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1.发明授权Substituted 1-(1H-imidazol-4-yl)alkyl-benzamides as anti-ischemics and as alpha-2-adrenergic receptor agonists 失效取代的1-（1H-咪唑-4-基）烷基 - 苯甲酰胺作为抗缺血剂和作为α-2-肾上腺素能受体激动剂
公开(公告)号：US4923865A
公开(公告)日：1990-05-08
申请号：US334854
申请日：1989-04-06
IPC分类号： C07D233/56 , A61K31/415 , A61K31/4164 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P29/00 , C07D233/54 , C07D233/64
CPC分类号： C07D233/64
摘要： New substituted 1-(1H-imidazol-4-yl)alkyl-benzamides and their salts, processes for the preparation thereof and pharmaceutical compositions.These compounds have the formula ##STR1## wherein R.sub.1, R.sub.2 =hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sub.3 =hydrogen, amino, hydroxyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -hydroxyalkyl,R.sub.4 =hydrogen or C.sub.1 -C.sub.4 -alkyl, orR.sub.3 R.sub.4 N=pyrrolidino, piperidino or morpholino,R.sub.5 and R.sub.6 =hydrogen, hydroxyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, at least one ofR.sub.5 and R.sub.6 being other than hydrogen.These compounds are prepared either by reacting a nitrogen compound with an alkyl 1-(1H-imidazol-4-yl)alkyl-benzoate or with a 1-(1H-imidazol-4-yl)alkyl-benzoic acid, or by hydrolyzing in an acid medium a 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzonitrile.The compounds have anti-ischemic and .alpha..sub.2 -adrenoceptor agonist activities.
摘要翻译： 新的取代的1-（1H-咪唑-4-基）烷基 - 苯甲酰胺及其盐，其制备方法和药物组合物。 这些化合物具有下式：其中R1，R2 =氢或C1-C4-烷基，R3 =氢，氨基，羟基，C1-C4-烷基或C1-C4-羟烷基，R4 =氢或C1-C4-烷基 或R3R4N =吡咯烷子基，哌啶子基或吗啉代，R5和R6 =氢，羟基，C1-C4-烷基或C1-C4-烷氧基，R5和R6中的至少一个不是氢。 这些化合物可以通过使氮化合物与1-（1H-咪唑-4-基）烷基 - 苯甲酸烷基酯或1-（1H-咪唑-4-基）烷基 - 苯甲酸烷基酯反应，或通过水解 酸性介质为2-羟基-3- [1-（1H-咪唑-4-基）烷基] - 苄腈。 该化合物具有抗缺血和α2-肾上腺素受体激动剂活性。
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公开(公告)号：US4814343A
公开(公告)日：1989-03-21
申请号：US116325
申请日：1987-11-02
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/495 , A61P9/08 , A61P9/10 , A61P9/12 , C07D233/54 , C07D233/58 , C07D233/64 , C07D405/06 , C07D413/06
CPC分类号： C07D233/64 , C07D405/06
摘要： New substituted 1H-imidazoles and their salts, processes for the preparation thereof and pharmaceutical compositions.These compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.5 =hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sub.4 =hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy;Y.sub.1 =hydrogen and Y.sub.2 =OZ.sub.2 or the reverse;Z.sub.1 =Z.sub.2 =hydrogen or C.sub.1 -C.sub.4 -alkyl or Z.sub.1 and Z.sub.2 =--CH.sub.2 -- or --C(CH.sub.3).sub.2 --.These compounds are prepared either by reducing a corresponding imidazole compound having a hydroxyl or alkoxy group on the methyl bridge between the imidazole and phenyl rings, or by hydrolyzing a 4-[[2,2-dimethyl-4H-1,3-benzodioxin-6(or 8)-yl]methyl]-1H-imidazole, or yet by reducing an alkyl 3-[(1H-imidazol-4-yl)methyl]-2-hydroxybenzoate.These compounds have cardiac, cerebral and tissular anti-ischemic activities.
