Title of Invention	A SYNERGISTIC PESTICIDAL COMPOSITION
Abstract	This invention relates to a synergistic pesticidal composition comprising Imidacloprid cartap hydrochloride and a carrier wherein the proportion of imidacloprid to cartap hydrochloride in terms mass is in the range of 1:20 to 1:30.

Full Text

FORM-2 THE PATENT ACT, 1970 (39 of 1970) & THE PATENT RULES, 2003 PROVISIONAL SPECIFICATION (See section 10 and Rule 13) PESTICIDE FORMULATIONS SUDARSHAN CHEMICAL INDUSTRIES LIMITED An Indian Company of 162, Wellesley Road, Pune-411 001, Maharashtra, India. THE FOLLOWING SPECIFICATION DESCRIBES THE INVENTION This invention relates to pesticide formulations. Particularly, this invention relates to pesticide formulations, typically useful for the management and eradication methods of Nilaparvata lugens (Stal) Latin name: Nilaparvata lugens (Stal) Order: Homoptera Family: Delphacidae Common name: Brown plant hopper, Asian brown planthopper The Nilaparvata lugens, commonly known as Asian rice brown planthopper (BPH), is major pest of rice plant especially the wet rice fields. The nymphs and adults suck the sap from the xylem and phloem tissues of the shoots of rice plant result in drying the tillers, destroying the plant. Severely damaged plants dry and take on the brownish appearance of plants that have been damaged by fire. Heavy infestations produce symptoms of 'hopper burn'. Leaves dry and turn brown after insect feeding, and insects congregate in large numbers, causing hopper burn in circular patches of 'burned' plants. Hence, hopper damage is called "hopper burn". It is a vector of serious rice virus diseases, grassy stunt and ragged stunt virus diseases that is transmitted by the brown planthopper, Nilaparvata lugens. The rice plant is most sensitive to attack at late vegetative and reproductive stages. Hopperburn typically causes yellowing, browning and drying of plant, Ovipositional marks exposing the plant to fungal and bacterial infections, 2 Presence of honeydew and sooty molds in the bases of areas infected, and ragged stunt or grassy stunt virus disease plant may be observed. Various chemical and non chemical means have been attempted to counter the problem of BPH. Breeding resistant varieties to BPH is one of the non-chemical preventive method to counter the problem of BPH. Various species offering high to moderate level of resistance such as ptb 33, Bg 379-2, Bg 300, Bg 403, Bg 304, Bg 357, Bg 358 and Bg 360 and tolerant species like Ratna, Triveni, Jyoti and IET 7575 have been known to be used in this method. Other non chemical methods of control include: • Cultivating resistant varieties. • Ensuring early transplanting • Avoiding close spacing • Avoiding heavy application of nitrogenous fertilizer • Ensuring frequent and adequate drainage to reduce moisture help prevent BPH multiplication. Various chemicals belonging to different broader classes, have been used for controlling the menace of BPH at various stages of the plant life cycle( Planting to Pre-tillering stage, Mid-Tillering stage, Pancile Initiation and Booting stage ) 3 Provided herein below is a list of compounds with their broader chemical class which have been used either alone or in combination with other compounds in variety of proportions for control and eradication of BPH. Carbamates Carbofuran Fenobucarb Propoxur BPMC 410 Carbaryl Etrofolan Neonicotinoids Imidacloprid Acetamiprid Thiamethoxam Phenyl pyrazole Fipronil Others IGR/ Molt accelerating compounds/ chitin inhibitors Buprofezin Nuvaluron Organophosphorus Monocrotophos Phorate (Thimet) 4 phosphamidon (Dimecron) dimethoate (Rogor) triazophos Imdacloprid is a chlorinated analog of nicotine and belongs to the class of Neonicotinoids. IUPAC name: l-(6-chloro-3-pyridylmethyl)-A'-nitroimidazolidin-2-ylideneamine Chemical Abstracts name: l-[(6-chloro-3-pyridinyl)methyl]-ALnitro-2-imidazolidinimine CAS No : 138261-41-3 Imidacloprid acts as an antagonist by binding to postsynaptic nicotinic receptors in the insect central nervous system. Imidacloprid is a systemic insecticide with trans-laminar activity and with contact and stomach action and is used for control of sucking insects, including rice-, leaf- and planthoppers, aphids, thrips and whitefly. It is also effective against soil insects, termites and some species of biting insects, such as rice water weevil and Colorado beetle. 5 Other compounds belonging to the class of neonicotinoids are clothianidin, imidacloprid, dinotefuran, acetamiprid, nitenpyram and thiamethoxam clothianidin, thiacloprid, dinotefuran, nitenpyram. All neonicotinoids bind at a specific site in the central nervous system of insects. This causes excitation of the nerves and eventual paralysis, which leads to death. All insecticides in the neonicotinoid chemical family closely resemble nicotine in mode of action. Neonicotinoids act as acute contact and stomach poisons, combine systemic properties with relatively low application rates, and are relatively nontoxic to vertebrates. These chemicals are highly systemic in the plant roots and new leaf tissues. Neonicotinoids have high activity against sucking insects such as aphids and against chewing pests such as beetles and some Lepidoptera (cutworms, for instance). Cartap hydrochloride, a derivative of nereistoxin, a naturally occurring insecticidal substance isolated from the marine segmented worms Lumbrinereis heteropoda and L. brevicirra is another useful chemical compound. 6 IUPAC: S,S'-(2-dimethylaminotrimethylene) bis(thiocarbamate) hydrochloride CAS: 15263-53-3 Formula: C7H16CIN3O2S2 Cartrap hydrochloride is a highly effective, broad-spectrum, low toxic and low residual insecticide, causing paralysis by ganglionic blocking action on the central nervous system. It is a systemic insecticide with stomach and contact action. Insects discontinue feeding, and die of starvation. Cartap hydrochloride is used against a relatively broad spectrum of insects, e.g., Lepidoptera, Coleoptera, Diptera and Hemiptera. It is especially effective against Lepidopter such as the rice stem borer, diamond-back moth and common cabbage worm, and Coleoptera such as the Colorado potato beetle, Mexican bean beetle etc. Approximately 70% of the world production of cartap hydrochloride is applied to rice and 30% to other crops, vegetables, potatoes, fruit, tea, etc. Cartap hydrochloride is also used for controlling the rice white-tip nematode by soaking rice seed in an aqueous solution of the insecticide. 