4-(l,4-dia2epan-l-yI)-2-((phenyIsulfonyl)aminolphenyl}-2,4,6-trimethylbenzenesuiroaamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-r-butyloxycarbonyl-l,4-diazepan-1-ylV phenyl)benzenesulfonamide and 2-mesitylenesulfonylchloride (59 mg, 0.27 mmol) to give 56 mg as purple solid. M+1 529.3 Calcd 529.70; 'HNMR 5 7.80-7.47 (m, 5H), 6,93 (s br, 2H), 6.64 (d, IH), 6.46-6.39 (m, 2H), 3.60 (app t, 2H), 3.39 (app t, 2H), 3.21 (app t, 2H), 3.12 (app t. 2H). 2.36 (s, 6H), 2.26 (s, 3H), 2.0S-2.00 (m, 2H). EXAMPLE 59 N-{4-(],4-diazepaD-l-yl>-2-|(phenylsuironyl)amino|phenyl}-4-methylbenzenesuiroDamide hydrochloride (Scheme 3) The compound was s>'nthesi2cd from of N-{2-amino-5-(4-/-bulyloxycarbonyl-l,4-diazepan-1-yl)- phenyl} benzcnesulfonamidc and p-toluenesulfonykhloride (51 mg, 027 mmol) to give 22 mgas purple solid. M+1 501.3 Calcd 501.15; 'HNMR 5 7.77-7.26 (m, 9H), 6.54 (d, IH), 6.50 (d, IH), 6.40 (dd, IH), 3.63 (app t 2H), 3.42 (app t, 2H), 3.25 (app t, 2H), 3.16 (app t, 2H), 2.38 (s, 3H), 2.11-2.03 (m, 2H). EXAMPLE 60 N-(5-(l,4-diazepan-l-yl)-2-({((E)-2-phenylethenyl]sulfon}i}aniino)phenyl]benzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-f-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl}benzenesulfonamide and beta-styrenesulfonylchloride (55 mg, 0.27 mmol) to give before Boc-deprotection 12 mg as puiple solid. M+1 513.6 Calcd 512.15; 'HNMR5 7.7S-7.3S(m, lOH), 7.20(d, IH), J= 15.4 Hz), 7.10(d, IH), 6.98(d, IH), J = 15.4 Hz), 6.56 (dd, IH), 6.44 (d, IH), 3.62 (app t, 2H), 3.41 (app t, 2H), 3.23 (app t, 2H). 3.15 (app t, 2H), 2.09-2.01 (m, 2H). EXAMPLE 61 N-{4-(l,4-diazepan-l-yI)-2-[(pbenylsulfonyl)aminolphenyI}-2.5-dimethoxybenzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yl)-phenyl}benzenesulfonamide and 2,5-dimethoxybenzenesulfonylchloride (64 mg, 0.27 mmol) to give 14 mg as puiple solid. M+1 547.3 Calcd 547.16; 'HNMR 5 7.71-7.00 (m, 9H), 6.4S (dd, IH), 6.16 (d, IH), 4.04 (s, 3H), 3.68 (s, 3H), 3.56 (app t, 2H), 3.33 (app t, 2H), 3.17 (app t, 2H), 3.11 (app t, 2H), 2.03-1.95 (m, 2H), EXAMPLE 62 I«i;.{4^],4-diazepan-l-yl)-2-|(phenyisulfonyl)amino|phenyl}-2-metbylbenzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yl)- phenyl}benzenesulfonamide and o-toluen€sulfonylchloridc(51 mg, 0.269 mmol) to give 18 mg as purple solid. M+1 501.3 Calcd 501.15; 'HNMR 5 7.78-7.17 (m, 9H), 6.68-6.35 (m, 3H), 3.63-3.10 (m, 8H), 2.59 (s, 3H), 2.09-2.01 (m, 2H). EXAMPLE 63 4-Butoxy-N-{4-(l,4-diazepan-l-yl)-2-|(phenyisulfonyl)amino|phenyl}-benzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-aniino-5-(4-r-butyloxycarbonyl-l,4-diazepan-1-yl)- phenyl} benzenesulfonamide and 4-n-butoxybenzenesulfonylchloride (67 mg, 0.269 mmol) to give 27 mg as puiple solid. M+1 559.4 Calcd 559.20; 'HNMR 5 7.77-7.47 (m, 7H), 6.96-6.93 (m, 2H), 6.55 (d, IH), 6.52 (d, IH), 6.41 (d, IH), 4.01 (t. 2H), 3.63 (app t, 2H), 3.43 (app t. 2H), 3.25 (app t, 2H), 3.17 (app t, 2H), 2.11-2.03 (m, 2H), 1.80-1.71 (m, 2H), 1.53-1.45 (m, 2H), 0.98 (t, 3H). EXAMPLE 64 N-{4-(l,4-diazepan-l-yl)-2-((phenylsulfonyI)amino)phenyl)-3,5-dimethyl-4-iso.vazolesulfonamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-^butyloxycarbonyI-l,4-diazepan-l-yl)- phenyl}benzenesulfonamide and 3,5-dimethylisoxazolesulfonylchloride (53 mg, 0.269 mmol) to give 32 mg as purple solid. M+1 506.3 Calcd 506.15; 'HNMR 6 7.75-7.48 (m, 5H), 6.92 (d, IH), 6.59 (dd, IH), 6.28 (d, IH), 3.62 (app t, 2H), 3.41 (app t, 2H), 3.21 (app t, 2H), 3.12 (app t, 2H), 2.23 (s, 3H), 2.13 (s, 3H), 2.09-2.01 (m, 2H). EXAMPLE 65 N-{4-(l,4-diazepan-l-yl)-2-I(phenylsulfonyl)amino|phenyI}-5-fluoro-2-metbylbeDzeDesulfonamide hydrocbloride (Scheme 3) The compound was s>Tithcsized from of N-{2-amino-5-(4-/-butyIoxycarbonyI-l,4-dia2epan-l-yl)- phenyl {benzenesulfonamide and 5-nuoro-2-methylbenzcncsuironylchloride (56 mg, 0.269 mmolc) to give 7 mg as purple solid. M+1 519.3 Calcd 519.15; 'HNMR 6 7.7S-7.18 (m, 8H), 6.72 (d, IH), 6.45 (dd, IH), 6.34 (d, IH), 3.59 (app t, 2H), 3.38 (app t, 2H), 3.21 (app t, 2H), 3.13 (app t, 2H), 2.57 (s, 3H), 2.06-1.98 (m, 2H). EXAMPLE 66 N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyI)amino]ph€nyl}-4-(methylsulfonyl)benzenesulfonamide hydrochloride (Scheme 3) The compound was synthesized from of N-{2-amino-5-(4-r-butyloxycal•bonyl-l,4-diazepan-l-yl)- phenyl}benzenesulfonamide and 4-methylsulfonylbenzenesulfonylchloride (69 mg, 0.269 mmole) to give 38 mg as purple solid. M+1 565.3 Calcd 565.12; 'HNMR 5 8.08-7.48 (m, 9H), 6.76 (d, IH), 6.48 (dd, IH), 6.32 (d, IH), 3.61 (app t, 2H), 3.38 (app t, 2H), 3.21 (app t, 2H), 3.17 (app t, 2H), 3.14 (app t, 2H), 2.08-2.00 (m, 2H). EXAMPLE 67 N-{4-(l,4-diazepan-l-yl)-2-I(niethylsulfonyl)aminojphenyl}-N-methylbenzenesulfonamide (Scheme 3) N-methyI-{2-amino-5-(4-/-butyloxycarbonyl-l,4-diazepan-l-yI)- phenyl}-benzenesulfonamide (0.196 g, 0.426 mmol) was dissolved in pyridine (1.67 ml) followed by the addition of methyl sulphonylchloride (57 mg, 0.50 mmol) The ractiom was stirred at rt for 3 h. The mixture was concentrated and treated with trifluoroacetic acid (50%) in DCM for 30 min then concentrated and left for our HPLC Separation specialists. Further purification by column cheomatography DCM/ MeOH (9:1) afforded 32 mg, 0.058 ntmol in 13% yield of the title compound. 'H NMR (CD3OD) 5 2,17 (m, 2 H), 3,05 (s, 3 H), 3,14 (s, 3 H), 3,27 (m, 2 H), 3,38 (m, 2 H), 3,57 (m, 2 H), 3.77 (m. 2 H), 6,28 (d, 1 H), 6,41 (dd, 1 H), 7,06 (d, 1 H), 7.65 (m, 5 H); '^C NMR (CD3OD) 6 25.0, 38,7. 39,0, 45,1, 45,5. 45,8, 47,0, 100, 103.9, 108,1. 121,4.125, 126.128, 133,4, 136, 137,5. 148,5; M/ZCalc for (C19H26N4O4S2) 438.14 found M*+1=43 9.2 EXAMPLE 68 N-{5-(l,4-diazepan-l-yl)-2-[niethyl(phenylsulfonyl)amino)phenyl}-4-nietbylbenzenesulfonamide (Scheme 3) N-methyl- {2"amino-5-(4-/-butyloxycarbonyl-1,4-diazepan-1 -yl)- phenyl}-benzenesulfonamide (0.196 g, 0.426 mmol) was dissolved in pyiidine (1.67 ml) followed by the addition of p-methylphenyl-sulphonylchlride (88 mg, 0.50 mmol) the reaction was stin-ed at rt for 3h. The mixture was concentrated and treated with trifluoroacetic acid (50%) in DCM for 30 niin then concentrated and left for our HPLC Separation specialists. Further purificaction by flash column chromatography DCM / MeOH (9:1) afforded 0.110 g, 0.175 mmol in 40% yield of title compound. ^H NMR (CD3OD) 6 2,17 (m, 2 H),2,52, (s,3H), 3,0-3,4 (m, 7 H), 3,52 (m, 2 H), 3,74 (m, 2 H), 6,15 (d, 1 H), 6,41 (d, 1 H), 6,92 (s, 1 H), 7,5-7.80 (m, 6 H); M/Z Calc for(C25H3oN404S2) 514.1708 found M^ 514.1708. General method for the preparation of moDosulfonaniides EXAMPLE 69 N-(2-Aniino-4- lert-Butyl 4-(3-amino-4-nitrophenyl)-l-piperazinecarboxylate (1.5 g, 3.5 mmol) was dissolved in mcthanoI:THF (4:1). Raney-Ni (900 mg) was added followed by addition of hydrazine monohydratc (900 mg). The reaction was stirred at r. t. under N: atmosphere overnight. Starting material w as present. Raney-Ni (400 mg) was added and the reaction was stirred ovemighL The reaction was Hltered through celite pad followed by washings w^ith ethanol. The volatiles were evaporated to afford 93% of 2-amino-5-(4-t-buthylcaboxyl-l-piperaziny]) aniline. 2-amino-5-(4-t-buthylcaboxyl-l-pipera2inyl) aniline (150 mg, 0.382 mmol) was dissolved in CH2CI2 (2 mL). 3-fluorophenylsulfonylchloride (74 mg, 0.382 mmol), p>aidine (215 )LiL, 2.67 mmol) were added and the reaction was stined at room temperature for 2 hr. The reaction was quenched with NaHC03 (saturated aqueous solution), extracted with CH2CI2. The organic phase was dried (MgS04), filtered and concentrated to give an oil residue that was purified by flash column chromatography (Si02, CH3Cl:MeOH:NH3 9:1:0.4%) to afford ofN-[2-amino-4-(4-ten-butylcarboxyl-l-piperazinyl)-3 fluorobenzenesulfonamide (80 %). N-[2-amino-4-(4-tert-butylcarboxyl-l-piperazinyl)-3-fluorobenzenesulfonamide (110 mg) were dissolved in methanol (0.5 mL) followed by the addition of diethylether (2 niL). Ether/HCl gas was added till pH == 1. The reaction was stined at room temperature for 5 h to afford the title product as a white solid ^H NMR (niethanol-d3) 5 3.25-3.50 (m, 8H); 6.5 (d, IH); 6.75 (dd, IH). 7.0 (bs, IH); 7.3-7.6 (m, 4H); MS (posEI-DIP) m/z = 351.2 (M+H). EXAMPLE 70 N-(2-(ethylaniino)-4-(4-niethyl-l-piperazinyI)phenyll-3-fluorobenzenesuIfonaniide hydrochloride (Scheme 4) To a solution ofN-2-ethyl-4-(4-methyl-l-piperazinyl)-l,2-benzenediamine (0.200 g, 0.853 mmol) and pyridine (0.48 mL, 5.97 mmol) in DCM (8 mL) was added a solution of 3-fluorobenzenesulfonyl chloride (249 mg, 1.28 mmol) in DCM (2 mL). The mixture was stirred at room temperature for 16 hours. DCM (10 mL) was added and the mixture was washed with saturated aqueous NaHCO^. The organic layer was dried overNa2S04, filtered and concentrated. Column chromatography on A^Oj using EtOAc/5% McOH as eluent gave nvo products. First fraction contains 110 mg of N-[2-{ethyl[(3-fluorophcnyl)sulfonyI]amino}-4-(4-methyl-l-piperazinyl)phenyl]-3-fluorobcnzenesulfonamide hydrochloride. Second fraction contains 100 mg of N-[2- (ethylamino)-4-(4-meihyl-1 -piperazinyl)phenyl]-3-fluorobenzen€sulfonamid€ hydrochloride. Both products were converted to the HC!