Title:
【発明の名称】スクアレンシンターゼ阻害物質としてのキヌクリジン誘導体
Document Type and Number:
Japanese Patent JPH08504803
Kind Code:
A
Abstract:
PCT No. PCT/GB93/02617 Sec. 371 Date Jun. 5, 1995 Sec. 102(e) Date Jun. 5, 1995 PCT Filed Dec. 21, 1993 PCT Pub. No. WO94/14805 PCT Pub. Date Jul. 7, 1994 Compounds of formula (I) and their pharmaceutically acceptable salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1-CR2 is a double bond; X is selected from -CH2CH2-, -CH=CH-, -C=C-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -N=CH-, -CH=N-, -CH2S- and -SCH2- (wherein the sulphur atom in the latter two groups may optionally bear one or two oxygen atoms); Ar is a heterocyclic moiety containing up to three heteroatoms independently selected from nitrogen, oxygen and sulphur, and wherein Ar may optionally be unsubstituted or may bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, alkanoylamino, ureido, N'-alkylureido, alkanoyl and oxime derivatives thereof and O-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 medecine.
Inventors:
Howamore, Paul Robert Owen
Application Number:
JP51494394A
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)