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21. 发明申请

US20050288303A1 Cyclic protein tyrosine kinase inhibitors 有权
标题翻译：循环蛋白酪氨酸激酶抑制剂
公开(公告)号：US20050288303A1
公开(公告)日：2005-12-29
申请号：US11138942
申请日：2005-05-26
申请人： Joel Barrish , John Wityak , Jagabandhu Das , Ping Chen , Derek Norris , Gary Schieven
发明人： Joel Barrish , John Wityak , Jagabandhu Das , Ping Chen , Derek Norris , Gary Schieven
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/438 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P1/00 , A61P5/14 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C237/40 , C07D213/81 , C07D213/82 , C07D231/38 , C07D233/90 , C07D239/42 , C07D263/48 , C07D277/30 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/56 , C07D277/62 , C07D409/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/20
CPC分类号： C07D277/56 , C07C233/65 , C07C237/40 , C07D213/81 , C07D213/82 , C07D231/38 , C07D233/90 , C07D239/42 , C07D263/48 , C07D409/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/113
摘要： Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
摘要翻译：新的环状化合物及其盐，含有这些化合物的药物组合物，以及使用这些化合物治疗蛋白质酪氨酸激酶相关疾病如免疫学和肿瘤学疾病的方法。

22. 发明申请

US20050004176A1 Pyrazole-amide compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的吡唑酰胺化合物
公开(公告)号：US20050004176A1
公开(公告)日：2005-01-06
申请号：US10837778
申请日：2004-05-03
申请人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
发明人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
IPC分类号： A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D231/18 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14 , C07
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中G，X，R 1，R 2，R 3，R 4，R 5，R 6和m如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

23. 发明授权

US06706717B2 Thiazolyl inhibitors of Tec family tyrosine kinases 有权
公开(公告)号：US06706717B2
公开(公告)日：2004-03-16
申请号：US10027982
申请日：2001-12-20
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： A61K31496
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.

24. 发明授权

US5691356A Disubstituted heterocyclic thrombin inhibitors 失效
标题翻译：二取代杂环凝血酶抑制剂
公开(公告)号：US5691356A
公开(公告)日：1997-11-25
申请号：US708292
申请日：1996-09-04
申请人： Jagabandhu Das , Spencer D. Kimball , Wan Fang Lau
发明人： Jagabandhu Das , Spencer D. Kimball , Wan Fang Lau
IPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/445 , A61K31/40 , A61K31/495 , A61K31/535 , A61K31/54 , C07D207/09 , C07D211/28
CPC分类号： C07D401/14 , C07D207/16 , C07D211/60 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.
摘要翻译：提供具有以下结构的二取代杂环凝血酶抑制剂：其中G为0,1或2或3; m为0,1,2或3; Y是NH或S; p为0,1或2，Q为单键或，Z，A，R，R 1，R 2，R 3，R 4和R 6如本文所定义。

25. 发明授权

US5260449A Method for preparing 7-oxabicycloheptyl substituted bromooxazole amide prostaglandin analog intermediates useful in the preparation of anti-thrombotic and anti-vasospastic compounds 失效
标题翻译：制备7-氧杂二环庚基取代的溴恶唑酰胺前列腺素类似物中间体的方法，用于制备抗血栓形成和抗血管痉挛性化合物
公开(公告)号：US5260449A
公开(公告)日：1993-11-09
申请号：US928394
申请日：1992-08-12
申请人： Janak Singh , Richard H. Mueller , Jagabandhu Das , Philip M. Sher
发明人： Janak Singh , Richard H. Mueller , Jagabandhu Das , Philip M. Sher
IPC分类号： C07D493/08 , C07D413/04
CPC分类号： C07D493/08
摘要： A method is provided for preparing bromooxazole intermediates of the structure ##STR1## wherein a vinyl compound of the structure ##STR2## wherein X.sup.1 and X.sup.2 are independently H and Br, is treated with a metal halide such as cupric bromide, and a base such as 1,8-diazabicyclo-[5.4.0]undec-7-ene (DBU). The resulting bromooxazole may be hydrolyzed and hydrogenolyzed to the final anti-thrombotic-anti-vasospastic compounds.
摘要翻译：提供了一种制备结构“IMAGE”的溴恶唑中间体的方法，其中X1和X2独立地为H和Br的结构的乙烯基化合物用金属卤化物如溴化铜处理，碱例如 1,8-二氮杂双环 - [5.4.0]十一碳-7-烯（DBU）。所得到的溴代恶唑可以水解并氢解成最终的抗血栓形成 - 抗血管痉挛型化合物。

