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1. 发明申请

WO1996009293A1 BENZ[g]INDAZOLYL DERIVATIVES FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译： BENZ [g]用于治疗炎症的丁唑衍生物
公开(公告)号：WO1996009293A1
公开(公告)日：1996-03-28
申请号：PCT/US1995011402
申请日：1995-09-14
申请人： G.D. SEARLE & CO. , ROGERS, Kathy, L. , TALLEY, John, J. , BERTENSHAW, Stephen, R.
发明人： G.D. SEARLE & CO. , ROGERS, Kathy, L. , ROGERS, Roland, S. +di
IPC分类号： C07D231/54
CPC分类号： C07D231/54
摘要： A class of benz[g]indazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (I) wherein A is -CH=CH-; wherein B is phenyl or pyridyl; wherein R is selected from lower haloalkyl, cyano, lower alkoxycarbonyl, lower N-monoalkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R is phenyl optionally substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R is one or more radicals selected from halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, lower alkoxycarbonyl, aminocarbonyl, lower N-monoalkylaminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower haloalkoxy, amino, lower N,N-dialkylamino and nitro; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类苯并[g]吲唑基衍生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A为-CH = CH-; 其中B是苯基或吡啶基; 其中R 1选自低级卤代烷基，氰基，低级烷氧基羰基，低级N-单烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。其中R 2是在可取代的位置任选被一个选自低级烷基磺酰基和氨基磺酰基的基团取代的苯基; 并且其中R 3是一个或多个选自卤素，低级烷硫基，低级烷基亚磺酰基，低级烷基，氰基，低级烷氧基羰基，氨基羰基，低级N-单烷基氨基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟烷基，低级卤代烷氧基，氨基，低级N，N-二烷基氨基和硝基; 或其药学上可接受的盐。

2. 发明申请

WO1995015315A1 1,5-DIPHENYL PYRAZOLE COMPOUNDS FOR TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的1,5-二苯基吡唑化合物
公开(公告)号：WO1995015315A1
公开(公告)日：1995-06-08
申请号：PCT/US1994012718
申请日：1994-11-14
申请人： G.D. SEARLE & CO. , LEE, Len, F. , BERTENSHAW, Stephen, R.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , A61K31/415
摘要： A class of 1,5-diphenyl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of formula (I), wherein R1 is methylsulfonyl; wherein R2 is selected from -CF3, -CF2Cl, -CF2H, -CF2CF3 and -CF2CF2CF3; and wherein R is fluoro or chloro; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类1,5-二苯基吡唑用于治疗炎症，包括治疗疼痛和疾病如关节炎。特别感兴趣的化合物具有式（I），其中R 1是甲基磺酰基; 其中R 2选自-CF 3，-CF 2 Cl，-CF 2 H，-CF 2 CF 3和-CF 2 CF 2 CF 3; 并且其中R 3是氟或氯; 或其药学上可接受的盐。

3. 发明申请

WO0023433A8 SUBSTITUTED BENZOPYRAN ANALOGS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：替代苯并吡喃类似物用于治疗炎症
公开(公告)号：WO0023433A8
公开(公告)日：2000-07-27
申请号：PCT/US9921460
申请日：1999-10-15
申请人： SEARLE & CO , CARTER JEFFREY S , DEVADAS BALEKUDRU , TALLEY JOHN J , BROWN DAVID L , GRANETO MATTHEW J , ROGIER DONALD J JR , NAGARAJAN SRINIVASAN R , HANAU CATHLEEN E , HARTMANN SUSAN J , LUDWIG CINDY L , METZ SUZANNE , KORTE DONALD E , BERTENSHAW STEPHEN R , OBUKOWICZ MARK G
发明人： CARTER JEFFREY S , DEVADAS BALEKUDRU , TALLEY JOHN J , BROWN DAVID L , GRANETO MATTHEW J , ROGIER DONALD J JR , NAGARAJAN SRINIVASAN R , HANAU CATHLEEN E , HARTMANN SUSAN J , LUDWIG CINDY L , METZ SUZANNE , KORTE DONALD E , BERTENSHAW STEPHEN R , OBUKOWICZ MARK G
IPC分类号： C07D335/06 , A61K20060101 , A61K31/35 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/4184 , A61K31/443 , A61K31/4433 , A61K31/453 , A61K31/47 , A61K31/5377 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D215/54 , C07D221/00 , C07D307/00 , C07D311/00 , C07D311/12 , C07D311/22 , C07D311/38 , C07D311/58 , C07D311/92 , C07D317/00 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/052 , C07D493/04
CPC分类号： C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D335/06 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04
摘要： A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I') wherein X, A , A , A , A , R, R'', R and R are as described in the specification.
摘要翻译：描述了一类苯并吡喃，苯并硫杂吡喃，二氢喹啉，二氢萘及其类似物用于治疗环氧合酶-2介导的病症。特别感兴趣的化合物由式（I'）定义，其中X，A 1，A 2，A 3，A 4，R，R“，R 1和R 2' 如说明书中所述。

