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    Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them
    21.
    发明授权
    Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them 失效
    具有降血压和β-阻断性能的喹喔啉氧基 - 氨基 - 丙醇化合物，它们的用途和含有它们的药物组合物

    公开(公告)号：US4438116A

    公开(公告)日：1984-03-20

    申请号：US302894

    申请日：1981-09-16

    申请人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

    发明人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

    IPC分类号： A61K31/505 ,  A61P9/00 ,  C07D241/38 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  A61K31/495 ,  C07D241/42

    CPC分类号： C07D241/38 ,  C07D241/44 ,  Y10S514/929

    摘要： An aminopropanol compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from hydrogen and lower alkyl; orR.sub.1 and R.sub.2 together represent an alkylene radical;R.sub.3 is hydrogen or acyl;A is one of the following structures ##STR2## wherein R.sub.4 is hydrogen or lower alkyl optionally substituted by hydroxyl halogen and lower alkylthio; andR.sub.5 and R.sub.6 are individually selected from lower alkyl;B is alkylamino which optionally carries a phenyl and a phenoxy radical optionally substituted by at at least one of halogen, hydroxyl or lower alkyl, lower acyl, lower alkylthio, acylamino, aminocarbonyl, lower alkoxy, lower alkenyloxy, phenoxy, lower alkenyl, lower alkylsulphonyl, lower alkylsulphinyl or haloalkyl; orB is an aryl- or heteroaryloxymethylpiperidine radical optionally substituted by at least one of halogen hydroxyl or lower alkyl, hydroxyl alkyl or carboxamido alkyl, or by lower alkoxy, lower acyl, amino, carboxamido, lower alkylcarbonylamido or lower alkylsulphonylamino;and the pharmacologically acceptable salts thereof, are outstandingly effective beta blockers and blood-pressure depressants.

    摘要翻译： 式IMAMA的氨基丙醇化合物，其中R 1和R 2分别选自氢和低级烷基; 或者R 1和R 2一起表示亚烷基; R3是氢或酰基; A是下列结构之一，其中R4是氢或任选被羟基卤素和低级烷硫基取代的低级烷基; 并且R 5和R 6分别选自低级烷基; B是烷基氨基，其任选地带有苯基和苯氧基，其任选被至少一个卤素，羟基或低级烷基，低级酰基，低级烷硫基，酰氨基，氨基羰基，低级烷氧基，低级烯氧基，苯氧基，低级烯基，低级烷基磺酰基 ，低级烷基亚磺酰基或卤代烷基; 或B是任选被卤素羟基或低级烷基，羟基烷基或甲酰胺基烷基中的至少一个取代的芳基或杂芳氧基甲基哌啶基，或由低级烷氧基，低级酰基，氨基，甲酰氨基，低级烷基羰基酰氨基或低级烷基磺酰基氨基取代; 和其药理学上可接受的盐是显着有效的β受体阻滞剂和降压药。

    N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods
    22.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods 失效
    N-取代的氮丙啶-2-羧酸衍生物及其免疫刺激组合物和方法

    公开(公告)号：US4410532A

    公开(公告)日：1983-10-18

    申请号：US334614

    申请日：1981-12-28

    申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D213/36

    CPC分类号： C07D203/06 ,  Y10S514/885

    摘要： A 2-cyanaziridine derivative of the formula ##STR1## wherein R' is a straight-chained or branched, saturated or mono- or polyunsaturated aliphatic hydrocarbon radical with up to 8 carbon atoms, which is substituted by an aromatic nitrogen-containing heterocyclic radical with 5 or 6 ring-members and 1, 2 or 3 nitrogen atoms optionally substituted by halogen, alkoxy with up to 8 carbon atoms, alkyl with up to 8 carbon atoms, hydroxyl, carbalkoxy with up to 9 carbon atoms, carbamoyl, dialkylamino the alkyl moieties of which having up to 8 carbon atoms, cycloalkylamino, the cycloalkyl moiety having 3-10 carbon atoms, acetylamino, nitro, cyano, acetyl, alkylthio with up to 8 carbon atoms, alkylsulphinyl with up to 8 carbon atoms, alkylsulphonyl with up to 8 carbon atoms, sulphamoyl, phenyl, trifluoromethyl, phenoxy, acetoxy or methylenedioxy;or a pharmacologically acceptable salt thereof, exhibits immune stimulating activity.

    摘要翻译： 具有式“IMAGE”的2-氰基氮丙啶衍生物，其中R'是具有至多8个碳原子的直链或支链，饱和或单或多不饱和脂族烃基，其被含芳族含氮杂环基团取代， 5或6个环成员和1,2或3个任选被卤素取代的氮原子，具有至多8个碳原子的烷氧基，至多8个碳原子的烷基，羟基，至多9个碳原子的烷氧基，氨基甲酰基，二烷基氨基烷基 其具有至多8个碳原子的部分，环烷基氨基，具有3-10个碳原子的环烷基部分，乙酰氨基，硝基，氰基，乙酰基，具有至多8个碳原子的烷硫基，具有至多8个碳原子的烷基亚磺酰基，烷基磺酰基， 8个碳原子，氨磺酰基，苯基，三氟甲基，苯氧基，乙酰氧基或亚甲二氧基; 或其药理学上可接受的盐显示免疫刺激活性。

