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1. 发明授权

US4780474A Use of alkylenediamine derivatives for the treatment of blood flow disturbances and pharmaceutical compositions containing them 失效
标题翻译：使用亚烷基二胺衍生物治疗血流紊乱和含有它们的药物组合物
公开(公告)号：US4780474A
公开(公告)日：1988-10-25
申请号：US6275
申请日：1987-01-20
申请人： Erwin Bohm , Jens-Peter Holck , Wolfgang Kampe , Herbert Leinert , Bernd Muller-Beckmann , Klaus Strein
发明人： Erwin Bohm , Jens-Peter Holck , Wolfgang Kampe , Herbert Leinert , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： C07D295/20 , A61K31/135 , A61K31/165 , A61K31/22 , A61K31/33 , A61K31/415 , A61K31/505 , A61K31/535 , A61K31/5375 , A61P7/00 , A61P9/00 , C07C67/00 , C07C213/00 , C07C217/84 , C07C231/00 , C07C233/25 , C07C233/78 , C07C235/44 , C07C235/46 , C07C235/50 , C07C237/22 , C07C237/34 , C07C239/00 , C07C241/00 , C07C253/00 , C07C255/54 , C07C275/00 , C07C313/00 , C07C323/36 , C07C323/60 , C07D231/38 , C07D231/56 , C07D239/54 , C07D521/00 , A61K31/40 , A61K31/405 , A61K31/41
CPC分类号： A61K31/505 , A61K31/135 , A61K31/165 , A61K31/415
摘要： The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.
摘要翻译：本发明涉及以下通式的化合物的用途：其中A是任选取代的苯基或杂芳族基团，R 6和R 7是氢或低级烷基，X是含有至多6个亚烷基的亚烷基链碳原子，Y是价键或> C = O基团，B是任选取代的苯基或杂芳族基团，以及它们的药理学上可接受的盐用于治疗血流紊乱。本发明还提供含有这些化合物的药物组合物。

2. 发明授权

US4880805A Use of alkylenediamine derivatives for the treatment of blood flow disturbances and pharmaceutical compositions containing them 失效
标题翻译：使用亚烷基二胺衍生物治疗血流紊乱和含有它们的药物组合物
公开(公告)号：US4880805A
公开(公告)日：1989-11-14
申请号：US222215
申请日：1988-07-21
申请人： Erwin Bohm , Jens-Peter Holck , Wolfgang Kampe , Herbert Leinert , Bernd Muller-Beckmann , Klaus Strein
发明人： Erwin Bohm , Jens-Peter Holck , Wolfgang Kampe , Herbert Leinert , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： C07D295/20 , A61K31/135 , A61K31/165 , A61K31/22 , A61K31/33 , A61K31/415 , A61K31/505 , A61K31/535 , A61K31/5375 , A61P7/00 , A61P9/00 , C07C67/00 , C07C213/00 , C07C217/84 , C07C231/00 , C07C233/25 , C07C233/78 , C07C235/44 , C07C235/46 , C07C235/50 , C07C237/22 , C07C237/34 , C07C239/00 , C07C241/00 , C07C253/00 , C07C255/54 , C07C275/00 , C07C313/00 , C07C323/36 , C07C323/60 , C07D231/38 , C07D231/56 , C07D239/54 , C07D521/00
CPC分类号： A61K31/505 , A61K31/135 , A61K31/165 , A61K31/415
摘要： The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.
摘要翻译：本发明涉及以下通式的化合物的用途：其中A是任选取代的苯基或杂芳族基团，R 6和R 7是氢或低级烷基，X是含有至多6个亚烷基的亚烷基链碳原子，Y是价键或> C = O基团，B是任选取代的苯基或杂芳族基团，以及它们的药理学上可接受的盐用于治疗血流紊乱。本发明还提供含有这些化合物的药物组合物。