7 Prior Art: Imidacloprid was first disclosed in United States Patent No. 4,742,060. Synergistic Pesticidal composition esp. for insects comprising a combination of amitraz and imidacloprid is disclosed in W09300009 which shows increased synergistic activity against pests. The composition of imidacloprid with carbamate pesticides containing imidacloprid (0.5-5 Wt.%), Etrofolan (20-25 Wt.%), adsorbent (20-25 Wt.%), assistant (5-9 Wt.%) and filler (35-40.5 Wt.%) is disclosed in CN1187300. Another composition of imidacloprid(0.5-20 Wt.%) with carbendazim(20-25 Wt.%) along with assistant (40-49 Wt.%) and filler (20-25.5 Wt.%) is also disclosed in this Chinese patent(CNl187300). Another Insecticidal emulsifiable concentrate for fruit trees containing imidacloprid and triazophos is disclosed in CN1220087. The composite insecticide emulsifiable solution is made up by using 10-19 of triazophos, 1-10% of imidacloprid, emulsifying agent and solvent through a certain preparation process. Chinese Patent CN1223794 discloses an emulsifiable concentrate of Imidacloprid-fenobucarb which contains imidacloprid as basic raw material alongwith fenobucarb and other excipients such as an emulsifier, dimethyl formamide, boric acid and toluene. 8 A synergistic insecticidal mixture of imidacloprid and 0,S-dimethyl phosphoamidothioate is disclosed in US 5,994,331. An Insecticide composition containing imidacloprid and monosultap is disclosed in Chinese Patent CN1256864 . Another composition of imidacloprid and monosultap with weight portion ratio of 49:0.1-10 is disclosed in CN1281644. A pesticide composition of imidacloprid and chlorpyrifos, with a solvent, emulsifier and penetrant, is disclosed in CN1299596. A kind of insecticide composite, mainly containing imidacloprid and buprofezin is disclosed in Chinese Application CN1325628. This composite can be manufactured as a wettable powder or as an emulsion. A Synergistic fungicidal and insecticidal composition, useful in plant protection, containing imidacloprid is disclosed in New Zealand Patent NZ0508749. The patent discloses that the Fungicidal compound that can be combined with Imidacloprid is selected from tebucanazole, propiconazole, difenconazole, cyproconazoleflutriafol, hexaconazole, myclobutanil, penconazole, furconazole, etaconazole, bromuconazole, fenbuconazole, tetraconazole, tridimenol, tridimefon, diclobutrazole, diniconazole, flusilazolefluquinconazole, tridemorph, aldimorph, fenpropimorph, fenpropidin, pyrifenox and vinclozolin. 9 Dermally applicable liquid formulations comprising permethrin and agonists or antagonists or nictonic acetylcholine receptors of insects are disclosed in New Zealand Patent. A composition as disclosed in NZ0528664 comprises by weight 35-60% of the active compound permethrin; 2.5-12.5% of imidacloprid or an imidacloprid analogue; 27.5-62.5% of N-methylpyrrolidone; 0-5% of water; 0-0.5% of phenolic antioxidants and 0-0.5% of organic acids. Chinese patent CNl717998 disclose a combination of imidacloprid and phoxim with strong systemic action with high effect and has low poison. Another Chinese patent CN1729781 also disclose a combination of imidacloprid and phoxim . This combination is suitable for controlling crop soil insect and particularly useful for peanut and garlic. German Patent DEI9956098 disclose a Synergistic plant fungicide composition containing spiroxamine, quinoxyfen and imidacloprid, thiacloprid and/or thiamethoxam, especially effective against cereal diseases Chinese Patent CN1541535 disclose a mixture containing heteroaralkyl amine, e.g. imidacloprid, and fungicide which is useful in control of phytopathogenic fungi, esp. on cereals, and arthropods, esp. insects. Insecticidal and pesticidal compositions containing neonicotinoids with other insectidal/fungicidal/pesticidal compounds are disclosed in WO06069655( neonicotinoids with benalaxyl or metalaxyl), DE102004034272 10 (neonicotinoids with acetyl salicylic acid), WO05122769 (neonicotinoids with ethiprole) WO05096819 (neonicotinoids with ethoprophos and aldicarb) EP1719409(neonicotinoids with pyrazole derivatives) WO0028825(neonicotinoids with phenylamide, phenylpyrrole and/or triazole). JP 2001081003 discloses a microbicidal insecticidal composition containing Cartap hydrochloride (as an active ingredient) along with at least one kind of phenyl alkanic acid amide derivative for paddy field. JP 09124406 discloses a granulated water dispersible powder containing cartap hydrochloride, alongwith Acephate, Nitenpyram, Bensultao in combination with zinc oxide, MgO, TiO2, A12O3 JP 08225404, discloses a stabilized agrochemical preparation of cartap hydrochloride and cyclodextrins. JP 02174702 discloses an active agrochemical composition of cartap hydrochloride mixed with octyldiphenyl phosphate. None of the compounds per se or the formulations have been effective in the treatment of rice plants affected by BPH. There is a need for a formulation for a formulation that can effectively control BPH, particularly BPH resistant to individual chemical compounds or existing formulations. This invention discloses a formulation containing a synergistic formulation containing and intimate mixture of cartap hydrochloride and at least one 11 compound selected from a group of neonicotinoids, typically imidacloprid, acetamiprid and thiamethoxam as a suitable formulation for the treatment of plants, particularly, rice plants affected by BPH. Aqueous solutions of the formulation of this invention can be sprayed on the pest affected plants for treatment and control of pests. The ratio of the compounds in the formulation with respect to each other may range from 1 to 99 parts. A typical ratio being 1:6. Initial trials have revealed that the formulation has shown synergistic activity far significant to the activity of the individual compounds even on resistant varieties of the pest. Dated this 28th day of December, 2006. MOHAN DEWAN OF R.K. DEWAN & COMPANY APPLICANTS' PATENT ATTORNEY 12

