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28 条记录 (耗时 0.028 秒)

    Heterocyclic-substituted indoles and pharmaceutical compositions containing them
    3.
    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
    4.
    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
    5.
    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。

    Method of treatment for decreasing mortality resulting from congestive heart failure
    6.
    发明授权
    Method of treatment for decreasing mortality resulting from congestive heart failure 失效
    减少充血性心力衰竭引起的死亡率的治疗方法

    公开(公告)号：US5760069A

    公开(公告)日：1998-06-02

    申请号：US483635

    申请日：1995-06-07

    申请人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    发明人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    IPC分类号： C07D207/16 ,  A61K31/196 ,  A61K31/34 ,  A61K31/40 ,  A61K31/401 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/54 ,  A61K31/549 ,  A61K31/662 ,  A61K31/70 ,  A61K31/702 ,  A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P9/00 ,  A61P9/04 ,  C07D209/88 ,  A61K31/585

    CPC分类号： A61K31/403 ,  A61K31/7048

    摘要： A method of treatment using a compound of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms; R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--; X is a valency bond, --CH.sub.2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R.sub.5 and R.sub.6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.

    摘要翻译： 使用式I化合物的方法：其中：R1是氢，至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R2是氢，至多6个碳原子的低级烷基或选自苄基，苯基乙基和苯基丙基的芳基烷基; R3是氢或至多6个碳原子的低级烷基; R4是氢或至多6个碳原子的低级烷基，或当X是氧时，R4与R5一起可以代表-CH2-O-; X是价键，-CH 2，氧或硫; Ar选自苯基，萘基，茚满基和四氢萘基; R 5和R 6分别选自氢，氟，氯，溴，羟基，至多6个碳原子的低级烷基，-CONH 2 - 基，至多6个碳原子的低级烷氧基，苄氧基，至多6个碳的低级烷硫基 原子，低至6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R5和R6一起表示亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭（CHF）引起的死亡率的ACE抑制剂，利尿剂和地高辛，所述药物单独或与一种或多种其它治疗剂联合使用，或其药学上可接受的盐， 人类。

    Method of treatment for decreasing mortality resulting from congestive heart failure
    7.
    再颁专利
    Method of treatment for decreasing mortality resulting from congestive heart failure 有权
    减少充血性心力衰竭引起的死亡率的治疗方法

    公开(公告)号：USRE40000E1

    公开(公告)日：2008-01-08

    申请号：US10721020

    申请日：2003-11-25

    申请人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    发明人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    IPC分类号： A61K31/40 ,  A61K31/585 ,  A61K31/54 ,  A61K31/41 ,  A61K31/34

    CPC分类号： A61K31/403 ,  A61K31/7048 ,  A61K2300/00

    摘要： A method of treatment using a compound of Formula I: wherein: R1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R3 is hydrogen or lower alkyl of up to 6 carbon atoms; R4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R4 together with R5 can represent —CH2—O—; X is a valency bond, —CH2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronapthyl; R5 and R6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a —CONH2— group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R5 and R6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.

    摘要翻译： 使用式I化合物的方法：其中：R 1是氢，至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R 2是氢，至多6个碳原子的低级烷基或选自苄基，苯基乙基和苯基丙基的芳基烷基; R 3是氢或至多6个碳原子的低级烷基; R 4是氢或至多6个碳原子的低级烷基，或者当X是氧时，R 4与R 5一起可代表 - CH 2 -O-; X是价键，-CH 2，氧或硫; Ar选自苯基，萘基，茚满基和四氢萘基; R 5和R 6分别选自氢，氟，氯，溴，羟基，至多6个碳原子的低级烷基，-CONH 2， 最多6个碳原子的低级烷氧基，至多6个碳原子的低级烷硫基，至多6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R 5和R 6一起代表亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭（CHF）引起的死亡率的ACE抑制剂，利尿剂和地高辛，所述药物单独或与一种或多种其它治疗剂联合使用，或其药学上可接受的盐， 人类。