摘要翻译： 新的取代的1H-咪唑及其盐，其制备方法和药物组合物。 这些化合物具有下式：其中R1，R2，R3和R5 =氢或C1-C4-烷基; R4 =氢，C1-C4-烷基或C1-C4-烷氧基; Y1 =氢，Y2 = OZ2或相反; Z 1 = Z 2 =氢或C 1 -C 4 - 烷基或Z 1和Z 2 = -CH 2 - 或-C（CH 3）2 - 。 这些化合物可以通过在咪唑和苯环之间的甲基桥上还原相应的具有羟基或烷氧基的咪唑化合物，或通过水解4 - [[2,2-二甲基-4H-1,3-苯并二恶英 - 6（或8） - 基]甲基] -1H-咪唑，或还原3 - [（1H-咪唑-4-基）甲基] -2-羟基苯甲酸烷基酯。 这些化合物具有心脏，脑和组织的抗缺血活性。
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公开(公告)号：US4837223A
公开(公告)日：1989-06-06
申请号：US25277
申请日：1987-03-12
申请人： Jean Gobert , Jean-Pierre Geerts , Guy Dodson
发明人： Jean Gobert , Jean-Pierre Geerts , Guy Dodson
IPC分类号： C07D207/26 , A61K31/40 , A61K31/4015 , A61P7/06 , A61P9/00 , A61P9/10 , C07D207/12 , C07D207/27 , C07D295/185
CPC分类号： C07D207/27
摘要： (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (S)-2-amino-butanamide of the formula X--CH.sub.2 CH.sub.2 -NHCH (C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 --radical when X represents a ZOOC--radical and Y is a --CO-- radical when X represents a HalCH.sub.2 --radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom.This laevorotatory enantiomer has been found to have significantly higher protective activity against hypoxia and ischemia than the corresponding racemate.
摘要翻译： （S）-α-乙基-2-氧代-1-吡咯烷乙酰胺，其制剂和含有它们的药物组合物。 其可以通过使（S）-α-乙基-2-氧代-1-吡咯烷乙酸与卤代甲酸烷基酯和氨反应，或通过使式X的（S）-2-氨基 - 丁酰胺环化 -CH 2 CH 2 -NHCH（C 2 H 5）CONH 2，其中当X表示ZOOC基团时，Y是-CH 2 - 基，当X表示HalCH 2 - 基团时，Y表示-CO-基，Z表示C1-C4烷基，Hal表示 卤素原子。 已经发现，这种左旋对映异构体具有比相应的外消旋物显着更高的抗缺氧和缺血的保护活性。
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4.发明授权Treatment of memory impairment using (R)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide 失效使用（R）-α-乙基-2-氧代-1-吡咯烷乙酰胺治疗记忆障碍
公开(公告)号：US4696942A
公开(公告)日：1987-09-29
申请号：US733791
申请日：1985-05-14
申请人： Jean Gobert , Corneliu Giurgea , Jean-Pierre Geerts , Guy Bodson
发明人： Jean Gobert , Corneliu Giurgea , Jean-Pierre Geerts , Guy Bodson
IPC分类号： C07D207/26 , A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/27 , C07D295/185
CPC分类号： C07D207/27
摘要： (R)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (R)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (R)-2-amino-butanamide of the formula X--CH.sub.2 CH.sub.2 --Y--NHCH(C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 -- radical when X represents a ZOOC-- radical and Y is a --CO-- radical when X represents a HalCH.sub.2 -- radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom. This dextrorotatory enantiomer has been found to have significantly higher mnemic activity and lower toxicity than the corresponding racemate.
摘要翻译： （R）-α-乙基-2-氧代-1-吡咯烷乙酰胺，其制备方法和含有它们的药物组合物。 其可以通过使（R）-α-乙基-2-氧代-1-吡咯烷乙酸与卤代甲酸烷基酯和氨反应，或通过使式X的（R）-2-氨基 - 丁酰胺环化 -CH 2 CH 2 -Y-NHCH（C 2 H 5）CONH 2，其中当X表示ZOOC-基团时，Y是-CH 2 - 基，当X表示HalCH 2 - 基时，Y是-CO-基，Z是C 1 -C 4烷基， Hal卤素原子。 已发现这种右旋对映异构体具有比相应的外消旋物显着更高的杀虫活性和较低的毒性。
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公开(公告)号：US4837224A
公开(公告)日：1989-06-06
申请号：US25278
申请日：1987-03-12
申请人： Jean Gobert , Corneliu Giurgea , Jean-Pierre Geerts , Guy Bodson
发明人： Jean Gobert , Corneliu Giurgea , Jean-Pierre Geerts , Guy Bodson
IPC分类号： C07D207/26 , A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/27 , C07D295/185
CPC分类号： C07D207/27
摘要： (R)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (R)-alpha-ethyl-2-oxo-1-pyrrolidineactic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (R)-2-amino-butanamide of the formula X--CH.sub.2 CH.sub.2 --Y--NHCH (C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 --radical when X represents a ZOOC--radical and Y is a --CO--radical when X represents a HalCH.sub.2 --radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom.This dextrorotatory enantiomer has been found to have significantly higher mnemic activity and lower toxicity than the corresponding racemate.
