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1. 发明公开

EP1640003A2 Compositions comprising a Cyclooxygenase-2 Inhibitor and a Leukotriene B4 receptor antagonist 失效
标题翻译： Zubereitungen enthaltend einen cyclooxygenase-2-Inhibitor and einen leukotrien-b4-Rezeptor Antagonisten
公开(公告)号：EP1640003A2
公开(公告)日：2006-03-29
申请号：EP05003990.8
申请日：1997-02-11
申请人： G.D. Searle & Co.
发明人： Gregory, Susan A. , Isakson, Peter C , Anderson, Gary
IPC分类号： A61K31/4164 , A61K31/4178 , A61K38/13 , A61P37/06
CPC分类号： A61K31/10 , A61K31/00 , A61K31/18 , A61K31/4164 , A61K31/4178 , A61K38/13 , A61K45/06 , A61K2300/00
摘要： Use of a leukotriene B 4 receptor antagonist and a cyclooxygenase-2 inhibitor,
wherein the cyclooxygenase-2 inhibitor is selected from compounds of Formula I:

wherein A is pyrazolyl;
wherein R 1 is at least one substituent selected from heterocyclo, cycloalkyl, cycloalkenyl and aryl, wherein R 1 is optionally substituted at a substitutable position with one or more radicals selected from alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio;
wherein R 2 is selected from alkyl and amino; and
wherein R 3 is a radical selected from halo, alkyl, alkenyl, alkynyl, oxo, cyano, carboxyl, cyanoalkyl, heterocyclooxy, alkyloxy, alkylthio, alkylcarbonyl, cycloalkyl, aryl, haloalkyl, heterocyclo, cycloalkenyl, aralkyl, heterocycloalkyl, acyl, alkylthioalkyl, hydroxyalkyl, alkoxycarbonyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxyaralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, carboxyalkyl, alkylamino, N-arylamino, N-aralkylamino, N-alkyl-N-aralkylamino, N-alkyl-N-arylamino, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-aralkylaminoalkyl, N-alkyl-N-aralkylaminoalkyl, N-alkyl-N-arylaminoalkyl, aryloxy, aralkoxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl, and N-alkyl-N-arylaminosulfonyl;
or a pharmaceutically-acceptable salt thereof, for preparing a medicament to suppress immune, acute or delayed-type hypersensitivity response in a subject.
摘要翻译：使用白三烯B 4受体拮抗剂和环加氧酶-2抑制剂，其中所述环加氧酶-2抑制剂选自式I化合物：其中A为吡唑基; 其中R 1是选自杂环基，环烷基，环烯基和芳基中的至少一个取代基，其中R 1任选地在可取代位置被一个或多个选自烷基，卤代烷基，氰基，羧基，烷氧基羰基，羟基，羟基烷基，卤代烷氧基氨基，烷基氨基，芳基氨基，硝基，烷氧基烷基，烷基亚磺酰基，卤素，烷氧基和烷硫基; 其中R 2选自烷基和氨基; 并且其中R 3是选自卤素，烷基，烯基，炔基，氧代，氰基，羧基，氰基烷基，杂环氧基，烷氧基，烷硫基，烷基羰基，环烷基，芳基，卤代烷基，杂环基，环烯基，芳烷基，杂环烷基，酰基，烷硫基烷基羟烷基，烷氧羰基，芳基羰基，芳烷基羰基，芳烯基，烷氧基烷基，芳硫基烷基，芳氧基烷基，芳烷硫基烷基，芳烷氧基烷基，烷氧基烷氧基烷基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基，N-芳基氨基羰基，N-烷基-N-芳基氨基羰基，烷基氨基羰基烷基，羧基烷基，烷基氨基，N 芳基氨基，N-芳烷基氨基，N-烷基-N-芳烷基氨基，N-烷基-N-芳基氨基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-芳烷基氨基烷基，N-烷基-N-芳烷基氨基烷基，N-烷基-N-芳基氨基烷基芳氧基，芳烷氧基，芳硫基，芳烷硫基，烷基亚磺酰基，烷基磺酰基，氨基磺酰基，烷基氨基磺酰基，N-芳基氨基磺酰基，芳基磺酰基和N-烷基-N-芳基氨基磺酰基; 用于制备抑制受试者中的免疫，急性或迟发型超敏反应的药物的ƒ€ƒ€或其药学上可接受的盐。

