发明公开
EP1060162A1 VON AZACYCLOALKANEN ABGELEITETE URETHANE, IHRE THIO- UND DITHIOANALOGA, DEREN HERSTELLUNG UND DEREN VERWENDUNG ALS 2,3-EPOXISQUALEN-LANOSTEROL-CYCLASE INHIBITOREN
有权
衍生氮杂环烷烃氨酯您的硫和DITHIOANALOGA,生产及其作为2,3-环氧角鲨烯 - 羊毛甾醇环化酶抑制剂的
- 专利标题: VON AZACYCLOALKANEN ABGELEITETE URETHANE, IHRE THIO- UND DITHIOANALOGA, DEREN HERSTELLUNG UND DEREN VERWENDUNG ALS 2,3-EPOXISQUALEN-LANOSTEROL-CYCLASE INHIBITOREN
- 专利标题(英): Urethanes derived from azacycloalkanes, thio and dithio analogues, production and use thereof as 2,3 epoxysqualene lanesterol cyclase inhibitors
- 专利标题(中): 衍生氮杂环烷烃氨酯您的硫和DITHIOANALOGA,生产及其作为2,3-环氧角鲨烯 - 羊毛甾醇环化酶抑制剂的
-
申请号: EP98962423.4申请日: 1998-12-08
-
公开(公告)号: EP1060162A1公开(公告)日: 2000-12-20
- 发明人: MAIER, Roland , MÜLLER, Peter , SCHILCHER, Gebhard , ADELGOSS, Gebhard , HURNAUS, Rudolf , MARK, Michael , EISELE, Bernhard
- 申请人: Boehringer Ingelheim Pharma KG
- 申请人地址: Binger Strasse 173 55218 Ingelheim am Rhein DE
- 专利权人: Boehringer Ingelheim Pharma KG
- 当前专利权人: Boehringer Ingelheim Pharma KG
- 当前专利权人地址: Binger Strasse 173 55218 Ingelheim am Rhein DE
- 代理机构: Laudien, Dieter, Dr.
- 优先权: DE19754796 19971210
- 国际公布: WO9929669 19990617
- 主分类号: C07D211/54
- IPC分类号: C07D211/54 ; C07D211/32 ; C07D211/26 ; C07D211/70 ; A61K31/445
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 R2¿ are a straight-chain or branched C¿1-6? 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 R2 ¿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, R3-R6 can be identical or different and represent hydrogen atoms or alkyl groups, R7 is a C¿3-7? 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(R9R10)- group, wherein R10 and adjacent group R8 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.
公开/授权文献
信息查询