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1. 发明申请

US20050256104A1 Protease inhibitors 失效
标题翻译：蛋白酶抑制剂
公开(公告)号：US20050256104A1
公开(公告)日：2005-11-17
申请号：US11152745
申请日：2005-06-14
申请人： Robert Marquis , Yu Ru , Daniel Veber , Maxwell Cummings , Scott Thompson , Dennis Yamashita
发明人： Robert Marquis , Yu Ru , Daniel Veber , Maxwell Cummings , Scott Thompson , Dennis Yamashita
IPC分类号： A61K31/55 , A61K38/00 , C07D223/08 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07K5/078 , C07D43/02
CPC分类号： C07D405/14 , A61K38/00 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07K5/06139
摘要： The present invention provides 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, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译：本发明提供了抑制蛋白酶的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，包括组织蛋白酶K，这类化合物的药物组合物，这些化合物的新中间体，以及治疗疾病的方法骨质疏松过多或软骨或基质降解，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，其包括通过向有需要的患者施用本发明的化合物来抑制所述骨丢失或过度软骨或基质降解。

2. 发明申请

US20060194787A1 Protease inhibitors 失效
公开(公告)号：US20060194787A1
公开(公告)日：2006-08-31
申请号：US11410558
申请日：2006-04-25
申请人： Maxwell Cummings , Robert Marquis , Yu Ru , Scott Thompson , Daniel Veber , Dennis Yamashita
发明人： Maxwell Cummings , Robert Marquis , Yu Ru , Scott Thompson , Daniel Veber , Dennis Yamashita
IPC分类号： A61K31/55 , C07D413/02 , C07D403/02
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.

3. 发明申请

US20070066610A1 Acylhydrazones as kinase modulators 有权
标题翻译：酰腙作为激酶调节剂
公开(公告)号：US20070066610A1
公开(公告)日：2007-03-22
申请号：US11377077
申请日：2006-03-16
申请人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
发明人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/404 , C07D413/14 , C07D405/14
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的抑制剂以及这些化合物在细胞或受试者中降低或抑制c-Met的激酶活性并调节细胞或受试者中的c-Met表达的用途，以及这些化合物用于预防或在受试者中治疗与c-Met相关的细胞增殖性疾病和/或障碍。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。

4. 发明申请

US20060025412A1 Peptide deformylase inhibitors 审中-公开
标题翻译：肽变性酶抑制剂
公开(公告)号：US20060025412A1
公开(公告)日：2006-02-02
申请号：US11178823
申请日：2005-10-14
申请人： Kelly Aubart , Jia-Ning Xiang , Siegfried Christensen , Xiangmin Liao , Maxwell Cummings
发明人： Kelly Aubart , Jia-Ning Xiang , Siegfried Christensen , Xiangmin Liao , Maxwell Cummings
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/506 , A61K31/4015 , A61K31/4025
CPC分类号： C07D207/26 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06
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。

5. 发明申请

US20070203136A1 TRIAZOLOPYRIDAZINES AS KINASE MODULATORS 有权
标题翻译：三唑吡啶作为激酶调节剂
公开(公告)号：US20070203136A1
公开(公告)日：2007-08-30
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
发明人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
IPC分类号： A61K31/503 , A61K31/5377 , C07D487/04
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，以及这些化合物用于降低或抑制激酶活性的用途 c-Met在细胞或受试者中的调节，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疾病和/或与c-Met有关的障碍的用途。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。

6. 发明申请

US20060148792A1 Substituted 1,4-benzodiazepines and uses thereof 审中-公开
标题翻译：取代的1,4-苯并二氮杂及其用途
公开(公告)号：US20060148792A1
公开(公告)日：2006-07-06
申请号：US11371964
申请日：2006-03-09
申请人： Tianbao Lu , Louis LaFrance , Daniel Parks , Karen Milkiewicz , Raul Calvo , Maxwell Cummings , Alexander Kim , Bruce Grasberger , Theodore Carver
发明人： Tianbao Lu , Louis LaFrance , Daniel Parks , Karen Milkiewicz , Raul Calvo , Maxwell Cummings , Alexander Kim , Bruce Grasberger , Theodore Carver
IPC分类号： A61K31/551 , C07D243/12 , C07D243/18
CPC分类号： C07D401/04 , C07D243/14 , C07D403/10 , C07D405/04 , C07D409/04
摘要： The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M arm defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl: aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0-8, m is 0-8, i is 1-8 and j is 0-8.
摘要翻译：本发明涉及新的1,4-苯二氮卓类药物，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d，R d和M臂; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 9是环烷基：芳基，杂芳基，饱和或部分不饱和的杂环，环烷基（烷基），芳烷基或杂芳基烷基，其各自任选被取代; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

