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公开(公告)号:US20060293372A1
公开(公告)日:2006-12-28
申请号:US10774043
申请日:2004-02-05
申请人: Maher Qabar , Michael McMillan , Michael Kahn , John Tulinsky , Cyprian Ogbu , Jessymol Mathew
发明人: Maher Qabar , Michael McMillan , Michael Kahn , John Tulinsky , Cyprian Ogbu , Jessymol Mathew
IPC分类号: A61K31/43 , A61K31/424 , A61K31/4196
CPC分类号: A61K31/4035 , A61K31/407 , A61K31/4152 , A61K31/4196 , A61K31/424 , A61K31/428 , A61K31/43 , A61K31/437 , A61K31/5025 , C07K1/047 , C07K5/021 , C07K5/06139 , C07K5/06191 , C07K5/0821 , C07K5/1024 , C07K7/06
摘要: β-sheet mimetics and methods relating to the same are disclosed. The β-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a β-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.
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公开(公告)号:US20050250780A1
公开(公告)日:2005-11-10
申请号:US11108267
申请日:2005-04-18
申请人: Maher Qabar , Marcin Stasiak , Jessymol Mathew , Thomas Little , Danwen Huang
发明人: Maher Qabar , Marcin Stasiak , Jessymol Mathew , Thomas Little , Danwen Huang
IPC分类号: A61K31/525 , A61P29/00 , C07D487/04
CPC分类号: C07D487/04
摘要: Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.
摘要翻译: 公开了具有下列结构的逆转模拟物及其相关方法:包括其药学上可接受的盐和立体异构体,其中R 1,R 2,R 2, 3>和R 4>如本文所定义。 这些化合物在广泛的应用中具有应用价值,包括用作诊断和治疗剂。 特别地,本发明的化合物和含有这些化合物的药物组合物是神经激肽(速激肽)拮抗剂。 还公开了包含本发明的反转模拟物的文库。
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公开(公告)号:US20090005344A1
公开(公告)日:2009-01-01
申请号:US11718277
申请日:2005-10-27
申请人: James F. Burns , Leonardo A. Cabana , Glenn C. Collupy , John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
发明人: James F. Burns , Leonardo A. Cabana , Glenn C. Collupy , John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
IPC分类号: A61K31/4184 , A61K31/381 , A61P43/00 , A61P29/00 , A61P19/02 , A61P17/06 , A61P19/08 , A61P11/06
CPC分类号: C07F5/025 , C07D235/18 , C07D417/04
摘要: Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要翻译: 描述了咪唑和苯并咪唑硼酸化合物,其类似物和药物制剂,以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α(TNF-α)的方法。
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公开(公告)号:US20080319044A1
公开(公告)日:2008-12-25
申请号:US11718286
申请日:2005-10-27
申请人: John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , Jan J. Scicinski , David Middlemiss
发明人: John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , Jan J. Scicinski , David Middlemiss
IPC分类号: A61K31/404 , C07D209/04 , A61P1/00 , A61P19/02 , A61P17/06 , A61P25/28 , A61P9/00 , A61P3/10 , A61P35/00 , A61P9/12 , A61P15/10
CPC分类号: C07D491/04 , C07D209/08 , C07F5/025
摘要: Indole boronic acid compounds, and analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要翻译: 描述了吲哚硼酸化合物及其类似物和药物制剂,以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α(TNF-α)的方法。
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公开(公告)号:US07405212B2
公开(公告)日:2008-07-29
申请号:US11121337
申请日:2005-05-03
申请人: Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
发明人: Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
IPC分类号: C07D498/08 , C07D263/00
CPC分类号: C40B40/04 , C07D487/08 , C07D513/08 , C40B30/04
摘要: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.
摘要翻译: 模拟具有以下结构的生物活性肽和蛋白质的螺旋区域的二级结构的化合物:包括其药学上可接受的盐和立体异构体,其中Y,A,B,R 1和R 2 SUB>如本文所定义。 这些化合物在广泛的应用中具有应用价值,包括用作诊断和治疗剂。 特别地,本发明的化合物和含有它们的药物组合物是神经激肽(速激肽)拮抗剂。 还公开了含有本发明化合物的文库,以及筛选这些文库以鉴定生物活性成员的方法。
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公开(公告)号:US06372744B1
公开(公告)日:2002-04-16
申请号:US09501052
申请日:2000-02-09
申请人: Maher N. Qabar , Michael K. McMillan , Michael S. Kahn , John E. Tulinsky , Cyprian O. Ogbu , Jessymol Mathew
发明人: Maher N. Qabar , Michael K. McMillan , Michael S. Kahn , John E. Tulinsky , Cyprian O. Ogbu , Jessymol Mathew
IPC分类号: A61K315025
CPC分类号: A61K31/4035 , A61K31/407 , A61K31/4152 , A61K31/4196 , A61K31/424 , A61K31/428 , A61K31/43 , A61K31/437 , A61K31/5025 , C07K1/047 , C07K5/021 , C07K5/06139 , C07K5/06191 , C07K5/0821 , C07K5/1024 , C07K7/06
摘要: &bgr;-sheet mimetics and methods relating to the same are disclosed. The &bgr;-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a &bgr;-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.