-salts. N-[2-(ethylamino)-4-(4-methyl-l-piperazinyl)phenyl]-3-fluoroben2enesulfonamide hydrochloride: 'H NMR (DMSO-rf(J) 5 11.24 (br s, ]H), 9.76 (br s, IH), 7.66-7.59 (m, IH), 7.56-7.50 (m, 3 H), 6.62 (app d, J=8.8 Hz, IH), 6.55-6.35 (m, 2H), 3.80-3.70 (m, 2 H), 3.46-3.40 (m, 2H), 3,15-2.96 (m, 6H), 2.76 (appd, J=4.4Hz,3H), 1.08 (tr, J=7.2 Hz,3H); 13CNMR(CD30D) 6 161.03 (d, JCF=248 Hz), 149.32, 142.13 (d, JCF=6.4 Hz), 140.72, 131.43 (d, JCF=7.4 Hz), 128.56, 123.22,119.93 (d, JcF=20Hz), 115.91, 113.86 (d,JcF=24 Hz), 107.78, 103.12,51.83,45.04,41.80,40.62, 12.88; AccMs (posES-FIA) found: 392.1672, calc: 392.1782; Ms (posES-FIA) m/z 393 (M+H). EXAMPLE 71 4-Chloro-N-|5-(4-methyM,4-diazepan-l-yl)-2-nitrophenyl]benzenesulfonaniide (Scheme 4) 4-chloroben2ene sulfonamide (3.5 g, 18.3 mmol) was added slowly to a suspension of sodium hydride (1.6 g, 55% suspension in mineral oil, 36.6 mmol) in anhydrous DMF (50 mL) under an atmosphere of nitrogen. The mixture was wanned to 40^C for 1 hour and 2,4-difluoronitrobenzene (2 mL) was added dropwise. This mixture was stirred at 60°C overnight. The cooled reaction mixture was poured into hydrochloric acid (1 N, 250 mL) and extracted with ethyl acetate (2 x 50 mL). The organic extracts were washed with water, dried over MgS04 and evaporated to give a yellow solid. The product was re-crystallized fix)m ethanol. Yield 2.4g (40%). 'H NMR (400 MHz, CDCI3) 6 6.85 (m, 1 H), 7.4S (AB, J= 8.3 Hz, 2 H), 7.56 (dd, 7= 10.01, 2.68 Hz, 1 H), 7.84 (AB, 7 = 8.3 Hz, 2 H). 8.21 (dd, 7 = 9.28, 5.61 Hz, I H), 10 (bs, 1 H). Calculated N S.47%, C 43.58%, S 9.70%, H 2.44%; Found N 8.54%, C43.89%. SIO.10%, H 2.76%. 4-Chloro-N-[5-nuoro-2- nitrophcnyl]bcnzenesuIfonamidc (Ig, 3mmol) and N-mcthylhomopiperazine (0.4mL) were heated together at 130 'C for 3 hours. The product was allowed to cool, dissolved in CH:Cl2 (50 mL) and washed w ith aqueous sodium bicarbonate. The organic phase was dried over MgSOa and evaporated to give 1.05 g of a yellow solid which was re-crystallized from lolucnc. Yield 0.65g (51%), 'H NMR(400MHz, CDOj^S 1.98 (q, 7= 5.62 Hz, 1 H),2.37 (s, 3 H), 2.52 (t, 7= 5.62 Hz, 2 H), 2.67 (t, 7= 5.12 Hz, 2 H), 3.55 (t, J- 6.35 Hz, 2 H), 3.60 (t, 7 = 5.12 Hz, 2 H), 6.34 (dd, J= 9.77, 2.68 Hz, 1 H), 6.86 (d, J= 2.6S Hz, 1 H), 7.43 (ab, J = 8.79 Hz, 2 H), 7.79 (ab, 7 = 8.79 Hz, 2 H), 8.01 (d, 7 = 9.77 Hz, 1 H), 11.6 (br s, 1 H). Calculated N13.19%,C 50.88%, H 4.98%; Found N 13.27%. C 50.99%, H 4,83%. EXAMPLE 72 N-|2-amina-5-(l,4-dlazepan-l-yI)phen}iJbenzenesuIfonamide (Scheme 4) N-{5-(4-t-butyloxycarbonyl-l,4-diazepan-l-yl)-2-nitro-phenyl}benzenesulfonamide (1.85 g, 3.8S mmol) was dissolved in EtOH/THF (1:4). Hydrazine (0.970 mL, 19.4 mmol) and Raney-Ni (0.180 g) was added. After 1 h at room temperature, the reaction was filtered through wet celite and the solvent was removed to afford 1.71 g of colorless oil. Boc-deprotection was achieved by dissolving N-{5-(4-t-bulyloxycarbonyl-l,4-diazepan-l-yl)-2-aTnino-phenyl}benzenesulfonamide (0.039 g) in small amount of MeOH and adding HCl/ether. The mixture was left at room temperature for 0.5 h after which the solvent was removed. Re-crystallization from MeOH/ether gave PHA-509592A (23 mg) as a white solid. M+1 347.4 Calcd 347.15; ^H-NMR 5 7.73-7.54 (m, 5H), 7.30 (d, IH), 6.84 (dd, IH), 5.78 (d, IH), 3.55 (app t, 2H), 3.32-3.26 (m, 2H), 3,13-3.08 (m, 4H), 2.03-1.92 (m, 2H). EXAMPLE 73 N-|2-ani!nO"5-(4-methyl-l,4-diazepan-l-yl)phenyl)benzenesulfonamide hydrochloride (Scheme 4) The above sulfonamide (0.6 g, 1.8 mmol) in methanol (50 mL) with Palladium (10% on C, 0.3g) was hydrogenated at atmospheric pressure for one hour during which lime 140 mL of hydrogen was consumed. The solution was filtered and evaporated to give colorless oil. The oil was dissolved in toluene (20 mL) and treated with a solution of hydrogen chloride in ethyl acetate. The product was triturated with cyclohexane, collected by filtration and dried. Yield 0.44g (73%). A portion was recrystallizcd from toluene:ethano1 1:1. 'H NMR (400 MHz, CDCb) 6 1.95 (br, 1 H), 2.17 (br. 1 H), 2.72 (s, 3 H). 2.80.3,65 (br iru 8 H). 5.92 (br, 1 H), 6.66 (dd. J = 2.69. 9.03 Hz, 1 H). 7.20 (d. J = 9.03 Hz, 1 H), 7.63 (t, 7 = 7.81 Hz, 2 H), 7.71 (t, y= 7.32 Hz, 1 H), 7.81 (d, J= 132 Hz, 2 H), 9.8 (br, 3 H), 11 (br s, 1 H). MS (ESI+) for C1SH24N4O2S m/z 360.1634 (M+f (Calculated 360.1620) EXAMPLE 74 IV-(4-lSitro-3-(l-piperazinyl)phenyI]benzenesulfonamide hydrochloride (Scheme 4) A mixture of difluoronitiobenzene (1.31 g, 8.21 mmol), Boc-piperazine (1.84 g, 9.8 mmol) and K2CO3 in DMF was stiixed at room temperature overnight. The mixture was filtered and the DMF was removed. The residue was dissolved in CH2CI2 and extracted with HCl (1M) three times. The organic layers were dried (MgSOa), filtered and the solvent was removed. Purification by column chromatography (Si02, CH2Cl2/heptane, 1:4) gave 1.14 g of yellow solid. 'H-NMR 5 7.90 (dd, IH), 6.77-6.69 (m, 2H), 3.60-3.57 (m, 4H), 3.03-3.00 (m, 4H), 1.46 (s, 9H); MS (posEI-DIP) m/z = Found: 34S.2 (M^ + Na^. NaH (17.2 mg, 0.43 mmol) was added to a solution of 4-(2-nitio-5-fluorophenyl)-l-(/- butyloxycarbonyl)piperazine (0.079 g, 0.215 mmol) and benzensulfonamide (0.044g, 0.280 mmol) in DMF. Tlie mixture was heated at 80°C over night and filtered. Purification by column chromatography (Si02, CH2Cl2/heptane, 1:4) gave 0.075 g ofN-[2-nitro-4-(t-butyloxycarbonylpiperazinyI)]phenyl]benzenesulfonamide of which 0.025 mg was Boc-deprotected by dissolving the compound in MeOH and adding HCl/ether. The mixture was stirred for 0.5 h after which the solvent was removed. Re-crystallization M^OH/ether gave 24.6 mg of a yellow solid. 'H-NMR 5 7.88 (app d, 3H), 7.63-7.52 (m, 3H), 7.07 (d, IH), 6.89 (dd, IH), 3.38-3.34 (m, 4H), 3.25-3.21 (m, 4H); MS (posEI-DIP) m/z = Found: 363.3 (M^ + EXAMPLE 75 N-(4-amino-3*(l-piperazinyl)pbenyl]benzeDesuironamide hydrochloride (Scheme 4) To a solution of N-[2-nitro-4-(t-butyloxycarbonylpipcrazinyl)]phcn>1] benzensulfonamide (50 mg, O.IOS mmol) in THF/EtOH 4:1 was added Rancy-Ni (5 mg) and hydrazine hydrate (27 ^L, 0.54 mmol). The mixture was stirred at room temperature for 6 h followed by filtration of the reaction mixture through wet Celite. Removal of the solvent and purification by column chromatography (Si02, CH2Cl2/heptane/MeOH, 4:5:1) gaveN-[2-amino-4-(t-butyloxycarbonyl-piperazinyI)]phenyi]-benzenesulfonamide. Boc deprotection was achieved by dissolving the compound in MeOH and adding HCl/ether. The mixture was stirred for 0.5 h after which the solvent was removed. Re-crystallization (MeOH/ether) gave a white solid that had to be purified by preparative HPLC to obtain 10 mg of the final product. 'H-NMR 6 7.66-7.45 (m, 5H), 6.78 (d, IH), 6.62 (d, IH), 6.50 (dd, IH), 3.39-3.35 (m, 4H), 3.02-2.99 (m, 4H); MS (posEI-DIP) m/z = Found: 333.0 (M^ + H"). 4-Chloro-3-nitrobenzenesulfonyI chloride, taken from a prepared stock solution, (1.78 mmol, 1.0 eq) in CH2CI2 (2 mL) was added to a solution of the appropriate R"-substituted anilines (R'-NH2 orR'-NH-R3 (1.62 mmol, 1.0 equiv.) in the presence of pjTidine (11.34 mmol, 7.0 equiv.). The reactions were stiired overnight at room temperature. Each mixture was washed with IN HCl followed by NaHCOa (sat. aqueous). Each organic phase was separated, dried (Na2S04), and filtered. CH2CI2 (2 mL) were added to each reaction mixture followed by the addition of K2CO3 (3.24 mmol, 2.0 equiv.) and homopiperazine or other amii>es of choice (i.e. R3) (2.11 mmol, 1.3 equiv.). Each reaction mixture was stirred at room temperature for 2 days. The volatiles were eliminated using a speed vac. Each reaction mixture was dissolved in a 4:1 EtOH:THF (25 mL) followed by addition of Rancy-Ni (0.5 mL susj>ension in EtOH) and hydrazine nionohydrate (8.10 mmol, 5.0 equiv.). Each mixture was stirred at room temperature for 2 da)^ and then filtered (Celite pad pretrcated with water). The filtrates were concentrated to give the crude products (LC-MS). An aliquot of each reaction mixture was purified by reversed phase preparative HPLC to give analytical samples which were converted to their HCl-salts and sent for pharmacological testing. EXAMPLE 76 3-Amino-4-(l,4-diazepan-l-yl)-N-(4-methoxyphenyl)benzenesulfonamidehydrochloridt (Scheme 5, Method 5) The compound was prepared from p-anisidine; (crude jaeld 0.238 g, yield analytical pure sample 0.137 g); 'H NMR (CDCI3) 5 7.43-7.39 (m, 2H), 7.37-7.33 (m, IH), 7.00-6.96 (m, 2H), 6.78-6.74 (m, 2H), 3.71 (s, 3H), 3.47-3.38 (m, 6H), 3.17-3.13 (m, 2H), 2.19-2.12 (m, 2H); MS (posESI) m/z = 377 (M+H*). EXAMPLE 77 3-Amino-4-(l,4-diazepan-l-yl)-N-(3-niethoxypbenyl)benzenesulfouamide hydrochloride (Scheme 5, Method 5) The compound v/as prepared from m-anisidine; (crude yield 0.546 g, yield analytical pure sample 0.020 g); 'H NMR (CDCI3) 6 7.71-7.67 (m, 2H), 7.51-7.47 (m, IH), 7.12-7.07 (m, IH), 6.72-6.69 (m, IH), 6.6S-6.65 (m, IH), 6.63-6.59 (m, IH), 3.71 (s, 3H), 3.48-3.40 (m. 6H), 3.18-3.14 (m, 2H), 2.21-2.15 (m, 2H); MS (posES-FIA) m/z = 377 (M+H*). EXAMPLE 78 3-Amino-4-(l,4-dia2epan-l-yl)-N-(2-niethoxyphenyI)benzenesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from o-anisidine; (crude yield 0.469 g, yield analytical pure sample 0.010 g); 'H NMR (CDCI3) 5 7.51-7.47 (m, 2H), 7.42-7.35 (m, 2H), 7.11-7.06 (m, IH), 6.89-6.82 (m, 2H). 