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公开(公告)号：US06897233B2
公开(公告)日：2005-05-24
申请号：US10469560
申请日：2002-03-01
IPC分类号： A61K31/4015 , A61P31/00 , A61P31/04 , A61P43/00 , C07D207/26 , C07D207/12 , A61K31/40
CPC分类号： C07D207/26
摘要： PDF inhibitors and novel methods for their use are provided.
摘要翻译： 提供PDF抑制剂及其使用的新方法。
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公开(公告)号：US07456211B2
公开(公告)日：2008-11-25
申请号：US11683089
申请日：2007-03-07
申请人： Kelly M. Aubart , Jia-Ning Xiang , Siegfried B. Christensen, IV , Xiangmin Liao , Maxwell D. Cummings
发明人： Kelly M. Aubart , Jia-Ning Xiang , Siegfried B. Christensen, IV , Xiangmin Liao , Maxwell D. Cummings
IPC分类号： A61K31/4015 , C07D207/10
CPC分类号： C07D207/26 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06
摘要： The present invention involves novel anti-bacterial compounds represented by Formula (I), pharmaceutical compositions thereof, their use as PDF inhibitors, and their use in the treatment of bacterial infections.
摘要翻译： 本发明涉及由式（I）表示的新型抗菌化合物，其药物组合物，它们作为PDF抑制剂的用途及其在治疗细菌感染中的用途。
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公开(公告)号：US07375120B2
公开(公告)日：2008-05-20
申请号：US10553142
申请日：2003-04-16
IPC分类号： A61K31/44 , A61K31/24 , A61K31/235 , A61K31/18
CPC分类号： C07C311/51 , C07D213/70
摘要： Novel PDF inhibitors and novel methods for their use are provided.
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公开(公告)号：US06852882B2
公开(公告)日：2005-02-08
申请号：US10478620
申请日：2002-06-04
IPC分类号： A61K31/166 , A61K31/19 , A61K31/381 , A61K31/4184 , A61P31/04 , C07C259/06 , C07D235/08 , C07D333/38 , C07C259/04
CPC分类号： A61K31/19 , C07C259/06 , C07D333/38
摘要： Novel PDF inhibitors and novel methods for their use are provided.
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公开(公告)号：US08173654B2
公开(公告)日：2012-05-08
申请号：US12187524
申请日：2008-08-07
申请人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
发明人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
IPC分类号： A61K31/4985 , C07D487/04 , A61P3/10 , A61P17/06 , A61P25/18 , A61P19/02 , A61P9/10 , A61P9/00 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译： 本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及使用 的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。
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公开(公告)号：US07662824B2
公开(公告)日：2010-02-16
申请号：US11377077
申请日：2006-03-16
申请人： Kristi Leonard , Tianbao Lu , Robert W. Tuman , Dana L. Johnson , Anna C. Maroney , Jan L. Sechler , Richard W. Connors , Richard S. Alexander , Maxwell D. Cummings , Robert A. Galemmo , Thomas P. Markotan
发明人： Kristi Leonard , Tianbao Lu , Robert W. Tuman , Dana L. Johnson , Anna C. Maroney , Jan L. Sechler , Richard W. Connors , Richard S. Alexander , Maxwell D. Cummings , Robert A. Galemmo , Thomas P. Markotan
IPC分类号： A61K31/496 , A61K31/404 , C07D405/14 , C07D405/12 , C07D407/14
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译： 本发明涉及式I的酰腙化合物：其中R 1，R 2和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及使用这些化合物来减少或抑制 c-Met在细胞或受试者中的激酶活性和调节细胞或受试者中的c-Met表达，以及这些化合物用于预防或治疗受试者的细胞增殖性病症和/或与c- 遇见 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。
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公开(公告)号：US07563784B2
公开(公告)日：2009-07-21
申请号：US11410558
申请日：2006-04-25
申请人： Maxwell D. Cummings , Robert W. Marquis, Jr. , Yu Ru , Scott K. Thompson , Daniel F. Veber , Dennis S. Yamashita
发明人： Maxwell D. Cummings , Robert W. Marquis, Jr. , Yu Ru , Scott K. Thompson , Daniel F. Veber , Dennis S. Yamashita
IPC分类号： A61P19/08 , A61P19/10 , A61K31/55 , C07D401/00 , C07D403/00 , C07D413/00
CPC分类号： C07C271/12 , C07C271/14 , C07D223/04 , C07D223/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D491/04 , C07D495/04
摘要： The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
摘要翻译： 本发明提供了C 1-6烷基-4-氨基 - 氮杂-3-酮蛋白酶抑制剂及其药学上可接受的盐，水合物和溶剂合物，其抑制蛋白酶，包括组织蛋白酶K，这些化合物的药物组合物，这些化合物的新中间体和方法 用于治疗过度骨丢失或软骨或基质降解的疾病，包括骨质疏松症; 牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特病 恶性高钙血症; 和代谢性骨病; 和寄生虫病，包括疟疾，通过向有需要的患者施用一种或多种本发明的化合物。
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公开(公告)号：US20090098181A1
公开(公告)日：2009-04-16
申请号：US12187524
申请日：2008-08-07
申请人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
发明人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
IPC分类号： A61F2/04 , C07D487/04 , A61K31/5025 , C12N9/99 , A61K31/541
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译： 本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及使用 的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。
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公开(公告)号：US08030305B2
公开(公告)日：2011-10-04
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
发明人： Tianbao Lu , Richard Alexander , Richard W. Connors , Maxwell D. Cummings , Robert A. Galemmo , Heather Rae Hufnagel , Dana L. Johnson , Ehab Khalil , Kristi A. Leonard , Thomas P. Markotan , Anna C. Maroney , Jan L. Sechler , Jeremy M. Travins , Robert W. Tuman
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译： 本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及使用 的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中用于预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。
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10.发明授权Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions 失效噻吩脒，其组合物和治疗补体介导的疾病和病症的方法公开(公告)号：US07138530B2
公开(公告)日：2006-11-21
申请号：US10515554
申请日：2003-05-28
申请人： Nalin Subasinghe , Ehab Khalil , Kristi A. Leonard , Farah Ali , Heather Hufnagel , Jeremy M. Travins , Shelley K. Ballentine , Kenneth T. Wilson , Maxwell D. Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen , Jonathan M. Rudolph , Hui Huang
发明人： Nalin Subasinghe , Ehab Khalil , Kristi A. Leonard , Farah Ali , Heather Hufnagel , Jeremy M. Travins , Shelley K. Ballentine , Kenneth T. Wilson , Maxwell D. Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen , Jonathan M. Rudolph , Hui Huang
IPC分类号： C07D333/32 , A61K31/38
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D495/04 , C07F7/0812 , C07F9/655345
摘要： Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
摘要翻译： 公开了一种治疗由补体级联的经典途径介导的急性或慢性病症症状的方法，包括向需要这种治疗的哺乳动物施用治疗有效量的式（I）化合物或溶剂合物， 水合物或其药学上可接受的盐; 其中R 1，R 2，R 3，R 4和R 7， 在本说明书中定义，Z是SO或SO 2，Ar是如本文所定义的芳族或杂芳族基团。
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