3. 发明授权

US4810801A Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of them to treat certain heart and circulatory diseases 失效
标题翻译：吡咯并苯并咪唑，含有它们的药物组合物，以及它们用于治疗某些心脏和循环系统疾病
公开(公告)号：US4810801A
公开(公告)日：1989-03-07
申请号：US103895
申请日：1987-10-01
申请人： Alfred Mertens , Jens-Peter Holck , Wolfgang Kampe , Bernd Muller-Beckmann , Klaus Strein , Wolfgang Schaumann
发明人： Alfred Mertens , Jens-Peter Holck , Wolfgang Kampe , Bernd Muller-Beckmann , Klaus Strein , Wolfgang Schaumann
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , A61P9/04 , C07D209/34 , C07D209/42 , C07D487/04 , C07D209/54 , C07D211/22 , C07D405/12 , C07D413/12
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42
摘要： The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 -R.sub.5, X and T are as defined in the specification. The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
摘要翻译：本发明提供了以下通式的新的吡咯并苯并咪唑：其中R1-R5，X和T如说明书中所定义。本发明还提供了制备这些化合物的方法和含有它们的药物用于预防和治疗心脏和循环系统疾病。

4. 发明授权

US4963686A Certain pyridinoylamino-indolin-2-one derivatives 失效
标题翻译：某些吡啶基氨基 - 二氢吲哚-2-酮衍生物
公开(公告)号：US4963686A
公开(公告)日：1990-10-16
申请号：US217143
申请日：1988-07-05
申请人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
发明人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/12 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D403/14 , C07D487/04 , C07D487/10 , C07D487/14
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D487/10
摘要： The new pyrrolobenzimidazoles according to the present invention are compounds of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom, an alkyl or alkenyl radical or a cyano group or a carbonyl group substituted by a hydroxyl or hydrazino group or by an alkyl, alkoxy, amino, alkylamino or dialkylamino group or together with R.sub.1 represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical, X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinylene radical, T is an oxygen or sulphur atom and Py is a 2-, 3- or 4-pyridyl radical which optionally carries an oxygen atom on the ring heteroatom and/or can be substituted one or more times by alkyl, alkoxy, hydroxyl, cyano or nitro, as well as by halogen; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.

5. 发明授权

US4666923A Pyrrolobenzimidazoles for treating heart or circulatory diseases 失效
标题翻译：用于治疗心脏或循环系统疾病的吡咯并苯并咪唑
公开(公告)号：US4666923A
公开(公告)日：1987-05-19
申请号：US731500
申请日：1985-05-07
申请人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
发明人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/12 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D403/14 , C07D487/04 , C07D487/10 , C07D487/14
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D487/10
摘要： Pyrrolobenzimidazoles, processes for the preparation thereof and pharmaceutical compositions thereof for the treatment of coronary insufficiencies, cardiac failure, blood circulatory disturbances and occlusive diseases. The new pyrrolobenzimidazoles are of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkenyl or cycloalkyl, R.sub.2 is hydrogen, alkyl, alkenyl, cyano or a substituted carbonyl or R.sub.1 and R.sub.2 together represent cycloalkylene or form alkylidene or cycloalkylidene, X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene, T is oxygen or sulphur and Py is pyridyl or substituted pyridyl and including the tautomers thereof and the physiologically acceptable salts thereof.
摘要翻译：吡咯并苯并咪唑，其制备方法及其药物组合物，用于治疗冠状动脉不全，心力衰竭，血液循环障碍和闭塞性疾病。新的吡咯并苯并咪唑具有下式（Ⅰ）其中R1是氢，烷基，烯基或环烷基，R2是氢，烷基，烯基，氰基或取代的羰基，或者R1和R2一起代表亚环烷基或亚烷基或亚环烷基， X是价键，C1-C4亚烷基或亚乙烯基，T是氧或硫，Py是吡啶基或取代的吡啶基，并包括其互变异构体及其生理上可接受的盐。