3.57 (s. 3H), 3.47-3.38 (m, 6H). 3.17-3.12 (m, 2H), 2.20.2.13 (m, 2H); MS (posES-FL\) m'z = 377 (M+H*). EXAMPLE 79 3-Amino-4-(l,4-diazepan-l-yl)-N-(3-fluorophenyl)benzenesulfonaraide hydrochloride (Scheme 5, Method 5) The compound was prepared from 3-fluoroaniline; (crude yield 0.580 g, yield analytical pure sample 0.043 g); 'HNMR (CD3OD) 5 7.5S-7.49 (m, 2H), 7.41-7.35 (m. IH), 7.23-7.17 (m, IH), 6.93-6.87 (m, 2H), 6.79-6.73 (m, IH), 3.46-3.37 (m, 6H), 3.17-3.13 (m, 2H), 2.20-2.12 (m, 2H); MS (posES-FIA) m/z = 365 (M+H^. EXAMPLE 80 3-Amino-4-(l)4-diazepan-l-yl)-N-methyI-N-phenylbenzenesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from N-methylaniline; (cioide yield 0.590 g, yield analytical pure sample 0.010 g); 'HNMR (CD3OD) 5 7.41-7.36 (m, IH), 7.35-7.22 (m, 5H). 7.15-7.11 (m, 2HX 3.50-3.44 (m, 6H), 3.23-3.17 (m, 5H), 2.33-2.16 (m, 2H); MS (posEI) m/2 = 360(M+H^. ■ EXAMPLE 81 3-Amino-4-(l,4-diazepan-l-yI)-N-(4-isopropyIphenyI)benzenesuIfonaniide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-isopropylaniline; (crude yield 0.600 g, yield analjtical pure sample 0.015 g); 'H NMR (CD3OD) 5 7.4S-7.41 (m, 2H), 7.35-7.31 (m, IH), 7.10-7.05 (m, 2H), 7.03-6.98 (m, 2H), 3.47-3.35 (m, 6H), 3.17-3.12 EXAMPLE 82 3-Amino-4- The compound was prepared from p-toluidine; (crude yield 0.590 g, yield analytical pure sample 0.020 g); 'H NMR (CD3OD) 5 7.35-7.33 (m, IH), 7.31-7.27 (m, IH), 7.25-7.22 (m, IH), 7.03-6.94 (m, 4H), 3.47-3.30 (m, partly obscured by solvent signal, 6H), 3.16-3.11 (m, 2H), 2.23 (s, 3H), 2.17-2.10 (m, 2H); MS (posESI) nVz = 360 (M+H"). EXAMPLE 83 3-Amino-4-(l,4-diazepan-l-yl)-N-(2,5-dimethylphenyl)benzenesulfonamide hydrochloride (Scheme 5, Method 5) Th ecompound was prepared from 2,4-dimethylaniline; (crude yield 0.306 g, yield analytical pure sample 0.015 g); 'H NMR (CD3OD) 5 7.33-7.28 (m, 3H), 6.99-6.95 (m, IH), 6.93-6.88 (m, 2H), 3.50-3.37 (m, 6H), 3.19-3.14 (m, 2H), 2.22-2.13 (m, 5H), 1.96 (s, 3H); MS (posES-FIA) m/z = 375 (M+U"). EXAMPLE 84 3-Amino-N-(3-chlorophenyI)-4-(l,4-diazepan-l-yI)ben2enesuIfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 3-chIoroaniline; (crude yield 0.610 g, yield analytical pure sample 0.015 g); 'H NMR (CD3OD) 6 7.25-7.24 (m, IH), 7.19-7.14 (m, 3H), 7.12-7.10 (m, IH), 7.04-6.99 (m, 2H), 3.45-3.30 (m, partly obscured by solvent signal, 6H), 3.15-3.11 (m, 2H), 2.14-2.08 (m, 2H); MS (posES-FIA) m/z = 381 (M+H^. EXAMPLE 85 3-Amino-4-(l,4-diazepaD-l-yl)-N-(2-chlorophenyl)benzenesuifonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 2-chloro3niline; (crude yield 0.506 g, yield analytical pure sample 0.020 g); 'H NMR (CD3OD) 6 7.55-7.50 (m, IH), 7.40-7.20 (m. 5H), 7.15-7.10 (m, IH), 3.48-3.34 (m. 6H), 3.18-3.12 (m, 2H), 2.20-2.10 (m, 2H); MS (posEI) m'z = 381 (M+H*). EXAMPLE 89 3-Ainino-N-(4-trifluoro-phenyl)-4-(l,4-diazepan-l-yl)benzenesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-trifluoroaniline; (crude yield 0.319 g, yield analytical pure sample 0.013 g); 'H NMR (CD3OD) 5 7.53-7.45 (m, 2H), 7.27-7.22 (m, 3H), 7.13-7.08 (m, 2H), 3.43-3.30 (m, partly obscured by solvent signal, 6H), 3.14-3.09 (m, 2H), 2.12-2.06 (m, 2H); MS (posESI) m/z = 415 (M+H*). EXAMPLE 90 3-Ainino-N-(4-fIuorophenyl)-4-(l,4diazepan-l-yI)benzenesulfonaniide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-fluoroaniline; (crude yield 0.700 g, yield analytical pure sample 0.021 g); 'H NMR (CD3OD) 5 7.13-7.04 (m, 4H), 7.03-6.98 (m, IH), 6.97-6.91 (m, 2H), 3.45-3.30 (ni, partly obscured by solvent signal. 6H), 3.15-3.09 (m, 2H); MS (posEI) m/z = 365 (M+H*). EXAMPLE 91 3-Amino-N-(2-fluorophenyl)-4-(l,4diazepan-l-yl)benzenesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 2-fluoroaniline; (crude yield 0.646 g, yield analytical pure sample O.OSO g); 'H NMR(CD30D) 6 7.48-7.43 (m, IH). 7.36-7.34 (m, IH), 7.36-7.27 (m, IH), 7.25-7.21 (m, IH), 7.15-7.05 (m, 2H), 7.02-6.95 (m, IH), 3.46-3.34 (m, 6H), 3.17-3.12 (m, 2H), 2.16-2.10 (m, 2H); MS (posESI) m/z = 365 (M+H*). EXAMPLE 93 4- 4-Chloro-3-nitro-N-benzenesulfonamide (1.52 g, 4.87 mmol), K2CO3 (1.01 g, 7.3 mmol) and homopiperazine (0.5S5 g, 5.8 mmol) in CH3CN (100 mL) was heated to 70°C for 2h. The mixture was filtered and the solvent was removed. Column chromatography (CH2CL2/MeOH/heptane 4:1:5 x 0.2 % NH3) gave 1.34 g of 4-(l,4-diazepan-l-yl)-3"nitro-N-benzenesulfonamide together with 0.152 g of the dialkylated product. The product (0.040 g) was transferred to its HCl-salt to give 0.038 g of the final product. Anal. (C17H21CIN4O4S x O.5H2O) C, H, N.; MS (posESI) m/z = 377,4 (M+H^. EXAMPLE 94 3-Amino-4-(l,4"diazepan-l-yl)-N-phenylbeuzenesulfonamide hydrochloride (Scheme 5, Method 5) 4-(l,4-Diazepan-l-yl)-3-nitro-N-phenylbenzenesulfonamide (0.599 g, 1.6 mmol) was dissolved in EtOH/THF(l:4). Hydrazine (0,398 mL, 8.0 mmol) and Raney-Ni (0.060 g) were added. After 1 h at room temperature the reaction was filtered through wet celite and the solvent was removed. The product was transferred to its HCl-salt by dissolving it in MeOH and adding HCl/ether. The solvent was removed and re-crystallized from (MeOH/ether) to give 0.537 g of a white solid. Anal. (C17H21CIN4O4S x 1.5H20) C, H, N.; MS (posESI) nVz = 347.4 (M+H^. EXAMPLE 92 3-Aniino-4-(4-methyM,4-diazepan-l-yl)-N-phenylbenzenesulfonaraide (Scheme 5, Method 5) 4-Chloro-3-nitroben2enesulfonyl chloride (460 mg, 1.8 mmol) was added to a colorless solution of aniline (250 mg, 2.7 mmol) in CH2CI2 (10 mL) followed by pyridine (O.SO mL, 10.0 mmol). The resulting orange solution was stirred at room temperature for 30 minutes, after which time the mixture was concentrated under vacuum. Acidification with 2M aq. HCl followed by extraction using EiOAc and drying with Na2S04 followed by filtration through a plug of silica, gave 500 mg (62%) of 4-chIo^o-3-nit^o-N-phenylbcnzcncsuIfonamide. 'H NMR (CDCI3) 6 8.30 (d, 1H), 7.80 (dd. 2H), 7.55 (d, 1H). 7.20 (m, 5H). MS(negESI) m/z = 311(M- H"). Mvlethylhomopiperazine (258 mg, 2.3 mmol) was added to a solution of 4-chloro-3-nitro-N-phenylbenzenesu!fonaTnide obtained as above (500 mg, 1.6 mmol) in CH2CI2 (20 mL) followed by addition of K2CO3 (310 mg, 2.3 mmol). The reaction mixture was heated to reflux. After 2.5 h, the solution was concentrated under i vacuum. After adjusting to pH = 6, the product was exti-acted using EtOAc to give, after drying with Na2S04 and concentration, 450 mg (72%) of 4-(4-methyl"l,4-diazepan-l-yl)-3-nitro-N-phenylbenzenesulfonanlide as an orange oil. *H NMR (CDCI3) 5 S.15 (d, IH), 7.60 (dd, IH), 7.15 (m), 6.95 (d, IH), 3.45 (m, 2H), 3.30 (m, 2H), 2.75 (m, 2H), 2.60 (m, 2H), 2.35 (s, 3H), 1.95 (m, 2H). MS (posESI) m/z = 391(M+H'). To a solution of 4^(4.methyl- I 1,4-diazepan-l -yl)-3-nitro-N-phenylbenzenesulfonamide (225 mg, 0.58 mmol) in EtOH/THF (4/1, 25 mL) activated Raney-Ni (slurry in EtOH) and hydrazine monohydrate (142 }aL, 2.9 mmol) were added. After stirring for 30 minutes at room temperature, the mixture was filtered and the yellow solution concentrated to give yellow oil. The oil was dissolved in a mixture diethyl ether/EtOAc followed by addition of excess of HCl/ether. The resulting precipitate was filtered and washed with ether to give, after drying under vacuum at 40*^0, 88 mg (38%) of 3-amino-4-(4-methyI-l,4-diazepan-l-yl)-N-phenylbenzenesulfonamide as a beige solid. Mp 84.85°C. MS (posESI) m/z = 361 (M+H*). *H NMR (MeOH-d3) 6 7.85 (d, 2H), 7.60 (d, IH), 7.15 (m, 5H), 3.50 (m, 7H), 3.15 (m, 2H), 3.00 (s, 3H), 2.30 (m. IH), 2.20 (m, IH). Anal.(C,8H24N4S02.2HCl)C,H,N,S. EXAMPLE 98 3-Amino-N-(3-chlorophenyl)-4-(4-methyl-l-l-piperazinyl)benzenesulfonamide hydrochloride (Scheme S, Method 5) A mixture of 4-chloro-3-nitroben2enesulfonylchloride (Ig, 3.9 mmol), 3-chloroaniline (0.5 mL, 4.7 mmol) and pyridine (1.6 mL) in CH2CI2 (2 mL) was stirred at room temperature. The reaction was quenched with NaHCOi (sat aq solution, 30 mL x 3). The organic phase was separated, dried (MgSOa), and filtered. The volatiles were evaporated and the residue was purified by column chromatography (SiOj, pentancrElOAc, 4:1) to give 4-chloro-N-(3-chlorophcnyI)-3-nitrobcn2encsulfonamidc; MS (posESI) m/z« 349.2 (M+H*). 'H NMR (CDCh) 6 7.00-7.40 (m, 3H), 7.60-7.90 (m, 3H), 8.70 (bs, IH). 4-ChIoro.N- chloropheny])-3-nitrobenzenesulfonamide(0.45 g, 1.3 nimol),N-methylpiperazine (0.191 mL, 1.73 mmol) and K2CO3 (359 mg, 2.6 mmol) in CH3CN (2.5 mL) as the filtrated was concentrated to give a residue which was purified by column (Si02, CHClsiMeOH: NH3 9:1:0.4 %) to give 420 mg of N-(3-chlorophenyl)-4-(4-methyM-piperazinyl)-3-niti-obenzenesulfonamide (85 %). Purity >95 % according to HPLC analysis. The compound was dissolved in THF (1 mL) and ethanol (5 mL) was added. The solution was heated with Raney-Ni (50 mg) and hydrazine monohydrate (0.05 mL) overnight. The Raney-Ni was filtered (celite pad), the volatiles were evaporated and the residue was purified by column chromatography (Si02, CHChiMeOH: NH3 9:1:0.4 %). The product was isolated as hydrochloride salt by treatment with HCl gas in diethyl ether to yield 170 mg of final product (32 %). 