发明授权
US5650427A Centrally acting 6,7,8,9-tetrahydro-3H-benz(e) indole heterocyclics
失效
中心作用的6,7,8,9-四氢-3H-苯并(e)吲哚杂环
- 专利标题: Centrally acting 6,7,8,9-tetrahydro-3H-benz(e) indole heterocyclics
- 专利标题(中): 中心作用的6,7,8,9-四氢-3H-苯并(e)吲哚杂环
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申请号: US460449申请日: 1995-06-02
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公开(公告)号: US5650427A公开(公告)日: 1997-07-22
- 发明人: Hakan Vilhelm Wikstrom , Per Arvid Emil Carlsson , Bengt Ronny Andersson , Kjell Anders Ivan Svensson , Stig Thomas Elebring , Nils Peter Stjernlof , Arthur Glenn Romero , Susanne R. Haadsma-Svensson , Chiu-Hong Lin , Michael Dalton Ennis
- 申请人: Hakan Vilhelm Wikstrom , Per Arvid Emil Carlsson , Bengt Ronny Andersson , Kjell Anders Ivan Svensson , Stig Thomas Elebring , Nils Peter Stjernlof , Arthur Glenn Romero , Susanne R. Haadsma-Svensson , Chiu-Hong Lin , Michael Dalton Ennis
- 申请人地址: MI Kalamazoo
- 专利权人: The Upjohn Company
- 当前专利权人: The Upjohn Company
- 当前专利权人地址: MI Kalamazoo
- 主分类号: A61K31/40
- IPC分类号: A61K31/40 ; A61K31/403 ; A61K31/407 ; A61K31/435 ; A61K31/4427 ; A61K31/4433 ; A61K31/454 ; A61K31/475 ; A61P11/14 ; A61P25/00 ; A61P25/20 ; A61P25/24 ; A61P25/26 ; A61P25/28 ; A61P43/00 ; C07D209/56 ; C07D209/60 ; C07D209/66 ; C07D401/06 ; C07D401/12 ; C07D403/04 ; C07D409/12 ; C07D413/04 ; C07D471/04 ; C07D491/04 ; C07D491/052 ; C07D495/04
摘要:
A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --X--Ar where X is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thiophenyl or 3-thiophenyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, cyclopropylmethyl, CF.sub.3, 2,2,2-trifluoroethyl, CN, CONR.sup.1 R.sup.2, .dbd.O, 2(4,5-dihydro)imidazolyl, 2(4,5-dihydro)oxazolyl, 2-oxazolyl, 3-oxadiazolyl, or 3,3,3-trifluoropropyl; R.sup.5 is hydrogen, R.sup.1, OCH.sub.3, C(O)CH.sub.3 or C(O)OR.sup.1 ; X is (a) a valence bond, (b) CH.sub.2, or (c) O, S or NR.sup.5 where R.sup.5 is H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl, COR.sup.6 where R.sup.6 is a C.sub.1 -C.sub.3 alkyl, phenyl, or CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are independently H or C.sub.1 -C.sub.3 alkyl; andZ is a hydrogen or halogen; provided that when X is CH.sub.2, at least one of R.sub.3 and R.sub.4 is other than hydrogen or C.sub.1 -C.sub.3 alkyl. The compounds of Formula I are suitable for treating disorders of the central nervous system, particularly as 5-HT.sub.1A receptor agonists.
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