4. 发明申请

WO1996009304A1 BENZOPYRANOPYRAZOLYL DERIVATIVES FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗感染的苯并吡喃并吡唑衍生物
公开(公告)号：WO1996009304A1
公开(公告)日：1996-03-28
申请号：PCT/US1995011403
申请日：1995-09-15
申请人： G.D. SEARLE & CO. , TALLEY, John, J. , BERTENSHAW, Stephen, R. , GRANETO, Matthew, J. , ROGIER, Donald, J.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D491/048
CPC分类号： C07D491/04 , C07D495/04
摘要： A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I) wherein A is -(CH2)m-X-(CH2)n-; wherein X is S(O)p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R is selected from lower haloalkyl, cyano, lower hydroxyalkyl, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and aminosulfonyl; and wherein R is one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, aminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, amino, lower N-alkylamino, lower N,N-dialkylamino, lower hydroxyalkyl and lower haloalkoxy; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类苯并吡喃并吡唑基衍生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A是 - （CH 2）m -X-（CH 2）n - ; 其中X是S（O）p或O; 其中m为0或1; 其中n为0或1; 其中p为0或1; 其中B选自苯基和五元和六元杂芳基; 其中R 1选自低级卤代烷基，氰基，低级羟烷基，甲酰基，低级烷氧基羰基，低级烷氧基，低级N-烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。其中R 2是在可取代位置被选自低级烷基磺酰基和氨基磺酰基的基团取代的苯基; 其中R 4是一个或多个选自氢，卤素，低级烷硫基，低级烷基亚磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，氨基羰基，低级卤代烷基，羟基，低级烷氧基，氨基，低级N-烷基氨基，低级N，N-二烷基氨基，低级羟烷基和低级卤代烷氧基; 或其药学上可接受的盐。

5. 发明申请

WO1994015932A1 NOVEL 3,4-DIARYL THIOPHENES AND ANALOGS THEREOF HAVING USE AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译：新型3,4-DIARYL THIOPHENES及其作为抗炎剂的模拟物
公开(公告)号：WO1994015932A1
公开(公告)日：1994-07-21
申请号：PCT/US1994000466
申请日：1994-01-14
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , BERTENSHAW, Stephen, R. , COLLINS, Paul, W. , PENNING, Thomas, D. , REITZ, David, B. , ROGERS, Roland, S.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07D333/18
CPC分类号： C07D409/04 , A61K31/341 , A61K31/365 , C07D307/38 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38
摘要： A class of 3,4-diaryl substitued thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein Y is selected from O, S and NR ; wherein R is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R and R are independently aryl or heteroaryl; and wherein R and R are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式（I）定义，其中Y选自O，S和NR 1; 其中R 1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R 2和R 3独立地为芳基或杂芳基; 并且其中R 2和R 3在可取代的位置任选被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

6. 发明申请

WO1995015316A1 SUBSTITUTED PYRAZOLYL BENZENESULFONAMIDES FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的取代的吡唑并苯并呋喃
公开(公告)号：WO1995015316A1
公开(公告)日：1995-06-08
申请号：PCT/US1994012720
申请日：1994-11-14
申请人： G. D. SEARLE & CO. , TALLEY, John, J. , PENNING, Thomas, D. , COLLINS, Paul, W. , ROGIER, Donald, J., Jr. , MALECHA, James, W. , MIYASHIRO, Julie, M. , BERTENSHAW, Stephen, R. , KHANNA, Ish, K. , GRANETS, Matthew, J. , ROGERS, Roland, S. , CARTER, Jeffery, S. , DOCTER, Stephen, H. , YU, Stella, S.
发明人： G. D. SEARLE & CO.
IPC分类号： C07D231/12
CPC分类号： C07D495/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), whrein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺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，R 2选自氢，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基，烷氧羰基氰基烯基和羟烷基; 其中R 3选自氢化，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基，烷氧基，卤代烷氧基，氨磺酰基，杂环和氨基; 条件是R 2和R 3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2为三氟甲基时R 4为未取代的噻吩基; 或其药学上可接受的盐。

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