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1. 发明授权

US4663337A 7-oxabicycloheptane substituted amides useful in the treatment of thrombotic disease 失效
标题翻译：可用于治疗血栓性疾病的7-氧杂双环庚烷取代的酰胺
公开(公告)号：US4663337A
公开(公告)日：1987-05-05
申请号：US853813
申请日：1986-04-18
申请人： Jagabandhu Das , Masami Nakane
发明人： Jagabandhu Das , Masami Nakane
IPC分类号： C07D493/08 , A61K31/34 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted amides are provided having the structural formula ##STR1## wherein m is 0 to 4; A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; R.sup.1 is H, lower alkyl or aryl; q is 1 to 6; X is ##STR3## (wherein q is 1) or ##STR4## (wherein R.sup.3 is H or lower alkyl); R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aralkyloxy, cycloalkyl or cycloalkylalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
摘要翻译：提供7-氧杂二环庚烷取代的酰胺，其结构式为：其中m为0至4; A是-CH = CH-或-CH 2 -CH 2 - ; n为1至5; R是CO 2 H，CO 2烷基，CO 2碱金属，CO 2多羟基胺盐，其中R 4和R 5相同或不同，是H，低级烷基，羟基，低级烷氧基或芳基，R 4和R 5中的至少一个不同于羟基，低级烷氧基 R1是H，低级烷基或芳基; q为1〜6; X为（其中q为1）或（其中R 3为H或低级烷基）; R2是低级烷基，低级烯基，低级炔基，芳基，芳烷基，低级烷氧基，芳烷氧基，环烷基或环烷基烷基。这些化合物是可用于例如治疗血栓形成疾病的心血管药。

2. 发明申请

US20120214767A1 TRICYCLIC HETEROCYCLIC COMPOUNDS 有权
标题翻译：三元杂环化合物
公开(公告)号：US20120214767A1
公开(公告)日：2012-08-23
申请号：US13504541
申请日：2010-10-29
申请人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
发明人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
IPC分类号： A61K31/423 , C07D498/04 , A61K31/454 , C07D413/04 , A61P37/00 , A61K31/5377 , C07F9/09 , A61K31/675 , A61P35/00 , A61P7/00 , C07D413/14 , A61K31/506
CPC分类号： C07D413/04 , C07D231/54 , C07D261/20 , C07D277/84 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D487/10 , C07D498/04
摘要： Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其立体异构体或其盐，其中：X1，X2，X3，W，Q1，Q2和G2在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

3. 发明授权

US07683171B2 1H-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same 有权
标题翻译： 1H-咪唑并[4,5-d]噻吩并[3,2-b]吡啶基三环化合物和包含它们的药物组合物
公开(公告)号：US07683171B2
公开(公告)日：2010-03-23
申请号：US11346986
申请日：2006-02-03
申请人： William J. Pitts , Jagabandhu Das , Yuping Qiu , Steven H. Spergel
发明人： William J. Pitts , Jagabandhu Das , Yuping Qiu , Steven H. Spergel
IPC分类号： A61K31/4365 , C07D491/12
CPC分类号： C07D495/14
摘要： The present invention provides for thiazolopyridine-based tricyclic compounds having the formula (I), wherein R1, R2, R5, R6 and R7 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
摘要翻译：本发明提供具有式（I）的噻唑并吡啶类三环化合物，其中R 1，R 2，R 5，R 6和R 7如本文所述。本发明还提供包含这些化合物的药物组合物，以及这些化合物用于治疗炎症和免疫疾病的用途。

4. 发明申请

US20080275092A1 ARYL-SUBSTITUTED PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权
标题翻译： ARYL替代的吡唑酰胺化合物可用作激酶抑制剂
公开(公告)号：US20080275092A1
公开(公告)日：2008-11-06
申请号：US12118794
申请日：2008-05-12
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bank-Chi Chen , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bank-Chi Chen , Stephen T. Wrobleski
IPC分类号： A61K31/4439 , C07D231/38 , C07D401/04 , C07D413/12 , A61P29/00 , A61K31/4245 , A61K31/402
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl ring; R2 is alkyl or an amino group as defined herein; and Z is optionally-substituted oxadiazolyl or —C(═O)NR6, wherein R6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.
摘要翻译：本发明涉及具有下式的化合物及其药学上可接受的盐，前体药物，溶剂合物，异构体和/或其水合物，其中Q是任选取代的苯基，吡啶基，哒嗪基，嘧啶基或吡嗪基; R 2是如本文所定义的烷基或氨基; 和Z是任选取代的恶二唑基或-C（-O）NR 6，其中R 6是低级烷基或环丙基。该化合物在制备用于治疗p38激酶相关病症的药物组合物和/或治疗与患者中p38激酶活性相关的病症的方法中令人惊奇地有利。