7. 发明申请

US20070155792A1 Peptide Deformylase Inhibitors 有权
标题翻译：肽脱甲酰酶抑制剂
公开(公告)号：US20070155792A1
公开(公告)日：2007-07-05
申请号：US11683089
申请日：2007-03-07
申请人： Kelly Aubart , Jia-Ning Xiang , Siegfried Christensen , Xiangmin Liao , Maxwell Cummings
发明人： Kelly Aubart , Jia-Ning Xiang , Siegfried Christensen , Xiangmin Liao , Maxwell Cummings
IPC分类号： A61K31/4439 , A61K31/454 , A61K31/42 , A61K31/4015 , A61K31/4025 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号： C07D207/26 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06
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。

8. 发明申请

US20060229341A1 Peptide deformylase inhibitors 失效
公开(公告)号：US20060229341A1
公开(公告)日：2006-10-12
申请号：US10553142
申请日：2003-04-16
申请人： Siegfried Christensen , Maxwell Cummings , Jinhwa Lee , Jia-ning Xiang
发明人： Siegfried Christensen , Maxwell Cummings , Jinhwa Lee , Jia-ning Xiang
IPC分类号： A61K31/44 , A61K31/19 , C07C311/45
CPC分类号： C07C311/51 , C07D213/70
摘要： Novel PDF inhibitors and novel methods for their use are provided.

9. 发明申请

US20050234081A1 Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions 失效
标题翻译：新型噻吩脒，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：US20050234081A1
公开(公告)日：2005-10-20
申请号：US10515554
申请日：2003-05-28
申请人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Hufnagel , Jeremy Travins , Shelley Ballentine , Kenneth Wilson , Maxwell Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen
发明人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Hufnagel , Jeremy Travins , Shelley Ballentine , Kenneth Wilson , Maxwell Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen
IPC分类号： C07D333/22 , A61K31/381 , A61K31/404 , A61K31/41 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4535 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/662 , A61P1/04 , A61P3/10 , A61P5/14 , A61P5/48 , A61P7/00 , A61P7/06 , A61P7/08 , A61P7/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P37/00 , A61P37/06 , A61P37/08 , A61P41/00 , A61P43/00 , C07D333/12 , C07D333/38 , C07D333/54 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D495/04 , C07F7/08 , C07F7/10 , C07F9/6553 , C07D49/02
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。

10. 发明申请

US20070066667A1 Novel thiophene sulfoximines, compositions thereof, and methods treating complement-mediated diseases and conditions 有权
标题翻译：新型噻吩亚磺酰亚胺，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：US20070066667A1
公开(公告)日：2007-03-22
申请号：US11375503
申请日：2006-03-14
申请人： Nalin Subasinghe , Shelley Ballentine , Jeremy Travins , Ehab Khalil , Farah Ali , Kristi Leonard , Joan Gushue , Michael Winters , Heather Hufnagel , Maxwell Cummings
发明人： Nalin Subasinghe , Shelley Ballentine , Jeremy Travins , Ehab Khalil , Farah Ali , Kristi Leonard , Joan Gushue , Michael Winters , Heather Hufnagel , Maxwell Cummings
IPC分类号： A61K31/422 , A61K31/381 , C07D413/02 , C07D333/16
CPC分类号： C07D413/12 , C07D333/38 , C07D409/12 , C07D417/12
摘要： Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are defined in the specification, as are A Z, Q, R1 and R2.
摘要翻译：公开了用于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化合物。所述化合物具有式I或其溶剂化物，水合物，药学上可接受的盐或前药; 其中R a，R b和R c在本说明书中定义，AZ，Q，R 1， SUP>和R 2 2。

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