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1. 发明授权

US4981864A Method for inhibition of erythrocyte aggregation using anellated tricyclic compounds 失效
标题翻译：使用安定的三环化合物抑制红细胞聚集的方法
公开(公告)号：US4981864A
公开(公告)日：1991-01-01
申请号：US278190
申请日：1988-11-30
申请人： Wolfgang von der Saal , Alfred Mertens , Jens-Peter Hoelck , Erwin Boehm , Ulrich Martin
发明人： Wolfgang von der Saal , Alfred Mertens , Jens-Peter Hoelck , Erwin Boehm , Ulrich Martin
IPC分类号： C07D487/04 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/50 , A61P1/04 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/02 , A61P29/00 , A61P35/00 , C07D498/04 , C07D513/04
CPC分类号： A61K31/44 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/50
摘要： The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## or R.sub.1 is a 5 or 6 membered heterocycle or when X is a valency bond R.sub.1 is also H, OH, mercapto, amino, alkyl, alkenyl, alkynyl, haloalkyl, alkylthio, formylaminoalkyl, pyridylcarbonylamino, cycloalkyl, or cycloalkenyl, alkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl or hydroxyalkyl of claim 1 or 2 for the preparation of pharmaceutical compositions with an erythrocyte aggregation inhibition action useful, for example, in states of shock or circulatory disturbance.
摘要翻译：本发明涉及以下通式的化合物的用途：其中R 1为下列通式的苯基或其中R 1为5或6元杂环，或当X为化合价时键R1也是权利要求1或2的H，OH，巯基，氨基，烷基，烯基，炔基，卤代烷基，烷硫基，甲酰基氨基烷基，吡啶基羰基氨基，环烷基或环烯基，烷氧基烷基，羧基烷基，烷氧基羰基烷基或羟烷基，用于制备具有红细胞聚集抑制作用可用于例如休克或循环障碍的状态。

2. 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。

3. 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。

4. 发明授权

US5135949A Pharmaceutical compositions containing phenylamides 失效
标题翻译：含有苯甲酸的药物组合物
公开(公告)号：US5135949A
公开(公告)日：1992-08-04
申请号：US402185
申请日：1989-09-05
申请人： Wolfgang von der Saal , Alfred Mertens , Harald Zilch , Erwin Boehm
发明人： Wolfgang von der Saal , Alfred Mertens , Harald Zilch , Erwin Boehm
IPC分类号： A61K31/165 , A61K31/275 , A61K31/357 , A61K31/36 , A61P7/00 , A61P9/00 , A61P9/12 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/76 , C07C233/80 , C07C233/81 , C07C235/22 , C07C235/38 , C07C235/56 , C07C237/22 , C07C237/30 , C07C237/40 , C07C255/40 , C07C255/41 , C07C255/42 , C07C255/46 , C07C255/60 , C07C309/66 , C07C311/05 , C07C311/06 , C07C311/09 , C07C317/40 , C07C317/44 , C07C323/42 , C07C323/44 , C07C323/62 , C07D213/65 , C07D317/66
CPC分类号： C07C309/66 , A61K31/165 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/80 , C07C235/22 , C07C235/38 , C07C235/56 , C07C237/22 , C07C237/40 , C07C255/41 , C07C255/46 , C07C255/60 , C07C323/42 , C07D213/65 , C07D317/66 , C07C2101/14 , Y10S514/822
摘要： Pharmaceutical compositions for inhibiting the aggregation of erthyrocytes or thrombocytes which include phenylamides which conform to the formula: ##STR1## with R.sub.1-6, X, A and B being as defined. Processes for the preparation of novel phenylamides coming within the above formula are also discussed.
摘要翻译：用于抑制红细胞或血栓细胞聚集的药物组合物，其包括符合下式的苯酰胺：R1-6，X，A和B的定义如下。还讨论了在上述配方中制备新型苯酰胺的方法。

5. 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.