'HNMR(DMS0-rf6) 5 7.25 (appt, IH), 7.15-7.17 (m, IH), 7.10-6.12 (m, 1H),7.00-7.10 (m, 4H); 3.43-3.45 (ni, 2H), 3.22-3.24 (m, 4H), 2.96-3.01 (m, 2H), 2.77-2.78 (s, 3H); MS (posESI) m/z = 380.1(M+H*). EXAMPLE 99 3-A!nino-N-(2-methoxyphenyn-4-(4-methyI-l-piperazinyl)benzenesuIfonannide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-ch!oro-3-nitroben2enesulfonylchloride (Ig, 3.9 mmol), 2-methoxyaniline (0.53 niL, 4.7 mmol) and pyridine (1.6 mL) in CH2CI2 (2 mL). 4-Chloro-N-(2-methoxyphenyI)-3-nitrobenzenesulfonamide (0.345 mg) was reacted with N-methylpiperazine (0.144 mL) to afford N-(2-methoxyphenyl)-4-(4-n^thyl-l-piperazinyl)-3-nitrobenzenesulfonamide which was treated with Raney-Ni and hydrazine monohydrate. The final product was isolated as its HCl salt 'H NMR (DMS0-rf EXAMPLE 100 3-Ainino-N-(2-niethox)phenyI)-4-(l-piperazinyl)benzenesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-chloro-3-nitroben2enesulfonyl chloride (1 g, 3.9 mmol), 2-methoxyaniline (0.53 mL, 4.7 nimol) and pyridine (1.6 mL) in CH2CL2 (2 mL). 4-Chloro-N-(2-methoxyphenyI)-3-nitrobenzenesulfonamide (0.345 g) was reacted with piperazine (0.111 g) to afford N-(2-methoxyph€nyl)-4-(piperazinyl)-3-nitrobenzenesulfonamide. This was then treated with Raney-Ni and hydrazine monohydrate. The final product was isolated as its HCl salt. *H NMR (DMS0-rf6) 5 7.18-7.20 (m, IH), 7.08-7.10 (m, 2H), 6.93-6.96 (m, IH), 6.91-6.93 (m, 2H); 6.84 (dt, IH), 3.56 (s, 3H), 3.22-3.27 (m, 4H), 3.00-3.02 (m, 4H); MS (posESI) m/z = 362,1 (M+H^). EXAMPLE 95 2-(l,4-diazepan-l-yl)-5-(4-morpholinylsulfonyl)aniline hydrochloride (Scheme 5, Method 5) A suspension of homopiperazine (0.196 g, 1.95 mmol), 4-[(4-chloro-3-nitrophenyl)sulfonyl]morpholine (0.461 g, 1.50 mmol) and K2CO3 (0.415 g, 3.00 mmoi) in CH3CN (10 mL) was stiued at 65 °C for 16 h. CH2CL2 (10 mL) was added and the mixture was filtered and concentrated. The crude product was purified by column chromatography on silica using CHCl3->CHCl3/10% MeOH + 0.4% aqueous ammonia to yield 0.546 g of the product as a yellow solid (yield 98%); 'H NMR (CDCI3) 5 8.13-8.07 (m, IH), 7.70-7.64 (m, IH), 7.16-7.12 (m, IH), 3.78-3.73 (m, 4H), 3.55-3.49 (m, 2H), 3.44-3.36 (m, 2H), 3.19-3.13 (ni, 2H), 3.06-3.00 (m, 6H), 2.05-1.95 (m, 2H) ; *^C NMR (CDCI3) 5 147.88,137.39, 131.60, 127,81, 122.66,118.02,66.23,54.45,51.02,49.30.48.27,46.16,29.46; MS(posES-FIA) m/z = 372 (M+H*). To a solution of l-[4-(4-morpholinylsulfonyl)-2-nitrophcnyl]-l,4-diazcpane (0.445 g, 1.20 mmol) in 30 mL of a 4:1 EtOH:THF solvent system was added Raney-Ni (100 mg suspension in EtOH) followed by hydrazine monohydrate (300 mg, 6.00 mmol). The mixture was stirred vigorously for 4 h and then filtered through celite that was prctreated with water. The filtrate was concentrated, and then re-dissolved in CH3CN, concentrated again and finally toluene was added and the mixture concentrated once more to give a brown solid. The crude product was purified by column chromatography (SiOj, CHCh/MeOH/NHa 9:1:0.4%) to give 0.365g (yield 89%) of the pure product as a solid. The free base was converted to its HCl salt; *H NMR {DMS0-rf5) 5 9.34 (s, 2H), 7.23-7.16 (m, 2H), 7.04-6.98 (m, IH), 3.65-3.60 (m, 4H), 3.35-3.20 (m, 6H), 3.11-3.04 (m, 2H), 2.86-2.80 (m, 4H), 2.09-1.99 (m,2); MS (posESI) m/z = 341 (M+H^. INTERJ^^EDIATE 17 4-Chloro-N-(2-methoxy-phenyl)-3-nltrobenzenesuIfonainide (Scheme 5, Method 5) 4-Chloro-3-nitrobenzenesulfonamide (1.73 g, 6.78 mmol) was dissolved in CH2CI2 (7.0 mL). o-Anisidine (1.00 g, 8.13 mmol) was added dropwise at room temperature, followed by a slow addition of pyridine (2.0 mL). After 16 h of continued stining, the reaction mixture was diluted with EtOAc (50 mL) and washed with 1 M HCl (3 x 50 mL). The organic phase was dried (MgSOa) filtered and evaporated to a brown solid, upon which re-crystallization from ethanol/water gave 2.22 g (95%) of the product as white crystals. *H NMR (CDCI3) 6 8.20 (s, IH), 7.80 (dd, IH), 7.56 (d, IH), 7.53 (d, IH), 7.13 (t, IH), 6.96 (t, IH), 6.76 (d, IH), 3.66 (s, 3H). The sulfonamide proton was not obsei^ved. INTERMEDL^TE 18 ^-Chloro-S-nitro-N-phenyl-benzenesulfonaniide (Scheme 5, Method 5) Two portions of 4-Chloro-3-nitroben2enesulfonamide (1.73 g, 6.78 mmol) were dissolved in CH2CI2 (7.0 mL) in reaction flasks. Aniline (757 mg, 8.13 mmol) was added drop-wise at room temperature, followed by slow additions of pyridine (2.0 niL). Aft^r 16 h of continued stirring, the reaction mixtures were diluted with ethyl acetate (50 mL) and washed with 1 M HCl (3x50 mL). The organic phases were dried (MgS04) and evaporated to brown solids, which upon re-crystallization from ethanol/water gave off-white solid of the product 2.04 g (96%): 'H NMR98%. General procedure for reactions between 4-Chloro-3-nitro-A^-aryl-benzenesulfonamid€s and amines (R3) (Scheme 5, Method 5) Solutions of InteiTOediate 17 (343 mg, 1.00 mmol) and Intermediate 12 (313 mg, 1.00 mmol) in CH3CN (5 mL) were treated with K2CO3 (276 mg, 2.00 mmol) and amines (R3) (1.30 mmol) and heated to 80°C for 16 h. The reaction mixtures were diluted with ethyl acetate (50 mL), washed with saturated Na2C03 (3x50 mL), dried (Na2S04) and-evaporated to products that could be used for the next step without purification. [NTERMEDIATE 19 N-^2-Methoxyphenyl)-4-(3-methyl-piperazin-l-yI)-3"nitrobenzenesulfonamide (Scheme 5, Method 5) A solution of Intermediate 17 (343 mg, 1.00 mmol) and K2CO3 (276 mg, 2.00 mmol) in CH3CN (5 mL) was treated with 2-methylpiperazine (130 mg, 1.30 mmol). After 16 h of stirring at 80°C, the reaction mixture was diluted with EtOAc (50 mL) and washed with saturated Na2C03 (aq) (3x50 mL). The organic phases were dried (Na2S04) and evaporated to give 398 mg of a yellow foam of the title compound (9S%). 'H NMR (CDCh) 5 8.16 (d, IH), 7.70 (dd, IH), 7.50 (d, IH), 7.06 (t, IH), 6.97 (d, IH), 6.91 (t, IH), 6.75 (d, IH), 3.69 (s, 3H), 2.92-3.17 (m, 6H), 2.61 (t, IH), 1.05 (d, 3H). The sulfonamide and amine protons were lot observed. [NTERMEDIATE 20 t-(Hexahydro-pyrrolo(l,2-aJpyrazin-2-yl)-N-(2-methoxyphenyI)-3-nitro-i>enzenesulfonaniide (Scheme 5, Method 5) A solution of Intermediate 17 (343 mg, 1.00 mmol) and K2CO3 (276 mg, 2.00 mmol) n CH3CN (5 mL) was treated with oclahydropyrroIo[I,2-fl]pyrazine (164 mg, 1,30 mmol). \ftcr 16 h of stirring at 80 **C, the reaction mixture was diluted with EtOAc (50 mL) and vashed with saturated Na;C03 (3 x 50 mL). The organic phases were dried (NajSOH) and r\'aporatcd to give 407 mg a yellow foam of the title compound (94%), 'H NMR(CDCIj) 5 ;.16(s. lH),7J0(dd, lH),7.50(d, IH),7.06(t, lH).7.00(d, 1H),6.91 (t, lH).6.75(d, IH). 3.69 (s, 3H), 3.02-3.33 (m. 5H), 2.80 (t, IH), 2.39 (t, IH), 2.18-2.22 (m, 2H), 1.76-1.85 (m, 3H), 1.37-1.40 (m, IH). The sulfonamide and amine protons were not observed. INTERMEDIATE 21 3-Nitro-N-phenyl-4-pipera2in-l-yI-benzenesulfonamide (Scheme 5, Method 5) The compound was prepared from Intermediate 18 and piperazine to give 362 mg bright orange solid (100%): 'H NMR (CDCI3, 400 MHz) 5 8.16 (d, IH), 7.68 (d, IH), 7.27 (t, 2H), 7.15 (t, IH), 7.08 (d, 2H), 7.01 (d, IH), 3.13 (t, 4H), 2.98 (t, 4H); MS (CI) 362.8 (M + H)'361.2 (M - H)'; Purity (HPLC, Hichrom 200x4.6 mm I.D.) 91%. INTERMEDIATE 22 4-(3-MethyI-piperazin-l-yl)-3-nitro-N-phenyl-benzenesulfonaniide (Scheme 5, Method 5) The compound was prepared from Intermediate 18 and 1-methylpiperazine to give 373 mg orange-brown solid (99%): 'H NMR (CDCI3, 400 MHz) 5 S.17 (s, IH), 7.68 (d, IH), 7.27 (t, 2H), 7.15 (t, IH), 7.08 (d, 2H), 7.00 (d, IH), 3.14-3.22 (m, 2H), 2.97-3.06 (m, 4H), 2.64 (dd, IH), 1.06 (d, 3H); MS (CI) 391.0 (M + Uf 389.4 (M - H)'; Purity (HPLC, Hichrom 200x4.6 mm I.D.) >95%. INTERMEDIATE 23 4-(4-Ethyl-piperazin-l-yl)-3-nitro-N-phenyI-benzenesulfooamide (Scheme S, Method 5) The compound was prepared from Intermediate 18 and 1-ethylpiperazine to give 386 mg orange foam (99%): 'H NMR (CDCI3,400 MHz) 6 8.19 (s, IH), 7.72 (dd, IH), 7.31 (t, 2H), 7.18 (t, IH), 7.11 (d, 2H), 7.04 (d, IH), 3.22 (bs. 4H). 2.60 (bs, 4H), 2.50 (q. 2H), 1.13(t, 3H); MS (CI) 377.0 (M + H)* 375.4 (M - H)"; Purity (HPLC, Hichrom 200x4.6 mm I.D.) >98%. INTERMEDIATE 24 4-(Hexahydro-pyrrolo(l,2-a]pyrazin-2-yl)-3-nitro-N-phenyl-benzenesulfonamide (Scheme 5, Method 5) The compound was prepared from Intermediate 18 and hexahydro-pyrrolo[l,2-a]2-pyi-azine 372 mg orange foam (92%): 'H NMR (CDCI3.400 MHz) 5 S.16 (s, IH), 7.67 (d, IH), 7.27 95%. INTERMEDIATE 25 4-(5-Methyl-2,5-diaza-bicycIo[2.2.1]hept-2-yI)-3-nitro-N-phenyl-benzenesuIfonamide (Scheme 5, Method 5) The compound was prepared from Intermediate 18 and 5-methyl-2,5-diaza-bicyclo[2.2.1]2-heptane to give 374 mg yellow solid (96^0): 'H NMR (CDCI3,400 MHz) 6 8.12 (d, IH), 7.58 (d, IH), 7.26 (t, 2H), 7.13 (t, IH), 7.07 (d, 2H), 6.76 (d, IH), 4.24 (bs, IH), 3.46-3.49 (m, 2H), 2.88 (d, IH), 2.80 (t, 2H); 2.33 (s, 3H), 1.89 (d, IH), 1.53 (bs, IH); MS (CI) 3S9.0 (M + H)*3S7.0 (M - H)'; Purity (HPLC, Hichrom 200x4.6 mm I.D.) >95%. INTERMEDIATE 26 4-(trans-2,5-Dimethyl-piperazin-l-yI)-N-(2-methoxyphenyI)-3-nitro-benzeaesulfonamide (Scheme 5, Method 5) The compound was prepared from Intermediate 17 and 4-(trans-2,5-dimethyI-piperazinc to give 409 mg of yellow solid resulted (97%): 'H NMR (CDCI3, 400 MHz) 5 7.94 (4 IH), 7.76 (dd, IH), 7.50 (dd, IH). 7.28 (d, IH), 7.10 (t, IH). 