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    Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of them to treat certain heart and circulatory diseases
    4.
    发明授权
    Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of them to treat certain heart and circulatory diseases 失效
    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。

    Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases
    5.
    发明授权
    Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases 失效
    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。

    Heterocyclic-substituted indoles and pharmaceutical compositions containing them
    7.
    发明授权
    Heterocyclic-substituted indoles and pharmaceutical compositions containing them 失效
    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。

    Pyridazinone derivatives, and pharmaceutical compositions containing them
    8.
    发明授权
    Pyridazinone derivatives, and pharmaceutical compositions containing them 失效
    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。

    Tricyclic benzotriazoles, processes for the preparation thereof and pharmaceutical compositions containing them
    9.
    发明授权
    Tricyclic benzotriazoles, processes for the preparation thereof and pharmaceutical compositions containing them 失效
    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。