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1. 发明申请

US20070078146A1 Substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译：取代的吡唑作为p38激酶抑制剂
公开(公告)号：US20070078146A1
公开(公告)日：2007-04-05
申请号：US10840734
申请日：2004-05-05
申请人： Ashok Naraian , Michael Clare , Paul Collins , Joyce Crich , Rajesh Devraj , Daniel Flynn , Lifeng Geng , Matthew Graneto , Cathleen Hanau , Gunnar Hanson , Susan Hartmann , Michael Hepperle , He Huang , Ish Khanna , Francis Koszyk , Shuyuan Liao , Suzanne Metz , Win Naing , Richard Partis , Thao Perry , Shashidhar Rao , Shaun Selness , Michael South , Michael Stealey , John Talley , Michael Vazquez , John Walker , Richard Weier , Xiangdong Xu , Syaulan Yang , Yi Yu
发明人： Ashok Naraian , Michael Clare , Paul Collins , Joyce Crich , Rajesh Devraj , Daniel Flynn , Lifeng Geng , Matthew Graneto , Cathleen Hanau , Gunnar Hanson , Susan Hartmann , Michael Hepperle , He Huang , Ish Khanna , Francis Koszyk , Shuyuan Liao , Suzanne Metz , Win Naing , Richard Partis , Thao Perry , Shashidhar Rao , Shaun Selness , Michael South , Michael Stealey , John Talley , Michael Vazquez , John Walker , Richard Weier , Xiangdong Xu , Syaulan Yang , Yi Yu
IPC分类号： A61K31/506 , A61K31/4439 , C07D43/02
CPC分类号： C07D401/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D473/00 , C07D487/04 , C07D491/10 , C07D495/04
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase medicated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译：描述了一类吡唑衍生物用于治疗p38激酶药物障碍。特别感兴趣的化合物由式IA定义，其中R 1，R 2，R 3和R 4是如说明书中所述。

2. 发明申请

US20050256180A1 Substituted pyrazolyl compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基化合物
公开(公告)号：US20050256180A1
公开(公告)日：2005-11-17
申请号：US11113926
申请日：2005-04-25
申请人： Arija Bergmanis , Michael Clare , Joyce Crich , Lifeng Geng , Timothy Hagen , Gunnar Hanson , Stephen Houdek , He Huang , Donna Iula , Francis Koszyk , Shuyuan Liao , Scott Mohler , Maria Nguyen , Richard Partis , Michael Stealey , Michael Tollefson , Richard Weier , Xiangdong Xu , Dominique Bonafoux , Theresa Fletcher , Bruce Hamper , Patrick Lennon , Subo Liao , Suzanne Metz , David Oburn , Thomas Owen , Angela Scates , Michael Vazquez , Serge Wolfson
发明人： Arija Bergmanis , Michael Clare , Joyce Crich , Lifeng Geng , Timothy Hagen , Gunnar Hanson , Stephen Houdek , He Huang , Donna Iula , Francis Koszyk , Shuyuan Liao , Scott Mohler , Maria Nguyen , Richard Partis , Michael Stealey , Michael Tollefson , Richard Weier , Xiangdong Xu , Dominique Bonafoux , Theresa Fletcher , Bruce Hamper , Patrick Lennon , Subo Liao , Suzanne Metz , David Oburn , Thomas Owen , Angela Scates , Michael Vazquez , Serge Wolfson
IPC分类号： A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61P19/02 , A61P25/04 , A61P29/00 , A61P35/00 , C07D231/54 , C07D333/62 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/4162
CPC分类号： C07D403/12 , C07D231/54 , C07D333/62 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
摘要翻译：本发明涉及取代的吡唑基衍生物，包含这些的组合物，中间体，制备取代的吡唑基衍生物的方法，以及用于治疗癌症，炎症和炎症相关疾病如关节炎的方法。