6.93 (t, IH), 6.73 (d, IH), 2.93-3.08 (m, 4H), 2.60 (dd, IH), 2.31 (dd.l H), 1.01 (d, 3H), 0.73 (d, 3H); MS (CI) 420.8 (M + H)*41S.8 (M - H)"; Purity (HPLC. Hichrom 200x4.6 mm I.D.) >95%. General procedure for reductioa of the amino groups (Scheme 5, Method 5) Solutions of the nitro compounds (0.25 mmol) in THF (10 mL) and methanol (2 mL) were treated with Raney-Ni (100 nig) and hydrazine monohydrate (120 |il, 2.5 mmol). After stirring at room temperature for 7 h, the suspensions were filtered through celite and washed with ethyl acetate and ethanol. Evaporation with HCl in ether gave the products. Some of tne products were without impurities, others had to be purified with HPLC ((YMC combiprep ODS-AQ, 50x20mm I.D.). EXAMPLE 101 3-Ainino-N-(2-metbo,\yphenyI)-4-(3-methyl-piperazin-l-yl)-benzenesulfonamide (Scheme 5, Method 5) The compound was prepared from A'-(2-methoxyphenyl)-4-(3-methylpiperazin-l-yl)-S-nitro-benzenesulfonamide to give 90 mg of the title compound (96Vo). 'H NMR (CDCI3) 5 7.44 (d, IH), 7.11 (d, IH), 7.10 (d, IH), 6.97 (t, IH), 6.85 (d, IH), 6.84 (t, IH), 6.72 (d, IH), 3.97 (bs, 2H), 3.62 (s, 3H), 2.91-3.06 (m, 5H), 2.56 (t, IH), 2.23 (t, IH), 1.41 (s, IH). 1.05 (d, 3H). The sulfonamide protons were not observed. '^CNMR (CDCI3) 5 149.4, 143.1, 141.4, 134.6, 125.4, 124.4, 121.0, 120.4, 119.2, 117.7, 113.2, 110.5,55.6,51.1,50.8,46.3,30.3, 19.6. MS (CI neg) 375 (M-H*), (CI pos) 377 (M+H"^. EX.A.MPLE 102 3-Amino-4-(hexahydro-pyrrolo(l,2-ajpyrazin-2-yl)-N-(2-methoxyphenyl)-benzenesulfonamide (Scheme 5, Method 5) The compound was prepared from 4-(hexahydro-pyrrolo[ 1,2-a]pyrazin-2-yl)-A^-(2-methoxyphenyl)-3-nitrobenzenesulfonamide to give 97 mg of the title compound (96%). 'H NMR (CDCb) 6 7.44 (d, IH), 7.12 (d, IH), 7.11 (d, IH), 6.97 (t, IH), 6.90 (d, IH), 6.84 (t, IH). 6.72 id, IH), 3.96 (bs, 2H), 3.62 (s, 3H), 3.19 (d, IH), 3.09 (app t, 3H), 2.76 (t, IH), 2.45(1. IH), 2.31-2.38 (m, IH), 2.10-2.21 (m,2H). 1.72-1.87 (m,3H), 1.21 (t, lH).The sulfonamide protons were not obser\cd. "CNMR(CDCb)5 149.4, 143.1,14I.4, 134.4, 125.4.124.7, 121.0, 120.5,119.5, 117.7, 113.2, 110.5, 55.6, 55.0, 53.3. 52.0,49.7,30.3,27.3, 212. MS (CI neg) 401 (M-H*). EXAMPLE 103 3-Aniino-N-phenyl-4-piperazin-l-yl-benzeDesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from N-phenyl-4-piperazin-l-yl-3-nitro benzenesulfonamide to give 15 mg yellow solid (IS%): 'H NMR (MeOD, 400 MHz) 5 7.57-7.61 (m, 2H), 7.40 (d, IH), 7.23 (t, 2H), 7.13 (d, 2H), 7.07 (t, IH), 3.45 (t, 4H), 3.20 (t, 4H); MS (CI) 333.0 (M + H)* 331.4 (M - H)'; Purity (HPLC, Hichrom 200x4.6 mm I.D.) 96%. EXAMPLE 104 3-Amino-4-(3-methyl-piperazin-l-yl)-N-phenyl-benzenesuIfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-(3-methyl-pipera2in-l-yl)-N-3-nitrophenyl-benzenesulfonamide to give 3i mg white solid (35%): 'H NMR (MeOD, 400 MHz) 5 7.57-7.62 (m, 2H), 7.35-7.41 (m, IH), 7.12 (t, 2H). 7.02 (d, 2H), 6.97 (t, IH), 3.53-3.58 (m, IH), 3.31-3.40 (m, 2H), 3.16 (t, 2H), 2.99-3.05 (m, IH), 2.79 (t, IH), 1.27 (d, 3H); MS (CI) 346.8 (M + H)"" 345.4 (M - H)'; Purity (HPLC, Hichrom 200x4.6 mm LD.) 100%. EXAMPLE 105 3-Aniino-4-(4-ethyI-piperazin-l-yl)-N-phenyI-benzenesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 3-Amino-4-(4-ethyl-piperazin-l-yl)-N-phenyl-benzenesuifonamide to give 32 mg white solid (33%): 'H NMR (MeOD, 400 MHz) 6 7.52-7.57 (m, 2H), 7.36 (d, IH), 7.12 (t, 2H), 7.01 (d, 2H), 6.96 (t, IH), 3.56 (d, 2H), 3.26(t, 2H). 3.17-3.23 (m, 4H), 3.09 (t, 2H), 1.31 (t, 3H); MS (CI) 361.0 EXAMPLE 106 3-Amino-4-(hexahydro-pyrrolo(l,2-a]pyrazin-2-yl)-N-phenyI-benzenesulfonamide hydrochloride (Scheme 5, Method 5) j The compound was prepared from 4-(hexahydro-pyn*oIo[l,2-a]pyrazin-2-yl)-N- pheny]-3-nitro-benzenesulfonamide to give 50 mg white solid (49%): *H NMR (MeOD, 400 MHz) S 7.63-7.69 (m, 2H), 7.47-7.52 (m, IH), 7.23 (t, 2H), 7.13 (d, 2U), 7.08 (t, IH), 3.08-3.78 (m, 8H), 2.12-2-35 (m, 4H), 1.79-1.88 (m, IH); MS (CI) 372.8 (M + H)^ 371.4 (M - H)' ; Purity (HPLC, Hichrom 200x4.6 mm I.D.) 100%. EXAMPLE 107 3-Amino-4-(5-methyl-2,5-diaza-bicyclo(2.2.1)hept-2-yI)-N-phenyl-benzenesuIfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-(5-methyl-2,5-diaza-bioyclo[2.2.1]hept-2-yl)-N-phenyl-3- nitrobenzenesulfonamide to give 40 mg red solid (40%): 'H NMR (MeOD, 400 MHz, major confomier at 300 K) 5 7.49-7.56 (m, 2H), 7.09-7.15 (m, 3H), 6.99-7.05 (m, 2H), 6.95 (t, IH), 4.39 (bs, IH), 4.30 (bs, IH), 3.89 (d, IH), 3.56 (bs, 2H), 3.09 (d, IH), 2.88 (s, 3H), 2.34 (d, IH), 2.20 (d, IH); MS (CI) 359.0 (M + H)*357.4 (M - H)"; Purity (HPLC. Hichrom 200x4.6 mm I.D.) 93%. EXAMPLE 108 3-Amino-4-(trans-2,S-dimethyl-piperazin-l-yl)-N-(2-methoxy-phenyI)-benzeoesulfonamide hydrochloride (Scheme 5, Method 5) The compound was prepared from 4-(trans-2,5-dimethyl-piperazin-l-yl)-N-(2-methoxy-phcnyl)-3-nitrobenzenesuIfonamid€ to give 60 mg white solid (61%): 'H NMR (^^cOD. 400 MHz) 6 7.54-7.58 (m. 2H), 7.45 (d. IH). 7.32 (d, IH), 7.02 (t, IH). 6.S1 (d, IH), 6.76 (t, IH), 3.54-3.57 (m, IH), 3.47 (s, 3H), 3.37 (d. IH), 3.30-3.34 (m, IH), 3.01 (t, 2H), 2.71 (t, IH), 1.23 (d, 3H), 0.77 (d, 3H); MS (CI) 390.8 (M + H)*389.4(M - H)"; Purity (HPLC, Hichrom 200.X4.6 mm I.D.) 96%. EXAMPLE 112 4-[4-(3,4-Dihydro-2H-quinoline-l-sulfonyl)-2-amino-phenyl]-Il,41diazepane ditrifluoroacedc acid (Scheme 5, Method 5) The compound was prepared from 1,2,3,4-tetrahydio-quinoline 4-chloro-3-nitro-benzenesulfonyl chloride and [l,4]dia2epane-l-carboxylic acid tert-butyl ester (430 ^1, 2.2 mmol) to give (63%) as a solid. *H NMR (CD3OD) 5 7.69-7.62 (m, IH), 7.16-6.98 (m, 5H), 6.94-6.89 (m, IH), 3.78-3.71 (m, 2H), 3.46-3.27 (m, 6H), 3.13-3.06 (m, 2H), 2.4S-2.40 (m, 2H), 2.16-2.05 (m, 2H), 1.69-1.58 (m, 2H); MS m/z (M+1) 387. EXAMPLE 109 2-(3-Aniino-4-(l,4Jdiazepan-l-yl-benzenesuIfonyl)-benzamide diacetic acid (Scheme 5, Method 5) The compound was prepared from 2-amino-benzamide, 4-chloro-3-nitro-benzenesulfonyl chloride and I,4]diazepane-l-carboxylic acid tert-butyl to give (1%) as an oil. 'HNMR(CD30D) S 7.68-7.57 (m, 2H), 7.43-7.36 (m, IH), 7.17-7.15 (m, IH), 7.10-7.02 (m, 3H), 3.44-3.25 (m, 6H), 3.12-3.05 (m, 2H), 2.14-2.02 (m, 2H); MS /;//j(M+I) 390. EXAMPLE 111 2-Il,4|Diazepan-l-yl-5-(3,4-dihydro-lH-isoquinoline-2-suIfonyI)-aniline dibydrochloride (Scheme 5, Method 5) The compound was prepared from 1,2,3,4-tetrahydro-isoquinoline, 4-chloro-3-nitro-benzenesulfonyl chloride and l,4]diazepane-l-carboxylic acid tert-butyl ester to give (93%) as a white solid. 'H NMR (DMSO) S 9.28 (s, 2 H), 7.12 (m, 7 H), 4.12 (s. 2 H), 3.20 (m, 8 H), 3.02 (t, y = 5.81 Hz, 2 H), 2.«6 (t, / = 6,07 Hz, 2 H), 2.00 (m, 2 H); MS m/z 387 (M+l). EXAMPLE 110 4-(4-(3-Fluoro-2-methoxy-phenylsulfanioyI)-2-ainino-phenyl]-(l,4]dia2epane ditrifluoroacetic acid (Scheme S, Method 5) The compound was prepared from 3-fluoro-2-methoxyaniline, 4-chloro-3-nitro-benzenesulfonyl chloride and l,4]dia2epane-l-carboxylic acid tert-butyl ester to give (43%) as a solid. 'H NMR (DMSO) 5 9.70 (s, IH), 8.79 (br s, 2H), 7.17-6.87 (m, 6H), 3.53 (s, 3H), 3.32-3.13 (m, 6H), 2.99-2.91 (m, 2H), 2.0I-1.S9 (m, 2H); MS m/z (M+1) 395. Legend to Scheme 2: i: Py, CH2CL2; ii: K2CO3, CH3CN, diamine (i. e. homopiperazine); iii: (B0C)20, THF, NaOH; iv: Raney-Ni, Hydrazine monohydrate, THF/ElOH; v: sulfonylchloride (Y-SO2-CI), Py, EtsN, CH2CL2; vi: HC! ether/MeOH INTERMEDIATE 27 tert-Butyl-4-(4-(aniIinosulfonyi)-2-DitropheDyl]-l,4-diazepane-l-carboxylate (Scheme 6, Method 6) Di-r€r/-butyl dicarbonate (0.921 g, 4.22 mmol) in THF (20.0 mL) was added to a solution of 4-(l,4-diazepan-l-yI)-3-nitro-N-phcny1benzenesulfonamidc (0.530 g, 1,40 mmol) and NaOH (0.140 g, 3.50 mmol) dissolved in THF:watcr(30 mL, 1:1). The solution was stirred at room temperature for 3 h. The mixture was neutralized with 5 N HCl and then the THF was removed under vacuum. The aqueous phase was extracted with CHCh (2 x 50 mL) and the combined organic layers were dried over Na2S04, filtered and concentrated. Purification via flash column chromatography (Si02, using CHCb/MeOH/ 9.75:0.25) gave a solid, which w^as triturated with EtOAc/pentane to give 0.605 g (90%) of the pure product. *H NMR (DMSO-rf(5) 6 9.S4 (br s, IH), S.01-7.98 (m, IH), 7.70-7.65 (m, 1H), 7.32-7.28 (m,lH), 7.26-7.20 (m, 2H), 7.13-7.08 (m, 2H), 7.07-7.02 (m, IH), 3.61-3.48 (m, 4H), 3.39-3.33 (m, 2H), 3.23-3.15 (m, 2H), 1.85-1.76 (m, 2H), 1.18 (s, 9H); MS (posESI-FIA) m/z = 477 (M+H"*). /er/-Butyl- 4-[2-nitro-4-(anilinosulfonyl)phenyl]-l,4-diazepane-l-carboxylate was reduced to the final product by treatment with Raney-Ni and hydrazine monohydrate using method C to yield 0.477 g (91%) ofthe free base; *HNMR(DMS0-rf6) 5 9.81 (s, IH), 7.24-7.18 (m, 2H), 7.13-7.08 (m, 3H), 7.02-6.92 (m, 3H), 4.99 (m, 2H), 3.53-3.45 (m, 4H), 3.02-2.94 (m, 4H), 1.86-1.79 (m, 2H), 1.42 (9H) ; MS (posESI-FIA) m/z = 447 (M+H^). EXAMPLE 97 4-(l,4-Diazepan-l-yI)-N-phenyI-3-((methylsulfonyl)amino]benzeDesulfonaniide hydrochloride (Scheme 6, Method 6) A mixture of tert-butyl 4-[2-amino-4-(aniIinosulfonyI)phenyl]-l,4-diazepane-l-carboxylaie (176 mg, 0.39 mmol), methylsulfonyl chloride (0.040 mL, 0.47 mmol) and pyridine (0.285 mL, 3.51 mmol) in CH2CL2 (5 mL) was stirred at room temperature overnight. The reaction mixture was quenched with NaHCOs aq (3 x 30 mL). The organic phase was separated, dried (MgS04) and filtered. The volatiles were evaporated followed by purification ofthe oily residue by chromatography (SiOi, hexane/EtOAc 4:1) to give 110 mg of tert-butyl 4- {4-(anilinosulfonyl)-2-[(methylsulfonyl)amino]phenyl} -1,4-diazepane-l -carboxylate (yield 58 %). 