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公开(公告)号：US08242280B2
公开(公告)日：2012-08-14
申请号：US12101110
申请日：2008-04-10
申请人： Chixu Chen , Brian Eastman , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie Hopkins , Khanh Thi Tuong Nguyen , Richard Pracitto , Paul E. Sprengeler , Ruo W. Steensma
发明人： Chixu Chen , Brian Eastman , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie Hopkins , Khanh Thi Tuong Nguyen , Richard Pracitto , Paul E. Sprengeler , Ruo W. Steensma
IPC分类号： C07D401/00
CPC分类号： C07D487/04
摘要： The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity.
摘要翻译： 本发明提供作为激酶调节剂的稠环杂环，含有这些调节剂的药物组合物，以及使用这些调节剂治疗由激酶活性介导的疾病的方法。
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公开(公告)号：US20080261921A1
公开(公告)日：2008-10-23
申请号：US12101110
申请日：2008-04-10
申请人： Chixu Chen , Brian Eastman , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie Hopkins , Khanh Thi Tuong Nguyen , Richard Pracitto , Paul E. Sprengeler , Ruo W. Steensma
发明人： Chixu Chen , Brian Eastman , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie Hopkins , Khanh Thi Tuong Nguyen , Richard Pracitto , Paul E. Sprengeler , Ruo W. Steensma
IPC分类号： A61K31/437 , C07F5/02 , C07D471/04 , A61K31/541 , A61P35/02 , C07D279/12 , A61K31/69
CPC分类号： C07D487/04
摘要： The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity.
摘要翻译： 本发明提供作为激酶调节剂的稠环杂环，含有这些调节剂的药物组合物，以及使用这些调节剂治疗由激酶活性介导的疾病的方法。
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3.发明授权公开(公告)号：US08158647B2
公开(公告)日：2012-04-17
申请号：US12129546
申请日：2008-05-29
申请人： Jeffrey M. Blaney , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie A. Hopkins , Paul A. Sprengeler , Ruo W. Steensma , Johnny Uy
发明人： Jeffrey M. Blaney , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie A. Hopkins , Paul A. Sprengeler , Ruo W. Steensma , Johnny Uy
IPC分类号： A61K31/437 , A61K31/5377 , A61K31/497 , A61P35/00 , C07D491/147 , C07D471/04
CPC分类号： C07D471/04
摘要： Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.
摘要翻译： 本文提供取代的吡咯并吡啶杂环和取代的吡唑并吡啶杂环，包含所述杂环的药物组合物和使用所述杂环治疗疾病的方法。 本文公开的杂环体作为激酶调节剂起作用，可用于治疗疾病如癌症，变态反应，哮喘，炎症，阻塞性气道疾病，自身免疫性疾病，代谢疾病，感染，CNS疾病，脑肿瘤，肥胖，哮喘，血液病症 ，退行性神经疾病，心血管疾病或与血管发生，新生血管形成或血管发生相关的疾病。
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4.发明申请公开(公告)号：US20090005356A1
公开(公告)日：2009-01-01
申请号：US12129546
申请日：2008-05-29
申请人： Jeffrey M. Blaney , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie A. Hopkins , Paul A. Sprengeler , Ruo W. Steensma , Johnny Uy
发明人： Jeffrey M. Blaney , Andreas Gosberg , Stefan N. Gradl , Gavin Hirst , Stephanie A. Hopkins , Paul A. Sprengeler , Ruo W. Steensma , Johnny Uy
IPC分类号： A61K31/437 , A61P35/00 , A61K31/5377 , C07D491/147 , A61K31/497 , C07D471/04
CPC分类号： C07D471/04
摘要： Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.
