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39 条记录 (耗时 0.026 秒)

    Heterocyclic-substituted indoles and pharmaceutical compositions containing them
    12.
    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
    13.
    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
    14.
    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。

    Flue housing for a coke oven
    16.
    发明授权
    Flue housing for a coke oven 失效
    焦炉烟道

    公开(公告)号：US4361468A

    公开(公告)日：1982-11-30

    申请号：US177992

    申请日：1980-08-15

    申请人： Alfred Mertens ,  Franz Schafer

    发明人： Alfred Mertens ,  Franz Schafer

    IPC分类号： C10B29/00 ,  C10B21/16 ,  C10B21/10 ,  C10B21/14

    CPC分类号： C10B21/16

    摘要： A regulating device for the flue housing of a coke oven for alternately opening and closing channels of the flue housing including a rotatable shaft, frames mounted on the shaft, preferably, 90.degree. relative to each other, in alternating sequence along the shaft, peripheral seals about the frames for sealing a channel when the frame is disposed across it. The seals are arcuate in configuration and lie on a circle having its center at the center axis of the shaft. Rotation of the shaft selectively opens and closes alternate channels of the flue housing.

    摘要翻译： 一种用于焦炉的烟道壳体的调节装置，用于交替地打开和关闭烟道外壳的通道，包括可旋转的轴，相对于彼此安装在轴上的框架优选地相对于彼此以90°交替顺序地沿着轴，周边密封 关于当框架布置在其上时用于密封通道的框架。 密封件呈弓形构型并且位于其轴线的中心轴线上的圆形上。 轴的旋转选择性地打开和关闭烟道外壳的交替通道。

    Isoquinoline aminopyrazole derivatives
    17.
    发明授权
    Isoquinoline aminopyrazole derivatives 失效
    异喹啉氨基吡唑衍生物

    公开(公告)号：US07572809B2

    公开(公告)日：2009-08-11

    申请号：US11637733

    申请日：2006-12-12

    申请人： Li Chen ,  Guy Georges ,  Alfred Mertens ,  Xihan Wu

    发明人： Li Chen ,  Guy Georges ,  Alfred Mertens ,  Xihan Wu

    IPC分类号： C07D403/14 ,  A61K31/4709

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

    摘要： The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.

    摘要翻译： 本发明涉及式I化合物：其药学上可接受的盐或酯，对映体形式，非对映异构体和外消旋体，这些化合物的制备，含有它们的药物组合物及其制备，以及这些化合物在对照中的用途 或预防癌症等疾病。