5. 发明申请

US20080171741A1 HETEROCYCLIC AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权
标题翻译：杂环化合物作为激酶抑制剂有用
公开(公告)号：US20080171741A1
公开(公告)日：2008-07-17
申请号：US11923760
申请日：2007-10-25
申请人： Stephen T. Wrobleski , Jagabandhu Das , T.G. Murali Dhar , Alaric J. Dyckman , John Hynes , Katerina Leftheris , James Lin , Shuqun Lin
发明人： Stephen T. Wrobleski , Jagabandhu Das , T.G. Murali Dhar , Alaric J. Dyckman , John Hynes , Katerina Leftheris , James Lin , Shuqun Lin
IPC分类号： A61K31/5377 , C07D261/06 , C07D271/10 , C07D271/06 , C07D211/86 , C07D253/06 , C07D333/06 , C07D413/10 , A61P29/00 , C07D413/06 , A61K31/42 , A61K31/4245 , A61K31/4412 , A61K31/53 , A61K31/381
CPC分类号： C07D261/18 , C07C237/42 , C07C2601/02 , C07D207/456 , C07D209/08 , C07D209/42 , C07D211/62 , C07D213/81 , C07D213/82 , C07D231/56 , C07D233/90 , C07D235/06 , C07D249/06 , C07D271/06 , C07D271/10 , C07D275/03 , C07D295/192 , C07D307/68 , C07D333/38 , C07D409/04 , C07D487/04 , C07D513/04
摘要： A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式I化合物及其对映异构体，非对映异构体和药学上可接受的盐。还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

6. 发明授权

US07396935B2 Aryl-substituted pyrazole-amide compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的芳基取代的吡唑酰胺化合物
公开(公告)号：US07396935B2
公开(公告)日：2008-07-08
申请号：US10838129
申请日：2004-05-03
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bang-Chi Chen , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bang-Chi Chen , Stephen T. Wrobleski
IPC分类号： C07D401/00
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted pyridyl, ring; R2 is alkyl or an amino group as defined herein; and Z is optionally-substituted C(═O)NR6, wherein R6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.
摘要翻译：本发明涉及具有下式的化合物及其药学上可接受的盐，前体药物，溶剂合物，异构体和/或水合物，其中Q是任选取代的吡啶基环; R 2是如本文所定义的烷基或氨基; 和Z是任选取代的C（= O）NR 6，其中R 6是低级烷基或环丙基。该化合物在制备用于治疗p38激酶相关病症的药物组合物和/或治疗与患者中p38激酶活性相关的病症的方法中令人惊奇地有利。

7. 发明授权

US06962915B2 Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的吡唑并嘧啶苯胺化合物
公开(公告)号：US06962915B2
公开(公告)日：2005-11-08
申请号：US10440864
申请日：2003-05-19
申请人： Jagabandhu Das , Chunjian Liu , Robert V. Moquin , Katerina Leftheris
发明人： Jagabandhu Das , Chunjian Liu , Robert V. Moquin , Katerina Leftheris
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/551 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/16 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts or prodrugs thereof, are useful as kinase inhibitors, wherein Y is —C(═O)NR1—, —NR1C(═O)—, —NR1C(═O)NR1—, —NR1SO2—, —SO2NR1—, —C(═O)—, —OC(═O)—, or —CO2—; B is alkyl, substituted alkyl, alkenyl, substituted alkenyl, hydroxy, alkoxy, aryl, cycloalkyl, heteroaryl, and heterocyclo; or when Y is —C(═O)NR1—, B also may be selected from —C(═O)R8, —C(═O)NR8R9, and —CO2R8; R1 is hydrogen, C1-4alkyl, or substituted C1-4alkyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen, methyl, perfluoromethyl, hydroxy, methoxy, halogen, cyano, NH2, or NH(CH3); and R4, R5, R6, R7, R8, and R9 are as defined in the specification.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐或前药可用作激酶抑制剂，其中Y是-C（-O）NR 1 - ， - NR 1 - C（-O） - ， - NR 1 C（-O）NR 1 - ， - NR 1 SO 2 - ， - SO 2 - ， - C（ - ） - ， - OC（-O） - 或-CO 2 - ; B是烷基，取代的烷基，烯基，取代的烯基，羟基，烷氧基，芳基，环烷基，杂芳基和杂环; 或当Y为-C（-O）NR 1 - ）时，B也可以选自-C（-O）R 8，-C（-O）NR 8个R 9和-CO 2 R 8;以及-CO 2 R 8。 R 1是氢，C 1-4烷基或取代的C 1-4烷基; R 2是氢或C 1-4烷基; R 3是氢，甲基，全氟甲基，羟基，甲氧基，卤素，氰基，NH 2或NH（CH 3）。和R 4，R 5，R 6，R 7，R 8，和R 9是如说明书中所定义的。