    Pharmaceutical phenylacetonitrile derivatives
    28.
    发明授权
    Pharmaceutical phenylacetonitrile derivatives 失效
    药用苯乙腈衍生物

    公开(公告)号：US4612313A

    公开(公告)日：1986-09-16

    申请号：US774354

    申请日：1985-09-10

    申请人： Herbert Leinert ,  Wolfgang Kampe ,  Klaus Strein ,  Bernd Muller-Beckmann ,  Wolfgang Bartsch

    发明人： Herbert Leinert ,  Wolfgang Kampe ,  Klaus Strein ,  Bernd Muller-Beckmann ,  Wolfgang Bartsch

    IPC分类号： A61K31/21 ,  A61K31/275 ,  A61K31/445 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07C67/00 ,  C07C253/00 ,  C07C255/24 ,  C07C255/32 ,  C07C255/42 ,  C07C255/43 ,  C07C255/53 ,  C07C255/58 ,  C07C255/59 ,  C07D207/08 ,  C07D211/22 ,  C07D241/04 ,  C07D295/16 ,  C07D295/18 ,  A61K31/495 ,  C07C121/80

    CPC分类号： C07C255/00 ,  C07D211/22

    摘要： The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.7 is a hydrogen atom or a straight-chained or branched, saturated alkyl radical containing up to 6 carbon atoms, m and n, which can be the same or different, are 2 or 3, p is 1 or 2 and X is a straight-chained, cyclic or branched alkyl radical containing 2 to 10 carbon atoms which is optionally substituted by an amino group or is a grouping of the general formula: ##STR3## wherein Y and Z, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 8 carbon atoms or cycloalkyl, alkylcycloalkyl or cycloalkylalkyl radicals, in which these radicals are optionally interrupted by an oxygen or sulphur atom, and one of the groups Z in general formula II can also be a hydrogen atom or both Z groups are joined to form a ring containing 4 to 6 carbon atoms which is optionally interrupted by a further nitrogen atom which can be substituted by alkyl or alkanoyl, the --O--NO.sub.2 groups being substituents of Y as well as of Z; as well as the salts thereof with physiologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

    摘要翻译： 本发明提供以下通式的苯乙腈衍生物：其中R 1，R 2，R 3，R 4和R 5可以相同或不同，为氢或卤素原子或烷基，烷氧基，硝基，氨基或 酰基氨基和两个相邻的取代基可以一起形成亚甲二氧基或亚乙二氧基，A是下列通式的基团：其中R 6是含有2至12个直链的直链，环状或支链的饱和或不饱和烷基 碳原子，R7是氢原子或含有至多6个碳原子的直链或支链饱和烷基，m和n可相同或不同，为2或3，p为1或2，X为 是含有2至10个碳原子的直链，环状或支链烷基，其任选被氨基取代，或者是通式如下的基团：其中Y和Z可以相同或不同， 是直链或支链烷基基团 引入多达8个碳原子或环烷基，烷基环烷基或环烷基烷基，其中这些基团任选地被氧或硫原子中断，通式II中的基团Z之一也可以是氢原子或两个Z基团连接 形成含有4至6个碳原子的环，其任选被可被烷基或烷酰基取代的另外的氮原子中断，-O-NO 2基团是Y和Z的取代基; 以及其与生理上可接受的酸的盐。 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。

    N-Substituted aziridine-2-carboxylic acid derivatives
    29.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives 失效

    公开(公告)号：US4517183A

    公开(公告)日：1985-05-14

    申请号：US495548

    申请日：1983-05-17

    申请人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    发明人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    IPC分类号： A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

    CPC分类号： C07D203/22 ,  Y10S514/885

    摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

    3-Cyano indoles as intermediates for cardioselective compounds
    30.
    发明授权
    3-Cyano indoles as intermediates for cardioselective compounds 失效
    3-氰基吲哚作为心脏选择性化合物的中间体

    公开(公告)号：US4442295A

    公开(公告)日：1984-04-10

    申请号：US288077

    申请日：1981-07-29

    申请人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch

    发明人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42 ,  C07D209/43 ,  C07D405/12 ,  C07D209/04

    CPC分类号： C07D405/12 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42

    摘要： The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, an aralkyl radical or a radical of the general formula: ##STR2## in which B is a reactive group or, together with R.sub.5, represents a valency bond, and R.sub.5 is a hydrogen atom or an aliphatic or aromatic acyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen atom, a methyl radical or a --CH.sub.2 --O--R.sub.5 radical, R.sub.5 having the same meaning as above, and R.sub.4 is an aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, with the proviso that R.sub.1 is not an aralkyl radical when R.sub.4 is a formyl radical. The present invention also provides processes for the preparation of these compounds. Furthermore, the present invention is concerned with the use of these compounds for the preparation of compounds with a heart and circulatory activity.

    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，芳烷基或具有以下通式的基团：其中B是反应性基团，或与R 5一起 表示价键，R5表示氢原子或脂肪族或芳香族酰基，R2表示氢原子或低级烷基，R3表示氢原子，甲基或-CH2-O-R5基， R5具有与上述相同的含义，R4是氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基，条件是当R 4是甲酰基时，R 1不是芳烷基。 本发明还提供了这些化合物的制备方法。 此外，本发明涉及这些化合物用于制备具有心脏和循环活性的化合物的用途。