THIENOPYRIDINE DERIVATIVES AS GABA-B ALLOSTERIC ENHANCERS Russian patent published in 2010 - IPC C07D495/04 C07D495/14 A61K31/4365 A61K31/435 A61K31/4427 A61P25/00 

Abstract RU 2388761 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I , where R1 is C1-C7-alkyl; R2 is C1-C7-alkyl, C1-C7-haloalkyl, C3-C8-cycloalkyl; R3 is -NRaRb; possibly substituted phenyl, thiophenyl, furanyl, where the substitutes are selected from a group consisting of halogen, C1-C7-alkoxy, C1-C7-alkylsulphonyl and -C(O)O-C1-C7-alkyl; R4 is hydrogen or C1-C7-alkyl; R5 is hydrogen, halogen, C1-C7-alkyl, phenyl; or R5 together with R4 can form a ring selected from a group consisting of C5-C7-cycloalkyl, tetrahydrofuranyl, piperidine, tetrahydropyran, phenyl or pyridinyl, which can possibly be substituted with -C(O)O-C1-C7-alkyl; Ra and Rb together with the nitrogen atom to which they are bonded form piperidine; and to pharmaceutically acceptable salts thereof. The invention also relates to a medicinal agent based on the said compounds which has GABA-B receptor allosteric enhancement effect.

EFFECT: obtaining novel compounds and a medicinal agent based on the said compounds, which can be used in medicine for treating central nervous system disorders.

13 cl, 42 ex

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RU 2 388 761 C2

Authors

Mal'Kherbe Parisher

Mashiadri Rafaehllo

Norkross Rodzher Dehvid

Ratni Khasan

Tomas Ehndrju Uill'Jam

Dates

2010-05-10Published

2005-12-09Filed