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1. 发明授权

US5373019A Pharmaceutical lactam compositions for inhibition of erythrocyte and thrombocyte aggregation 失效
标题翻译：用于抑制红细胞和血小板聚集的药物内酰胺组合物
公开(公告)号：US5373019A
公开(公告)日：1994-12-13
申请号：US640445
申请日：1991-01-11
申请人： Harald Zilch , Alfred Mertens , Wolfgang Von Der Saal , Erwin Boehm , Klaus Strein
发明人： Harald Zilch , Alfred Mertens , Wolfgang Von Der Saal , Erwin Boehm , Klaus Strein
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P7/02 , C07D209/34 , C07D209/54 , C07D215/38 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , B07D209/30 , B07D209/32 , B07D209/34
CPC分类号： C07D209/34 , C07D209/54 , C07D215/38 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides compounds and pharmaceutical compositions containing indolones of the general formula: ##STR1## These indolones where n.dbd.o and the pharmaceutical compositions containing these compounds are used for the treatment of diseases in which erythrocyte and thrombocyte aggregation play an important part, especially for the inhibition of aggregation of these cells.
摘要翻译：本发明提供含有以下通式的吲哚酮的化合物和药物组合物：其中n = 0的这些吲哚酮和含有这些化合物的药物组合物用于治疗其中红细胞和血小板聚集起重要作用的疾病特别是抑制这些细胞聚集的部分。

2. 发明授权

US4954498A Tricyclic benzimidazole compounds, pharmaceutical compositions and methods of use 失效
标题翻译：三环苯并咪唑化合物，药物组合物和使用方法
公开(公告)号：US4954498A
公开(公告)日：1990-09-04
申请号：US144514
申请日：1988-01-15
申请人： Alfred Mertens , Wolfgang von der Saal , Erwin Boehm , Klaus Strein
发明人： Alfred Mertens , Wolfgang von der Saal , Erwin Boehm , Klaus Strein
IPC分类号： A61K31/47 , A61K31/495 , A61P7/02 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： The present invention provides tricyclic benzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or diferent as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.
摘要翻译：本发明提供下式的三环苯并咪唑：其中R 1是下列通式的苯基：其中R 2，R 3和R 4可以与权利要求1中相同或不同。对于A，B，C和D，理解为A，B，C或D中的一个或两个为氮的化合物。这些化合物可用于抑制凝血细胞和红细胞的聚集，降低血压并可增加心脏的功能。

3. 发明授权

US5116843A Tricyclic benzimidazole compounds, pharmaceutical compositions and methods of use 失效
标题翻译：三聚苯并咪唑化合物，药物组合物及其使用方法
公开(公告)号：US5116843A
公开(公告)日：1992-05-26
申请号：US543350
申请日：1990-06-25
申请人： Alfred Mertens , Wolfgang von der Saal , Erwin Boehm , Klaus Strein
发明人： Alfred Mertens , Wolfgang von der Saal , Erwin Boehm , Klaus Strein
IPC分类号： A61K31/47 , A61K31/495 , A61P7/02 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： The present invention provides tricyclic benzimidazoles of the formula ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or different as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.

4. 发明授权

US4985448A Ureidoindoles, pharmaceutical compositions and methods for erythrocyte and thrombocyte aggregation inhibition 失效
标题翻译：脲基吲哚，用于红细胞和血小板聚集抑制的药物组合物和方法
公开(公告)号：US4985448A
公开(公告)日：1991-01-15
申请号：US307417
申请日：1989-02-06
申请人： Harald Zilch , Alfred Mertens , Wolfgang Von Der Saal , Erwin Boehm , Klaus Strein
发明人： Harald Zilch , Alfred Mertens , Wolfgang Von Der Saal , Erwin Boehm , Klaus Strein
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P7/02 , C07D209/34 , C07D209/54 , C07D215/38 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D209/34 , C07D209/54 , C07D215/38 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Lactam compounds of the formula ##STR1## in which: R is hydrogen, alkyl or cycloalkyl;R.sup.1 is hydrogen, alkyl, alkenyl or cycloalkyl;R.sup.2 is alkyl, alkenyl, cyano or a carbonyl substituted hydroxyl, alkyl, alkoxy, amino, alkylamino or hydrazino; orR.sup.1 and R.sup.2 together represent alkylidene cycloalkylidene; orR.sup.1, R.sup.2 and the adjacent carbon atom form a spirocyclic ring;n is 0 or 1;A is a --Co--NH--, --NH--CO--NH-- or --O--CO--NH--;X is a valency bond, alkylene or alkenylene; andR.sup.3 is optionally substituted phenyl, pyridyl, methylenedioxyphenyl or a five-membered heterocycle; or when X is a valency bond, R.sup.3 can also be an optionally substituted alkyl or alkino group, or cycloalkyl. The compounds are useful for the inhibition of erythrocyte and thrombocyte aggregation.
摘要翻译：式（I）的内酰胺化合物，其中：R为氢，烷基或环烷基; R1是氢，烷基，烯基或环烷基; R2是烷基，烯基，氰基或羰基取代的羟基，烷基，烷氧基，氨基，烷基氨基或肼基; 或者R1和R2一起表示亚烷基亚环烷基; 或R 1，R 2和相邻碳原子形成螺环; n为0或1; A是-Co-NH-，-NH-CO-NH-或-O-CO-NH-; X是价键，亚烷基或亚烯基; 并且R 3是任选取代的苯基，吡啶基，亚甲二氧基苯基或五元杂环; 或当X是价键时，R 3也可以是任选取代的烷基或烷基或环烷基。该化合物可用于抑制红细胞和血小板聚集。

5. 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。

6. 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。

7. 发明授权

US4863945A Pyrrolobenzimidazoles and pharmaceutical compositions containing them 失效
标题翻译：吡咯并苯并咪唑和含有它们的药物组合物
公开(公告)号：US4863945A
公开(公告)日：1989-09-05
申请号：US131367
申请日：1987-12-10
申请人： Walter-Gunar Friebe , Alfred Mertens , Klaus Strein , Erwin Boehm
发明人： Walter-Gunar Friebe , Alfred Mertens , Klaus Strein , Erwin Boehm
IPC分类号： A61K31/40 , A61P7/02 , A61P9/04 , A61P9/12 , C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.
摘要翻译：下式的吡咯并苯并咪唑：可用于治疗心脏和循环系统疾病。 R1是取代的苯基; 或任选取代的萘基或可与苯环缩合形成双环基团的五元或六元杂环基。 R2是氢，烷基，烯基或环烯基; R3是烷基，烯基或羟基烷基或与R2一起形成亚环烷基; 或者R 2和R 3一起形成亚烷基或亚环烷基。 R4是氢或低级烷酰基。 X是价键，亚烷基，亚乙烯基，亚氨基或羰基氨基。 T代表两个氢原子。当X是价键时，R 1也可以是氢，也可以含有氧，氨基，硫，羰基和磺酰基的烃基。当X是亚氨基或羰基氨基时，或当R1是双环基时，T也可以是氧。化合物还包括与无机和有机酸形成的互变异构体和生理上可接受的盐。

8. 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.

9. 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。

10. 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。

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