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1. 发明授权

US4695567A Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using 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和使用它们治疗某些心脏和循环系统疾病的方法
公开(公告)号：US4695567A
公开(公告)日：1987-09-22
申请号：US820259
申请日：1986-01-17
申请人： Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
发明人： Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/50 , A61K31/505 , A61P9/00 , A61P9/04 , C07D403/12 , C07D405/12 , C07D487/04 , C07D403/06
CPC分类号： C07D403/12 , C07D405/12 , C07D487/04
摘要： The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要翻译：本发明提供了以下通式的吡咯并苯并咪唑或其互变异构体：其中R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 7环烷基; R2是氢，氰基，C1-C6烷基，C2-C6烯基或被羟基，C1-C6烷基，C1-C6烷氧基，氨基，C1-C6烷基氨基，C2-C12二烷基氨基或肼基取代的羰基或R2 并且R 1与它们所连接的碳一起形成C 3 -C 8螺环烷基环，或者R 1和R 2一起形成C 3 -C 7亚烷基或C 3 -C 7环烷基，X是价键，C 1 -C 4亚烷基或亚乙烯基，T是氧或硫; 并且Het是呋喃基，噻吩基，吡咯基，吡唑基，咪唑基，恶唑基，噻唑基，三唑基，恶二唑基，噻二唑基，吡嗪基，嘧啶基或哒嗪基，其中杂环五元和六元环是未取代的或被一个或多个C 1 -C 6烷基 C 1 -C 6烷氧基，C 1 -C 6烷硫基，羟基，氧代，硝基，氨基，卤素，羧基，C 2 -C 7烷氧基羰基，氨基羰基或氰基; 或其生理上可接受的盐与无机或有机酸反应。这些化合物可用于治疗心脏或循环系统疾病，特别是那些响应血压变化，心输出量增加和/或微循环变化的化合物。

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

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

US4835280A Indoline compounds for synthesis of pharmaceutically active pyrrolobenzimidazoles 失效
标题翻译：用于合成药物活性吡咯并苯并咪唑的二氢吲哚化合物
公开(公告)号：US4835280A
公开(公告)日：1989-05-30
申请号：US72917
申请日：1987-07-14
申请人： Alfred Martens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckman , Klaus Strein , Egon Roesch
发明人： Alfred Martens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckman , Klaus Strein , Egon Roesch
IPC分类号： C07D403/12 , C07D405/12 , C07D487/04
CPC分类号： C07D403/12 , C07D405/12 , C07D487/04
摘要： The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要翻译：本发明提供下式的吲哚衍生物：下式的有用的药物活性吡咯并苯并咪唑或其互变异构体：（I）这些化合物可用于治疗心脏或循环系统疾病，特别是那些对血压变化作出反应，心输出量增加和/或微循环变化的疾病。

7. 发明授权

US4831032A Cardiotonic benzimidazoles 失效
标题翻译：强心苯并咪唑
公开(公告)号：US4831032A
公开(公告)日：1989-05-16
申请号：US881983
申请日：1986-07-03
申请人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
发明人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P9/04 , A61P9/12 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/58 , C07D277/62 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D263/58 , C07D413/12 , C07D417/12 , C07D487/04 , C07D513/04
摘要： The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
摘要翻译：本发明提供以下通式的苯并咪唑：其中R1，X，A和R2如说明书中所定义。本发明还提供制备这些新的苯并咪唑和含有它们的药物组合物的方法，以及制备它们的中间体。新的苯并咪唑可用于治疗对降低血压，正性肌力作用和/或微循环改善作出反应的心脏或循环系统疾病。

8. 发明授权

US4874756A Benzodipyrroles, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：苯并二吡咯，其制备方法和含有它们的药物组合物
公开(公告)号：US4874756A
公开(公告)日：1989-10-17
申请号：US902182
申请日：1986-08-29
申请人： Alfred Mertens , Wolfgang von der Saal , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
发明人： Alfred Mertens , Wolfgang von der Saal , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： A61K31/40 , A61K31/415 , A61K31/44 , A61K31/50 , A61P9/00 , C07D209/34 , C07D487/04
CPC分类号： C07D487/04 , C07D209/34
摘要： The present invention provides compounds of the general formula ##STR1## wherein the variables are as defined herein. The present invention also provides processes for the preparation thereof, pharmaceutical compositions containing them and intermediates for the preparation thereof.
摘要翻译：本发明提供了通式（I）（I）的化合物，其中变量如本文所定义。本发明还提供其制备方法，含有它们的药物组合物和其制备中间体。

9. 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。

10. 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。

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