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1. 发明公开

EP1313705A1 GEM-SUBSTITUTED ALPHA V BETA 3 INTEGRIN ANTAGONISTS 审中-公开
标题翻译：偕取代的α-V BETA 3整联蛋白拮抗剂
公开(公告)号：EP1313705A1
公开(公告)日：2003-05-28
申请号：EP01968257.4
申请日：2001-08-29
申请人： Pharmacia Corporation , Khanna, Ish Kumar , Yu, Yi , Fun-Lu, Hwang , Chandrakumar, Nizal S. , Huff, Renee M. , Russell, Mark A. , Boys, Mark L. , Schretzman, Lori A. , Chen, Barbara B. , Desai, Bipinchandra N. , Nagarajan, Srinivasan Raj , Gasiecki, Alan F. , Penning, Thomas D. , Rogers, Thomas , Wendt, John Adam , Khilevich, Albert , Wang, Yaping
发明人： KHANNA, Ish, Kumar , YU, Yi , FUN-LU, Hwang , CHANDRAKUMAR, Nizal, S. , HUFF, Renee, M. , RUSSELL, Mark, A. , BOYS, Mark, L. , SCHRETZMAN, Lori, A. , CHEN, Barbara, B. , DESAI, Bipinchandra, N. , NAGARAJAN, Srinivasan, Raj , GASIECKI, Alan, F. , PENNING, Thomas, D. , ROGERS, Thomas , WENDT, John, Adam , KHILEVICH, Albert , WANG, Yaping , DEVADAS, Balekudra
IPC分类号： C07D213/74 , C07D401/12 , C07D213/73 , C07D471/04 , A61K31/4427 , A61K31/553 , A61P35/00 , A61P31/00
CPC分类号： C07D213/73 , C07D213/74 , C07D401/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively inhibiting or antagonizing the αvβ3 and/or the αvβ5 integrin.

2. 发明专利

AU8851501A Gem-substituted alpha v beta 3 integrin antagonists 未知
公开(公告)号：AU8851501A
公开(公告)日：2002-03-13
申请号：AU8851501
申请日：2001-08-29
申请人： PHARMACIA CORP , KHILEVICH ALBERT , WANG YAPING , KHANNA ISH KUMAR , YU YI , LU HWANG FUN , CHANDRAKUMAR NIZAL S , HUFF RENEE M , RUSSELL MARK A , BOYS MARK L , SCHRETZMAN LORI A , CHEN BARBARA B , DESAI BIPINCHANDRA N , NAGARAJAN SRINIVASAN RAJ , GASIECKI ALAN F , PENNING THOMAS D , ROGERS THOMAS , WENDT JOHN ADAM
发明人： KHANNA ISH KUMAR , YU YI , LU HWANG FUN , CHANDRAKUMAR NIZAL S , HUFF RENEE M , RUSSELL MARK A , BOYS MARK L , SCHRETZMAN LORI A , CHEN BARBARA B , DESAI BIPINCHANDRA N , NAGARAJAN SRINIVASAN RAJ , GASIECKI ALAN F , PENNING THOMAS D , ROGERS THOMAS , WENDT JOHN ADAM , KHILEVICH ALBERT , WANG YAPING
IPC分类号： A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/444 , A61K31/4545 , A61K45/00 , A61P1/02 , A61P3/10 , A61P3/14 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D213/73 , C07D213/74 , C07D401/12 , C07D471/04 , A61K31/4427 , A61K31/553
摘要： The present invention relates to a class of compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively inhibiting or antagonizing the alpha v beta 3 and/or the alpha v beta 5 integrin.

3. 发明申请

WO2004058761A1 PYRAZOLE COMPOUNDS AS INTEGRIN RECEPTOR ANTAGONISTS DERIVATIVES 审中-公开
标题翻译：作为激素受体拮抗剂衍生物的吡唑化合物
公开(公告)号：WO2004058761A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/040630
申请日：2003-12-19
申请人： PHARMACIA CORPORATION , PENNING, Thomas, D. , KHILEVICH, Albert , CHEN, Barbara, B. , GANDHI, Preete , WANG, Yaping , DOWNS, Victoria , BOYS, Mark, L. , RUSSELL, Mark , SPANGLER, Dale, P. , HUFF, Renee, M.
发明人： PENNING, Thomas, D. , KHILEVICH, Albert , CHEN, Barbara, B. , GANDHI, Preete , WANG, Yaping , DOWNS, Victoria , BOYS, Mark, L. , RUSSELL, Mark , SPANGLER, Dale, P. , HUFF, Renee, M.
IPC分类号： C07D471/04
CPC分类号： C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04
摘要： The present invention relates to pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the α V β3 and/or the α V β 5 integrin without significantly inhibiting the α V β 6 integrin.
摘要翻译：本发明涉及包含式（I）化合物的药物组合物，以及选择性抑制或拮抗αVβ3和/或αBbeta5整联蛋白而不显着抑制αVbeta6整联蛋白的方法。

