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1. 发明申请

US20160159771A1 THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE 有权
公开(公告)号：US20160159771A1
公开(公告)日：2016-06-09
申请号：US14903952
申请日：2014-07-10
申请人： Tao GUO , Jeremy M. TRAVINS , LI Zhang , AGIOS PHARMACEUTICALS, INC.
发明人： Jeremy M. Travins , Tao Guo , Li ZHANG
IPC分类号： C07D401/12 , A61K45/06 , C07D401/14 , A61K31/53
CPC分类号： C07D401/12 , A61K31/53 , A61K45/06 , C07D251/18 , C07D401/14 , A61K2300/00
摘要： Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.

2. 发明授权

US08030305B2 Triazolopyridazines as kinase modulators 有权
标题翻译：三唑并嘧啶作为激酶调节剂
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。

3. 发明授权

US07138530B2 Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions 失效
标题翻译：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。

4. 发明授权

US07482376B2 Conjugated complement cascade inhibitors 失效
标题翻译：共轭补体级联抑制剂
公开(公告)号：US07482376B2
公开(公告)日：2009-01-27
申请号：US10869430
申请日：2004-06-16
申请人： Nalin Subasinghe , Ehab Khalil , Farah Ali , Heather Rae Hufnagel , Shelley Ballentine , Jeremy M. Travins , Kristi A. Leonard , Roger F. Bone
发明人： Nalin Subasinghe , Ehab Khalil , Farah Ali , Heather Rae Hufnagel , Shelley Ballentine , Jeremy M. Travins , Kristi A. Leonard , Roger F. Bone
IPC分类号： A61K31/381 , C07D333/10
CPC分类号： A61K47/60
摘要： The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.
摘要翻译：本发明涉及缀合的补体级联抑制剂，以及使用缀合的补体级联抑制剂治疗患者的方法。

5. 发明授权

US08173654B2 Triazolopyridazine compounds 有权
标题翻译：三唑并哒嗪化合物
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。

6. 发明申请

US20080255108A1 NOVEL THIOPHENE SULFOXIMINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS 有权
标题翻译：新型噻吩磺酰胺，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：US20080255108A1
公开(公告)日：2008-10-16
申请号：US12061873
申请日：2008-04-03
申请人： Nalin L. Subasinghe , Shelley Ballentine , Jeremy M. Travins , Ehab M. Khalil , Farah Ali , Kristi A. Leonard , Joan M. Gushue , Michael Peter Winters , Heather Hufnagel , Maxwell David Cummings
发明人： Nalin L. Subasinghe , Shelley Ballentine , Jeremy M. Travins , Ehab M. Khalil , Farah Ali , Kristi A. Leonard , Joan M. Gushue , Michael Peter Winters , Heather Hufnagel , Maxwell David Cummings
IPC分类号： A61K31/538 , C07D333/02 , A61K31/381 , C07D263/30 , A61K31/421 , C07D213/02 , A61P11/00 , A61P19/00 , A61P25/00 , A61P37/00 , A61P9/00 , A61P3/00 , A61P31/00 , A61K31/44 , C07D277/20 , A61K31/426 , C07D265/36
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。

7. 发明授权

US07385066B2 Thiophene sulfoximines, compositions thereof, and methods of treating complement-mediated diseases and conditions 有权
标题翻译：噻吩磺亚胺，其组合物，以及治疗补体介导的疾病和病症的方法
公开(公告)号：US07385066B2
公开(公告)日：2008-06-10
申请号：US11375503
申请日：2006-03-14
申请人： Nalin L. Subasinghe , Shelley Ballentine , Jeremy M. Travins , Ehab M. Khalil , Farah Ali , Kristi A. Leonard , Joan M. Gushue , Michael Peter Winters , Heather Hufnagel , Maxwell David Cummings
发明人： Nalin L. Subasinghe , Shelley Ballentine , Jeremy M. Travins , Ehab M. Khalil , Farah Ali , Kristi A. Leonard , Joan M. Gushue , Michael Peter Winters , Heather Hufnagel , Maxwell David Cummings
IPC分类号： C07D333/34
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. The 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。化合物为式I化合物或其溶剂化物，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。

