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18 条记录 (耗时 0.04 秒)

    Heterocyclic substituted indolinones
    2.
    发明授权
    Heterocyclic substituted indolinones 失效
    杂环取代的二氢吲哚酮

    公开(公告)号：US4870077A

    公开(公告)日：1989-09-26

    申请号：US94871

    申请日：1987-09-10

    申请人： Wolfgang Von Der Saal ,  Walter-Gunar Friebe ,  Alfred Mertens ,  Bernd Muller-Beckmann ,  Lothar Kling

    发明人： Wolfgang Von Der Saal ,  Walter-Gunar Friebe ,  Alfred Mertens ,  Bernd Muller-Beckmann ,  Lothar Kling

    IPC分类号： A61K31/50 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  C07D209/34 ,  C07D209/46 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D403/04 ,  C07D209/34 ,  C07D413/04 ,  C07D417/04

    摘要： Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.6 independently being hydrogen atoms or alkyl radicals wherein the alkyl groups independently contain 1 to 6 carbon atoms; as well as the tautomers thereof and the physiologically acceptable salt thereof and the physiologically acceptable salts thereof with inorganic and organic acids, are disclosed, such as, for instance, the compound 5-(2,3,4,5-tetrahydro-3-oxopyridazin-6-yl)-3-ethoxycarbonyl-3-methyl-1H-indol n-2-one. The compounds of the invention are useful in the treatment of heart and circulatory diseases, for example, by producing a positive inotropic action in a patient to whom the compounds are administered.

    摘要翻译： 式（I）的杂环取代的二氢吲哚酮：其中R 1是氢原子或烷基或羟烷基，R 2是羧基或烷氧羰基，羟基烷基或烷基羰基氧基烷基或R 1和R 2与碳 它们连接的原子形成具有4,5或6个环原子的内酯，AB是-CH 2 -CH（R 3） - ， - CH = CR 3 - ， - CH 2 -NH-，-NH-CH 2 - ， - CH 2 -O-，-O-CH 2 - ， - CH 2 -S-或-S-CH 2 - 基，R 3是氢原子或烷基或羟烷基，或A是价键，B是亚甲基。 或亚氨基基团R4，R5和R6独立地为氢原子或烷基，其中烷基独立地含有1至6个碳原子; 以及其与无机和有机酸的互变异构体及其生理上可接受的盐及其生理上可接受的盐，例如化合物5-（2,3,4,5-四氢-3- 氧基哒嗪-6-基）-3-乙氧基羰基-3-甲基-1H-吲哚-2-酮。 本发明的化合物可用于治疗心脏和循环系统疾病，例如通过在施用化合物的患者中产生正性肌力作用。

    Heterocyclic-substituted indoles and pharmaceutical compositions containing them
    5.
    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
    6.
    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
    7.
    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。