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21. 发明申请

WO1992017469A2 N-ARYLHETEROARYLALKYL IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的N-亚油酸二甲基咪唑-2-酮化合物
公开(公告)号：WO1992017469A2
公开(公告)日：1992-10-15
申请号：PCT/US1992002439
申请日：1992-04-01
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D401/14
CPC分类号： C07D401/06 , A61K31/4439 , C07D401/10 , C07D401/14
摘要： A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of formula (I) wherein A is selected from (a), (b), (c), (d), (e) and (f), wherein m is one; R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenetyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R0 is hydrido; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R?3, R4, R6, R7, R8, R9, R10 and R11¿ is hydrido and R5 must be seleted from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (g), (h) and (i) wherein each of R?42 and R43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

22. 发明申请

WO1992016523A1 5-ARYLHETEROARYLALKYL-1,3,5-TRISUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的5-亚乙基二甲基-1,3,5-三唑-1,2,4-三唑化合物
公开(公告)号：WO1992016523A1
公开(公告)日：1992-10-01
申请号：PCT/US1992002076
申请日：1992-03-20
申请人： G.D. SEARLE & CO. , REITZ, David, B.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D401/14
CPC分类号： C07D401/06 , C07D401/10 , C07D401/14 , Y10S514/824 , Y10S514/913
摘要： A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of formula (I); wherein A is selected from (1), (2), (3), (4), (5) and (6); wherein m is one; wherein R1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R?3, R4, R6¿ through R11 is hydrido and R5 is selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (a), (b) and (c); wherein each of R?42 and R43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.

23. 发明申请

WO1992007834A1 N-SUBSTITUTED IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的N-取代的咪唑烷-2-酮化合物
公开(公告)号：WO1992007834A1
公开(公告)日：1992-05-14
申请号：PCT/US1991007729
申请日：1991-10-28
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D233/70
CPC分类号： C07D403/10 , C07D233/70 , C07D409/14
摘要： A class of N-substituted imidazol-2-one compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, chlorophenyl, thienylethyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R0 is selected from hydrido, methyl, fluoro, chloro, monofluoromethyl, difluoromethyl, trifluoromethyl, formyl, carboxyl and dimethoxymethyl; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R?3, R4, R5, R6, R7, R8, R10 and R11¿ is hydrido; wherein R9 is selected from COOH and (II) or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

24. 发明申请

WO1992002257A2 RENAL-SELECTIVE ANGIOTENSIN II ANTAGONISTS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：选择性血管紧张素II治疗高血压的拮抗剂
公开(公告)号：WO1992002257A2
公开(公告)日：1992-02-20
申请号：PCT/US1991005476
申请日：1991-08-06
申请人： G.D. SEARLE & CO. , MANNING, Robert, E. , REITZ, David, B.
发明人： G.D. SEARLE & CO.
IPC分类号： A61K47/48
CPC分类号： C07D403/10 , A61K47/54 , A61K47/545 , C07D233/68
摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted imidazole compounds, of which N-acetyl-L-glutamic acid, 5-[[4'-[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-ylmethyl] [1,1'-biphenyl]-2-yl]carbonyl]hydrazide shown above is an example.
摘要翻译：描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。特别感兴趣的结合物是联苯甲基1H-取代的咪唑化合物的谷氨酰基衍生物，其中N-乙酰基-L-谷氨酸5 - [[4' - [2-丁基-4-氯-5-（羟甲基）咪唑-1-基甲基] [1,1'-联苯] -2-基]羰基]酰肼是一个例子。

25. 发明申请

WO0242272A2 SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
标题翻译：用于选择性抑制凝聚剂CASCADE的取代的多环芳烃和异丁基吡啶
公开(公告)号：WO0242272A2
公开(公告)日：2002-05-30
申请号：PCT/US0143280
申请日：2001-11-20
申请人： PHARMACIA CORP , SOUTH MICHAEL S , CASE BRENDA , GARLAND DANNY J , HAYES MICHAEL J , HUANG HORNG CHIH , HUANG WEI , JONES DARIN E , NEUMANN WILLIAM L , PARLOW JOHN J , REITZ DAVID B , RUEPPEL MELVIN L , WEBBER RONALD K
发明人： SOUTH MICHAEL S , CASE BRENDA , GARLAND DANNY J , HAYES MICHAEL J , HUANG HORNG-CHIH , HUANG WEI , JONES DARIN E , NEUMANN WILLIAM L , PARLOW JOHN J , REITZ DAVID B , RUEPPEL MELVIN L , WEBBER RONALD K
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D213/00
CPC分类号： C07D213/74 , C07D213/89
摘要： The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译：本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

