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11. 发明授权

US4910208A Method of inhibiting leukotriene biosynthesis by oral administration of p-aminophenols or derivatives thereof 失效
标题翻译：通过口服给予对氨基苯酚或其衍生物抑制白三烯生物合成的方法
公开(公告)号：US4910208A
公开(公告)日：1990-03-20
申请号：US157759
申请日：1988-02-19
申请人： Raj N. Misra
发明人： Raj N. Misra
IPC分类号： A61K31/135 , A61K31/165 , A61K31/195 , A61K31/22 , A61K31/24 , A61K31/47 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C213/00 , C07C215/74 , C07C217/82 , C07C219/34 , C07C227/00 , C07C229/38 , C07C229/64 , C07C229/68 , C07C231/00 , C07C237/06 , C07C237/44 , C07C313/00 , C07C323/36 , C07D215/12 , C07D215/38
CPC分类号： C07D215/12 , C07D215/38 , Y10S514/826 , Y10S514/863
摘要： A method is provided for inhibiting leukotriene biosynthesis and thus treating asthma, psoriasis or inflammation by oral administration of p-aminophenols having the structure ##STR1## wherein m is 0 to 5; X is CH or N; R.sup.1 and R.sup.2 may be the same or different and are H, lower alkyl, aryl, hydroxy, hydroxyalkyleneoxy, alkylthio, alkoxy, alkanoyloxy, aryloxy, halo, carboxy, alkoxycarbonyl or amido; R.sup.3 is H, lower alkyl, alkanoyl or aroyl; and R.sup.4 is H, lower alkyl, benzoyl or alkanoyl, and including acid-addition salts thereof, with the proviso that when R.sup.4 is benzoyl, R.sup.2 is other than H.
摘要翻译：提供了抑制白细胞三烯生物合成并因此通过口服给予具有结构“IMAGE”的对氨基苯酚治疗哮喘，牛皮癣或炎症的方法，其中m为0至5; X是CH或N; R 1和R 2可以相同或不同，为H，低级烷基，芳基，羟基，羟基亚烷基氧基，烷硫基，烷氧基，烷酰氧基，芳氧基，卤素，羧基，烷氧基羰基或酰胺基。 R3是H，低级烷基，烷酰基或芳酰基; 并且R4是H，低级烷基，苯甲酰基或烷酰基，并且包括其酸加成盐，条件是当R 4是苯甲酰基时，R 2不是H.

12. 发明授权

US4814454A Quinoline compounds and compositions thereof 失效
标题翻译：喹啉化合物及其组合物
公开(公告)号：US4814454A
公开(公告)日：1989-03-21
申请号：US64716
申请日：1987-06-22
申请人： Raj N. Misra
发明人： Raj N. Misra
IPC分类号： A61K31/135 , A61K31/165 , A61K31/195 , A61K31/22 , A61K31/24 , A61K31/47 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C213/00 , C07C215/74 , C07C217/82 , C07C219/34 , C07C227/00 , C07C229/38 , C07C229/64 , C07C229/68 , C07C231/00 , C07C237/06 , C07C237/44 , C07C313/00 , C07C323/36 , C07D215/12 , C07D215/38
CPC分类号： C07D215/12 , C07D215/38 , Y10S514/826 , Y10S514/863
摘要： p-Aminophenols are provided having the structure ##STR1## wherein m is 0 to 5; X is CH or N; R.sup.1 and R.sup.2 may be the same or different and are H, lower alkyl, aryl, hydroxy, hydroxyalkyleneoxy, alkylthio, alkoxy, alkanoyloxy, aryloxy, halo, carboxy, alkoxycarbonyl or amido; R.sup.3 is H, lower alkyl, alkanoyl or aroyl; and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof, with the proviso that when X is CH, m is 0 and R.sup.1 is H, and when R.sup.4 is H, R.sup.2 is other than alkoxy, H or hydroxy, and when R.sup.4 is benzoyl, R.sup.2 is other than H.These compounds together with the compounds defined in the above proviso are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.
摘要翻译：提供具有结构的对氨基苯酚，其中m为0至5; X是CH或N; R 1和R 2可以相同或不同，为H，低级烷基，芳基，羟基，羟基亚烷基氧基，烷硫基，烷氧基，烷酰氧基，芳氧基，卤素，羧基，烷氧基羰基或酰胺基。 R3是H，低级烷基，烷酰基或芳酰基; 并且R4为H，低级烷基或烷酰基，并且包括其酸加成盐，条件是当X为CH时，m为0且R 1为H，当R 4为H时，R 2为烷氧基，H或羟基，当R 4为苯甲酰基时，R 2不是H.这些化合物与上述条件中定义的化合物一起用作白三烯生产的抑制剂，因此可用作抗炎，抗炎和抗牛皮癣药。