Documents:

2156-mum-2006-abstract(24-12-2007).pdf

2156-mum-2006-abstract(granted)-(20-8-2010).pdf

2156-mum-2006-claims(24-12-2007).pdf

2156-mum-2006-claims(granted)-(20-8-2010).pdf

2156-mum-2006-correspondance-received.pdf

2156-mum-2006-correspondence(24-12-2007).pdf

2156-mum-2006-correspondence(26-5-2008).pdf

2156-mum-2006-correspondence(ipo)-(25-8-2010).pdf

2156-mum-2006-description (provisional).pdf

2156-mum-2006-description(complete)-(24-12-2007).pdf

2156-mum-2006-description(granted)-(20-8-2010).pdf

2156-mum-2006-form 18(26-5-2008).pdf

2156-mum-2006-form 2(24-12-2007).pdf

2156-mum-2006-form 2(granted)-(20-8-2010).pdf

2156-mum-2006-form 2(title page)-(24-12-2007).pdf

2156-mum-2006-form 2(title page)-(granted)-(20-8-2010).pdf

2156-mum-2006-form 5(24-12-2007).pdf

2156-mum-2006-form-1.pdf

2156-mum-2006-form-2.doc

2156-mum-2006-form-2.pdf

2156-mum-2006-form-26.pdf

2156-mum-2006-form-3.pdf