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1. 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。

2. 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.

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

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。

5. 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。

6. 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。

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

US4146630A Blood pressure lowering and adrenergic .beta.-receptor inhibiting 3-(4-phenoxymethylpiperidino)-propyl-phenyl ethers 失效
标题翻译：血压降低和ADRENERGIC“ - 抑制3-（4-苯甲酰氨基哌啶）丙基苯基醚
公开(公告)号：US4146630A
公开(公告)日：1979-03-27
申请号：US846057
申请日：1977-10-27
申请人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
发明人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07D401/12 , A61K31/403 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D209/90 , C07D211/22 , C07D231/56
CPC分类号： C07D211/22 , C07D231/56
摘要： A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.

9. 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.

10. 发明授权

US4468520A 3-Cyano-indoles as cardioselective agents 失效
标题翻译： 3-氰基 - 吲哚作为心脏选择剂
公开(公告)号：US4468520A
公开(公告)日：1984-08-28
申请号：US288075
申请日：1981-07-29
申请人： Helmut Michel , Wolfgang Kampe , Roland Ofenloch , Karl Dietmann , Gisbert Sponer
发明人： Helmut Michel , Wolfgang Kampe , Roland Ofenloch , Karl Dietmann , Gisbert Sponer
IPC分类号： C07D209/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , C07D209/08 , C07D209/42 , C07D209/43 , C07D209/04
CPC分类号： C07D209/08
摘要： The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for the prophylaxis and treatment of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的氨基丙醇衍生物：其中R1是氢原子或低级烷酰基或芳酰基，R2是低级烷基或通式如下的基团：其中 X是价键，亚甲基或氧或硫原子，Ar是单环，碳或杂环芳基，R6和R7可以相同或不同，是氢原子或低级烷基，R8和 R9可相同或不同，为氢或卤原子，羟基，低级烷酰基，烯基，炔基，烷基，低级烷氧基，芳烷氧基，烯氧基，炔氧基，低级烷硫基，氨基羰基自由基，氨基磺酰基或酰氨基; 或R 2为1,4-苯并二恶烷-2-基甲基，R'2为氢原子或苄基，R 3为羧基或低级烷氧基羰基，氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基 R4是氢原子或低级烷基或-CH2-O-R1基，R1具有与上述相同的含义，R 5是氢原子或低级烷基; 其任选活性形式和外消旋物及其药理学上可接受的盐。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组合物。此外，本发明涉及这些化合物用于预防和治疗心脏和循环系统疾病的用途。

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