13. 发明授权

US07417040B2 Fused tricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3 有权
标题翻译：稠合三环化合物作为17β-羟基类固醇脱氢酶3的抑制剂
公开(公告)号：US07417040B2
公开(公告)日：2008-08-26
申请号：US11066373
申请日：2005-02-25
申请人： Brian E. Fink , Ashvinikumar V. Gavai , Gregory D. Vite , Wen-Ching Han , Raj N. Misra , Hai-Yun Xiao , Derek J. Norris , John S. Tokarski
发明人： Brian E. Fink , Ashvinikumar V. Gavai , Gregory D. Vite , Wen-Ching Han , Raj N. Misra , Hai-Yun Xiao , Derek J. Norris , John S. Tokarski
IPC分类号： A61K31/33 , C07D225/04 , C07D267/22 , C07D281/18 , C07D291/00 , C07D337/16 , A01N43/00
CPC分类号： C07D225/02 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D491/04
摘要： Disclosed are fused tricyclic compounds of the following formula I, or an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof. The disclosed compounds are useful as inhibitors of 17β-hydroxysteriod dehydrogenase 3 (17βHSD3). Also disclosed are methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer and pharmaceutical compositions comprising such compounds.
摘要翻译：公开了下式I的稠合三环化合物或其对映体，非对映异构体，互变异构体或其药学上可接受的盐。所公开的化合物可用作17β-羟基二氢脱氢酶3（17βHSD3）的抑制剂。还公开了使用这些化合物治疗激素敏感性疾病如前列腺癌的方法和包含这些化合物的药物组合物。

14. 发明授权

US06414156B2 Process for preparing azacycloalkanoylaminothiazoles 有权
标题翻译：制备氮杂环烷酰氨基噻唑的方法
公开(公告)号：US06414156B2
公开(公告)日：2002-07-02
申请号：US09746060
申请日：2000-12-22
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
IPC分类号： C07D41714
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2，R 3， R4和R5各自独立地为氢，烷基，芳基或杂芳基; R6和R7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R8为氢，烷基，芳基，杂芳基，CONR9R10，COR11或COOR12; R9，R10，R11和R12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

15. 发明授权

US06407124B1 Carbon substituted aminothiazole inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶的碳取代的氨基噻唑抑制剂
公开(公告)号：US06407124B1
公开(公告)日：2002-06-18
申请号：US09329616
申请日：1999-06-10
申请人： David B. Rawlins , S. David Kimball , Kyoung S. Kim , Raj N. Misra , Kevin R. Webster
发明人： David B. Rawlins , S. David Kimball , Kyoung S. Kim , Raj N. Misra , Kevin R. Webster
IPC分类号： A61K314439
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/46 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof are provided.
摘要翻译：提供式及其药用盐的化合物

