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31. 发明授权

US4883811A 7-Oxabicycloheptane imino interphenylene substituted prostaglandin analogs useful in the treatment of thrombotic disease 失效
标题翻译： 7-氧杂双环庚烷亚氨基亚氨基取代的前列腺素类似物可用于治疗血栓性疾病
公开(公告)号：US4883811A
公开(公告)日：1989-11-28
申请号：US272373
申请日：1988-11-17
申请人： Raj N. Misra , Steven E. Hall
发明人： Raj N. Misra , Steven E. Hall
IPC分类号： A61K31/34 , A61P7/02 , A61P11/08 , A61P43/00 , C07D493/08 , C07D493/18
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane imino interphenylene substituted prostaglandin analogs are provided having the structural formula ##STR1## wherein n is 1 or 2; m is 1 or 2; R is H, lower alkyl, or alkali metal; and R.sup.1 is --OR.sup.2, ##STR2## where R.sup.2 is lower alkyl, aryl, aralkyl, cycloalkylalkyl, alkanoyl or aroyl; and R.sup.3 is lower alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, --NHaralkyl, --NHalkyl, --NHalkylcycloalkyl or --NHaryl.These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic disease.

32. 发明授权

US4883809A 7-Oxabicycloheptane imino interphenyleneoxy substituted prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease 失效
标题翻译：可用于治疗血栓和血管痉挛疾病的7-氧杂双环庚烷亚氨基亚氨基苯氧基取代的前列腺素类似物
公开(公告)号：US4883809A
公开(公告)日：1989-11-28
申请号：US272378
申请日：1988-11-17
申请人： Raj N. Misra
发明人： Raj N. Misra
IPC分类号： A61K31/34 , A61P7/02 , A61P11/08 , A61P43/00 , C07D493/08
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane imino interphenyleneoxy substituted prostaglandin analogs are provided having the structural formula ##STR1## wherein n is 1 or 2;R is H; lower alkyl, or alkali metal; andR.sup.1 is --OR.sup.2, ##STR2## where R.sup.2 is lower alkyl, aryl, aralkyl, alkanoyl or aroyl; andR.sup.3 is lower alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, --NHaralkyl, --NHalkyl or --NHaryl. The compounds are useful in the treatment of thrombotic disease.

33. 发明授权

US4599439A Arachidonic acid analogs 失效
公开(公告)号：US4599439A
公开(公告)日：1986-07-08
申请号：US638335
申请日：1984-08-06
申请人： Raj N. Misra
发明人： Raj N. Misra
IPC分类号： C07C33/05 , C07C45/58 , C07C47/21 , C07C57/26 , C07F7/08 , C07F7/18
CPC分类号： C07F7/1856 , C07C17/26 , C07C33/05 , C07C45/58 , C07C47/21 , C07C57/26 , C07F7/0818
摘要： Analogs of arachidonic acid are provided having the structure ##STR1## wherein R is CH.sub.2 OH or CO.sub.2 H and m is 1 or 2. These compounds are useful as inhibitors of leukotriene and prostaglandin biosynthesis and as such are useful an antiallergy and antiinflammatory agents.

34. 发明授权

US4555520A 2-Pyridylcarboxamides which inhibit arachidonic acid release 失效
标题翻译：抑制花生四烯酸释放的2-吡啶基羧酰胺
公开(公告)号：US4555520A
公开(公告)日：1985-11-26
申请号：US642006
申请日：1984-08-20
申请人： Raj N. Misra , Donald S. Karanewsky
发明人： Raj N. Misra , Donald S. Karanewsky
IPC分类号： C07D213/127 , A61K31/4402 , A61K31/4412 , A61K31/4418 , A61K31/455 , A61P29/00 , A61P43/00 , C07D213/16 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/84 , C07D213/89 , C07F9/54
CPC分类号： C07D213/16 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07F9/5442
摘要： 2-Pyridylcarboxamides are provided having the structure ##STR1## wherein n is 1 to 10; R is hydrogen, lower alkyl, alkali metal or an amine salt; andR.sup.1 is C.sub.6 -C.sub.20 alkyl, C.sub.6 -C.sub.20 alkenyl, C.sub.6 to C.sub.20 alkoxy or phenyl. These compounds are useful as inhibitors of arachidonic acid release and as such are useful as antiallergy agents.
摘要翻译：提供具有结构的2-吡啶基甲酰胺，其中n为1至10; R是氢，低级烷基，碱金属或胺盐; 且R 1为C 6 -C 20烷基，C 6 -C 20烯基，C 6至C 20烷氧基或苯基。这些化合物可用作花生四烯酸释放的抑制剂，因此可用作抗过敏剂。

35. 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。

36. 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。

37. 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

38. 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。

39. 发明授权

US5371091A Heteroaromatic amine thrombin inhibitors 失效
标题翻译：杂芳胺凝血酶抑制剂
公开(公告)号：US5371091A
公开(公告)日：1994-12-06
申请号：US76224
申请日：1993-06-14
申请人： Raj N. Misra , Steven E. Hall
发明人： Raj N. Misra , Steven E. Hall
IPC分类号： C07D213/38 , C07D213/74 , C07D237/20 , C07D239/42 , C07D241/20 , C07D401/12 , A61K31/445 , A61K31/415 , A61K31/42 , C07D215/14
CPC分类号： C07D213/74 , C07D213/38 , C07D237/20 , C07D239/42 , C07D241/20 , C07D401/12
摘要： Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R.sup.1 and R.sup.2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 4- to 8-membered ring; R.sup.3 is monocyclic heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.
摘要翻译：提供磺酰胺凝血酶抑制剂，其具有包括其所有立体异构体的结构，其中n为1,2或3; m为0,1或2; R 1和R 2独立地为H，低级烷基，环烷基，芳基，杂芳基或杂芳基 - 烷基，或者R 1和R 2可以与它们所连接的N原子一起形成4-至8-元环; R3是单环杂芳基; 和R4是烷基，环烷基，芳基，杂芳基，喹啉基或四氢喹啉基，及其药学上可接受的盐。

40. 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。

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