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RU

(11)

2 545 456

(13)

C2

(51)

IPC

C07D231/12(2006-01-01)

C07D263/32(2006-01-01)

C07D307/40(2006-01-01)

C07D405/10(2006-01-01)

C07D405/14(2006-01-01)

C07D407/10(2006-01-01)

C07D413/10(2006-01-01)

C07D417/10(2006-01-01)

A61K31/341(2006-01-01)

A61K31/41(2006-01-01)

A61K31/4155(2006-01-01)

A61K31/4192(2006-01-01)

A61K31/421(2006-01-01)

A61K31/422(2006-01-01)

A61K31/4245(2006-01-01)

A61K31/425(2006-01-01)

A61K31/427(2006-01-01)

A61K31/433(2006-01-01)

A61K31/443(2006-01-01)

A61K31/454(2006-01-01)

A61K31/4545(2006-01-01)

A61K31/4709(2006-01-01)

A61K31/497(2006-01-01)

A61K31/5377(2006-01-01)

A61P25/00(2006-01-01)

A61P25/08(2006-01-01)

A61P25/14(2006-01-01)

A61P25/16(2006-01-01)

A61P25/18(2006-01-01)

A61P25/20(2006-01-01)

A61P25/22(2006-01-01)

A61P25/24(2006-01-01)

A61P25/28(2006-01-01)

A61P25/30(2006-01-01)

(21) (22)

Application

2012143610/04, 2011-03-10

(24)

Start date

2011-03-10

(22)

Actual filing date

2011-03-10

(45)

Published

2015-03-27

(72)

Inventor

Katshell Nil S.Gejdzh Dzhennifer LinnUiler Tomas NilLittl Tomas L.

(73)

Holder

Omeros Korporejshn

PDE10 INHIBITORS AND COMPOSITIONS CONTAINING THEM AND METHODS Russian patent published in 2015 - IPC C07D231/12 C07D263/32 C07D307/40 C07D405/10 C07D405/14 C07D407/10 C07D413/10 C07D417/10 A61K31/341 A61K31/41 A61K31/4155 A61K31/4192 A61K31/421 A61K31/422 A61K31/4245 A61K31/425 A61K31/427 A61K31/433 A61K31/443 A61K31/454 A61K31/4545 A61K31/4709 A61K31/497 A61K31/5377 A61P25/00 A61P25/08 A61P25/14 A61P25/16 A61P25/18 A61P25/20 A61P25/22 A61P25/24 A61P25/28 A61P25/30 

Abstract RU 2545456 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts, wherein A is thiazolyl, oxazolyl, thienyl, furyl, imidazolyl, pyrazolyl or oxadiazolyl (structures of which are presented in cl.1 of the patent claim), R1 represents C1-6alkyl; R2 represents (i) phenyl substituted by halogen; C1-6alkyl optionally substituted by morpholine or C1-6dialkylamino; C1-6alkoxy optionally substituted by halogen; or heterocyclyl, wherein a heterocyclyl substitute is specified in morpholine; pyrazolyl optionally substituted by C1-6alkyl; piperidinyl; pyrrolidinyl; oxadiazolyl substituted by C1-6alkyl; furyl substituted by C1-6alkyl; dioxydoisothiazolidinyl; triazolyl; tetrazolyl substituted by C1-6alkyl, tridiazolyl substituted by C1-6alkyl; thiazolyl substituted by C1-6alkyl; pyridyl; or pyrazinyl; (ii) substituted or unsubstituted heterocyclyl specified in quinolinyl; pyridyl substituted by C1-6alkoxy or morpholinyl; or benzo [d] [1, 2, 3] triazolyl substituted by C1-6alkyl; R3 represents phenyl substituted by 2 or 3 substitutes specified in halogen; C1-6alkyl; C1-6alkoxy optionally substituted by halogen; hydroxy group; cyano; or -C(=O)ORa, wherein Ra represents phenyl; R4 represents hydrogen, C1-6alkyl or C1-6halogenalkyl. The invention also refers to a pharmaceutical composition containing the compounds of formula (I), a method for PDE10 inhibition, a method of treating neurological disorders, and to intermediate compounds: 2-(4-chlor-3,5-dimethoxyphenyl)furan and 4-(5-methyl-1,3,4-thiadiazol-2-yl)benzaldehyde.

EFFECT: compounds of formula (I) as PDE10 inhibitors.

39 cl, 13 ex, 2 tbl, 77 dwg

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RU 2 545 456 C2

Authors

Katshell Nil S.

Gejdzh Dzhennifer Linn

Uiler Tomas Nil

Littl Tomas L.

Dates

2015-03-27—Published

2011-03-10—Filed

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