'H NMR (CDCI3) 5 7.90 -7.85 (m, IH), 7.50-7.43 (m, IH), 7.30-7.24 (m, 2H), 7,20-7.08 (m, 4H), 6.84-6.79 (m, IH), 3.65-3.51 (m, 4H), 3.12-3.06 (m, IH), 3.04-2.96 (m, 6H), 2.04-1.91 (m, 2H), 1.49 (s, 3H); MS (posEI-DIP) m/z - 524 (M+H*). tcrt-Butyl4-{4-(amHnosuIfonyI)-2-[(methylsulfonyl)amino]phcnyl}-l,4-diazepane-l-carboxyla(c (0.077 g, 0.147 mmol) was dissolved in MeOH. and ether saturated with HCl gas was added. The mixture was stirred at room temperature for 4 h and then concentrated. The crude solid was dissolved in a small amount of MeOH, and ether was added. The precipiiate was collected and dried to give 30 mg of the pure product as the HCl salt (yield 4S%): *H NMR PMS0-d6) 5 7.72-7.70 (m, IH), 7.46-7.42 (m, IH), 7.25-7.20 (m, SH), 7.14-7.09 (m, 2H). 7.03-6.99 (m, IH), 3.45-3.15 (m, partly obscured by solvent signal, HDO, 6H), 2.96 (s, 3H), 2.02-1.95 (m, 2H); MS (posES-FIA) m/z = 425 (M-hH^. EXAMPLE 96 4-(l,4-Diazepan-l-yl)-N-phenyl-3-((phenylsuIfonyl)aminoJbenzenesuIfonamide hydrochloride (Scheme 6, Method 6) To a solution of tert-butyl 4-[2-amino-4-(anilinosulfonyl)phenyl]-l,4-diazepane-l-carboxylate (0.268 g g, 0.599 mmol), pyridine (338 (iL, 4,19 mmol) and EtaN (337 ^L, 2.40 mmol), in CH2CI2 (S.O mL) was added benzenesulfonyl chloride (153 ^L, 1.20 mmol) in CH2CI2 (2 mL). The mixture was stirred at room temperature for 16 h. The reaction mixture was washed with saturated aqueous NaHCOa, dried with Na2S04, filtered and concentrated. The crude material was dissolved in EtOH (5 niL) and KOH (0.134 g, 4.0 equiv.) was added. TTie reaction was stirred at room temperature for 2 days. Water (5 mL) was added to the reaction mixture and most of the EtOH was evaporated under vacuum. The water phase was extracted with CH2CI2 (3x20 mL). The combined organic phases were dried with NazSOa, filtered and concentrated. The crude boc-protected material was dissolved in MeOH, and ether saturated with HCl gas was added. The mixture was stirred for 16 h and then concentrated to give 0.543 g of the crude product, which was purified by reversed phase preparative HPLC to give 0.153 g of the pure product as the acetic acid salt which was converted to the HCl-salt: 'H NMR (DMS0-d6) 5 10.25 (s, IH), 9.09 (br s, 2H), 7.68-7.5S (m, 4H), 7.54-7.48 (m, 2H), 7.46-7.42 (m, IH), 7.23-7.16 (m, 3H), 7.05-6.28 (m, 3H), 3.35-3.15 (m. partly obscured by solvent signal HDO, 6H), 2.81-2.75 (m, 2H), 1.92-1.85 (m, 2H); MS (posES-FL\) m/z = 487 (M+H"^. INTERMEDIATE 28 N-NaphthaIen-l-yl-3-nitro-4-piperazin-l-}i-benzenesuIfonamide, hydrochloride 4-Chloro-3-nitroben2enesulphonyl chloride (0.992 g, 3.87 mmol) was added to a solution of naphthalen-l-ylamine (0.665 g, 4.64 mmol) and pyridine (3.1 mL, 38.7 mmol) dissolved in DCM (5 mL). The solution was stirred at room temperature for 2 days and the volatiles were evaporated. The crude mixture was dissolved in EtOAc and the organic phase was washed with 1 N HCl, dried with MgS04, filtered and concentrated to give 1.1 g of naphthalen-1 -yl-3•nitro-4-chloro-benzenesulphonamide. Naphthalen-1 -yl-3-nitro-4-chloro-benzenesulphonamide was dissolved in CH3CN (10 mL) and piperazine (0.683 g, 7.93 mmol) was added. The mixture was stirred at 65 °C for 16 hours. The mixture was concentrated and the ciaide product was purified by flash chromatography on silica using DCM->DCM/MeOH (10%) + aqueous NH3 (0.4 as eluent to give 0.531 g of the free base which was converted to its HCl-salt. *H NMR (DMSO-do) 5 10.36 (brs, IH), 9.33 (brs, 2H), 8.12 (D, J = 2.1 Hz. IH), S.05-7.99 (m, IH), 7.94-7.S8 (ni, IH), 7.85-7.72 (m, 2H), 7.55-7.38 (m, 4H), 7.22-7.16 (m, IH), 3.40-3.30 (m, obscured by solvent signal, 4H), 3.24-3.12 (m, 4H); MS (posES-FIA) m/z = 413 (M+H). EXAMPLE 113 S-Amino-Z-chloro-N-naphthalen-l-yM-piperazin-l-yl-benzenesuIfonamide, bydrocblorlde To a solution of N-naphthalen-l-yl-3-nitro-4-piperaz in-l-yl-benzenesulfonamide (0.4602 g, 11.2 mmol) in 40 mL of a 4:1 EtOH:THF solvent system was added Raney-Ni (-1.0 mL suspension in EtOH) followed by hydrazine mono-hydrate (2.80 g, 56.0 mmol). The mixture was stirred vigorously for 3 hours and then filtered through celite. The filtrate was concentrated and the crude product was triturated with MeOH/ether. The product was converted to its HCI-salt. Yield (90%) as the free base. An aliquot was purified by preparative LC/MS. 'H NMR (DMS0-d6) 6 9,20-8.90 (brs 2H), 8.25-8.21 (m, IH), 7.90-7.86 Hz, IH), 6.91 (m, d, J = 8.4S Hz, IH), 3.32-3.25 (m„ obscured by solvent signal, 4H), 3.03-2.98 (m, 4H); MS (posES-FIA) m/z = 383. BIOLOGICAL TESTS The ability of a compound according to the invention to bind a S-HTe receptor, and to be pharmaceutically useful, can be detennined using w vivo and in vitro assays known in the art. (a) S-HTe Intfinsic Activity Assay Antagonists to the S-HTo receptor were characterized by measuring inhibition of 5-HT induced increase in cAMP in HEK 293 ceils expressing the human S-HTe receptor (see Boess et al. (1997) Neuropharmacology 36: 713-720). Briefly, HEK293/5-HT6 cells were seeded in polylysine coated 96-well plates at a density of 25,000 / well and grown in DMEM (Dulbecco's Modified Eagle Medium) (without phenol-red) containing 5% dialyzed Foetal Bovine Serum for 4S h at 37°C in a 5% CO: incubator. The medium was then aspirated and replaced by 0.1 ml assay medium (Hanks Balance Salt Solution containing 20 niM HEPES, 1.5 mM isobutylmethylxanthine and 1 mg/ml bovine serum albumin). After addition of test substances, 50 |il dissolved in assay medium, the cells were incubated for 10 min at 37°C in a 5% COz incubator. The medium was again aspirated and the cAMP content was determined using a radioactive cAMP kit (Amersham Pharmacia Biotech, BIOTRAK RPA559). The potency of antagonists was quantified by determining the concentration that caused 50% inhibition of 5-HT (at [5-HT]= 8 times EC50) evoked increase in cAMP, using the formula Ki.cfT IC5o/( 1+[5HT]/EC5o). The compounds in accordance with the invention have a selective affinity to 5-HT6 receptors with Kj values between 1 nM and 5 pM and they antagonized the 5-HT indiced increase of cAMP. There is correlation between the K* binding and the Ki^ff,cacy Moreover, the compounds show good selectivity (>I00 fold) against S-HT:^, 5-HT2b, S-HTjc, 5-HTu, 5-HTib- (bj In vivo assay of reduction of food intake For a review on serotonin and food intake, see Blundell, J.E. and Halford, J.C.G. (1998) Serotonin and Appetite Regulation. Implications for the Pharmacological Treatnient of Obesity. CNS Drugs 9:473-495. Obese (ob/ob) mouse is selected as the primary animal model for screening as this mutant mouse consumes high amounts of food resulting in a high signal to noise ratio. To further substantiate and compare efficacy data, the effect of the compounds on food consumption is also studied in wild type (C57BL/6J) mice. The amount of food consumed during 15 hours of infusion of compounds is recorded. Male mice (obese C57BL/6JBom-Lep°*' and lean wild-type C57Bl/6JBom; Bomholtsgaard, Denmark) 8-9 weeks with an average body weight of 50 g (obese) and 25 g (lean) are used in all the studies. The animals are housed singly in cages at 23±l^C, 40-60 % humidity and have free access to water and standard laboratoiy chow. The 12/12-h light/dark ..cycle is set to lights off at 5 p.m. The animals are conditioned for at least one week before start of study. The test compounds are dissolved in solvents suitable for each specific compound such as cj'clodextrin, cyclodextrin/methane sulfonic acid, polyethylene glycol/methane sulfonic acid, saline. Fresh solutions are made for each study. Doses of 30, 50 and 100 mg kg'^day"* are used. The purity of the test compounds is of analytical grade. The animals are weighed at the start of the study and randomized based on body weight. Alzet osmotic minipumps (Model 2001D; infusion rate S |il/h) are used and loaded essentially as recommended by the Alzet technical information manual (Alza Scientific Products, 1997; Teeuwcs and Yam, 1976). Continuous subcutaneous infusion with 24 hours duration is used. The minipumps arc cither filled with different concentrations of test compounds dissolved in vehicle or with only vehicle solution and maintained in vehicle prc-warmed to 37^C (approx. Ih). The minipumps are implanted subcutaneously in the neck/back region under short acting anesthesia (metofane/enflurane). This surgical procedure lasts approximately 5 min. It takes about 3 h to reach steady state delivery of the compound. The weight of the food pellets are measured at 5 p.m. and at 8 p. m. for two days before (baseline) and one day after the implantation of the osmotic minipumps. The weigh-in is performed with a computer assisted Mettler Toledo PR 5002 balance. Occasional spillage is corrected for. At the end of the study the animals are killed by neck dislocation and trunk blood sampled for later analysis of plasma dmg concentrations. The plasma sample proteins are precipitated with methanol, centrifuged and the supernatant is ti*ansferred to HPLC vials and injected into the liquid chromatography /mass spectrometric system. The mass spectrometer is set for electrospray positive ion mode and Multiple Reaction Monitoring (MRM with the tiansition m/z 316 => 221). A linear regression analysis of the standards forced through the origin is used to calculate the concentrations of the unknown samples. Food consumption for 15 hours is measured for the three consecutive days and the percentage of basal level values is derived for each animal from the day before and after treatment. The values are expressed as mean ± SD and ± SEM from eight animals per dose group. Statistical evaluation is performed by Kruskal-Wallis one-way ANOVA using the percent basal values. If statistical significance is reached at the level of p WHAT IS CLAIMED IS: 1. A compound of the formula ([) —^ * —^' • • * . (a)K (c) C1-6aikoxv. (d) straight or branched Ci.6 hydroxyalkyl. (e) straight or branched C1-6 alkylhalides; or (f) a group .Ar; .