Title of Invention | ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY |
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Abstract | The invention provides compounds of formula I wherein m, n, A, R, R', R", Ro, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals. |
Full Text | Abstract of the disclosure The invention provides compounds of formula I wherein m, n, A, R, R', R", Ro, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals. Claims 1. A compound of fomnula I wherein m isOorl, n is 0 or 1 and A is liydroxy X is liydrogen and Y is hydrogen, or A forms a single bond with X or with Y; Ro is hydrogen, (Ci)all optionally substituted phenyl, 2-pyridyl or 2-thienyl, R4 and R5, independently, are hydrogen or (Ci)alkyl and Re is (Ci)alkyl, (C3.7)cycloalkyl or optionally substituted phenyl, R' is hydrogen or (Ci)alkyl and R" Is hydrogen, or (CM)alkyl, or R' and R" together form a group -CH2-(CH2)p- wherein p is 0,1 or 2, in which case one of n and p Is different from 0, with the proviso that Ro is different from hydrogen, trifluoromethyl and methoxy when m is 1, n is 0, A is hydroxy, X and Y are both hydrogen, R is COOEt and R' and R" together form a group -(CH2)2-, in free base or acid addition salt form. 2. The compound of claim 1 which is (-)-(3aR, 4S, 7aR)-4-hydroxy-4-m-tolylethynyl-octahydroindole-1-carboxylic acid methyl ester in free base or acid addition salt form. 3. A process for the preparation of a compound of formula I as defined in claim 1, or a salt thereof, which comprises the step of a) for the production of a compound of formula I wherein A is hydroxy, reacting a compound of formula II b) for the production of a compound of formula I wherein A fomis a single bond with X or with Y, dehydrating a compound of formula I wherein A is hydroxy, and recovering the resulting compound of formula I in free base or acid addition salt form. 4. A compound of claim 1 in free base or pharmaceutically acceptable acid addition salt form, for use as a pharmaceutical. 5. A compound of claim 1 in free base or pharmaceutically acceptable acid addition salt form, for use in the treatment of disorders associated with irregularities of the glutamatergic signal transmission, and of nervous system disorders mediated full or in part by mGluRS. 6. A pharmaceutical composition comprising a compound of claim 1 in free base or pharmaceutical!/ acceptable acid addition salt form, in association with a pharmaceutical carrier or diluent. 7. The use of a compound of claim 1 in free base or phamriaceutically acceptable acid addition salt form, in the treatment of disorders associated with in-egularities of the glutamatergic signal transmission, and of nervous system disorders mediated full or in part by mGluRS. 8. The use of a compound of claim 1 in free base or pharmaceutically acceptable acid addition salt form, for the manufacture of a pharmaceutical composition designed for the treatment of disorders associated with irregularities of the glutamatergic signal transmission, and of nervous system disorders mediated full or in part by mGluRS. 9. A method of treating disorders associated with irregularities of the glutamatergic signal transmission, and nervous system disorders mediated full or in part by mGluRS, which method comprises administering to a subject in need of such treatment a therapeutically effective amount of a compound of claim 1 in free base or pharmaceutically acceptable acid addition salt form. 10. A combination comprising a therapeutically effective amount of a compound of claim 1 in free base or pharmaceutically acceptable acid addition salt form and a second dmg substance, for simultaneous or sequential administration. 11. A pharmaceutical composition substantially as herein described and exemplified. |
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1200-CHENP-2004 AMENDED PAGES OF SPECIFICATION 09-05-2011.pdf
1200-CHENP-2004 AMENDED CLAIMS 09-05-2011.pdf
1200-chenp-2004 description(complete).pdf
1200-chenp-2004 form-3 09-05-2011.pdf
1200-CHENP-2004 CORRESPONDENCE OTHERS 27-07-2010.pdf
1200-CHENP-2004 CORRESPONDENCE PO.pdf
1200-CHENP-2004 EXAMINATION REPORT REPLY RECIEVED 09-05-2011.pdf
1200-CHENP-2004 OTHER PATENT DOCUMENT 09-05-2011.pdf
1200-chenp-2004 power of attorney.pdf
1200-chenp-2004 correspondence others.pdf
1200-chenp-2004 correspondence po.pdf
abs 1200-chenp-2004 abstract.jpg
Patent Number | 248218 | ||||||||||||
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Indian Patent Application Number | 1200/CHENP/2004 | ||||||||||||
PG Journal Number | 26/2011 | ||||||||||||
Publication Date | 01-Jul-2011 | ||||||||||||
Grant Date | 28-Jun-2011 | ||||||||||||
Date of Filing | 01-Jun-2004 | ||||||||||||
Name of Patentee | NOVARTIS AG | ||||||||||||
Applicant Address | LICHTSTRASSE 35, CH-4056 BASEL | ||||||||||||
Inventors:
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PCT International Classification Number | A61K31/4709 | ||||||||||||
PCT International Application Number | PCT/EP02/13670 | ||||||||||||
PCT International Filing date | 2002-12-03 | ||||||||||||
PCT Conventions:
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