8. 发明授权

US6080838A Peptidomimetic of helix-turn-helix or gamma-turn 失效
标题翻译：螺旋转旋螺旋或γ-转弯的拟肽
公开(公告)号：US6080838A
公开(公告)日：2000-06-27
申请号：US978023
申请日：1997-11-25
申请人： Felicia A. Etzkorn , Jeremy M. Travins
发明人： Felicia A. Etzkorn , Jeremy M. Travins
IPC分类号： C07K5/097 , C07K14/47 , A61K38/00
CPC分类号： C07K14/4702 , C07K5/0821
摘要： A peptidomimetic of the turn in the helix-turn-helix (HTH) motif of DNA-binding proteins was designed and synthesized. Conformational constraint was achieved by an unusual linking of two amino acids with a side-chain carbon--carbon bond. A phenyl ring provides the potential for new hydrophobic contacts with the hydrophobic core of the HTH motif. In the mimic, the peptide backbone and the central residue were retained in native form within a 12-membered cyclic tripeptide. The target compound 1b was synthesized by two sequential Horner-Wittig couplings followed by enantioselective hydrogenation with Rh(MeDuPHOS) in 8 steps and 35% overall yield. The stereochemical outcome of the key hydrogenation was determined by aromatic ring oxidation with RuO.sub.2 /NalO.sub.4 to give two equivalents of Boc-Asp-OMe.
摘要翻译：设计并合成了DNA结合蛋白的螺旋 - 转旋螺旋（HTH）基序的转录的拟肽。通过两个氨基酸与侧链碳 - 碳键的异常连接实现构象约束。苯环提供与HTH基序的疏水核心的新的疏水接触的潜力。在模拟物中，肽骨架和中心残基以天然形式保留在12-元环状三肽内。目标化合物1b通过两个顺序的Horner-Wittig偶联合成，然后用Rh（MeDuPHOS）以8步的对映选择性氢化和35％的总收率合成。通过RuO2 / NalO4的芳环氧化测定关键氢化的立体化学结果，得到两当量的Boc-Asp-OMe。

9. 发明授权

US07109354B2 Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions 失效
标题翻译：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：US07109354B2
公开(公告)日：2006-09-19
申请号：US10445817
申请日：2003-05-28
申请人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Rae Hufnagel , Jeremy M. Travins , Shelley K. Ballentine , Kenneth T. Wilson , Maxwell D. Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen , M. Jonathan Rudolph , Hui Huang
发明人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Rae Hufnagel , Jeremy M. Travins , Shelley K. Ballentine , Kenneth T. Wilson , Maxwell D. Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen , M. Jonathan Rudolph , Hui Huang
IPC分类号： C07D333/02 , C07D333/32
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，其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. 发明授权

US07868023B2 Thiophene sulfoximines, compositions thereof, and methods of treating complement-mediated diseases and conditions 有权
标题翻译：噻吩磺亚胺，其组合物，以及治疗补体介导的疾病和病症的方法
公开(公告)号：US07868023B2
公开(公告)日：2011-01-11
申请号：US12061873
申请日：2008-04-03
申请人： Nalin L. Subasinghe , Shelley Ballentine , Jeremy M. Travins , Ehab M. Khalil , Farah Ali , Kristi A. Leonard , Joan M. Gushue , Michael Peter Winters , Heather Hufnagel , Maxwell David Cummings
发明人： Nalin L. Subasinghe , Shelley Ballentine , Jeremy M. Travins , Ehab M. Khalil , Farah Ali , Kristi A. Leonard , Joan M. Gushue , Michael Peter Winters , Heather Hufnagel , Maxwell David Cummings
IPC分类号： A61K31/381 , A61K31/44 , C07D409/12
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. The compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are as 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。化合物为式I化合物或其溶剂化物，水合物，药学上可接受的盐或前药; 其中Ra，Rb和Rc如说明书中所定义，A Z，Q，R 1和R 2也是如此。

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