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公开(公告)号:US5861409A
公开(公告)日:1999-01-19
申请号:US835774
申请日:1997-04-08
申请人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号: C07D471/04 , A61K31/44
CPC分类号: C07D471/04
摘要: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
摘要翻译: 本发明提供具有有用的中枢神经系统活性的新颖的四氢-β-咔啉化合物。 此外,提供了四氢-β-咔啉相关化合物,其是有用的中间体并具有有益的中枢神经系统活性。 本发明提供了使用新型四氢-β-咔啉及相关化合物的配方和方法。 这些化合物特别可用于5-HT 2B受体的调节。
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公开(公告)号:US5861408A
公开(公告)日:1999-01-19
申请号:US835452
申请日:1997-04-08
申请人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号: C07D471/04 , A61K31/44 , C07D471/10
CPC分类号: C07D471/04
摘要: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
摘要翻译: 本发明提供具有有用的中枢神经系统活性的新颖的四氢-β-咔啉化合物。 此外,提供了四氢-β-咔啉相关化合物,其是有用的中间体并具有有益的中枢神经系统活性。 本发明提供了使用新型四氢-β-咔啉及相关化合物的配方和方法。 这些化合物特别可用于5-HT 2B受体的调节。
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公开(公告)号:US5869691A
公开(公告)日:1999-02-09
申请号:US838377
申请日:1997-04-08
申请人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号: C07D471/04 , C07D209/18 , C07D209/10 , C07D209/20
CPC分类号: C07D471/04
摘要: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
摘要翻译: 本发明提供具有有用的中枢神经系统活性的新颖的四氢-β-咔啉化合物。 此外,提供了四氢-β-咔啉相关化合物,其是有用的中间体并具有有益的中枢神经系统活性。 本发明提供了使用新型四氢-β-咔啉及相关化合物的配方和方法。 这些化合物特别可用于5-HT 2B受体的调节。
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公开(公告)号:US5861410A
公开(公告)日:1999-01-19
申请号:US833751
申请日:1997-04-09
申请人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号: C07D471/04 , A61K31/44 , C07D487/04
CPC分类号: C07D471/04
摘要: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
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公开(公告)号:US5663178A
公开(公告)日:1997-09-02
申请号:US380565
申请日:1995-02-06
申请人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号: A61K31/40 , A61K31/42 , A61K31/44 , A61K31/475 , A61K31/48 , A61K31/495 , A61K31/55 , C07D471/04
CPC分类号: C07D471/04 , A61K31/40 , A61K31/42 , A61K31/44 , A61K31/475 , A61K31/48 , A61K31/495 , A61K31/55
摘要: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
摘要翻译: 本发明提供具有有用的中枢神经系统活性的新颖的四氢-β-咔啉化合物。 此外,提供了四氢-β-咔啉相关化合物,其是有用的中间体并具有有益的中枢神经系统活性。 本发明提供了使用新型四氢-β-咔啉及相关化合物的配方和方法。 这些化合物特别可用于5-HT 2B受体的调节。
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公开(公告)号:US5643916A
公开(公告)日:1997-07-01
申请号:US444449
申请日:1995-05-19
申请人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人: James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号: A61K31/40 , A61K31/42 , A61K31/44 , A61K31/475 , A61K31/48 , A61K31/495 , A61K31/55 , C07D471/04 , C07D487/04
CPC分类号: C07D471/04 , A61K31/40 , A61K31/42 , A61K31/44 , A61K31/475 , A61K31/48 , A61K31/495 , A61K31/55
摘要: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
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公开(公告)号:US5739164A
公开(公告)日:1998-04-14
申请号:US713624
申请日:1996-09-13
申请人: Jesus Ezquerra Carrera , Almudena Rubio Esteban , Andre Mann , Angele Schoenfelder , Darryle Darwin Schoepp , Concepcion Pedregal Tercero , Camille-Georges Wermuth
发明人: Jesus Ezquerra Carrera , Almudena Rubio Esteban , Andre Mann , Angele Schoenfelder , Darryle Darwin Schoepp , Concepcion Pedregal Tercero , Camille-Georges Wermuth
IPC分类号: A61K31/00 , A61K31/19 , A61K31/195 , A61K31/20 , A61K31/215 , A61K31/38 , A61K31/41 , A61P1/08 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07C229/36 , C07D257/04 , C07D333/24 , C07D409/06
CPC分类号: C07D257/04 , C07C229/36
摘要: Disclosed herein is a method of treating a disease of the central nervous system with a compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl, Y is --CH.dbd.CH--, and Z is (i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, (ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, (iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or (iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.
摘要翻译: 本文公开了一种用式“IMAGE”的化合物治疗中枢神经系统疾病的方法,其中m为0,1或2,n和q各自为0或1至5,p为0或1 X是-CO 2 H或四唑基,Y是-CH = CH-,Z是(i)苯基,萘基或噻吩基,所述苯基,萘基和噻吩基任选被取代,(ii)-CHR 1 R 2,其中R 1和R 2各自是苯基 萘基或噻吩基,所述苯基,萘基和噻吩基任选被取代,(iii)= CR1R2,其中R1和R2各自为苯基,萘基或噻吩基,所述苯基,萘基和噻吩基任选被取代,或(iv) r为0或1至3,苯环任选被取代; 条件是当Z为苯基且m为1时,p为1; 及其盐和酯。
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