4. 发明申请

WO1997027181A1 HETEROCYCLO-SUBSTITUTED IMIDAZOLES FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的杂环取代的咪唑
公开(公告)号：WO1997027181A1
公开(公告)日：1997-07-31
申请号：PCT/US1997000300
申请日：1997-01-24
申请人： G.D. SEARLE & CO. , KHANNA, Ish, K. , WEIER, Richard, M. , COLLINS, Paul, W. , YU, Ui , XU, Xiangdong , PARTIS, Richard, A. , KOSZYK, Francis, J. , HUFF, Renee, M.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R 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 R is a radical selected from hydrido, alkyl and halo; and wherein R and R are independently selected from aryl and heterocyclo, wherein R and R 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 R and R 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，烷氧基羰基，卤代烷基羰基，羧基，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在可取代的位置任选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; 提供R 13和R 14中的至少一个是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. 发明申请

WO2004058254A1 HETEROARYLALKANOIC ACIDS AS INTEGRIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为INTEGRIN受体拮抗剂的异氟烷酸
公开(公告)号：WO2004058254A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/040898
申请日：2003-12-22
申请人： PHARMACIA CORPORATION , BOYS, Mark, L. , SCHRETZMAN, Lori, A. , TOLLEFSON, Michael, B. , CHANDRAKUMAR, Nizal, S. , KHANNA, Ish, K. , NGUYEN, Maria , DOWNS, Victoria , MOHLER, Scott, B. , GESICKI, Glen, J. , PENNING, Thomas, D. , CHEN, Barbara, B. , WANG, Yaping , KHILEVICH, Albert , DESAI, Bipinchandra, N. , YU, Yi , WENDT, John, A. , STENMARK, Heather , WU, Lisa , HUFF, Renee, M. , NAGARAJAN, Srinivasan, R. , DEVADAS, Balekudru , LU, Hwang-Fun , RUSSELL, Mark , SPANGLER, Dale, P. , PARIKH, Mihir, D. , CLARE, Michael
发明人： BOYS, Mark, L. , SCHRETZMAN, Lori, A. , TOLLEFSON, Michael, B. , CHANDRAKUMAR, Nizal, S. , KHANNA, Ish, K. , NGUYEN, Maria , DOWNS, Victoria , MOHLER, Scott, B. , GESICKI, Glen, J. , PENNING, Thomas, D. , CHEN, Barbara, B. , WANG, Yaping , KHILEVICH, Albert , DESAI, Bipinchandra, N. , YU, Yi , WENDT, John, A. , STENMARK, Heather , WU, Lisa , HUFF, Renee, M. , NAGARAJAN, Srinivasan, R. , DEVADAS, Balekudru , LU, Hwang-Fun , RUSSELL, Mark , SPANGLER, Dale, P. , PARIKH, Mihir, D. , CLARE, Michael
IPC分类号： A61K31/4245
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 ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 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，以及在不显着抑制alphaneta 6整联蛋白的情况下选择性地抑制或拮抗氨化疟原虫3和/或囟化α5整联蛋白的方法。

6. 发明申请

WO1996003388A1 1,2-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的1,2-取代的咪唑啉化合物
公开(公告)号：WO1996003388A1
公开(公告)日：1996-02-08
申请号：PCT/US1995009506
申请日：1995-07-27
申请人： G.D. SEARLE & CO. , KHANNA, Ish, K. , WEIER, Richard, M. , COLLINS, Paul, W. , YU, Yi , XU, Xiangdong , HUFF, Renee, M. , PARTIS, Richard, A. , KOSZYK, Francis, J.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D233/54
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 (II), wherein R is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkyloxy, cycloalkyloxyalkyle, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cyanoalkyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, azidoalkyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, arylthio, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, aryloxy, heterocycloalkylcarbonyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, aminocarbonyl, alkylaminocarbonylalkyl, aralkylthio, heteroarylalcoxyalkyl, heteroaryloxyalkyl, aralkoxy, heteroarylthioalkyl, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl, wherein the aryl and heteroaryl radicals are optionally substitued at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsufinyl, alkyl, cyano, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl and haloalkoxy; wherein R is a radical selected from alkyl and amino; and wherein R is one or more radicals selected from hydrido, halo, alkyl, haloalkyl, alkoxy, amino, haloalkoxy, cyano, carboxyl, hydroxyl, hydroxyalkyl, alkoxyalkyl, alkylamino, nitro and alkylthio.
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（II）定义，其中R 3是选自氢，烷基，卤代烷基，芳烷基，杂环烷基，酰基，氰基，烷氧基，烷硫基，烷硫基烷基，烷基磺酰基，环烷氧基，环烷氧基烯烃，环烷基硫代烷基，环烷基磺酰基，氰基烷基，环烷基磺酰基烷基，卤代烷基磺酰基，叠氮基烷基，芳基磺酰基，卤素，羟基烷基，烷氧基烷基，芳硫基，烷基羰基，芳基羰基，芳烷基羰基，芳氧基，杂环烷基羰基，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，烷氧基羰基，卤代烷基羰基，氨基羰基，烷基氨基羰基烷基，芳烷硫基，杂芳基烷氧基烷基，杂芳氧基烷基，芳烷氧基，杂芳硫基烷基，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，芳烷硫基烷基，芳烷氧基烷基，芳基和杂芳基，其中芳基和杂芳基是优选的在一个可取代位置被一个或多个选自卤素，烷硫基，烷基亚磺酰基，烷基，氰基，卤代烷基，羟基，烷氧基，羟基烷基和卤代烷氧基的基团取代; 其中R 7是选自烷基和氨基的基团; 其中R 8是选自氢，卤代，烷基，卤代烷基，烷氧基，氨基，卤代烷氧基，氰基，羧基，羟基，羟基烷基，烷氧基烷基，烷基氨基，硝基和烷硫基中的一个或多个基团。

