发明名称 URETHANES DERIVED FROM AZACYCLOALKANES, THIO AND DITHIO ANALOGUES, PRODUCTION AND USE THEREOF AS 2,3- EPOXYSQUALENE LANESTEROL CYCLASE INHIBITORS
摘要 The present invention relates to urethanes derived from azacycloalkanes in addition to thio and dithio analogues of general formula (I), wherein m= 0 or 1, n=1or 2, A is a single bond, a straight-chain or branched C1-8 alkylene group, a C2-8 alkenylene or C2-8 alkylene group, whereby an unsaturated group is not directly bonded to radical Y; X and Y is an oxygen or sulphur atom, R<1> and R<2> are a straight-chain or branched C1-6 alkyl group, a C1-4 alkenyl group or a C1-4 alkinyl group, whereby a multiple bond is isolated from the nitrogen-carbon bond, or R<1> and R<2 >together with the nitrogen atom represent a 5-7 membered saturated heterocyclic ring, whereby one methylene group isolated from the nitrogen atom can be replaced by an oxygen or sulphur atom or by an -NH or -N (alkyl) group, R<3>-R<6> can be identical or different and represent hydrogen atoms or alkyl groups, R<7> is a C3-7 cycloalkyl group, optionally a phenyl or naphtyl group substituted by two halogen atoms, an alkyl, alkoxy, trifluoromethyl or cyano group or a hydrogen atom, provided that A does not represent a single bond, E is an oxygen or sulphur atom, a methylene, carbonyl or sulfinyl group and R<8> represents a hydrogen atom or E represents the -C(R<9>R<10>)- group, wherein R<10> and adjacent group R<8> represent a carbon-carbon bond. The invention also relates to enantiomers, diastereomers and salts thereof, especially physiologically acceptable acid additive salts with valuable properties such as exhibiting an inhibiting effect on cholesterol biosynthesis, in addition to medicaments containing said compounds, the use thereof and a method for the production thereof.
申请公布号 IL135738(D0) 申请公布日期 2001.05.20
申请号 IL19980135738 申请日期 1998.12.08
申请人 BOEHRINGER INGELHEIM PHARMA KG 发明人
分类号 A23K1/16;A23K1/18;A61K31/445;A61P1/16;A61P3/06;A61P9/00;A61P9/10;A61P31/10;A61P43/00;C07D211/26;C07D211/32;C07D211/54;C07D211/70 主分类号 A23K1/16
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