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公开(公告)号:US06355643B1
公开(公告)日:2002-03-12
申请号:US09516757
申请日:2000-03-01
申请人: William C. Lumma , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Christopher J. Dinsmore , Jeffrey M. Bergman
发明人: William C. Lumma , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Christopher J. Dinsmore , Jeffrey M. Bergman
IPC分类号: A61K31496
CPC分类号: C07D233/64 , A61K31/496
摘要: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.
摘要翻译: 本发明包括具有烷酰基,烷基磺酰基,烷基酰氨基或烷氧基羰基取代基的未取代和取代的含哌嗪化合物,并且具有抑制异戊烯基 - 蛋白质转移酶的式A。 特别地,本发明涉及在体内作为er牛儿基ger牛蛋白转移酶I型(GGTase-I)抑制剂有效的异戊烯基 - 蛋白转移酶抑制剂,并且抑制H-Ras蛋白和K4B-Ras蛋白两者的细胞加工 。 这些治疗化合物可用于治疗癌症。
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公开(公告)号:US06376496B1
公开(公告)日:2002-04-23
申请号:US09516756
申请日:2000-03-01
申请人: George D. Hartman , William C. Lumma, Jr. , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Jeffrey M. Bergman
发明人: George D. Hartman , William C. Lumma, Jr. , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Jeffrey M. Bergman
IPC分类号: C07D40304
CPC分类号: C07D233/64
摘要: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
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公开(公告)号:US07709476B2
公开(公告)日:2010-05-04
申请号:US10571857
申请日:2004-09-17
IPC分类号: C07D217/16 , A61K31/47
CPC分类号: C07D217/24 , A61K31/4725 , A61K31/5377 , A61K45/06 , C04B35/632 , C07D401/12 , C07D405/12
摘要: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构(I)的化合物等。
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公开(公告)号:US20100041652A1
公开(公告)日:2010-02-18
申请号:US12605690
申请日:2009-10-26
IPC分类号: A61K31/5377 , A61K31/445 , A61K31/40 , A61K31/4523
CPC分类号: C07D403/12 , C07D209/42 , C07D401/12 , C07D405/12 , C07D409/12
摘要: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译: 本发明涉及能够抑制,调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含吲哚磺酰胺部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐,水合物和立体异构体。
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公开(公告)号:US07560546B2
公开(公告)日:2009-07-14
申请号:US10523285
申请日:2003-08-05
IPC分类号: A01N55/02 , A01N43/62 , A01N43/40 , C07D413/00 , C07D415/00 , C07D265/30 , A61K31/54 , A61K31/535
CPC分类号: C07D487/10 , C07D209/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D491/04 , C07D491/10 , C07D513/04 , C07D513/08
摘要: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译: 本发明涉及能够抑制,调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含磺酰基吲哚部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐,水合物和立体异构体。
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公开(公告)号:US6103723A
公开(公告)日:2000-08-15
申请号:US170951
申请日:1998-10-13
IPC分类号: A61K31/504 , A61K31/553 , C07D487/08 , C07D498/08
CPC分类号: A61K31/504 , A61K31/553 , C07D487/08 , C07D498/08
摘要: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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公开(公告)号:US08008295B2
公开(公告)日:2011-08-30
申请号:US12605690
申请日:2009-10-26
IPC分类号: A61K31/5377 , A61K31/445 , A61K31/40 , A61K31/4523
CPC分类号: C07D403/12 , C07D209/42 , C07D401/12 , C07D405/12 , C07D409/12
摘要: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译: 本发明涉及能够抑制,调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含吲哚磺酰胺部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐,水合物和立体异构体。
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公开(公告)号:US07692017B2
公开(公告)日:2010-04-06
申请号:US10571841
申请日:2004-09-17
IPC分类号: C07D215/00 , C07D215/38 , C07D215/12
CPC分类号: C07D215/48 , C07D401/02 , C07D401/04 , C07D401/12 , C07D403/02 , C07D413/02 , C07D413/12 , C07D413/14
摘要: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构(I)的化合物等。
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公开(公告)号:US20080227778A1
公开(公告)日:2008-09-18
申请号:US10571857
申请日:2004-09-17
IPC分类号: A61K31/5377 , A61K31/472 , C07D413/12 , C07D401/12 , A61P9/06 , A61K31/4725 , C07D217/24
CPC分类号: C07D217/24 , A61K31/4725 , A61K31/5377 , A61K45/06 , C04B35/632 , C07D401/12 , C07D405/12
摘要: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构(I)的化合物等。
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公开(公告)号:US07569589B2
公开(公告)日:2009-08-04
申请号:US11188466
申请日:2005-07-25
申请人: Mark T. Bilodeau , Christopher J. Dinsmore , Jeffrey M. Bergman , B. Wesley Trotter , Lou Anne Neilson , Zhicai Wu , Peter Manley , John Hartnett
发明人: Mark T. Bilodeau , Christopher J. Dinsmore , Jeffrey M. Bergman , B. Wesley Trotter , Lou Anne Neilson , Zhicai Wu , Peter Manley , John Hartnett
IPC分类号: C07D403/14 , A61K31/44
CPC分类号: C07D213/57 , C07D213/06 , C07D213/30 , C07D213/42 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/84 , C07D401/14 , C07D413/14 , C07D417/14
摘要: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构的化合物等。
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