6. 发明授权

US4710510A Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of them to treat certain heart and circulatory diseases 失效
标题翻译：吡咯并苯并咪唑，含有它们的药物组合物，以及它们用于治疗某些心脏和循环系统疾病
公开(公告)号：US4710510A
公开(公告)日：1987-12-01
申请号：US807260
申请日：1985-12-10
申请人： Alfred Mertens , Jens-Peter Holck , Wolfgang Kampe , Bernd Muller-Beckmann , Klaus Strein , Wolfgang Schaumann
发明人： Alfred Mertens , Jens-Peter Holck , Wolfgang Kampe , Bernd Muller-Beckmann , Klaus Strein , Wolfgang Schaumann
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , A61P9/04 , C07D209/34 , C07D209/42 , C07D487/04 , A61K31/55
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42
摘要： The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, each represent a hydrogen atom or an alkanesulphonyloxy, trifluoromethanesulphonyloxy, alkanesulphonylamino, trifluoromethanesulphonylamino, N-alkyl-alkanesulphonylamino, N-alkyl-trifluoromethanesulphonylamino, alkylsulphenylmethyl, alkylsulphinylmethyl or alkylsulphonylmethyl radical, a carbonyl group substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino, a sulphonyl group substituted by amino, alkylamino, dialkylamino or cyclic imino, whereby a methylene group in the 4-position can be replaced by a sulphur or oxygen atom, an alkylcarbonylamino, aminocarbonylamino or alkylaminocarbonylamino radical, an alkylthio, alkylsulphinyl or alkylsulphonyl radical, a nitro, halogen, amino, hydroxyl, alkyl, trifluoromethyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, dialkylamino, 1-imidazolyl or cyano group; X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinyl radical; and T is an oxygen or sulphur atom; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
摘要翻译：本发明提供了以下通式的新的吡咯并苯并咪唑：其中R 1是氢原子或烷基，烯基或环烷基; R2是氢原子，氰基或烷基或烯基或被羟基，烷基，烷氧基，氨基，烷基氨基，二烷基氨基或肼基取代的羰基或与R1一起形成亚环烷基，或者R 1和R 2一起形成亚烷基或亚环烷基激进; 可以相同或不同的R 3，R 4和R 5各自表示氢原子或烷磺酰氧基，三氟甲磺酰氧基，烷磺酰氨基，三氟甲磺酰氨基，N-烷基 - 烷磺酰氨基，N-烷基 - 三氟甲磺酰氨基，烷基亚磺酰基甲基，烷基亚磺酰基甲基或烷基磺酰基甲基，羰基被羟基，烷氧基，氨基，烷基氨基或二烷基氨基取代的基团，被氨基，烷基氨基，二烷基氨基或环状亚氨基取代的磺酰基，其中4-位中的亚甲基可以被硫或氧原子，烷基羰基氨基，氨基羰基氨基或烷基氨基羰基氨基，烷硫基，烷基亚磺酰基或烷基磺酰基，硝基，卤素，氨基，羟基，烷基，三氟甲基，烷氧基，烯氧基，炔氧基，氰基烷氧基，羧基烷氧基，烷氧基羰基烷氧基，二烷基氨基，1-咪唑基或氰基; X是价键，C1-C4亚烷基或乙烯基; 和T是氧或硫原子; 其互变异构体及其与无机和有机酸的生理上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物用于预防和治疗心脏和循环系统疾病。

