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2. 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。

3. 发明申请

WO1996024584A1 2,3-SUBSTITUTED PYRIDINES FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的2,3-取代的吡啶
公开(公告)号：WO1996024584A1
公开(公告)日：1996-08-15
申请号：PCT/US1996001111
申请日：1996-02-08
申请人： G.D. SEARLE & CO. , WEIER, Richard, M. , LEE, Len, F. , PARTIS, Richard, A. , KOSZYK, Francis, J.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D213/61
CPC分类号： C07D213/64 , C07D213/61 , C07D213/70 , C07D213/76 , C07D213/82 , C07D213/85
摘要： A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R and R are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R and R is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的吡啶基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（II）定义，其中R 1选自氢，卤素，烷氧基，卤代烷氧基，芳基，烷硫基，烷基氨基，芳烷氧基，叠氮基和烯氧基; 氰基，羟基烷基，卤代烷基，氨基烷基，烷基氨基烷基，烷基羰氧基烷基，氨基羰基和烷基羰基氨基烷基;其中R 2选自氢，氰基，并且其中R 5和R 6是一个或多个独立地选自卤素，烷基磺酰基，氨基磺酰基，烷氧基和烷硫基的基团; 其中R 5和R 6之一被烷基磺酰基，氨基磺酰基或卤代烷基磺酰基取代; 或其药学上可接受的盐。

4. 发明申请

WO1994005635A1 ANTI-VIRAL SULFUR-ANALOGUES OF 1,5-DIDEOXY-1,5-IMINO-D-GLUCITOL (DEOXYNOJIRIMYCIN) 审中-公开
标题翻译： 1,5-二脱氧-1,5-IMINO-D-葡萄糖醇（脱氧维生素C）的抗虚拟硫酸类似物
公开(公告)号：WO1994005635A1
公开(公告)日：1994-03-17
申请号：PCT/US1993008219
申请日：1993-09-08
申请人： G.D. SEARLE & CO. , KOSZYK, Francis, J. , MUELLER, Richard, A.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D211/56
CPC分类号： C07D491/04 , C07D211/54 , C07D211/56 , C07D211/58
摘要： Novel derivatives of 1-deoxynojirimycin are disclosed which have thio or sulfinyl substituents at C-2 or C-3. They can be represented by formulae (I, II). These compounds are useful inhibitors of lentiviruses such as visna virus and human immunodeficiency virus. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
摘要翻译：公开了1-脱氧野尻霉素的新型衍生物，其在C-2或C-3具有硫基或亚磺酰基取代基。它们可以由公式（I，II）表示。这些化合物是慢病毒如粘膜病毒和人类免疫缺陷病毒的有用抑制剂。还公开了这些衍生物的化学合成方法及其中间体。

5. 发明申请

WO2003035625A1 SUBSTITUTED INDAZOLE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的替代的吲哚酚化合物
公开(公告)号：WO2003035625A1
公开(公告)日：2003-05-01
申请号：PCT/US2002/029626
申请日：2002-09-19
申请人： PHARMACIA CORPORATION , STEALEY, Michael, A. , CLARE, Michael , CRICH, Joyce, Z. , HANAU, Cathleen, E. , KOSZYK, Francis, J. , PARTIS, Richard, A. , XU, Xiangdong , WEIER, Richard, M.
发明人： STEALEY, Michael, A. , CLARE, Michael , CRICH, Joyce, Z. , HANAU, Cathleen, E. , KOSZYK, Francis, J. , PARTIS, Richard, A. , XU, Xiangdong , WEIER, Richard, M.
IPC分类号： C07D231/56
CPC分类号： C07D231/56 , C07D401/04 , C07D405/04 , C07D471/04
摘要： The present invention relates to substituted indazole derivatives, compositions comprising such, intermediates, methods of making substituted indazolel derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
摘要翻译：本发明涉及取代的吲唑衍生物，包含这些的组合物，中间体，制备取代的吲唑衍生物的方法，以及用于治疗癌症，炎症和炎症相关疾病如关节炎的方法。

6. 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。

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