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1. 发明申请

US20050004200A1 Pyrazole compounds as integrin receptor antagonists derivatives 审中-公开
标题翻译：吡唑类化合物作为整合素受体拮抗剂衍生物
公开(公告)号：US20050004200A1
公开(公告)日：2005-01-06
申请号：US10741860
申请日：2003-12-19
申请人： Thomas Penning , Albert Khilevich , Barbara Chen , Preete Gandhi , Yaping Wang , Victoria Downs , Mark Boys , Mark Russell , Dale Spangler , Renee Huff
发明人： Thomas Penning , Albert Khilevich , Barbara Chen , Preete Gandhi , Yaping Wang , Victoria Downs , Mark Boys , Mark Russell , Dale Spangler , Renee Huff
IPC分类号： A61K31/415 , A61K31/416 , C07D401/14 , C07D405/14 , C07D471/04 , C07
CPC分类号： C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αVβ3 and/or the αVβ5 integrin without significantly inhibiting the αVβ6 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物以及选择性抑制或拮抗αVbeta3和/或αVβ5整联蛋白而不显着抑制αVβ6的方法整合素

2. 发明申请

US20050043344A1 Heteroarylalkanoic acids as integrin receptor antagonists derivatives 审中-公开
标题翻译：杂芳基链烷酸作为整联蛋白受体拮抗剂衍生物
公开(公告)号：US20050043344A1
公开(公告)日：2005-02-24
申请号：US10743354
申请日：2003-12-22
申请人： Mark Boys , Lori Schretzman , Michael Tollefson , Nizal Chandrakumar , Ish Khanna , Maria Nguyen , Victoria Downs , Scott Mohler , Glen Gesicki , Thomas Penning , Barbara Chen , Yaping Wang , Albert Khilevich , Bipinchandra Desai , Yi Yu , John Wendt , Heather Stenmark , Hongwei Wu , Renee Huff , Srinivasan Nagarajan , Balekudru Devadas , Hwang-Fun Lu , Mark Russell , Dale Spangler , Mihir Parikh
发明人： Mark Boys , Lori Schretzman , Michael Tollefson , Nizal Chandrakumar , Ish Khanna , Maria Nguyen , Victoria Downs , Scott Mohler , Glen Gesicki , Thomas Penning , Barbara Chen , Yaping Wang , Albert Khilevich , Bipinchandra Desai , Yi Yu , John Wendt , Heather Stenmark , Hongwei Wu , Renee Huff , Srinivasan Nagarajan , Balekudru Devadas , Hwang-Fun Lu , Mark Russell , Dale Spangler , Mihir Parikh
IPC分类号： A61K31/4245 , A61K31/4745 , A61P19/02 , A61P19/10 , A61P27/00 , A61P35/00 , A61P35/04 , A61P43/00
CPC分类号： A61K31/4245 , A61K31/4745
摘要： The present invention relates to pharmaceutical compositions comprising compounds of the Formula I, or a pharmaceutically acceptable salt thereof, and methods of selectively inhibiting or antagonizing the αVβ3 and/or the αVβ5 integrin without significantly inhibiting the αVβ6 integrin.
摘要翻译：本发明涉及包含式I化合物或其药学上可接受的盐的药物组合物，以及选择性抑制或拮抗αVβ3和/或αVβ5整联蛋白而不显着抑制αVβ6整联蛋白的方法。

3. 发明授权

US06689754B1 Heterocyclic glycyl &bgr;-alanine derivatives 失效
标题翻译：杂环甘氨酰β-丙氨酸衍生物
公开(公告)号：US06689754B1
公开(公告)日：2004-02-10
申请号：US09289140
申请日：1999-04-08
申请人： Nizal Samuel Chandrakumar , Bipinchandra Nanubhai Desai , Balekudru Devadas , Alan Frank Gasiecki , Renee Huff , Ish K. Khanna , James W. Malecha , Julie M. Miyashiro , Shashidhar N. Rao , Joseph Gerace Rico , Thomas Edward Rogers , Peter Gerrard Ruminski , Mark Andrew Russell , Yi Yu
发明人： Nizal Samuel Chandrakumar , Bipinchandra Nanubhai Desai , Balekudru Devadas , Alan Frank Gasiecki , Renee Huff , Ish K. Khanna , James W. Malecha , Julie M. Miyashiro , Shashidhar N. Rao , Joseph Gerace Rico , Thomas Edward Rogers , Peter Gerrard Ruminski , Mark Andrew Russell , Yi Yu
IPC分类号： C07K506
CPC分类号： C07D213/82 , A61K38/00 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12 , C07D491/10 , C07K5/0202
摘要： The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and methods of treating conditions mediated by the &agr;v&bgr;3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，含有这些化合物的药物组合物以及治疗由alphavbeta3整联蛋白介导的病症的方法。