摘要翻译： 本文提供取代的吡咯并吡啶杂环和取代的吡唑并吡啶杂环，包含所述杂环的药物组合物和使用所述杂环治疗疾病的方法。 本文公开的杂环体作为激酶调节剂起作用，可用于治疗疾病如癌症，变态反应，哮喘，炎症，阻塞性气道疾病，自身免疫性疾病，代谢疾病，感染，CNS疾病，脑肿瘤，肥胖，哮喘，血液病症 ，退行性神经疾病，心血管疾病或与血管发生，新生血管形成或血管发生相关的疾病。
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5.发明授权公开(公告)号：US08178490B2
公开(公告)日：2012-05-15
申请号：US12613329
申请日：2009-11-05
申请人： Tomasz Glinka , Olga Rodny , Keith A. Bostian , David M. Wallace , Robert I. Higuchi , Chun Chow , Chi Ching Mak , Gavin Hirst , Brian Eastman
发明人： Tomasz Glinka , Olga Rodny , Keith A. Bostian , David M. Wallace , Robert I. Higuchi , Chun Chow , Chi Ching Mak , Gavin Hirst , Brian Eastman
IPC分类号： A61K38/00
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/06104 , C07K5/06113 , C07K5/06139 , C07K5/06191 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
摘要翻译： 公开了具有多碱性官能团的化合物。 该化合物抑制细菌外排泵抑制剂，并与抗菌剂组合使用以治疗或预防细菌感染。 这些组合可以有效地抵抗通过外排泵机制对抗细菌剂产生抗性的细菌感染。
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公开(公告)号：US20100152098A1
公开(公告)日：2010-06-17
申请号：US12613329
申请日：2009-11-05
申请人： Tomasz Glinka , Olga Rodny , Keith A. Bostian , David M. Wallace , Robert I. Higuchi , Chun Chow , Chi Ching Mak , Gavin Hirst , Brian Eastman
发明人： Tomasz Glinka , Olga Rodny , Keith A. Bostian , David M. Wallace , Robert I. Higuchi , Chun Chow , Chi Ching Mak , Gavin Hirst , Brian Eastman
IPC分类号： A61K38/05 , A61K38/02 , C07D265/30 , C07D241/42 , C07D215/38 , C07D211/58 , C07D211/06 , C07D213/643 , C07D213/74 , C07D231/12 , C07D209/20 , C07D207/14 , C07D333/24 , C07D321/10 , C07D319/18 , C07D309/10 , C07D307/79 , C07C311/46 , C07C237/20 , A61P31/08 , A61P31/06 , A61P31/04 , C07D217/22 , A61K31/472
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/06104 , C07K5/06113 , C07K5/06139 , C07K5/06191 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
摘要翻译： 公开了具有多碱性官能团的化合物。 该化合物抑制细菌外排泵抑制剂，并与抗菌剂组合使用以治疗或预防细菌感染。 这些组合可以有效地抵抗通过外排泵机制对抗细菌剂产生抗性的细菌感染。
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公开(公告)号：US08217067B2
公开(公告)日：2012-07-10
申请号：US11120718
申请日：2005-04-29
申请人： William A. Carroll , Arturo Perez-Medrano , Alan S. Florjancic , Derek W. Nelson , Sridhar Peddi , Tongmei Li , Eric M. Bunnelle , Gavin Hirst , Biqin C. Li
发明人： William A. Carroll , Arturo Perez-Medrano , Alan S. Florjancic , Derek W. Nelson , Sridhar Peddi , Tongmei Li , Eric M. Bunnelle , Gavin Hirst , Biqin C. Li
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D487/04 , C07D257/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/04 , C07D491/048 , C07D491/08
摘要： A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
摘要翻译： 公开了具有式（I）或式（II）的化合物作为P2X7拮抗剂，其中A，B，C，Y，Y，Z，m，v，R 1，R 2，R 3，R 4和R 5如 在说明中。 还公开了用于治疗由P2X7调节的疾病或病症的方法和组合物。
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公开(公告)号：US20190000981A1
公开(公告)日：2019-01-03
申请号：US16064061
申请日：2016-12-21
申请人： Nigel W. Bunnett , Christopher J.H. Porter , Derek Cole , Gareth Hicks , Junya Shirai , Gavin Hirst , Takeda Pharmaceutical Company Limited
发明人： Nigel W. Bunnett , Christopher J.H. Porter , Derek Cole , Gareth Hicks , Junya Shirai , Gavin Hirst
IPC分类号： A61K47/54 , A61K47/60 , A61K31/575 , A61K31/44 , A61P43/00
摘要： The present invention relates to tripartite compounds comprising a modulator moiety for endosomal G protein-coupled receptors like neurokinin-1 receptor, a linker and a lipid anchor suitable for anchoring the tripartite compound into a plasma membrane. The present invention also relates to a prodrug and a pharmaceutical composition comprising the tripartite compound and the use of the tripartite compound for the treatment of a disease or disorder mediated by endosomal G protein-coupled receptors signalling like NK1R signalling.
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公开(公告)号：US20120040932A1
公开(公告)日：2012-02-16
申请号：US13205112
申请日：2011-08-08
申请人： Gavin Hirst , Raja Reddy , Scott Hecker , Maxim Totrov , David C. Griffith , Olga Rodny , Michael N. Dudley , Serge Boyer
发明人： Gavin Hirst , Raja Reddy , Scott Hecker , Maxim Totrov , David C. Griffith , Olga Rodny , Michael N. Dudley , Serge Boyer
CPC分类号： A61K31/69 , A61K9/0019 , A61K9/0053 , A61K31/407 , A61K31/4196 , A61K31/427 , A61K31/4439 , A61K31/546 , A61K45/06 , C07F5/025 , Y02A50/401 , Y02A50/406 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483 , A61K2300/00
摘要： Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
摘要翻译： 本文公开了抗微生物化合物组合物，药物组合物，其用途和制备。 一些实施方案涉及1种环状硼酸酯衍生物及其作为治疗剂的用途。
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公开(公告)号：US20060052374A1
公开(公告)日：2006-03-09
申请号：US11221333
申请日：2005-09-07
申请人： William Carroll , Arturo Perez-Medrano , Alan Florjancic , Derek Nelson , Sridhar Peddi , Tongmei Li , Eric Bunnelle , Gavin Hirst , Biquin Li
发明人： William Carroll , Arturo Perez-Medrano , Alan Florjancic , Derek Nelson , Sridhar Peddi , Tongmei Li , Eric Bunnelle , Gavin Hirst , Biquin Li
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/415 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D487/04 , C07D257/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/04 , C07D491/048 , C07D491/08
摘要： A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
摘要翻译： 具有式（I）或式（II）的化合物
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