发明名称 QUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS
摘要 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.
申请公布号 WO9414804(A1) 申请公布日期 1994.07.07
申请号 WO1993GB02616 申请日期 1993.12.21
申请人 ZENECA LIMITED;BROWN, GEORGE, ROBERT 发明人 BROWN, GEORGE, ROBERT
分类号 A61K31/435;A61P9/10;C07D453/02;(IPC1-7):C07D453/02 主分类号 A61K31/435
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