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公开(公告)号：EP1784393B1
公开(公告)日：2009-07-01
申请号：EP05807734.8
申请日：2005-08-31
发明人： WILSON, Dean, M. , TERMIN, Andreas, P. , GONZALEZ, Jesus, E., III , FANNING, Lev, T., D. , NEUBERT, Timothy, D. , KRENITSKY, Paul , JOSHI, Pramod , HURLEY, Dennis, J. , SHETH, Urvi , BOGER, Joshua, S.
IPC分类号： C07D239/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , A61P9/06 , A61P25/00 , A61K31/498
CPC分类号： C07D401/04 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14
摘要： The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：EP0537269B1
公开(公告)日：1997-10-15
申请号：EP91913236.5
申请日：1991-07-02
发明人： ARMISTEAD, David, M. , BOGER, Joshua, S. , MEYERS, Harold, V. , SAUNDERS, Jeffrey, O. , TUNG, Roger, D.
IPC分类号： C07D211/60 , C07D207/16 , C07D401/06 , C07D405/06 , C07D409/06 , C07D317/60 , C07C235/72 , A61K31/395 , A61K31/215 , A61K31/335
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及一类对FK-506结合蛋白（FKBP）具有亲和性的新型免疫抑制化合物。 一旦与该蛋白质结合，免疫抑制化合物抑制FKBP的脯氨酰肽基顺反异构酶（旋转异构酶）活性并抑制T细胞活化。 这样，本发明的化合物可以用作免疫抑制药物以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物的各种自身免疫疾病。
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公开(公告)号：EP0537269A1
公开(公告)日：1993-04-21
申请号：EP91913236.0
申请日：1991-07-02
发明人： ARMISTEAD, David, M. , BOGER, Joshua, S. , MEYERS, Harold, V. , SAUNDERS, Jeffrey, O. , TUNG, Roger, D.
IPC分类号： A61K31 , A61P25 , A61P37 , C07C233 , C07C235 , C07D207 , C07D211 , C07D307 , C07D317 , C07D333 , C07D401 , C07D403 , C07D405 , C07D409
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： Nouvelle classe de composés immunosuppresseurs présentant une affinité vis-à-vis de la protéine de liaison FK-506 (PLFK). Une fois liés à cette protéine, les composés immunosuppresseurs inhibent l'activité d'isomérase (rotamase) cis-trans de peptidyle de propyle de la PBFK et ils inhibent l'activation des lymphocytes T. On peut utiliser les composés de l'invention en tant que tels comme médicaments immunosuppresseurs afin de prévenir ou de réduire significativement le rejet de greffe dans la moelle osseuse ainsi que les transplantations d'organes, et on peut les utiliser dans le traitement d'une large variété de maladies autoimmunitaires chez l'homme et chez l'animal.
摘要翻译： 一类新的对FK-506结合蛋白（PLFK）具有亲和力的免疫抑制化合物。 一旦与该蛋白质结合，免疫抑制化合物抑制PBFK的丙基肽基顺反异构酶（旋转异构酶）活性并抑制T淋巴细胞的活化。 作为预防或显着减少骨髓移植排斥反应和器官移植的免疫抑制药物，并且可用于治疗人类各种自身免疫性疾病， 在动物中。
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公开(公告)号：EP1784393A1
公开(公告)日：2007-05-16
申请号：EP05807734.8
申请日：2005-08-31
发明人： WILSON, Dean, M. , TERMIN, Andreas, P. , GONZALEZ, Jesus, E., III , FANNING, Lev, T., D. , NEUBERT, Timothy, D. , KRENITSKY, Paul , JOSHI, Pramod , HURLEY, Dennis, J. , SHETH, Urvi , BOGER, Joshua, S.
IPC分类号： C07D239/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , A61P9/06 , A61P25/00 , A61K31/498
CPC分类号： C07D401/04 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14
摘要： The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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5.发明授权1-(2-OXO-ACETYL)-PIPERIDINE-2-CARBOXYLIC ACID DERIVATIVES AS MULTI-DRUG-RESISTENT CANCER CELL SENSITIZERS 失效1-（2-氧代 - 乙酰基） - 哌啶-2-羧酸衍生物作为增感剂对多药耐药性的癌细胞
公开(公告)号：EP0662958B1
公开(公告)日：2002-12-11
申请号：EP93922748.4
申请日：1993-09-27
IPC分类号： C07D211/60 , C07D401/12 , C07D487/04 , A61K31/445
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： The present invention relates to novel compounds of formula (I) which maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance and for use in multi-drug resistant cancer therapy.
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6.发明公开1-(2-OXO-ACETYL)-PIPERIDINE-2-CARBOXYLIC ACID DERIVATIVES AS MULTI-DRUG-RESISTENT CANCER CELL SENSITIZERS 失效1-（2-氧代 - 乙酰基） - 哌啶-2-羧酸衍生物作为增感剂对多药耐药性的癌细胞。
公开(公告)号：EP0662958A1
公开(公告)日：1995-07-19
申请号：EP93922748.0
申请日：1993-09-27
IPC分类号： C07D211 , A61K31 , A61P35 , C07D207 , C07D401 , C07D403 , C07D405 , C07D409 , C07D471 , C07D473 , C07D487 , C07D235 , C07D239
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： The present invention relates to novel compounds of formula (I) which maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance and for use in multi-drug resistant cancer therapy.
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