Global Patent Index - EP 0662969 A1

EP 0662969 A1 19950719 - UREA AND THIOUREA DERIVATIVES AND PROCESS FOR THEIR PREPARATION.

Title (en)

UREA AND THIOUREA DERIVATIVES AND PROCESS FOR THEIR PREPARATION.

Title (de)

HARNSTOFF-UND THIOHARNSTOFFDERIVATE UND VERFAHREN ZU DEREN HERSTELLUNG.

Title (fr)

DERIVES DE L'UREE ET DE LA THIOUREE ET PROCEDE POUR LEUR PREPARATION.

Publication

EP 0662969 A1 19950719 (EN)

Application

EP 94921623 A 19940624

Priority

  • EP 9402058 W 19940624
  • GB 9316020 A 19930803

Abstract (en)

[origin: WO9504053A1] The invention provides a compound of formula (I), wherein Y is an aryl or heteroaryl group substituted by a group chosen from amino, C1-C6 monoalkylamino, 3-pyrrolin-1-yl, pyrrolidin-1-yl, morpholin-4-yl and piperidin-1-yl, the aryl or heteroaryl being optionally substituted in addition by 1 to 3 substituents independently chosen from halogen, C1-C6 alkyl, trihalo-C1-C3 alkyl, hydroxy, C1-C6 alkoxy, C1-C6 alkylthio and C1-C6 alkylsulfonyl; m is zero, 1 or 2; X is oxygen or sulphur; R1 and R2 are each, independently, a C1-C6 alkyl group or R1 and R2 taken together form a C2-C4 alkylene chain in which each carbon atom is optionally substituted by 1 or 2 substituents independently chosen from halogen and C1-C4 alkyl; n is 1, 2 or 3; Q is oxygen or sulphur; W is an aryl or heteroaryl group unsubstituted or substituted by 1 to 4 substituents independently chosen from halogen, C1-C6 alkyl, trihalo-C1-C3 alkyl, C1-C6 alkoxy, C1-C6 alkylthio and C1-C6 alkylsulfonyl; or a pharmaceutically acceptable salt thereof. The compounds of the invention show inhibitory activity of the enzyme acyl CoA: cholesterol acyltransferase (ACAT-EC 2.3.1.26) and thus have utility as antiatherosclerotic and antidyslipidaemic agents and in the prevention of coronary heart disease.

IPC 1-7

C07D 405/10; C07D 409/10; C07D 317/28; C07D 339/06; C07D 319/06; C07D 413/10; A61K 31/335

IPC 8 full level

C07D 317/30 (2006.01); A61K 31/38 (2006.01); A61K 31/40 (2006.01); A61K 31/4025 (2006.01); A61K 31/505 (2006.01); A61K 31/535 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); C07D 317/28 (2006.01); C07D 319/06 (2006.01); C07D 339/06 (2006.01); C07D 405/10 (2006.01); C07D 409/10 (2006.01); C07D 413/10 (2006.01)

CPC (source: EP)

A61P 9/08 (2017.12); A61P 9/10 (2017.12); C07D 317/28 (2013.01); C07D 319/06 (2013.01); C07D 339/06 (2013.01); C07D 405/10 (2013.01); C07D 409/10 (2013.01); C07D 413/10 (2013.01)

Citation (search report)

See references of WO 9504053A1

Designated contracting state (EPC)

DE GB IT

DOCDB simple family (publication)

WO 9504053 A1 19950209; EP 0662969 A1 19950719; GB 9316020 D0 19930915; JP H08511269 A 19961126

DOCDB simple family (application)

EP 9402058 W 19940624; EP 94921623 A 19940624; GB 9316020 A 19930803; JP 50551294 A 19940624