摘要翻译: 公开了β-折叠模拟物和与其相关的方法。 β-折叠模拟物可用作蛋白酶和激酶抑制剂,以及转录因子和蛋白质 - 蛋白质结合相互作用的抑制剂。 本发明的方法包括施用β-折叠模拟物,或其用途用于制备用于治疗与靶向蛋白酶,激酶,转录因子和/或蛋白质 - 蛋白质结合相互作用相关的多种病症的药物。
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公开(公告)号:US6117896A
公开(公告)日:2000-09-12
申请号:US22934
申请日:1998-02-12
申请人: Maher N. Qabar , Michael K. McMillan , Michael S. Kahn , John E. Tulinsky , Cyprian O. Ogbu , Jessymol Mathew
发明人: Maher N. Qabar , Michael K. McMillan , Michael S. Kahn , John E. Tulinsky , Cyprian O. Ogbu , Jessymol Mathew
IPC分类号: A61K31/4035 , A61K31/407 , A61K31/4152 , A61K31/428 , A61K31/437 , A61K31/5025 , A61K38/00 , A61K38/04 , A61K38/55 , C07D249/12 , C07K1/04 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/097 , C07K5/117 , C07K7/06 , A61K31/41 , C07K5/00 , C07K7/00 , C07K16/00
CPC分类号: A61K31/4035 , A61K31/407 , A61K31/4152 , A61K31/4196 , A61K31/424 , A61K31/428 , A61K31/43 , A61K31/437 , A61K31/5025 , C07K1/047 , C07K5/021 , C07K5/06139 , C07K5/06191 , C07K5/0821 , C07K5/1024 , C07K7/06
摘要: .beta.-sheet mimetics and methods relating to the same are disclosed. The .beta.-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a .beta.-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.
摘要翻译: 公开了β-折叠模拟物和与之相关的方法。 β-折叠模拟物可用作蛋白酶和激酶抑制剂,以及转录因子和蛋白质 - 蛋白质结合相互作用的抑制剂。 本发明的方法包括施用β-折叠模拟物,或其用途用于制备用于治疗与靶向蛋白酶,激酶,转录因子和/或蛋白质 - 蛋白质结合相互作用相关的多种病症的药物。
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公开(公告)号:US20080269204A1
公开(公告)日:2008-10-30
申请号:US11718284
申请日:2005-10-27
申请人: Tatyana Dyakonov , Michael L. Jones , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
发明人: Tatyana Dyakonov , Michael L. Jones , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
IPC分类号: C07D279/16 , A61K31/5415 , C07D265/36 , A61P1/00 , A61P17/06 , A61P11/00 , A61P3/10 , A61P9/12 , A61P15/10 , A61P35/00 , A61P25/28 , A61P11/06 , A61P19/02 , A61P29/00 , A61K31/536
CPC分类号: C07F5/025
摘要: Benzolactam boronic acid compounds and pharmaceutical formulations are described along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要翻译: 本文描述了苯甲酰硼酸化合物和药物制剂及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α(TNF-α)的方法。
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公开(公告)号:US07345040B2
公开(公告)日:2008-03-18
申请号:US11108267
申请日:2005-04-18
申请人: Maher N. Qabar , Marcin Stasiak , Jessymol Mathew , Thomas Little , Danwen Huang
发明人: Maher N. Qabar , Marcin Stasiak , Jessymol Mathew , Thomas Little , Danwen Huang
IPC分类号: A61K31/5025 , C07D471/04 , C07D487/04
CPC分类号: C07D487/04
摘要: Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.
摘要翻译: 公开了具有下列结构的逆转模拟物及其相关方法:包括其药学上可接受的盐和立体异构体,其中R 1,R 2,R 2, 3>和R 4>如本文所定义。 这些化合物在广泛的应用中具有应用价值,包括用作诊断和治疗剂。 特别地,本发明的化合物和含有这些化合物的药物组合物是神经激肽(速激肽)拮抗剂。 还公开了包含本发明的反转模拟物的文库。
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公开(公告)号:US20050222143A1
公开(公告)日:2005-10-06
申请号:US11121337
申请日:2005-05-03
申请人: Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Lee
发明人: Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Lee
IPC分类号: A61P25/06 , A61P25/28 , A61P29/00 , C07D487/08 , C07D498/08 , C07D513/08 , C40B30/04 , C40B40/04 , A61K31/538 , A61K31/519
CPC分类号: C40B40/04 , C07D487/08 , C07D513/08 , C40B30/04
摘要: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.
摘要翻译: 模拟具有以下结构的生物活性肽和蛋白质的螺旋区域的二级结构的化合物:包括其药学上可接受的盐和立体异构体,其中Y,A,B,R 1和R 2 SUB>如本文所定义。 这些化合物在广泛的应用中具有应用价值,包括用作诊断和治疗剂。 特别地,本发明的化合物和含有它们的药物组合物是神经激肽(速激肽)拮抗剂。 还公开了含有本发明化合物的文库,以及筛选这些文库以鉴定生物活性成员的方法。
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