8. 发明授权

US06953795B2 Thiazolyl inhibitors of Tec family tyrosine kinases 有权
标题翻译： Tec家族酪氨酸激酶的噻唑基抑制剂
公开(公告)号：US06953795B2
公开(公告)日：2005-10-11
申请号：US10642040
申请日：2003-08-15
申请人： Joel C. Barrish , Jagabandhu Das , Steven B. Kanner , Chunjian Liu , Steven H. Spergel , John Wityak , Arthur M. P. Doweyko , Joseph A. Furch III
发明人： Joel C. Barrish , Jagabandhu Das , Steven B. Kanner , Chunjian Liu , Steven H. Spergel , John Wityak , Arthur M. P. Doweyko , Joseph A. Furch III
IPC分类号： C07D277/20 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D277/32 , C07D277/46 , C07D277/54 , C07D417/12 , C07D417/14 , C07D491/10 , C07D491/107 , C07D419/10 , C07D419/12
CPC分类号： C07D417/12 , C07D277/46 , C07D277/54 , C07D417/14 , C07D491/10
摘要： Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.
摘要翻译：新的噻唑基化合物及其盐，含有这些化合物的药物组合物，以及使用这些化合物治疗Tec家族酪氨酸激酶相关疾病如癌症，免疫学障碍和过敏性疾病的方法。

9. 发明授权

US5741799A Heterocyclic thrombin inhibitors 失效
标题翻译：杂环凝血酶抑制剂
公开(公告)号：US5741799A
公开(公告)日：1998-04-21
申请号：US555561
申请日：1995-11-08
申请人： Spencer D. Kimball , Jagabandhu Das , Wan Fang Lau , Steven E. Hall , Wen-Ching Han
发明人： Spencer D. Kimball , Jagabandhu Das , Wan Fang Lau , Steven E. Hall , Wen-Ching Han
IPC分类号： A61K38/00 , C07D207/08 , C07D207/09 , C07D211/60 , C07D401/12 , C07D403/12 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/093 , A61K31/445 , A61K31/40 , C07D211/28
CPC分类号： C07D207/08 , C07D207/09 , C07D211/60 , C07D401/12 , C07D403/12 , C07K5/06026 , C07K5/06043 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/0806 , C07K5/081 , C07K5/0819 , A61K38/00
摘要： Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.
摘要翻译：其中n，R，R 1，R 2，R 3，G，G x，R 6'，R a，X a，R 6，R b，R b，R c， R3，p，Q，A和R4如本文所定义。

10. 发明授权

US5741792A Heterocyclic thrombin inhibitors 失效
公开(公告)号：US5741792A
公开(公告)日：1998-04-21
申请号：US555560
申请日：1995-11-08
申请人： Spencer D. Kimball , Jagabandhu Das , Wan Fang Lau , Steven E. Hall , Wen-Ching Han
发明人： Spencer D. Kimball , Jagabandhu Das , Wan Fang Lau , Steven E. Hall , Wen-Ching Han
IPC分类号： A61K38/00 , C07D207/08 , C07D207/09 , C07D211/60 , C07D401/12 , C07D403/12 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/093 , A61K31/535 , A61K31/495 , A61K31/54 , C07D413/12 , C07D417/12
CPC分类号： C07D207/08 , C07D207/09 , C07D211/60 , C07D401/12 , C07D403/12 , C07K5/06026 , C07K5/06043 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/0806 , C07K5/081 , C07K5/0819 , A61K38/00
摘要： Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6 ', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

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