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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：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：US20080287414A1
公开(公告)日：2008-11-20
申请号：US11630231
申请日：2005-06-27
申请人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Chunze Li , Lou Anne Neilson , Christy M. Olson , Edward S. Tasber
发明人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Chunze Li , Lou Anne Neilson , Christy M. Olson , Edward S. Tasber
IPC分类号： A61K31/5383 , A61P35/00 , A61K31/551 , A61K31/542 , C07D498/04
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的根据式（I）的三环吡唑。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US07632833B2
公开(公告)日：2009-12-15
申请号：US11630231
申请日：2005-06-27
申请人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Chunze Li , Lou Anne Neilson , Christy M. Olson , Edward S. Tasber
发明人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Chunze Li , Lou Anne Neilson , Christy M. Olson , Edward S. Tasber
IPC分类号： C07D498/04 , A61K31/5383 , A61K31/551 , A61K31/542
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的根据式（I）的三环吡唑。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20090118200A1
公开(公告)日：2009-05-07
申请号：US11920596
申请日：2006-05-22
申请人： Jeffrey M. Bergman , Paul J. Coleman , Christopher D. Cox , George D. Hartman , Craig Lindsley , Swati Pal Mercer , Anthony J. Roecker , David B. Whitman
发明人： Jeffrey M. Bergman , Paul J. Coleman , Christopher D. Cox , George D. Hartman , Craig Lindsley , Swati Pal Mercer , Anthony J. Roecker , David B. Whitman
IPC分类号： A61K38/05 , C07D403/12 , C07D401/14 , C07D413/14 , A61K31/4184 , A61P25/00
CPC分类号： C07D403/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的脯氨酸双酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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公开(公告)号：US20110207747A1
公开(公告)日：2011-08-25
申请号：US13126620
申请日：2009-10-26
IPC分类号： A61K31/497 , C07D213/56 , A61K31/4418 , C07D401/14 , A61K31/444 , C07D401/10 , C07D231/10 , A61K31/415 , A61K31/4439 , A61P3/04 , A61P25/00
CPC分类号： A61K31/437 , A61K31/4439 , C07D213/56 , C07D213/61 , C07D231/12 , C07D241/12 , C07D401/10 , C07D401/12 , C07D401/14
摘要： The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的2,5-二取代的苯基甲酰胺化合物，其可用于治疗或预防其中涉及食欲肽受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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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：US08362009B2
公开(公告)日：2013-01-29
申请号：US12739304
申请日：2008-10-27
IPC分类号： A61P43/00 , A61K31/551 , C07D243/06
CPC分类号： C07D403/14 , C07D403/04 , C07D413/14 , C07D417/14
摘要： The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的二氮杂环庚烷化合物，其可用于治疗神经性和精神疾病以及食欲素受体参与的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗其中涉及食欲素受体的疾病中的用途。
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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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