7. 发明申请

WO1996003387A1 4,5-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的4,5-取代的咪唑啉化合物
公开(公告)号：WO1996003387A1
公开(公告)日：1996-02-08
申请号：PCT/US1995009505
申请日：1995-07-27
申请人： G.D. SEARLE & CO. , WEIER, Richard, M. , COLLINS, Paul, W. , STEALEY, Michael, A. , BARTA, Thomas, E. , HUFF, Renee, M.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07D233/84 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04
摘要： A class of compounds is described for treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein R is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower alkenyloxyalkyl, mercapto, lower alkylcarbonyl, lower haloalkylcarbonyl, phenylcarbonyl, lower aralkylcarbonyl, lower aralkenyl, lower aryloxyalkyl, lower aralkyloxyalkyl, lower arylsulfonyl, lower aralkylsulfonyl, lower arylthioalkyl, lower heteroarylalkylthioalkyl, and heteroaryl selected from 2-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 4-pyridyl and 2-benzofuryl; wherein R and R are independently selected from heteroaryl, cycloalkyl and aryl, wherein the heteroaryl, cycloalkyl and aryl radicals are substituted at a substitutable position with one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminosulfonyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkoxy, amino, lower alkylamino, phenylamino and nitro; and wherein R is selected from hydrido, lower alkyl and acyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了一类化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式（I）定义，其中R 1选自低级烷基，低级卤代烷基，低级羟烷基，低级烷氧基烷基，低级烯氧基烷基，巯基，低级烷基羰基，低级卤代烷基羰基，苯基羰基，低级芳烷基羰基，低级芳烯基，低级芳氧基烷基，低级芳烷氧基烷基，低级芳基磺酰基，低级芳烷基磺酰基，低级芳基硫代烷基，低级杂芳基烷硫基烷基和选自2-噻吩基，2-呋喃基，3-呋喃基，2-吡啶基，4-吡啶基和2-苯并呋喃基的杂芳基。其中R 2和R 3独立地选自杂芳基，环烷基和芳基，其中杂芳基，环烷基和芳基在可取代的位置被一个或多个选自氢，卤代，低级烷硫基，低级烷基亚磺酰基低级烷基磺酰基，氨基磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟烷基，低级烷氧基烷基，低级卤代烷氧基，氨基，低级烷基氨基，苯基氨基和硝基。并且其中R 4选自氢，低级烷基和酰基; 或其药学上可接受的盐。

8. 发明申请

WO2004087687A1 CHROMENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：铬衍生物作为抗炎剂
公开(公告)号：WO2004087687A1
公开(公告)日：2004-10-14
申请号：PCT/IB2004/000939
申请日：2004-03-19
申请人： PHARMACIA CORPORATION , ASTON, Karl, W. , BROWN, David, L. , CARTER, Jeffrey, S. , DEPROW, Angela, M. , FLETCHER, Theresa, R. , HALLINAN, E., Ann , HAMPER, Bruce, C. , HUFF, Renee, M. , KIEFER, James, R., Jr. , KOSZYK, Francis , KRAMER, Steven, W. , LIAO, Subo , LIMBURG, David , SPRINGER, John, R. , TSYMBALOV, Sofya , WANG, Lijuan, Jane , XING, Li , YU, Yi
发明人： ASTON, Karl, W. , BROWN, David, L. , CARTER, Jeffrey, S. , DEPROW, Angela, M. , FLETCHER, Theresa, R. , HALLINAN, E., Ann , HAMPER, Bruce, C. , HUFF, Renee, M. , KIEFER, James, R., Jr. , KOSZYK, Francis , KRAMER, Steven, W. , LIAO, Subo , LIMBURG, David , SPRINGER, John, R. , TSYMBALOV, Sofya , WANG, Lijuan, Jane , XING, Li , YU, Yi
IPC分类号： C07D311/58
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 (I). 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（I）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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