*\r is (a) phenyl, (b) l-naphthyl (c) 2-naphthyI, (d) benzyl, (e) cinnamoyl, (f) a 5 to 7-membered, partially or completely saturated, heterocyclic ring containing 1 to 4 heteroatoms, selected from oxygen, nitrogen and sulfur, or (g) a bicyclic ring system consisting of two heterocyclic rings as defined under (f), or a bicyclic ring system consisting of one benzene ring and one heterocyclic nng as defined under (f); alternatively, R and R are linked to form a group (CH:)20, (CH:)40, or (CH2)3-5 in fonmula (lb); optionally, the group Ar is substituted with (a) Y, or (b) a 5 to 7-membered, partially or completely saturated, heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; Yis (a)H, (b) halogen, (c) C:-o alky], (d) CF3, (e) hydroxy, (f) Ci-^alkoxy, (g)Ci^alkenyl; (h) phenyl; (i) phenoxy, (j) benzyloxy, (I) OCF3, (m) CN, (n) straight or branched C1-6hydroxyalkyl, (0) straight or branched C1-6alkylhalides, (p)^fH2, (q) NHR^ (r) NR^R^ (s) NO2, (u) NHS02R'\ (v) NR^COR'. (ab) S(0)nR"; wherein n is 0, 1, 2 or 3; R' and R"* are independently: (a)-S02R', (b) H, (c)C,.6alkyl, (d)Ci-C3alkenyl, (e)Ci-C3alkylary], (0 Ar as defined above for R^, (g) -C(=0)R", (h) -C(0)NR"R(i)-C(S)NR'R~. (j) -C0:R'; (k) -C(S)R'; (1) straight or branched C\.r, hydrcxya'ikyi. or (m) straight or branched C:.^ alkyihalides: alternatively, R' and R"* are linked to form a group (CH:);0, (CH2)^0, or (CH:)3.5 in formula (lai: R' is selected from the group consisting of the following chemical groups: R' and R7arc independently (a) H, (b)C,-6alkyl, (c) C-^.y cycloalkyl, or (d) Ar, as defined above for R'; alteniatively, R^ and R'^ arc linked to form a group (CH:):©, (CH2)40 or (CH2)3.5; R^is (a)H, or (b)C,.oaIkyl. 2. A compound according to claim I wherein R is a group Ar; A-r is (a) phenyl, (b) 1-naphthyl, (c) 2-naphthyL or (f) a 5 to 7-membered, panially or completely saturated, heterocyclic ring containing 1 to 4 heteroatoms, selected from oxygen, nitrogen and sulflir; the group .Ar is substituted with Y, wherein Y is (a)H, (b) halogen, (c)C1-6alkyl, (d) CF3, (f)C1-6alkoxy, (g)Ci-4alkenyl; (h) phenyl; (1) 0CF3, or (n) straight or branched C1-6 hydroxyalkyl. 3. A compound according to claim 1 or 2, wherein 4. A compound according to any one of claims 1 to 3, wherein R^ is -SO2R . 5. A compound according to any one of claims 1 to 4, wherein R and R'^ are independently H, methyl or ethyl. 6. A compound according :o my or.e of claims 1 lo 5. wherein R' is selected from the group consisting of the following chemical groups: 7. A compound according to any one of claims I to 6, wherein R and R^ are independently (a) H, (b)Ci^alkyl, (c) C3.7 cycloalkyi, or (d)Ar. 8. A compound according to claim 1, which is the compound N-[2-{ethyl[(3-fluorophcnyl)sulfonyl]amino}-4-(4-mcthyM-piperazinyl)phenyl]-3-fluorobcnzenesulfonamide, N-[2-[ethyl(phenylsulfonyl)amino]-4-(4-mcthyl-l-piperazinyl)phenyl] benzenesulfonamide, 3-fluoro-N-[2-{[(3-fluorophenyl)sulfonyl]amino}-4-(4-methyl-l-piperazinyl) phenyl]benzenesulfonamide, N-{5-(4-methyl-l-piperazinyl)'2-[(8-quinoHny!sulfonyl)amino]phenyl}-7- quinolinesulfonamide, N-[2-chloro-4-({4-(4-methyl-l-piperazinyl)-2-[(phenylsulfonyl)amino]anilino} sulfonyl)phenyl]acetamide, 3,4-dimethoxy-N-{4-(4-methyI-l-piperazinyI)-2-[(phenylsulfonyl)amino]phenyl} benzenesulfonamide, 3-methoxy-4-methyl-N-{4-(4-mcthyl-l-piperazinyl)-2-[(phenylsulfonyl)amino] phenyl} benzenesulfonamide. 4-methyl-N-{4-(4-methyl-!-piperazinyl)-2-[(methylsulfonyI)aminojphenyl; benzenesulfonamide, 3,4-dimethoxy-N-{4-i4-me:hyi-l-piperazinyl)-2-[(methylsuifonyl)amir.o]phenyl} benzenesulfonamide, 3-cyano-N-{4-(4-meihyM-piperazinyI)-2-[(methylsulfonyl)amino]phenyI} benzenesulfonamide, N-{4-(l-piperazinyI)-2-[(phenylsulfonyl)amino]phenyl}-l-naphthalenesuIfonamide, 5-(dimethylamino)-N- {4-( I -piperazinyl)-2-[(phenylsulfonyl)amino]phenyl} -1 - naphthalenesulfonamide, N-[2-[(phenylsuifonyl)amino]-4-(l-piperazinyl)phenyl]-8-quinolinesulfonamide, 2,4,6-trimethyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide, 4-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide, N-[2-({[(E)-2-phenylethenyl]sulfonyl}amino)-5-(l-piperazinyl)phenyl] benzenesulfonamide, 2,5-dimethoxy-N-[2-[(phenylsuIfonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide, 2-methyl-N-[2-[(phenylsulfonyI)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide, 2,4-difluoro-N-[2-[(phenylsulfonyl)amino]-4-{ 1 -piperazinyl)phenyl] benzenesulfonamide, 4-butoxy-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl]benzenesulfonamide, 3,5-dimethyl-N-[24(phenyIsulfonyl)amino]-4-(l-pipera2inyl)phenyl]-4-isoxazoIesulfonaniid 5-fluoro-2-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyi)phcnyl] bcnzenesulfonamide, 4-(rnethylsulfonyl)-N-[2-[(phenylsulfonyl)amino]-4-(I-piperazinyl)phenyl] benzenesulfonamide, 2-(methylsulfonyl)-N-[2-[(phcnylsu!fonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide, 2-methoxy-4-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-piperazinyl)phenyl] benzenesulfonamide, 4-methoxy-2-methyl-N-[2-[(phenylsulfonyl)amino]-4-(l-pipcrazinyl)phenyl] benzenesulfonamide, N-[2-amino-4-(l-piperazinyl)phenyl]-3-nuorobenzcnesuIfonamide, N-[2-(ethylamino)-4-(l-piperazinyl)phenyl]-3-nuorobenzenesulfonamide, N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)aminojphenyl}benzenesulfonamide hydrochloride N-(4-( 1,4-diazepan-1 -yl)-2- {[(3-nuorophenyl)suI fonylj-amino} phenyl )-3 -fluorobenzenesulfonamide hydrochloride N-{5-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]pheny:!-N-ethy!ber.zenesulfonamide hydrochloride N-{5-(l,4-diazepan-l-yl)-2-[(methylsulfonyl)amino]phenyi}benzenesulfonamide hydrochloride N-{5-( 1,4-diazepan-1-yl)-2-[(ethylsulfonyl)amino]phenyl}benzenesulfonamide hydrochloride N- {4-( 1,4-diazepan-l -yl)-2-[(phenylsulfonyl)amino]phenyl} [ 1,1 '-biphenyl]-4-sulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(phenylsulfonyl)amino]phenyl} -2, i ,3-benzoxadia2ole-4-sulfonamide hydrochloride N-{4-(1^4-diazepan-I-yl)-2-[(phenylsulfonyl)amino]phenyl}-2-naphthalenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(methylsulfonyI)amino]phenyl}benzenesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[methyl(methylsulfonyl)amino]phenyl} benzenesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(methylsulfonyI)amino]phenyl} -N-methylbenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[methyl(phenylsulfonyl)amino]phenyl}ben2enesulfonam^ hydrochloride N-{4-( 1,4-diazepan-1-yl)-2-[( methylsulfon\i )arnino]phenyl} -1-naphthalenesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(methylsulfonyl)amino]phenyl J -2-naphthalenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(methylsulfonyl)amino]phenyl}-4'fluoroben2enesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(methylsulfonyl)amino]phenyl} -4-nitrobenzenesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(methylsul fonyI)amino]phcnyl} -3- (trifluoromethyl)benzenesulfonamide hydrochloride N-{4-( 1,4-diazepan-1-yl)-2-[(mcthylsLilfonyl)amino]phenyl}-2-methylbcnzencsulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[(methyIsulfonyI)amino]phenyl; -i- (trifiuoromeihoxy)benzenesulfonamide hydrochloride N-{4-(L4-diazepan-l-y!)-2-[(mcthyl5ulfonyI)amino]pher.yi;-r\5-dimethyI-4-isoxazolesulfonamid hydrochloride N-{4-( 1.4-dia2epan-1-yl)-2-[( methylsulfonyl)arnino]phenyI;--3-rneihoxybenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(methylsulfonyl)aniino]phenyl}-l-methylbenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[ethyl(methylsulfonyl)amino]phenyl}-4-methyIbenzenesulfonamide hydrochloride N- {4-( 1,4-diazepan-1 -yl)-2-[ethyl(methylsulfonyl)amino]phenyl} -3,4- dimethoxybenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[ethyl(methylsulfonyl)amino]phenyl}-7-quinohnesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[methyl(methylsulfonyl)amino]phenyl}-4-methylbenzenesulfonamide hydrochloride N-.j4.(l,4-diazepan-l-yl)-2-[methyl(methylsulfonyl)amino]phenyl;-l-naphU^ hydrochloride N.{4-(1^4-diazcpan-l-yl)-2-[methy!(nieihylsultb!rvijanuno]phcnyl;-5-(:^pvTidin thiophencsulfonamidc hydrochloride ]\\{4-(1^4-diazepan4-yl)-2-[(phenylsidfony!)amino]phcnyl!