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(19)

RU

(11)

2 317 982

(13)

C2

(51)

IPC

C07D223/14(2006-01-01)

C07D223/16(2006-01-01)

C07D487/00(2006-01-01)

C07D491/00(2006-01-01)

C07D513/00(2006-01-01)

A61K31/55(2006-01-01)

A61P3/04(2006-01-01)

A61P25/24(2006-01-01)

(21) (22)

Application

2004133068/04, 2003-04-11

(24)

Start date

2003-04-11

(22)

Actual filing date

2003-04-11

(45)

Published

2008-02-27

(72)

Inventor

Smit BrajanSmit Dzhefri

(73)

Holder

Arena Farmas'Jutikalz, Ink.

MODULATORS OF 5-HT RECEPTORS Russian patent published in 2008 - IPC C07D223/14 C07D223/16 C07D487/00 C07D491/00 C07D513/00 A61K31/55 A61P3/04 A61P25/24 

Abstract RU 2317982 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): wherein R1 means hydrogen atom (H) or (C1-C8)-alkyl; R2 means (C1-C8)-alkyl, -CH2-O-(C1-C8)-alkyl, -OH or -CH2OH; R2a means H; or R2 and R2a for in common -CH2-CH2-; R3 means halogen atom, perhalogenalkyl, -CN, -SR5, -NHR5, -N(R5)2, aryl or heteroaryl wherein indicated aryl can comprise optionally up to two substitutes chosen from (C1-C8)-alkyl, halogen atom, perhalogenalkyl and alkoxy-group, and indicated heteroaryl can comprise optionally up to two substitutes chosen from halogen atom and (C1-C8)-alkyl; R4 means H, halogen atom, perhalogenalkyl, -CN, -OR5, -SR5, -NHR5, -N(R5)2, -OH, aryl or heteroaryl wherein indicated aryl can comprise optionally up to two substitutes chosen from (C1-C8)-alkyl, halogen atom, perhalogenalkyl and alkoxy-group, and indicated heteroaryl can comprise optionally up to two substitutes chosen from halogen atom and (C1-C8)-alkyl; or R3 and R in common with atoms to which they are added can form 5- or 6-membered heterocyclic ring comprising one oxygen atom (O); each R5 means independently (C1-C8)-alkyl, (C2-C8)-alkenyl, aryl, heteroaryl, arylalkyl, alheteroarylalkyl, perhalogenalkyl or allyl; R6 means H or (C1-C8)-alkyl, or their pharmaceutically acceptable salts, solvates or hydrates under condition that if R6 differs from H then R4 can't mean H; if R1 and R2 mean methyl and R4 means H then R3 can't -NHR5 or -N(R5)2; if R1 and R2 mean methyl and R4 means H then R3 can't imidazole, substituted imidazole or imidazole derivative. Also, invention relates to a pharmaceutical composition used for modulation of 5-HT2C receptors, a method for modulation of 5-HT2C receptors, a method for prophylaxis or treatment of disorders of the central nervous system and obesity, a method for reducing food consumption in mammals, a method for inducing the satisfying sense in mammals and to a method for preparing the composition. Invention provides synthesis of novel compounds possessing useful biological properties and preparing pharmaceutical composition based on thereof.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

70 cl, 1 tbl, 57 ex

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RU 2 317 982 C2

Authors

Smit Brajan

Smit Dzhefri

Dates

2008-02-27—Published

2003-04-11—Filed

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