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1. 发明申请

US20100093721A1 PHENYL AND HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯并异噻唑并[2,3-d]嘧啶并用作腺苷A2a受体拮抗剂
公开(公告)号：US20100093721A1
公开(公告)日：2010-04-15
申请号：US12479247
申请日：2009-06-05
申请人： J. Kent Barbay , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
发明人： J. Kent Barbay , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
IPC分类号： A61K31/5377 , C07D495/04 , A61K31/519 , A61P25/16
CPC分类号： C07D495/04
摘要： This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.
摘要翻译：本发明涉及一种新颖的噻吩并[2,3-d]嘧啶Z及其治疗和预防用途，其中X，R 1和R 2在本说明书中定义。治疗和/或预防的疾病包括帕金森病。

2. 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。

3. 发明申请

US20060235007A1 Substituted 1,4-diazepines and uses thereof 审中-公开
标题翻译：取代的1,4-二氮杂及其用途
公开(公告)号：US20060235007A1
公开(公告)日：2006-10-19
申请号：US11452861
申请日：2006-06-14
申请人： Tianbao Lu , Karen Milkiewicz , Pierre Raboisson , Maxwell Cummings , Raul Calvo , Daniel Parks , Louis LaFrance , Juan Marugan Sanchez , Joan Gushue , Kristi Leonard
发明人： Tianbao Lu , Karen Milkiewicz , Pierre Raboisson , Maxwell Cummings , Raul Calvo , Daniel Parks , Louis LaFrance , Juan Marugan Sanchez , Joan Gushue , Kristi Leonard
IPC分类号： A61K31/5513 , C07D403/02 , C07D413/02 , C07D243/18
CPC分类号： C07D243/14
摘要： The present invention is directed to novel 1,4-diazepines, 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: R1, R2, R9, R10, Ra, Rd and M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and R3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino; or R3—X— is hydrogen or an electron pair; R4 is oxygen or —NR9R10; R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译：本发明涉及新的1,4-二氮杂，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：R 1，R 2，R 9，R 10，R SUP， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4，或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5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 6和R 8独立地是氢，烷基，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; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

4. 发明申请

US20100093756A1 HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代噻吩并[2,3-d]吡啶并用作腺苷A2a受体拮抗剂
公开(公告)号：US20100093756A1
公开(公告)日：2010-04-15
申请号：US12499370
申请日：2009-07-08
申请人： J. Kent Berbay , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
发明人： J. Kent Berbay , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
IPC分类号： A61K31/497 , C07D495/02 , A61K31/519 , A61P25/00
CPC分类号： C07D495/04
摘要： This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.
摘要翻译：本发明涉及一种新颖的噻吩并[2,3-d]嘧啶Z及其治疗和预防用途，其中X，R 1和R 2在本说明书中定义。治疗和/或预防的疾病包括帕金森病。

5. 发明授权

US07662824B2 Acylhydrazones as kinase modulators 有权
标题翻译：酰腙作为激酶调节剂
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。

6. 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。

7. 发明申请

US20100093763A1 PHENYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯基取代的噻吩并[2,3-d]嘧啶并用作腺苷A2a受体拮抗剂
公开(公告)号：US20100093763A1
公开(公告)日：2010-04-15
申请号：US12499357
申请日：2009-07-08
申请人： J. Kent Barbay , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
发明人： J. Kent Barbay , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
IPC分类号： A61K31/519 , C07D491/04 , A61P25/28
CPC分类号： C07D495/04
摘要： This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.
摘要翻译：本发明涉及一种新颖的噻吩并[2,3-d]嘧啶Z及其治疗和预防用途，其中R1和R2在本说明书中定义。治疗和/或预防的疾病包括帕金森病。

8. 发明申请

US20100093722A1 HETEROARYL AND PHENYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代三苯并[2,3-d]嘧啶并用作腺苷A2a受体拮抗剂
公开(公告)号：US20100093722A1
公开(公告)日：2010-04-15
申请号：US12499342
申请日：2009-07-08
申请人： J. Kent BARBAY , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
发明人： J. Kent BARBAY , Devraj Chakravarty , Kristi Leonard , Brian Christopher Shook , Aihua Wang
IPC分类号： A61K31/519 , C07D495/04 , A61K31/5377 , A61P25/00
CPC分类号： C07D495/04
摘要： This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.
摘要翻译：本发明涉及一种新颖的噻吩并[2,3-d]嘧啶Z及其治疗和预防用途，其中R1和R2在本说明书中定义。治疗和/或预防的疾病包括帕金森病。

9. 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。

10. 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。

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