Title:
【発明の名称】スクアレンシンターゼ阻害剤としてのキヌクリジン誘導体
Document Type and Number:
Japanese Patent JPH08504802
Kind Code:
A
Abstract:
Compounds of formula (I) and their pharmaceutically acceptable salts in which R<1> is hydrogen or hydroxy; R<2> is hydrogen; or R<1> and R<2> are joined together so that CR<1>-CR<2> is a double bond; X is selected from -CH2CH2-, -CH = CH-, -CC-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH = N-, -N = CH-, -O-, -NH-, -CO-, -CH2-, -CH2S-, -SCH2- and -S- (wherein the sulphur atom in the latter three groups may optionally bear one or two oxygen atoms); Ar<1> is a phenylene moiety; Ar<2> is a heterocyclic moiety; and wherein one or both of Ar<1> and Ar<2> may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkylamino, di-[(1-6C)alkyl]amino N-(1-6C)alkylcarbamoyl, di-N,N-[(1-6C)alkyl]carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno (1-6C)alkyl, (1-6C)alkanoylamino, ureido, N'-(1-6C)alkylureido, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial. Processes preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medicine.
Inventors:
Brown, George Robert
Application Number:
JP51494294A
Publication Date:
May 28, 1996
Filing Date:
December 21, 1993
Export Citation:
Assignee:
Zeneca Limited
International Classes:
A61K31/435; A61P9/10; C07D453/02; (IPC1-7): C07D453/02; A61K31/435
Attorney, Agent or Firm:
Kyozo Yuasa (6 people outside)