7. 发明授权

US4612313A Pharmaceutical phenylacetonitrile derivatives 失效
标题翻译：药用苯乙腈衍生物
公开(公告)号：US4612313A
公开(公告)日：1986-09-16
申请号：US774354
申请日：1985-09-10
申请人： Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
发明人： Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
IPC分类号： A61K31/21 , A61K31/275 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , C07C67/00 , C07C253/00 , C07C255/24 , C07C255/32 , C07C255/42 , C07C255/43 , C07C255/53 , C07C255/58 , C07C255/59 , C07D207/08 , C07D211/22 , C07D241/04 , C07D295/16 , C07D295/18 , A61K31/495 , C07C121/80
CPC分类号： C07C255/00 , C07D211/22
摘要： The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.7 is a hydrogen atom or a straight-chained or branched, saturated alkyl radical containing up to 6 carbon atoms, m and n, which can be the same or different, are 2 or 3, p is 1 or 2 and X is a straight-chained, cyclic or branched alkyl radical containing 2 to 10 carbon atoms which is optionally substituted by an amino group or is a grouping of the general formula: ##STR3## wherein Y and Z, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 8 carbon atoms or cycloalkyl, alkylcycloalkyl or cycloalkylalkyl radicals, in which these radicals are optionally interrupted by an oxygen or sulphur atom, and one of the groups Z in general formula II can also be a hydrogen atom or both Z groups are joined to form a ring containing 4 to 6 carbon atoms which is optionally interrupted by a further nitrogen atom which can be substituted by alkyl or alkanoyl, the --O--NO.sub.2 groups being substituents of Y as well as of Z; as well as the salts thereof with physiologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的苯乙腈衍生物：其中R 1，R 2，R 3，R 4和R 5可以相同或不同，为氢或卤素原子或烷基，烷氧基，硝基，氨基或酰基氨基和两个相邻的取代基可以一起形成亚甲二氧基或亚乙二氧基，A是下列通式的基团：其中R 6是含有2至12个直链的直链，环状或支链的饱和或不饱和烷基碳原子，R7是氢原子或含有至多6个碳原子的直链或支链饱和烷基，m和n可相同或不同，为2或3，p为1或2，X为是含有2至10个碳原子的直链，环状或支链烷基，其任选被氨基取代，或者是通式如下的基团：其中Y和Z可以相同或不同，是直链或支链烷基基团引入多达8个碳原子或环烷基，烷基环烷基或环烷基烷基，其中这些基团任选地被氧或硫原子中断，通式II中的基团Z之一也可以是氢原子或两个Z基团连接形成含有4至6个碳原子的环，其任选被可被烷基或烷酰基取代的另外的氮原子中断，-O-NO 2基团是Y和Z的取代基; 以及其与生理上可接受的酸的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

8. 发明授权

US4721717A .alpha.-(aminoalkylaminomethyl)phenylmethanols, composition containing them, and use thereof to treat certain heart and circulatory diseases 失效
标题翻译： α-（氨基烷基氨基甲基）苯基甲醇，含有它们的组合物及其用于治疗某些心脏和循环系统疾病的用途
公开(公告)号：US4721717A
公开(公告)日：1988-01-26
申请号：US760128
申请日：1985-07-29
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Erwin Bohm , Klaus Strein
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Erwin Bohm , Klaus Strein
IPC分类号： A61K31/135 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P9/00 , C07C67/00 , C07C213/00 , C07C213/04 , C07C215/30 , C07C215/60 , C07C301/00 , C07C303/40 , C07C311/08 , C07C313/00 , C07C315/04 , C07C317/32 , C07C317/36 , C07C317/48 , C07D209/30 , C07D231/38 , C07D231/56 , C07D235/04 , C07D239/54 , C07D235/30 , C07D239/10
CPC分类号： C07D231/38 , C07D231/56
摘要： The present invention provides aminoalcohols of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be same or different, are hydrogen atoms, hydroxyl groups, C.sub.1 -C.sub.4 -alkoxy, benzyloxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkanesulphonylamino, C.sub.1 -C.sub.4 -alkanesulphinyl or C.sub.1 -C.sub.4 -alkanesulphonyl radicals, m is 2, 3 or 4, X and Y, which can be the same or different, are hydrogen atoms or benzyl radicals and R.sub.3 is a phenyl radical substituted twice by C.sub.1 -C.sub.6 -alkyl radicals, a nitrophenyl radical, an aminophenyl radical, a 1,3,5-tri-C.sub.1 -C.sub.6 -alkyl-2,4-dioxo-1H,3H-pyrimidin-6-yl radical, an indolyl radical, an indazolyl radical, a benzimidazolyl radical, a 1,4-di-C.sub.1 -C.sub.6 -alkylpyrazol-5-yl radical or a radical of the general formula: ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different, are C.sub.1 -C.sub.4 -alkyl radicals and R.sub.6 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, phenyl or benzyl radical; and the pharmacologically acceptable salts there, as well as methods for making and using these compounds and compositions containing them. There are useful as cardiovascular medicaments.
摘要翻译：本发明提供以下通式的氨基醇：其中R 1和R 2可以相同或不同，为氢原子，羟基，C 1 -C 4 - 烷氧基，苄氧基，C 1 -C 4 - 烷氧基羰基，C 1 C 1-4烷基磺酰基氨基，C 1 -C 4烷基亚磺酰基或C 1 -C 4烷基磺酰基，m为2,3或4，X和Y可相同或不同，为氢原子或苄基，R 3为苯基由C 1 -C 6烷基取代两次，硝基苯基，氨基苯基，1,3,5-三-C1- C6-烷基-2,4-二氧代-1H，3H-嘧啶-6-基，吲哚基，吲唑基，苯并咪唑基，1,4-二-C1- C6烷基吡唑-5-基或通式如下的基团：其中R4和R5可以是 C 1 -C 4 - 烷基，R 6是C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，苯基或苄基; 和其中的药理学上可接受的盐，以及制备和使用这些化合物和含有它们的组合物的方法。有用的心血管药物。