4. 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。

5. 发明授权

US07259266B2 Benzopyran compounds useful for treating inflammatory conditions 失效
标题翻译：可用于治疗炎性疾病的苯并吡喃化合物
公开(公告)号：US07259266B2
公开(公告)日：2007-08-21
申请号：US10801429
申请日：2004-03-16
申请人： Jeffry Carter , David Brown , Li Xing , Karl Aston , John Springer , Francis Koszyk , Steven Kramer , Renee Huff , Yi Yu , Bruce Hamper , Subo Laio , Angela Deprow , Teresa Fletcher , E. Ann Hallinan , James Kiefer , David Limburg , Lijuan Wang , Cindy Ludwig , John McCall , John Talley
发明人： Jeffry Carter , David Brown , Li Xing , Karl Aston , John Springer , Francis Koszyk , Steven Kramer , Renee Huff , Yi Yu , Bruce Hamper , Subo Laio , Angela Deprow , Teresa Fletcher , E. Ann Hallinan , James Kiefer , David Limburg , Lijuan Wang , Cindy Ludwig , John McCall , John Talley
IPC分类号： C07D311/04
CPC分类号： C07D311/58 , C07D311/64 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D417/04 , C07D417/06 , C07D493/04
摘要： The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
摘要翻译：本发明涉及可用于治疗与环氧合酶-2介导的病症有关的病症的方法和化合物。特别感兴趣的化合物是苯并吡喃及其由式1定义的类似物，其中Z，X，R 1，R 2，R 3和R 3， ^{4如说明书中所述。}

6. 发明申请

US20050148627A1 Benzopyran compounds for use in the treatment and prevention of inflammation related conditions 审中-公开
标题翻译：苯并吡喃化合物用于治疗和预防炎症相关病症
公开(公告)号：US20050148627A1
公开(公告)日：2005-07-07
申请号：US10801446
申请日：2004-03-16
申请人： Jeffery Carter , David Brown , Li Xing , Karl Aston , John Springer , Francis Koszyk , Steven Kramer , Sofya Tsymbalov , Renee Huff , Yi Yu , Bruce Hamper , Subo Laio , Angela Deprow , Theresa Fletcher , E. Hallinan , James Kiefer , David Limburg , Lijuan Wang
发明人： Jeffery Carter , David Brown , Li Xing , Karl Aston , John Springer , Francis Koszyk , Steven Kramer , Sofya Tsymbalov , Renee Huff , Yi Yu , Bruce Hamper , Subo Laio , Angela Deprow , Theresa Fletcher , E. Hallinan , James Kiefer , David Limburg , Lijuan Wang
IPC分类号： A61K31/353 , A61K31/382 , A61K31/47 , A61P29/00 , C07D215/54 , C07D311/58 , C07D311/64 , C07D311/94 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/06 , C07D493/04
CPC分类号： C07D405/04 , C07D215/54 , C07D311/58 , C07D311/64 , C07D311/94 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/06 , C07D493/04
摘要： The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
摘要翻译：本发明涉及可用于治疗与环氧合酶-2介导的病症有关的病症的方法和化合物。特别感兴趣的化合物是苯并吡喃及其由式1定义的类似物，其中Z，X，R 1，R 2，R 3和R 3， ^{4如说明书中所述。}

7. 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.

8. 发明申请

US20050148777A1 Benzopyran compounds useful for treating inflammatory conditions 失效
标题翻译：可用于治疗炎性疾病的苯并吡喃化合物
公开(公告)号：US20050148777A1
公开(公告)日：2005-07-07
申请号：US10801429
申请日：2004-03-16
申请人： Jeffery Carter , David Brown , Li Xing , Karl Aston , John Springer , Francis Koszyk , Steven Kramer , Renee Huff , Yi Yu , Bruce Hamper , Subo Laio , Angela Deprow , Theresa Fletcher , E. Hallinan , James Kiefer , David Limburg , Lijuan Wang , Cindy Ludwig , John McCall , John Talley
发明人： Jeffery Carter , David Brown , Li Xing , Karl Aston , John Springer , Francis Koszyk , Steven Kramer , Renee Huff , Yi Yu , Bruce Hamper , Subo Laio , Angela Deprow , Theresa Fletcher , E. Hallinan , James Kiefer , David Limburg , Lijuan Wang , Cindy Ludwig , John McCall , John Talley
IPC分类号： A61K31/352 , A61K31/382 , A61K31/395 , A61K31/47 , A61K31/4709 , A61P29/00 , C07D20060101 , C07D215/38 , C07D215/54 , C07D311/58 , C07D311/64 , C07D311/92 , C07D335/06 , C07D401/02 , C07D405/02 , C07D407/02 , C07D409/02 , C07D493/04
CPC分类号： C07D311/58 , C07D311/64 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D417/04 , C07D417/06 , C07D493/04
摘要： The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R 2, R3, and R4 are as described in the specification.
摘要翻译：本发明涉及可用于治疗与环氧合酶-2介导的病症有关的病症的方法和化合物。特别感兴趣的化合物是苯并吡喃及其由式1定义的类似物，其中Z，X，R 1，R 2，R 3和R 4 >如说明书中所述。

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