16. 发明授权

US5550248A Substituted stryl heterocyclic amido prostaglandin analogs 失效
标题翻译：取代的苯乙烯基杂环酰胺前列腺素类似物
公开(公告)号：US5550248A
公开(公告)日：1996-08-27
申请号：US619569
申请日：1990-11-29
申请人： Raj N. Misra
发明人： Raj N. Misra
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: C.sub.m H.sub.p is an alkylene chain wherein m is 0, 1, 2, or 3 and p=(2.times.m)-1, except that when m is 0, p is also 0;n is 0, 1, 2 or 3;R is CO.sub.2 R', CH.sub.2 OH, CONHSO.sub.2 R.sup.3, CONHR.sup.4, or --CH.sub.2 --5--tetrazolyl;R' is hydrogen, alkyl, or alkali metal;X is O or NH;Y is --O--, a single bond or vinylene, except that Y cannot be --O-- when n is 0;and the remaining symbols are as defined in the specification.
摘要翻译：可用于治疗具有结构式的血栓形成和血管痉挛型疾病的前列腺素类似物，其中：CmHp是亚烷基链，其中m为0,1,2或3且p =（2xm）-1，除了当m为0时， p也是0; n为0,1,2或3; R是CO 2 R'，CH 2 OH，CONHSO 2 R 3，CONHR 4或-CH 2 5-四唑基; R'是氢，烷基或碱金属; X是O或NH; Y是-O-，单键或亚乙烯基，但当n为0时，Y不能为-O-; 其余符号如说明书中所定义。

17. 发明授权

US4757078A Cyclic aryl hydroxamic acids, derivatives thereof and method of use as anti-allergy agents 失效
标题翻译：环状芳基异羟肟酸，其衍生物和用作抗过敏剂的方法
公开(公告)号：US4757078A
公开(公告)日：1988-07-12
申请号：US936064
申请日：1986-11-28
申请人： Raj N. Misra
发明人： Raj N. Misra
IPC分类号： C07D217/24 , A61K31/235 , C07D217/22
CPC分类号： C07D217/24
摘要： Cyclic aryl hydroxamic acids and derivatives thereof are provided having the structure ##STR1## wherein R is H or arylalkyl, and including acid-addition salts thereof. These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.
摘要翻译：提供环状芳基异羟肟酸及其衍生物，其具有其中R为H或芳烷基且包括其酸加成盐的结构。这些化合物可用作白三烯生产的抑制剂，因此可用作抗过敏，抗炎和抗牛皮癣药。

18. 发明授权

US06720347B2 Carbon substituted aminothiazole inhibitors of cyclin dependent kinases 失效
标题翻译：细胞周期蛋白依赖性激酶的碳取代的氨基噻唑抑制剂
公开(公告)号：US06720347B2
公开(公告)日：2004-04-13
申请号：US10112133
申请日：2002-03-29
申请人： David B. Rawlins , S. David Kimball , Kyoung S. Kim , Raj N. Misra , Kevin R. Webster
发明人： David B. Rawlins , S. David Kimball , Kyoung S. Kim , Raj N. Misra , Kevin R. Webster
IPC分类号： A61K31426
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/46 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof, wherein R1 and A are defined herein, are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease and cardiovascular disease.
摘要翻译：其中R 1和A在本文中定义的式及其药学上可接受的盐的化合物是蛋白激酶抑制剂，可用于治疗增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗阿尔茨海默病和心血管疾病。

19. 发明授权

US06639074B2 Process for preparing azacycloalkanoylaminothiazoles 有权
标题翻译：制备氮杂环烷酰氨基噻唑的方法
公开(公告)号：US06639074B2
公开(公告)日：2003-10-28
申请号：US10100129
申请日：2002-03-18
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
IPC分类号： C07D47100
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2 R 3，R 4和R 5各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R 8是氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 且R 12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

20. 发明授权

US06521759B2 Aminothiazole inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶的氨基噻唑抑制剂
公开(公告)号：US06521759B2
公开(公告)日：2003-02-18
申请号：US09839751
申请日：2001-04-20
申请人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
发明人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
IPC分类号： C07D41712
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D417/14
摘要： The present invention describes compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, m and n are as defined in the specification. The compounds of formula I are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia, and cardiovascular disease.
摘要翻译：本发明描述了式I的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，m和n如说明书中所定义。式I的化合物是蛋白激酶抑制剂，可用于治疗增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗阿尔茨海默病，化学疗法诱发的脱发和心血管疾病。

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