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。

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。

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。

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.

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。

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.

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。

公开(公告)号：US5906985A

公开(公告)日：1999-05-25

申请号：US916028

申请日：1997-08-21

申请人： Stephen Richard Baker ,  Almudena Rubio Esteban ,  John Goldsworthy ,  Concepcion Pedregal Tercero

发明人： Stephen Richard Baker ,  Almudena Rubio Esteban ,  John Goldsworthy ,  Concepcion Pedregal Tercero

IPC分类号： A61K31/195 ,  A61P25/00 ,  A61P25/04 ,  C07C229/30 ,  C07C229/36 ,  C07C229/48 ,  A61K31/66

CPC分类号： C07C229/30 ,  Y02P20/55

摘要： Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.

摘要翻译： 下式的药物化合物，其中n为0,1或2，m为1或2，R1为氢，C1-10烷基，C2-10烯基，C2-10炔基，苯基，萘基，C1-10烷基 - 苯基 ，C 2-10烯基 - 苯基或C 2-10炔基 - 苯基，所述苯基和萘基任选被取代，R 2是氢或保护基，Q是酸性基团; 或其盐或酯。

公开(公告)号：US20120214784A1

公开(公告)日：2012-08-23

申请号：US13504176

申请日：2010-11-12

申请人： Ana Belen Benito Collado ,  Nuria Diaz Buezo ,  Alma Maria Jimenez-Aguado ,  Celia Lafuente Blanco ,  Maria Angeles Martinez-Grau ,  Concepcion Pedregal Tercero ,  Miguel Angel Toledo Escribano

发明人： Ana Belen Benito Collado ,  Nuria Diaz Buezo ,  Alma Maria Jimenez-Aguado ,  Celia Lafuente Blanco ,  Maria Angeles Martinez-Grau ,  Concepcion Pedregal Tercero ,  Miguel Angel Toledo Escribano

IPC分类号： A61K31/438 ,  A61P25/24 ,  A61P3/04 ,  A61P25/06 ,  C07D495/20 ,  A61K31/5377

CPC分类号： C07D495/20

摘要： An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraines.

摘要翻译： 描述了下式的ORL-1受体拮抗剂：其用途及其制备方法。 认为ORL-1拮抗剂可用于治疗抑郁症和/或用于超重或肥胖症治疗超重，肥胖和/或体重维持治疗。 某些化合物也通过动物模型证明了本发明的化合物可用于治疗偏头痛。

公开(公告)号：US5990165A

公开(公告)日：1999-11-23

申请号：US46445

申请日：1998-03-24

申请人： Concepcion Pedregal Tercero ,  Almudena Rubio Esteban

发明人： Concepcion Pedregal Tercero ,  Almudena Rubio Esteban

IPC分类号： A61K31/195 ,  A61K31/215 ,  A61P25/26 ,  C07C227/22 ,  C07C229/30 ,  C07C229/32 ,  C07C229/36 ,  C07C323/58

CPC分类号： C07C229/30 ,  C07C2101/08 ,  C07C2101/14 ,  Y02P20/55

摘要： A pharmaceutical compound of the formula: ##STR1## in which n is 1 or 2, R.sup.1 is --CO.sub.2 H, R.sup.2 is hydrogen or C.sub.1-4 alkyl andR.sup.3 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, optionally substituted phenyl C.sub.2-10 alkenyl,(optionally substituted phenyl).sub.2 -C.sub.1-4 alkyl, optionally substituted C.sub.3-7 cycloalkyl, optionally substituted C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl or optionally substituted C.sub.3-7 cycloalkyl-C.sub.2-10 alkenyl, orR.sup.2 and R.sup.3, together with the carbon atom to which they are attached, form an optionally substituted C.sub.4-7 cycloalkyl group;or a salt or ester thereof other than the compounds .gamma.-propylidene-L-glutamic acid, .gamma.-ethylidene-L-glutamic acid and .gamma.-methylidene-L-glutamic acid.

摘要翻译： 下式的药物化合物：其中n为1或2，R 1为-CO 2 H，R 2为氢或C 1-4烷基，R 3为氢，C 1-10烷基，C 2-10烯基，任选取代的苯基，任选取代的苯基 -C 1-4烷基，任选取代的苯基C 2-10烯基，（任选取代的苯基）2 -C 1-4烷基，任选取代的C 3-7环烷基，任选取代的C 3-7环烷基-C 1-4烷基或任选取代的C 3-7 环烷基-C 2-10烯基，或者R 2和R 3与它们所连接的碳原子一起形成任选取代的C 4-7环烷基; 或其除了γ-亚丙基-L-谷氨酸，γ-亚乙基-L-谷氨酸和γ-亚甲基-L-谷氨酸的化合物的盐或酯。