2. 发明授权

EP0833622B8 COMPOSITIONS COMPRISING A CYCLOOXYGENASE-2 INHIBITOR AND A 5-LIPOXYGENASE INHIBITOR 失效
标题翻译：培养基中环氧合酶-2抑制剂和5-脂氧合酶抑制剂
公开(公告)号：EP0833622B8
公开(公告)日：2005-10-12
申请号：EP96918465.4
申请日：1996-06-11
申请人： G.D. Searle & Co.
发明人： ISAKSON, Peter, C. , ANDERSON, Gary, D. , GREGORY, Susan, A.
IPC分类号： A61K31/00 , A61K31/10 , A61K31/18
CPC分类号： A61K31/415 , A61K31/47 , A61K45/06 , A61K31/155 , A61K2300/00
摘要： Combinations of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor are described for treatment of inflammation and inflammation-related disorders.

3. 发明公开

EP1466911A3 Preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake 审中-公开
标题翻译：一种用于与有效制备Benzothiepinen作为肺Ileumgallensäuretransportstaurocholates和记录的抑制剂处理
公开(公告)号：EP1466911A3
公开(公告)日：2005-09-07
申请号：EP03026649.8
申请日：1999-06-29
申请人： G.D. Searle & Co.
发明人： Lee, Len F. , Banerjee, Shyamal C. , Huang, Horng-Chih , Li, Jinglin J. , Miller, Raymond E. , Reitz, David B. , Tremont, Samuel J.
IPC分类号： C07D337/08
CPC分类号： A61K31/38 , C07C319/14 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/65539 , C07K5/06086 , C08G65/329 , C07C323/12 , C07C323/18
摘要： Methods are provided for preparing benzothiepines, derivatives, and analogs thereof, which have activity as inhibitors of ileal bile acid transport and taurocholate uptake.

4. 发明授权

EP0837883B1 METHOD OF SOLUBILIZING, PURIFYING, AND REFOLDING PROTEIN 失效
标题翻译：法解决，清洁和复性蛋白
公开(公告)号：EP0837883B1
公开(公告)日：2005-08-10
申请号：EP96924269.2
申请日：1996-06-07
申请人： CHIRON CORPORATION , G.D. Searle & Co.
发明人： DORIN, Glenn, J. , ARVE, Bo, H. , PATTISON, Gregory, L. , HALENBECK, Robert, F. , JOHNSON, Kirk , CHEN, Bao-Lu , RANA, Rajsharan, K. , HORA, Maninder, S. , MADANI, Hassan , GUSTAFSON, Mark, E. , TSANG, Michael , BILD, Gary, S. , JOHNSON, Gary, V.
IPC分类号： C07K14/81 , C07K1/113 , A61K38/57 , A61K9/08 , A61K47/30
CPC分类号： C07K14/475 , A23L7/111 , A23L7/165 , A23L9/10 , A23L9/22 , A23L19/09 , A23L19/18 , A23L21/15 , A23L29/212 , A23L29/219 , A23P20/12 , A61K9/0019 , A61K9/08 , A61K38/57 , A61K47/02 , A61K47/12 , A61K47/183 , A61K47/36 , C07K1/1136 , C07K14/8114 , Y10S514/97 , Y10S514/973
摘要： A method of modifying protein solubility employs polyionic polymers. These facilitate the solubilization, formulation, purification and refolding of proteins especially incorrectly folded proteins and aggregated proteins. Compositions are described that are suitable for formulating TFPI. The compositions allow preparation of pharmaceutically acceptable compositions of TFPI at concentrations above 0.2 mg/mL and above 10 mg/mL.

5. 发明公开

EP1466911A2 Preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake 审中-公开
标题翻译：一种用于与有效制备Benzothiepinen作为肺Ileumgallensäuretransportstaurocholates和记录的抑制剂处理
公开(公告)号：EP1466911A2
公开(公告)日：2004-10-13
申请号：EP03026649.8
申请日：1999-06-29
申请人： G.D. Searle & Co.
发明人： Lee, Len F. , Banerjee, Shyamal C. , Huang, Horng-Chih , Li, Jinglin J. , Miller, Raymond E. , Reitz, David B. , Tremont, Samuel J.
IPC分类号： C07D337/08 , C07D409/12 , C07C323/18
CPC分类号： A61K31/38 , C07C319/14 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/65539 , C07K5/06086 , C08G65/329 , C07C323/12 , C07C323/18
摘要： Methods are provided for preparing benzothiepines, derivatives, and analogs thereof, which have activity as inhibitors of ileal bile acid transport and taurocholate uptake.
摘要翻译：提供了制备benzothiepines，衍生物，及其类似物，其具有活性的回肠胆汁酸转运和牛磺胆酸盐摄取的抑制剂的方法。

