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    Centrally acting 6,7,8,9-tetrahydro-3H-benz(E)indole heterocyclics
    3.
    发明授权
    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

    公开(公告)号：US5461061A

    公开(公告)日：1995-10-24

    申请号：US144857

    申请日：1993-10-28

    申请人： Hakan V. Wikstrom ,  Per A. E. Carlsson ,  Bengt R. Andersson ,  Kjell A. I. Svensson ,  Stig T. Elebring ,  Nils P. Stjernlof ,  Arthur G. Romero ,  Susanne R. Haadsma-Svensson ,  Chiu-Hong Lin ,  Michael D. Ennis

    发明人： Hakan V. Wikstrom ,  Per A. E. Carlsson ,  Bengt R. Andersson ,  Kjell A. I. Svensson ,  Stig T. Elebring ,  Nils P. Stjernlof ,  Arthur G. Romero ,  Susanne R. Haadsma-Svensson ,  Chiu-Hong Lin ,  Michael D. Ennis

    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

    CPC分类号： C07D401/12 ,  C07D209/66 ,  C07D409/12 ,  C07D491/04

    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.

    摘要翻译： 其中R1为H，C1-C3烷基， - （CH2）nCONH2，其中n为2-6，（CH2）n-1-（4,4-二甲氧基苯基） 二甲基哌啶-2,6-二酮基）或环丙基甲基; R2是氢，C1-C8烷基，C3-C8环烷基或与R1结合以形成C 3 -C 8环烷基，C 2 -C 8烯基，C 2 -C 8炔基，（CH 2）n X-Ar，其中X是O，S或NH ，3,3,3-三氟丙基， - （CH 2）m -R 9，其中m为2或3，R 9为苯基，2-噻吩基或3-噻吩基; R3是氢，C1-C3烷基，2,2,2-三氟乙基，3,3,3-三氟丙基，甲酰基，CN，卤素，CH2OR2，C（O）C（O）OR1，C（O） - （CH2）q-NR1R2其中q为0至5，C = NOR2,2（4,5-二氢）恶唑基或COR 10，其中R 10为H，R 1，NR 1 R 2或CF 3; R4是氢，C1-C3烷基，环丙基甲基，CF3,2,2,2-三氟乙基，CN，CONR1R2，= 2,2（4,5-二氢）咪唑基，2（4,5-二氢）恶唑基， 恶唑基，3-恶二唑基或3,3,3-三氟丙基; R 5是氢，R 1，OCH 3，C（O）CH 3或C（O）OR 1; X是（a）价键，（b）CH 2或（c）O，S或NR 5，其中R 5是H，C 1 -C 8烷基，C 3 -C 8环烷基，苄基，COR 6，其中R 6是C 1 -C 3烷基， 苯基或CONR 7 R 8，其中R 7和R 8独立地为H或C 1 -C 3烷基; Z为氢或卤素; 条件是当X是CH 2时，R 3和R 4中的至少一个不是氢或C 1 -C 3烷基。 式I化合物适用于治疗中枢神经系统疾病，特别是5-HT 1A受体激动剂。

    4,4,5,5-Tetradehydro-.omega.-aryl-PGE.sub.1 analogs
    5.
    发明授权
    4,4,5,5-Tetradehydro-.omega.-aryl-PGE.sub.1 analogs 失效
    4,4,5,5-四氢-2H-吡喃-7-胺-L- PGE'1'类似物

    公开(公告)号：US4053502A

    公开(公告)日：1977-10-11

    申请号：US738724

    申请日：1976-11-04

    申请人： Chiu-Hong Lin

    发明人： Chiu-Hong Lin

    IPC分类号： C07C405/00 ,  C07F9/40 ,  C07C65/22

    CPC分类号： C07C405/00 ,  C07F9/4006

    摘要： This invention comprises certain analogs of the prostaglandins in which there is a triple bond between C-5 and C-6 or C-4 and C-5. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

    4,4,5,5-Tetradehydro-.omega.-aryl-PGF.sub.1.alpha. analogs
    6.
    发明授权
    4,4,5,5-Tetradehydro-.omega.-aryl-PGF.sub.1.alpha. analogs 失效
    4,4,5,5-TETRADEHYDRO-7 -ARYL-PGF'1“+ L模拟物

    公开(公告)号：US4053500A

    公开(公告)日：1977-10-11

    申请号：US738725

    申请日：1976-11-04

    申请人： Chiu-Hong Lin

    发明人： Chiu-Hong Lin

    IPC分类号： C07C405/00 ,  C07F9/40 ,  C07C65/22

    CPC分类号： C07C405/00 ,  C07F9/4006

    摘要： This invention comprises certain analogs of the prostaglandins in which there is a triple bond between C-5 and C-6 or C-4 and C-5. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

    4,4,5,5-Tetradehydro-PGE.sub.1 analogs
    7.
    发明授权
    4,4,5,5-Tetradehydro-PGE.sub.1 analogs 失效
    4,4,5,5-四脱氧-β-PGE'1'类似物

    公开(公告)号：US4013695A

    公开(公告)日：1977-03-22

    申请号：US619077

    申请日：1975-10-02

    申请人： Chiu-Hong Lin

    发明人： Chiu-Hong Lin

    IPC分类号： A61K31/23 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C57/30 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07F7/18 ,  C07F9/38 ,  C07F9/40 ,  C07C177/00

    CPC分类号： C07F7/1804 ,  C07C405/00 ,  C07C57/30 ,  C07F7/1852 ,  C07F9/4059

    摘要： This invention comprises certain analogs of the prostaglandins in which there is a triple bond between C-5 and C-6 or C-4 and C-5. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

    摘要翻译： 本发明包括其中在C-5和C-6或C-4和C-5之间存在三键的前列腺素的某些类似物。 本发明还提供了可用于制备上述前列腺素类似物的新颖化学方法。 这些前列腺素类似物表现出前列腺素样活性，因此可用于与前列腺素相同的药理学目的。 其中包括降血压，术中诱导，生殖周期调节，胃分泌作用等。