26. 发明申请

WO1996016934A1 SUBSTITUTED BIPHENYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的替代联苯化合物
公开(公告)号：WO1996016934A1
公开(公告)日：1996-06-06
申请号：PCT/US1995014943
申请日：1995-11-29
申请人： G.D. SEARLE & CO. , REITZ, David, B. , LI, Jinglin , NORTON, Monica, B.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C317/14
CPC分类号： C07D213/26 , C07C311/16 , C07C311/29 , C07C311/39 , C07C317/14 , C07C317/22 , C07C317/32 , C07D317/52 , C07D317/56 , C07D319/18
摘要： A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (III), wherein each of R through R is independently selected from hydrido, halo, lower alkoxy, lower haloalkyl, amino, lower alkylamino, lower dialkylamino, and lower haloalkoxy; or wherein R and R together form -O(CH2)nO-; wherein n is 1-2, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的联苯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（III）定义，其中R 11至R 13各自独立地选自氢，卤素，低级烷氧基，低级卤代烷基，氨基，低级烷基氨基，低级二烷基氨基和低级卤代烷氧基; 或其中R 11和R 12一起形成-O（CH 2）n O-; 其中n为1-2; 或其药学上可接受的盐。

27. 发明申请

WO1995021817A1 SUBSTITUTED SPIRO COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的替代性SPIRO化合物
公开(公告)号：WO1995021817A1
公开(公告)日：1995-08-17
申请号：PCT/US1995001385
申请日：1995-02-07
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E. , HUANG, Horng-Chi , LI, Jinglin
发明人： G.D. SEARLE & CO.
IPC分类号： C07C317/14
CPC分类号： C07D213/70 , C07C311/16 , C07C311/29 , C07C317/14 , C07C317/22 , C07C323/65 , C07D213/34 , C07D213/61 , C07D317/56
摘要： A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (III), wherein n is a number selected from 0, 1 and 2; wherein R is selected from hydrido and halo; wherein R is selected from hydrido and halo; wherein R is selected from hydrido, halo, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, and hydroxyl; wherein R is selected from hydrido, halo, and lower alkyl; or wherein R and R together form methylenedioxy; and wherein R is selected from lower alkyl and amino; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的螺环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（III）定义，其中n是选自0,1和2的数; 其中R 6选自氢和卤素; 其中R 7选自氢和卤素; 其中R 8选自氢，卤素，低级烷基，低级烷氧基，低级卤代烷基，低级卤代烷氧基和羟基; 其中R 9选自氢，卤素和低级烷基; 或其中R 8和R 9一起形成亚甲二氧基; 并且其中R 11选自低级烷基和氨基; 或其药学上可接受的盐。

28. 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。

29. 发明申请

WO9218092A3 I-arylheteroarylalkyl substituted-1h-1,2,4-triazo le compounds for treatment of circulatory disorders 审中-公开
标题翻译：用于治疗循环系统疾病的1-芳基杂芳基烷基取代的-1h-1,2,4-三唑类化合物
公开(公告)号：WO9218092A3
公开(公告)日：1992-12-10
申请号：PCT/US9202801
申请日：1992-04-10
申请人： SEARLE & CO , REITZ DAVID B
发明人： REITZ DAVID B
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/14
摘要： A class of 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula (I) wherein A is selected from (1, 2, 3, 4, 5 and 6), wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, 2-ethylbutyl, 1,1-difluorobutyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, ethylbutyl, n-pentyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, phenyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and buthylthio; wherein R5 is an acidic group selected from CO¿2?H and tetrazole radicals; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

30. 发明申请

WO1992005161A1 1,3,5-TRISUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的1,3,5-三唑-1,2,4-三唑化合物
公开(公告)号：WO1992005161A1
公开(公告)日：1992-04-02
申请号：PCT/US1991006509
申请日：1991-09-16
申请人： G.D. SEARLE & CO. , REITZ, David, B.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D249/08
CPC分类号： C07D249/08 , C07D403/10
摘要： A class of 1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I) wherein m is one; wherein R1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neopentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R3 through R11 is hydrido with the proviso that at least one of R?5 and R9¿ must be selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (a), (b) and (c), wherein each of R?42 and R43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

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