- 专利标题: Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof
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申请号: US588785申请日: 1996-01-19
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公开(公告)号: US5688787A公开(公告)日: 1997-11-18
- 发明人: Duane A. Burnett , John W. Clader , Sundeep Dugar , Wayne Vaccaro
- 申请人: Duane A. Burnett , John W. Clader , Sundeep Dugar , Wayne Vaccaro
- 申请人地址: NJ Kenilworth
- 专利权人: Schering Corporation
- 当前专利权人: Schering Corporation
- 当前专利权人地址: NJ Kenilworth
- 主分类号: C07D205/08
- IPC分类号: C07D205/08 ; C07D205/085 ; C07D401/04 ; C07D403/04 ; C07D405/04 ; C07D405/10 ; C07D409/04 ; C07F7/08 ; C07F7/18 ; A61K31/395 ; C07D403/10
摘要:
Novel compounds of the formula ##STR1## wherein A is --CH.dbd.CH--B; --C.tbd.C--B; --(CH.sub.2).sub.p --X--B, and X is a bone, --NH-- or --S(O).sub.0-2 --; optionally substituted heteroaryl or benzofused heteroaryl; --C(O)--B; or ##STR2## D is B'--(CH.sub.2).sub.m C(O)--, B'--(CH.sub.2).sub.q --, B'--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r, wherein Z is --O--, --C(O)--, phenylene, --NR.sub.8 -- or --S(O).sub.0-2 --, B'--(alkenylene)--; B'--(alkadienylene)--; B'--(CH.sub.2).sub.t --Z--(alkenylene), B'--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --, wherein V is cycloalkylene, B'--(CH.sub.2).sub.t --V--(alkenylene) or B'--(alkenylene)--V--(CH.sub.2).sub.t --, B'--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --, T--(CH.sub.2).sub.s --, wherein T is cycloalkyl; naphthylmethyl or optionally substituted heteroarylmethyl; B is optionally substituted phenyl; B' is naphthyl, optionally substituted heteroaryl or optionally substituted phenyl; R is hydrogen, fluoro, alkyl, alkenyl, alkynyl, or B--(CH.sub.2).sub.n --; R.sub.4 is optionally substituted phenyl, indanyl, benzofuranyl, tetrahydronaphthyl, pyridyl, pyrazinyl, pyrimidinyl or quinolyl; are disclosed, the method of using compounds of the formula II ##STR3## wherein R.sub.20 is optionally substituted phenyl, naphthyl, heteroaryl, or benzofused heteroaryl, R.sub.21, R.sub.22 and R.sub.23 are H or R.sub.20 ; E, F and G are independently a bond; cycloalkylene; alkylene; alkenylene; alkynylene; a substituted alkylene, alkenylene or alkynylene chain; an interrupted alkylene, alkenylene or alkynylene chain; or an interrupted alkylene, alkenylene or alkynylene chain substituted by one or more substituents; or one of R.sub.21 --E and R.sub.22 --F is selected from the group consisting of halogeno, OH, alkoxy, --OC(O)R.sub.5, --NR.sub.10 R.sub.11, --SH or --S(alkyl); R.sub.5 is alkyl, phenyl, R.sub.14 -phenyl, benzyl or R.sub.14 -benzyl; R.sub.10 and R.sub.11 are independently selected from H and lower alkyl, or a pharmaceutically acceptable salt thereof, in a pharmaceutically aceptable carrier as hypocholesterolemic agents is also disclosed.
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