6. 发明授权

EP1122245B1 2-Amino-benzoxazinones for the treatment of viral infections 失效
标题翻译： 2-氨基 - 苯并嗪酮用于病毒感染的治疗
公开(公告)号：EP1122245B1
公开(公告)日：2004-07-07
申请号：EP01110048.4
申请日：1996-05-23
申请人： G.D. Searle & Co.
发明人： Abood, Norman , Flynn, Daniel L. , Becker, Daniel P. , Bax, Brian M. , Li, Hui , Nosal, Roger A. , Schretzman, Lori A. , Villamil, Clara I.. , Bennett, Michael J. , Bedell, John L. , Williams, Kenneth
IPC分类号： C07D265/24 , C07D413/12 , A61K31/536 , A61P31/12
CPC分类号： C07D265/24 , C07D413/04 , C07D413/12 , C07D417/12

7. 发明公开

EP1380584A1 Process for making 5-substituted pyrazoles using dithietanes 审中-公开
标题翻译：一种用于制备使用Dithietanen 5-取代的吡唑过程
公开(公告)号：EP1380584A1
公开(公告)日：2004-01-14
申请号：EP03021671.7
申请日：1999-11-18
申请人： G.D. SEARLE & CO.
发明人： The designation of the inventor has not yet been filed
IPC分类号： C07D409/06 , C07D401/14 , C07D405/14 , C07D231/18 , C07D339/00 , C07D401/04 , A61K31/415 , A61K31/44
CPC分类号： C07D401/04 , C07D231/18 , C07D339/00 , C07D401/14 , C07D405/14 , C07D409/06
摘要： This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
摘要翻译：本发明涉及制备选择为p38激酶和COX-2抑制剂的5- substituiertem吡唑的新方法。

8. 发明公开

EP1331225A1 Method of preparing enantiomerically-enriched tetrahydrobenzothiepine oxides 审中-公开
标题翻译：维生素zur Herstellung von对映体 - angereicherten四氢苯并硫代奥昔芬
公开(公告)号：EP1331225A1
公开(公告)日：2003-07-30
申请号：EP03005459.7
申请日：1998-12-16
申请人： G.D. SEARLE & CO.
发明人： Li, James , Wang, Ching-Cheng , Reitz, David, B , Huang, Horng-Chih , Carpenter, Andrew, J. , Snieckus, Victor
IPC分类号： C07D337/08 , C07D487/08
CPC分类号： C07D487/08 , C07D337/08
摘要： A process for preparing enantiomerically-enriched tetrahydro-benzothiepine oxides comprises cyclizing an enantiomerically-enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.
摘要翻译：制备对映异构体富集的四氢苯并噻吩氧化物的方法包括环化富含对映异构体的芳基-3-丙醛亚砜，其中芳基-3-丙醛亚砜的硫原子是手性中心。

9. 发明授权

EP0741570B1 PREVENTING OR REDUCING PHOTOSENSITIVITY AND/OR PHOTOTOXICITY REACTIONS TO ANTIINFECTIVE MEDICATIONS 失效
标题翻译：预防或减少光敏或光毒反应的抗感染类药物
公开(公告)号：EP0741570B1
公开(公告)日：2003-05-07
申请号：EP95907337.0
申请日：1995-01-12
申请人： G.D. SEARLE & CO.
发明人： KLIMSTRA, Paul, Dale , RONIKER, Barbara , SWABB, Edward, Allen
IPC分类号： A61K31/495 , A61K31/00 , A61P31/04
CPC分类号： A61K31/65 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/505

10. 发明授权

EP0880504B1 HETEROCYCLO-SUBSTITUTED IMIDAZOLES FOR THE TREATMENT OF INFLAMMATION 失效
标题翻译：杂环取代的咪唑代替炎症的治疗
公开(公告)号：EP0880504B1
公开(公告)日：2003-04-02
申请号：EP97901952.8
申请日：1997-01-24
申请人： G.D. SEARLE & CO.
发明人： KHANNA, Ish, K. , WEIER, Richard, M. , COLLINS, Paul, W. , YU, Ui , XU, Xiangdong , PARTIS, Richard, A. , KOSZYK, Francis, J. , HUFF, Renee, M.
IPC分类号： C07D233/54 , A61K31/415 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
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 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 R?13 and R14¿ are independently selected from aryl and heterocyclo, wherein R?13 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 R?13 and R14¿ is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

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