摘要翻译： （R）-α-乙基-2-氧代-1-吡咯烷乙酰胺，其制备方法和含有它们的药物组合物。 其可以通过使（R）-α-乙基-2-氧代-1-吡咯烷酮酸与卤代甲酸烷基酯和氨反应，或通过使式X的（R）-2-氨基 - 丁酰胺环化 -CH 2 CH 2 -Y-NHCH（C 2 H 5）CONH 2其中当X表示ZOOC基团时，Y是-CH 2 - 基，当X表示HalCH 2 - 基团时，Y表示-CO-基，Z表示C1-C4烷基， Hal卤素原子。 已发现这种右旋对映异构体具有比相应的外消旋物显着更高的杀虫活性和较低的毒性。
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公开(公告)号：US4696943A
公开(公告)日：1987-09-29
申请号：US733790
申请日：1985-05-14
申请人： Jean Gobert , Jean-Pierre Geerts , Guy Bodson
发明人： Jean Gobert , Jean-Pierre Geerts , Guy Bodson
IPC分类号： C07D207/26 , A61K31/40 , A61K31/4015 , A61P7/06 , A61P9/00 , A61P9/10 , C07D207/12 , C07D207/27 , C07D295/185
CPC分类号： C07D207/27
摘要： (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (S)-2-aminobutanamide of the formula X--CH.sub.2 CH.sub.2 --Y--NHCH(C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 -- radical when X represents a ZOOC-- radical and Y is a --CO-- radical when X represents a HalCH.sub.2 -- radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom.This laevorotatory enantiomer has been found to have significantly higher protective activity against hypoxia and ischemia than the corresponding racemate.
摘要翻译： （S）-α-乙基-2-氧代-1-吡咯烷乙酰胺，其制剂和含有它们的药物组合物。 可以通过使（S）-α-乙基-2-氧代-1-吡咯烷基乙酸与卤代甲酸烷基酯和氨反应，或通过使式X-CH 2 CH 2的（S）-2-氨基丁酰胺环化 -Y-NHCH（C 2 H 5）CONH 2，其中当X代表ZOOC-基团时，Y是-CH2-基，当X代表HalCH2-基时，Y是-CO-基，Z是C1-C4烷基，Hala 卤素原子。 已经发现，这种左旋对映异构体具有比相应的外消旋物显着更高的抗缺氧和缺血的保护活性。
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公开(公告)号：US4943639A
公开(公告)日：1990-07-24
申请号：US311631
申请日：1989-02-16
申请人： Jean Gobert , Jean-Pierre Geerts , Guy Bodson
发明人： Jean Gobert , Jean-Pierre Geerts , Guy Bodson
IPC分类号： C07D207/26 , A61K31/40 , A61K31/4015 , A61P7/06 , A61P9/00 , A61P9/10 , C07D207/12 , C07D207/27 , C07D295/185
CPC分类号： C07D207/27
摘要： (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (S)-2-amino-butanamide of the formula X--CH.sub.2 CH.sub.2 --Y--NHCH(C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 -- radical when X represents a ZOOC-- radical and Y is a --CO-- radical when X represents a HalCH.sub.2 -- radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom.This laevorotatory enantiomer has been found to have significantly higher protective activity against hypoxia and ischemia than the corresponding racemate.
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公开(公告)号：US5658938A
公开(公告)日：1997-08-19
申请号：US569947
申请日：1995-12-08
IPC分类号： C07D233/64 , A61K31/415 , A61K31/4164 , A61P9/00 , A61P9/10 , A61P9/12 , C07D233/54 , C07D233/56
CPC分类号： C07D233/64
摘要： Substituted 4-(1,2,3,4-tetrahydro-1-naphthalenyl)-1H-imidazoles and 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles, their optical isomers and their racemic mixtures, their salts, methods for preparing them and therapeutic compositions containing them. These compounds have the general formula ##STR1## wherein n=1 or 2,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 =hydrogen, halogen, hydroxyl C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy,R.sub.5 = hydrogen of C.sub.1 -C.sub.4 alkyl with the proviso that R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, cannot simultaneously be hydrogen when n is equal to 2.These new compounds exhibit anti-ischemic and anti-hypertensive activities.
摘要翻译： 取代的4-（1,2,3,4-四氢-1-萘基）-1H-咪唑和4-（2,3-二氢-1H-茚-1-基）-1H-咪唑，它们的旋光异构体及其 外消旋混合物，其盐，制备它们的方法和含有它们的治疗组合物。 这些化合物具有通式如下：卤素，羟基C 1 -C 4烷基或C 1 -C 4烷氧基，R 5 = C 1 -C 4烷基的氢，条件是R 1，R 2，R 3，R 4和R 5不能同时为氢 当n等于2.这些新化合物表现出抗缺血和抗高血压活性。
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