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公开(公告)号：US06358985B1
公开(公告)日：2002-03-19
申请号：US09342577
申请日：1999-06-29
申请人： Neville J. Anthony , Ian M. Bell , Douglas C. Beshore , Terrence M. Ciccarone , S. Jane de Solms , Christopher J. Dinsmore , Gerald E. Stokker
发明人： Neville J. Anthony , Ian M. Bell , Douglas C. Beshore , Terrence M. Ciccarone , S. Jane de Solms , Christopher J. Dinsmore , Gerald E. Stokker
IPC分类号： A61K314164
CPC分类号： A61K31/4174 , A61K31/00
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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公开(公告)号：US06410534B1
公开(公告)日：2002-06-25
申请号：US09347673
申请日：1999-06-29
IPC分类号： A61K314188
CPC分类号： C07D498/04 , A61K31/415 , A61K31/335 , A61K2300/00
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation 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：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：US07763614B2
公开(公告)日：2010-07-27
申请号：US10572236
申请日：2004-09-22
申请人： Richard Isaacs , Christopher J. Dinsmore , B. Wesley Trotter , Nigel Liverton , Douglas C. Beshore , Nathan R. Kett , Charles J. McIntyre , Kausik K. Nanda , David A. Claremon
发明人： Richard Isaacs , Christopher J. Dinsmore , B. Wesley Trotter , Nigel Liverton , Douglas C. Beshore , Nathan R. Kett , Charles J. McIntyre , Kausik K. Nanda , David A. Claremon
IPC分类号： C07D401/02 , A61K31/47
CPC分类号： C04B35/632 , C07D217/22 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/04
摘要： The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译： 本发明涉及结构式I的化合物：可用作治疗心律失常的钾通道抑制剂等。
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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：US07879839B2
公开(公告)日：2011-02-01
申请号：US11658114
申请日：2005-07-27
申请人： Christopher J. Dinsmore , Jeffrey M. Bergman , Douglas C. Beshore , B. Wesley Trotter , Kausik K. Nanda , Richard Isaacs , Linda S. Payne , Lou Anne Neilson , Zhicai Wu , Mark T. Bilodeau , Peter J. Manley , Adrienne E. Balitza
发明人： Christopher J. Dinsmore , Jeffrey M. Bergman , Douglas C. Beshore , B. Wesley Trotter , Kausik K. Nanda , Richard Isaacs , Linda S. Payne , Lou Anne Neilson , Zhicai Wu , Mark T. Bilodeau , Peter J. Manley , Adrienne E. Balitza
IPC分类号： C07D401/14 , A61K31/438
CPC分类号： C07D213/36 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/55 , C07D213/56 , C07D213/64 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要： The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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公开(公告)号：US20090186871A1
公开(公告)日：2009-07-23
申请号：US12378473
申请日：2009-02-13
IPC分类号： A61K31/404 , C07D413/12 , A61K31/5377 , C07D403/12 , A61P35/00
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.
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公开(公告)号：US06441017B1
公开(公告)日：2002-08-27
申请号：US09656653
申请日：2000-09-07
IPC分类号： A61K314015
CPC分类号： C07D498/18 , A61K31/337 , A61K31/4178 , A61K45/06 , A61K47/665 , A61K47/6898 , B82Y5/00 , A61K2300/00
摘要： The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白转移酶（FTase）和癌基因蛋白Ras的异戊烯化的大环化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。
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公开(公告)号：US09139576B2
公开(公告)日：2015-09-22
申请号：US14115123
申请日：2012-04-30
申请人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
发明人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
IPC分类号： C07D413/12 , C07D401/14 , C07D403/10 , C07D249/18 , C07D401/10 , C07D401/12 , C07D413/10
CPC分类号： C07D413/12 , C07D249/18 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D413/10
摘要： The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增效剂的氨基甲基联芳基苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病 。 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预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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