6. 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。

7. 发明授权

US4851406A Heterocyclic-substituted indoles and pharmaceutical compositions containing them 失效
标题翻译：杂环取代的吲哚和含有它们的药物组合物
公开(公告)号：US4851406A
公开(公告)日：1989-07-25
申请号：US904092
申请日：1986-09-04
申请人： Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： C07D409/14 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/50 , A61K31/53 , A61K31/535 , A61P9/00 , C07D237/00 , C07D333/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14
摘要： The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.2 is ##STR2## 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 pharmaceutical compositions containing them.Furthermore, the present invention provides intermediates of the general formula: ##STR3## in which R.sub.1, R.sub.2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
摘要翻译：本发明提供以下通式的吲哚衍生物：其中R 1是氢原子或烷基，烯基，环烷基，环烯基，羧基，氰基，烷基羰基，烷氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基或芳基， R2是氢原子或烷基，三卤代甲基，羟基，环烷基，氰基，羧基，烷氧基羰基，烷基羰基，氨基羰基，烷基氨基羰基或二烷基氨基羰基; R2是含有1至4个杂原子的杂环五元环或含有1至5个杂原子的杂环六元环，五元和六元环的杂原子相同或不同，为氮，氧或硫，一个或多个氮原子任选地带有氧原子，所述五元和六元环任选被一个或多个烷基，烷氧基，烷硫基，氧代，羟基，硝基，氨基，卤素或氰基取代; 或者R2是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组合物。此外，本发明提供通式如下的中间体：其中R1，R2，A和X具有与上述相同的含义，以及制备这些中间体的方法。

8. 发明授权

US4847251A Pyridazinone derivatives, and pharmaceutical compositions containing them 失效
标题翻译：哒嗪酮衍生物和含有它们的药物组合物
公开(公告)号：US4847251A
公开(公告)日：1989-07-11
申请号：US80998
申请日：1987-08-03
申请人： Alfred Mertens , Wolfgang Von Der Saal , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Alfred Mertens , Wolfgang Von Der Saal , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： A61K31/50 , A61K31/53 , A61K31/535 , A61P1/10 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/14
摘要： The present invention provides pyridazinone derivatives of the general formula: ##STR1## wherein Het is a mono- or bicyclic heterocycle with one or two nitrogen atoms, B-C is a --CHR.sub.1 --CH.sub.2 --, --CR.sub.1 .dbd.CH--, --CHR.sub.1 --O--, --O--CHR.sub.1 --, --CHR.sub.1 --NH-- or --NH--CHR.sub.1 -- group, R.sub.1 being a hydrogen atom or an alkyl radical, and A is an amiono, alkylcarbonylamino, aminocarbonylamino, aminothiocarbonylamino, alkylaminothiocarbonylamino, alkylamionocarbonylamino, N'-cyanoguanidino or N'-cyano-N"-alkylguanidino group, a substituted phenyl ring or heterocycle attached via a nitrogen or sulphur atom, or a mono- or bicyclic substituted heterocycle with 1 to 3 nitrogen atoms, one ring nitrogen atom being directly attached to Het; as well as the physiologically acceptable salts thereof.The present invention also provides processes for the preparation of these pyridazinone drivatives and pharmaceutical compositions containing them for the treatment of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的哒嗪酮衍生物：其中Het是具有一个或两个氮原子的单环或双环杂环，BC是-CHR 1 -CH 2 - ，-CR 1 = CH-，-CHR 1 -O-，-O-CHR 1 - ， - CHR 1 -NH-或-NH-CHR 1 - 基，R 1为氢原子或烷基，A为酰胺基，烷基羰基氨基，氨基羰基氨基，氨基硫代羰基氨基，烷基氨基硫代羰基氨基，烷基氨基羰基氨基，N “氰基胍基”或“氰基-N” - 烷基胍基，经氮或硫原子连接的取代苯环或杂环，或具有1至3个氮原子的单环或双环取代杂环，一个环氮原子为直接附于Het; 以及其生理上可接受的盐。本发明还提供了制备这些哒嗪酮驱动剂和含有它们用于治疗心脏和循环系统疾病的药物组合物的方法。

9. 发明授权

US4835167A Tricyclic benzotriazoles, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：三环苯并三唑，其制备方法和含有它们的药物组合物
公开(公告)号：US4835167A
公开(公告)日：1989-05-30
申请号：US80658
申请日：1987-08-03
申请人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： C07D487/04 , C07D487/10 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D487/10 , C07D513/04
摘要： The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these tricyclic benzotriazoles and pharmaceutical compositions containing them for the treatment of heart and circulatory diseases.
摘要翻译：本发明提供了新的具有以下通式的三环苯并三唑：其中Z是氢原子或酰基，Y是氧或硫原子或两个氢原子，X是氧或硫原子或 > CR1R2或> NR3基团，R1是氢原子或烷基，烯基或环烷基，R2是氢原子或烷基，烯基或氰基或被羟基，烷基，烷氧基，氨基，烷基氨基取代的羰基，二烷基氨基或肼基或R 2与R 1一起代表亚环烷基或R 1和R 2一起形成亚烷基或亚环烷基，R 3为氢原子或烷基; 其互变异构体及其与无机和有机酸的生理上可接受的酸加成盐。本发明还提供了制备这些三环苯并三唑的方法和含有它们用于治疗心脏和循环系统疾病的药物组合物。

10. 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。

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