9. 发明授权

US4826847A Beta-blocking oxindole derivatives 失效
标题翻译： β-阻断羟吲哚衍生物
公开(公告)号：US4826847A
公开(公告)日：1989-05-02
申请号：US948422
申请日：1986-12-30
申请人： Helmut Michel , Wolfgang Kampe , Klaus Strein , Wolfgang Bartsch
发明人： Helmut Michel , Wolfgang Kampe , Klaus Strein , Wolfgang Bartsch
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/02 , C07D209/34 , C07D209/96 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , A61K31/505
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06
摘要： The present invention provides oxindole derivatives of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The above compounds display nitrate-like as well as .beta.-blocking actions.
摘要翻译：本发明提供下式的羟吲哚衍生物：其中各种取代基在下文定义。上述化合物显示硝酸盐样和β-阻断作用。

10. 发明授权

US4608383A Cardioactive pyrazole and imidazole aryloxypropanolamines 失效
公开(公告)号：US4608383A
公开(公告)日：1986-08-26
申请号：US538693
申请日：1983-10-03
申请人： Fritz Wiedemann, deceased , Wolfgang Kampe , Karl Dietmann, deceased , Gisbert Sponer
发明人： Fritz Wiedemann, deceased , Wolfgang Kampe , Karl Dietmann, deceased , Gisbert Sponer
IPC分类号： A61K31/38 , A61K31/045 , A61K31/135 , A61K31/138 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/00 , A61P9/04 , C07C217/32 , C07C217/72 , C07C217/78 , C07C219/06 , C07C219/08 , C07C219/14 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/46 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/54 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D241/44 , C07D249/18 , C07D333/36 , C07D473/16 , C07D473/32 , C07D473/34 , C07D487/00 , C07D487/04 , C07D231/54 , C07D233/48 , C07D233/88
CPC分类号： C07D473/16 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D333/36 , C07D473/34 , C07D487/04
摘要： The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, which may be the same or different, are mono- or divalent substituents selected from hydrogen, halogen, notro, hydraxylamino, amino, lower acylamino, lower alkylamino, di-(lower alkyl)-amino, hydroxyethylamino, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acylaminomethyl, halomethyl, aminomethyl, lower acylaminomethyl, di(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acyaminomethyl, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-hydroxyethyl, phenyl lower alkyl and phenyl, the phenyl radicals being optionally substituted with 1 or 2 hydroxyl or methoxy radicals, or from oxygen or sulphur; the optically-active forms and the racemic mixtures thereof, and the pharmacologically compatible salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. These compounds are useful for the prophylaxis and combatting of cardiac and circulatory diseases.

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