26. 发明授权

US4767756A 3-substituted benzazepines 失效
标题翻译： 3-取代苯并吖庚因
公开(公告)号：US4767756A
公开(公告)日：1988-08-30
申请号：US74734
申请日：1987-07-17
申请人： Jagabandhu Das , David M. Floyd
发明人： Jagabandhu Das , David M. Floyd
IPC分类号： A61K31/55 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P43/00 , C07D223/16 , C07D409/12 , C07D417/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14
CPC分类号： C07D223/16
摘要： Benzazepine derivatives useful, for example, as cardiovascular agents, are disclosed. These compounds have the general formula ##STR1## and pharmaceutically acceptable salts thereof.
摘要翻译：公开了用作例如作为心血管药物的苯并氮杂衍生物。这些化合物具有通式“IMAGE”及其药学上可接受的盐。

27. 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。

28. 发明授权

US4638011A Tetrahydrothienyl substituted prostaglandin analogs 失效
标题翻译：四氢噻吩基取代的前列腺素类似物
公开(公告)号：US4638011A
公开(公告)日：1987-01-20
申请号：US682713
申请日：1984-12-17
申请人： Jagabandhu Das
发明人： Jagabandhu Das
IPC分类号： A61K31/38 , A61K31/381 , A61K31/557 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/08 , C07D333/24
CPC分类号： C07D333/24
摘要： Tetrahydrothienyl substituted prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译：提供四氢噻吩基取代的前列腺素类似物，其结构式为“IMAGE”，并且包括其所有立体异构体。该化合物是可用于例如治疗溶栓性疾病的心血管药。

29. 发明授权

US4609671A 5,6-epoxy-7-oxabicycloheptane substituted amino prostaglandin analogs useful in the treatment of thrombotic disease 失效
标题翻译：可用于治疗血栓性疾病的5,6-环氧-7-氧杂双环庚烷取代的氨基前列腺素类似物
公开(公告)号：US4609671A
公开(公告)日：1986-09-02
申请号：US749232
申请日：1985-06-27
申请人： Jagabandhu Das
发明人： Jagabandhu Das
IPC分类号： A61K31/557 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/08 , A61P29/00 , A61P43/00 , C07D493/08 , C07D493/18 , A61K31/335 , C07D307/00
CPC分类号： C07D493/08
摘要： 5-6-Epoxy-7-oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## wherein A is CH.dbd.CH or (CH.sub.2).sub.2, m is 1 to 8, n is 0 to 5, R is H, lower alkyl, alkali metal or hydroxylamine salt, and R.sup.1 is lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, lower alkenyl, lower alkoxy, aralkoxy or ##STR2## including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
摘要翻译： 5-6-环氧-7-氧杂双环庚烷取代的氨基前列腺素类似物具有结构式为：其中A为CH = CH或（CH 2）2，m为1至8，n为0至5，R为H，低级烷基，碱金属或羟胺盐，R 1为低级烷基，芳基，芳烷基，环烷基，环烷基烷基，低级烯基，低级烷氧基，芳烷氧基或包括其所有立体异构体。这些化合物是可用于例如治疗血栓形成疾病的心血管药。

30. 发明授权

US4550120A 7-Oxabicycloheptane substituted ethers and their use in treating thrombolytic disease 失效
标题翻译： 7-氧杂双环庚烷取代醚及其在治疗溶栓性疾病中的应用
公开(公告)号：US4550120A
公开(公告)日：1985-10-29
申请号：US605535
申请日：1984-04-30
申请人： Jagabandhu Das , Steven E. Hall
发明人： Jagabandhu Das , Steven E. Hall
IPC分类号： A61K31/35 , A61K31/557 , A61P7/02 , A61P9/08 , A61P9/10 , A61P43/00 , C07D493/08 , A61K31/34 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein A is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译：提供7-氧杂双环庚烷取代的醚前列腺素类似物，其结构式为：其中A为O或IMA，并包括其所有立体异构体。该化合物是可用于例如治疗溶栓性疾病的心血管药。

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