-l-napiithalenesulfonarnide hydrochloride N-j4.(1^4-diazepan-l-yl)-2-[(phcnylsu!fonyl)am!no]phenyl}-5-(dirnethylarnino)-l- naphthalenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenyIsuironyl)amino]phcnyl[-8-quinotinesulfonamide hydrochloride N-{4-(l,4-diazcpan-l-yI)-2-[(phenylsuJfony])amino]phcnyll -2,4,6-trimcthylbenzcnesulfonamide hydrochloride N-{4-(l,4-diazcpan-l-yi)-2-[(pheny!sulfonyl)amino]pheny!j-4-rnethylbenzencsuironamide hydrochloride N-[5-{l,4-diazepan-l-yi)-2-(;[(E)-2-pheny!e:her:yiisulfonyi;am!r:omhenyl]bcnzenesul^^ hydrochloride N-{4-(I,4-diazepan-l-yl)-2-[(phenyl5ul:or.y:jarr:ino]pheny!I -2.5-dirnethoxybenzenesulton hydrochloride N'-{4-(l,4-diazepan-l-yI)-2-[^phenyisu!fonyl)aminojphenyi;-2-rnerhylbenzenesulfonarnide hydrochloride 4-butoxy-N-{4-(l,4-diazepan-l-yl)-2-[(phenyisu!fonyl)aminolphenyl[benzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyi)amino]phenyl}-3,5-dirnethyl-4-isoxazolesulfonarnide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]phenyl}-5-fluoro-2- methylbenzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(phenylsulfonyl)amino]phenyl}-4- (methylsulfonyl)benzenesulfonamide hydrochloride N-{4-(l,4-diazepan-l-yl)-2-[(methyIsulfonyl)amino]phenyl}-N-methyiben2enesulfonainide hydrochloride ^j, {5-( 1,4-diazepan-l-yl)-2-[methyl{pheny!su!fonyr)amino]phenyl}-4-methyl^ hydrochloride 3-amino-4-(l,4-diazt:pan-l^vi)-N-(4-mcthox>phenyl)bcnzenesulfonamide hydrochloride 3-aniino-4-(l,4-diazcpan-I-yIj-N-(3-methoxvphcn>'l)benzenesu!fonarnidc hydrochloride 3-amino-4-(l,4-diazepan-l-yl)-N-(2-mcthoxvphenyl)benzenesu!fonamide hydrochloride 3-amino-4-{ 1,4-diazepan-1 -yl)-N-(3-fluoropheny!)bcnzenesu!fonamide hydrochloride 3-amino-4-(l,4-dia2epan-l-yl)-N-mothyi-N-phenylbenzenesuIfonamide hydrochloride 3-amino-4-(l,4-diazepan-l-yl)'N-(4-isopropylphcny!)benzenesulfonamide hydrochloride 3-amino-4-(l,4-diazepan-l-yl)-N-(4-methylphenyl)bcnzcnesulfonamide hydrochloride 3-amino-4-(l,4-diazepan-l-yI)-N-(2,5-dimethylphenyl)benzenesulfonamide hydrochloride 3-amino-N-(3-chlorophcnyI)-4-(l,4-diazepan-l-yl)bcnzcnesuironamidc hydrochloride 3-amino-N-(2-chlorophenyl)-4-{K4-diazepan-l-yl)benzcnesulfonamidc hydrochloride 3-amino-N-(2,4-dichlorophenyI)-4-(I,4-diazepan-I-yl)bcnzcncsulfonamidc hydrochloride 3-amino-N-(2-methy!-5-chIoro-phenyI)-4-( !,4-dia-^epan-I-yl)benzcncsulfonamide hydrochloride 3-amino-N-(2-methy!-3-chioro-pnenyl)-4-(I,-^-diazepan-!-yl)bcnzenesuIfonaniide hydrochloride 3-amino-N-(4-triiluoro-pher//; --^-f I ,--diazepan-1 -yl ibenzenesulfonamide hydrochloride 3-amino-'N-(4-fiuoroDhenvrf-4-( I,4-uiazeDan-!-vl)benzenesulfonamide hvdrochloride 3-amino-N-(2-fiuorophenyri-4-( 1.4-diazepar.-I-yi)beri2enesulfonamide hydrochloride 3-amino-4-(4-meihyl-l,4-diazepan-l-yl)-X-phenylbenzenesulfonamide hydrochloride 3-amino-4-(l,4-diazepan-l~yl)-N'-phenylbenzenesulfonamide hydrochloride 2-(l,4-diazepan-l-yI)-5-(4-morphoIinylsulfonyl)phenylamine hydrochloride 4-(l,4-diazepan-l-yI)-N-phenyi-3-[(j)henylsulfonyl)arnino]benzenesulfonamide hydrochloride 4-(l,4-diazepan-l-y!)-N--phenyI-3-[(methyIsulfonyI)arTiino]berizenesulfonamide hydrochloride 3-arnirio-N-(3-chIorophenyl)-4-(4-rnethyM-piperazinyl)benzenesulfonamide hydrochloride 3-aniino-N-(2-rnethoxvphenyl)-4-(4-methyl-l-piperazinyl)beiizenesuIfonamide hydrochloride 3-amino-N-(2*methoxyphenyi)-4-( 1 -piperazinyl)beazenesulfonamide hydrochloride 3-aniino-N-(2-methoxyphenyl)-4-(3-methyl-I-piperazinyl)benzenesulfonamide hydrochloride 3-Amino-4-(hexahydro-pyrrolo[l,2-a]pyrazin-2-yl)-A-(2-niethoxyphenyl)-beruenesulfonar^ hydrochloride 3-Aniino-X -phcnyl-4-pipera2in-I-yl-benzenesulfonainide hydrochloride 3-An^no-4-(3-mcthy^pipe^azir^l-y!)-N-pheny!-bcnzencsu!fonamldc hydrochlonde 3-An-iino-4-(4-ethyl-piperazin-l-yl)-N-pheny!-bcnzcncsuironamidc hydrochloride 3-AnTino-4Mhexahydro-p\Tro!o[l,2-a]pyrazin-2^vI)A'-phenyl-benzencsu!fonamide hydrochlonde 3-Amino-4-(5-methyl-2,5-d!aza-bicyclo[2.2.1]hcpt--2-yl)-N-phenyl-bcnzenesulfonamide hydrochloride 3-Amino-4-(trans -2,5-dimethyl-p!perazin-lylj-N-(2mcthoxy-phenyl)ben2enesulfonamidc hydrochloride 2-(3-Amino-4-[l,4]diazepan-l-yl4:)cnzcnesulfonyl)-benzamide diacetic acid 4~[*^'(3-Fluoro-2-methoxy-phcnylsulfamoyl)-2-arriino-phenyl]-[l,4]diazepane ditrifluoroacetic acid 2~[l,4]Diazcpan-l-yIo-(3,4-dihydro-lH-isoquinolinc-2-suironyl)-anilinedihydrochloride 4-[4-(3,4-Dihydro-2H-quinoIinc-l-sulfonyl)-2-aniino-phcnyl]-[l,4]diazepane ditrifluoroacetic acid 3-Amin()-2-ch!oro-N-naphlhalcn-l-y!-4-pipcra/in-!-yl-bcnzenesulfonamide, hydrochloride 9. A process for the preparation of a compound according to an}' one of claims 1 to S corriprising: (a) introducricn of a cyclic d;amine mlo halogen and nitro substitu^.ed ber^ene under mild and basic conditions; (b) reduction of Uie nitro to the corresponding amine; (c) s'vTnmetric or assmmetric sulfonylation of the amine by a 5'aifon>Ich:onde; (d) introduction of groups R- and R" by alkylation procedure in basic conditions. 10. Aphairnaceutical formulation containing a compound according to any one of claims 1 to S as an active ingredient, in combination with a pharmaceutically acceptable diluent or carrier. 11. A method for the treatment or prophylaxis of obesity or type II diabetes, comprising administering to a mammal in need of such treatment an effective amount of a compound of any one of claims 1 to S. 12. A method for modulating 5-HT6 receptor activity for the treatment or prophylaxis of obesity or type 11 diabetes, comprising administering to a mammal in need thereof an effective amount of a compound of any one of claims 1 to 8. 13. A compound according to any one of claims 1 to 8 for use in the treatment or prophylaxis of obesity and^or t>pe 11 diabetes. i 14. Use of a compound according to any one of claims 1 to 8 for the manufacture of a medicament for use in the treatment or prophylaxis of obesity and/or type 11 diabetes. 15. A phamiaceutical formulation for use in the treatment or prophylaxis of obesity and/or type II diabetes wherein the active ingredient is a compound according to any one of claims I to 11. 16. A compound of the formula ([[) or a pharmaceiitically acceptable salt thereof, wherein R\ R'- and R" are H; or two of R', R" and R' are H; and the remaining of R', R'" and R"* is (a) -NH:, (b) -NHR^ (c) -NR'^R', (d) -N(CO)R^ (e) -N(CS)R^ or (f)-NO:; R'° is a group R"* as defined for the formula (I) in claim 1; R" is a group R' as defined for the formula (I) in claim 1; R' is (a) homopiperazine, (b) methylhomopiperazine, or (c) a group R^ as defined for the formula (I) in claim 1, wherein R8 is as defined for the formula (I) in claim 1; and Y is as defined for the formula (I) in claim 1, and each of R^ and R"^, independently, is as defined for the formula (I) in claim 1. ' 17. A compound according to claim 16 wherein R is (a) homopiperazine, (b) methylhomopiperazine. or and RSS (a) H, or (b) Ci.6 alkyl, in particular methyl; with the proviso that only one of R^ R'" and R^'^is -NH:, -NHR^ -NRV, -N(CO) R^ -N(CS) R\ -NO2; the other ones are H, 18. A compound according to claim 16, which is the compound 4-chloro-N-[5-(4-methyl-1,4-dia2epan-1 -yl)-2-rutrophenyI]berLzenesuIfonaniide, N-[2-aminoo-(I,4-d!azepan-.l-yl)phenyl]benzenesulfonamide, N-[2-amino-5-(4-methyl-l,4-diazepan-l-yI)phenyl]benzenesulfonamide, N-[4-nitro-5-(piperazinyl)phenyl]benzenesulfonamide, or N-[4-amino-5-(ptperazinyl)phenyl]benzenesulfonamide. 19. A process for the preparation of a compound according to any one of claims 16 to 18 comprising: (a) introduction of a cyclic diamine into halogen and nitro substituted benzene under mild and basic conditions; (b) reduction of the nitro to the corresponding amine; (c) selective introduction of a sulfonylamide group by a sulphonylchloride reacting with the amine; (d) introduction of a sulfonylamino group by aromatic nucleophilic substitution. 20. A pharmaceutical formulaiion containing a compound according to any one of claims 16 to 18 as an active ingredient, in combination with a pharmaceutically acceptable diluent or carrier. 2 L A method for the treatment or prophylaxis of obesity or type II diabetes, comprising administering to a mammal, in need of such treatment an effective amount of a compound according to any one of claims 16 to IS. 22. A method for modulating 5-HT6 receptor activity for the treatment or prophylaxis of obesity or type II diabetes, comprising administering to a mammal in need thereof an effective amount of a compound according to any one of claims 16 to 18. 23. A compound according to any one of claims 16 to 18 for use in the treatment or prophylaxis of obesity and/or type II diabetes. 24. Use of a compound according to any one of claims 16 to 18 for the manufacture of a medicament for use in the treatment or prophylaxis of obesity and/or type II diabetes. 25. A pharmaceutical formulation for use in the treatment or prophylaxis of obesity and/or typt II diabetes wherein the active ingredient is a compound according to any one of claims 16 to 18, A process for the preparation of a compound substantially as herein described and exemplified, A pharmaceutical formulation substantially as herein described and exemplified.

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