3. 发明申请

US20050096368A1 Heterocyclo-substituted imidazoles for the treatment of inflammation 审中-公开
标题翻译：杂环取代的咪唑用于治疗炎症
公开(公告)号：US20050096368A1
公开(公告)日：2005-05-05
申请号：US10653399
申请日：2003-09-02
申请人： Ish Khanna , Richard Weier , Paul Collins , Yi Yu , Xiangdong Xu , Richard Partis , Francis Koszyk , Renee Huff
发明人： Ish Khanna , Richard Weier , Paul Collins , Yi Yu , Xiangdong Xu , Richard Partis , Francis Koszyk , Renee Huff
IPC分类号： A61K31/4178 , A61K31/4439 , A61K31/4709 , A61K31/5377 , C07D233/32 , C07D233/54 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/02 , C07D419/04
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy. aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类咪唑基化合物用于治疗炎症。特别感兴趣的化合物由式（V）定义，其中R 3是选自氢，烷基，卤代烷基，芳烷基，杂环烷基，杂芳烷基，酰基，氰基，烷氧基，烷硫基，烷硫基烷基，烷基磺酰基环烷基硫基，环烷硫基烷基，环烷基磺酰基，环烷基磺酰基烷基，卤代烷基磺酰基，芳基磺酰基，卤素，羟基烷基，烷氧基烷基，烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，氰基烷基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-烷基-N-芳基氨基烷基，羧基烷基，烷氧基羰基烷基，卤代烷基羰基，羧基，氨基羰基，烷基氨基羰基，烷基氨基羰基烷基，杂芳基烷氧基烷基，杂芳氧基烷基，杂芳硫基烷基，芳烷氧基，芳烷硫基，杂芳烷氧基，杂芳烷硫基，杂芳基烷硫基烷基，杂芳氧基，杂芳硫基，芳硫基烷基，芳氧基烷基，芳硫基，芳氧基。芳烷硫基烷基，芳烷氧基烷基，芳基和杂芳基; 其中R 4是选自氢，烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环，其中R 13和R 14是任选地在可取代的位置被一个或多个独立地选自烷基磺酰基，氨基磺酰基，卤素，烷硫基，烷基，氰基，羧基，烷氧基羰基，卤代烷基，羟基，烷氧基，羟基烷基，烷氧基烷基，卤代烷氧基，氨基，烷基氨基，芳基氨基和硝基的基团取代。只要R 13和R 14中的至少一个为被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐。

4. 发明申请

US20050256120A1 Heterocyclo-substituted imidazoles for the treatment of inflammation 失效
公开(公告)号：US20050256120A1
公开(公告)日：2005-11-17
申请号：US11183016
申请日：2005-07-15
申请人： Ish Khanna , Richard Weier , Paul Collins , Yi Yu , Xiangdong Xu , Richard Partis , Francis Koszyk , Renee Huff
发明人： Ish Khanna , Richard Weier , Paul Collins , Yi Yu , Xiangdong Xu , Richard Partis , Francis Koszyk , Renee Huff
IPC分类号： A61K31/4178 , A61K31/4439 , A61K31/4709 , A61K31/5377 , C07D233/32 , C07D233/54 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/02 , C07D419/04 , C07D43/02
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxy-carbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

6. 发明申请

US20080027237A1 Processes for preparations of 9,11-epoxy steroids and intermediates useful therein 审中-公开
标题翻译： 9,11-环氧类固醇及其中有用的中间体的制备方法
公开(公告)号：US20080027237A1
公开(公告)日：2008-01-31
申请号：US11389937
申请日：2006-03-27
申请人： John Ng , Chin Liu , Dennis Anderson , Jon Lawson , Joseph Wieczorek , Sastry Kunda , Leo Letendre , Mark Pozzo , Yuen-Lung Sing , Ping Wang , Edward Yonan , Richard Weier , Thomas Kowar , Julio Baez , Bernhard Erb
发明人： John Ng , Chin Liu , Dennis Anderson , Jon Lawson , Joseph Wieczorek , Sastry Kunda , Leo Letendre , Mark Pozzo , Yuen-Lung Sing , Ping Wang , Edward Yonan , Richard Weier , Thomas Kowar , Julio Baez , Bernhard Erb
IPC分类号： C07J75/00
CPC分类号： C07J71/00 , C07D301/12 , C07J1/0059 , C07J21/00 , C07J21/003 , C07J31/006 , C07J41/0094 , C07J53/002 , C07J71/0005 , C07J71/0015 , C07J75/00 , C12P33/005 , C12P33/10
摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of 9,11-epoxy steroids.
摘要翻译：提供了多种新型反应方案，新工艺步骤和新型中间体，用于合成9,11-环氧类固醇。

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