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19 条记录 (耗时 0.018 秒)

    Triazolo-benzodiazepine derivatives
    5.
    发明授权
    Triazolo-benzodiazepine derivatives 失效
    三唑并苯并二氮杂衍生物

    公开(公告)号：US4374773A

    公开(公告)日：1983-02-22

    申请号：US225747

    申请日：1981-01-16

    申请人： Quirico Branca ,  Albert E. Fischli ,  Andre Szente

    发明人： Quirico Branca ,  Albert E. Fischli ,  Andre Szente

    IPC分类号： A61K31/55 ,  A61P1/16 ,  A61P9/04 ,  A61P9/12 ,  C07D243/24 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D243/24 ,  Y10S514/893

    摘要： There are presented compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 and R.sup.3 each are a hydrogen atom or a lower alkyl group, R.sup.4 is a halogen atom and either R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 is a lower alkyl or lower hydroxyalkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached are a 3-membered to 7-membered heterocycle,and pharmaceutically acceptable acid addition salts thereof.The compounds and their salts are novel and possess valuable pharmacodynamic properties.

    摘要翻译： 提供式Ⅰ的化合物，其中R 1是氢原子或低级烷基，R 2和R 3各自是氢原子或低级烷基，R 4是卤素原子，R 5是氢原子或 低级烷基，R 6为低级烷基或低级羟基烷基或R 5和R 6与它们所连接的氮原子一起为3-元至7-元杂环，及其药学上可接受的酸加成盐。 化合物及其盐是新颖的，具有有价值的药效学性质。

    Tetrahydronaphthalene derivatives as calcium antagonists
    9.
    发明授权
    Tetrahydronaphthalene derivatives as calcium antagonists 失效
    四氢萘衍生物作为钙拮抗剂

    公开(公告)号：US4808605A

    公开(公告)日：1989-02-28

    申请号：US119114

    申请日：1987-11-10

    申请人： Quirico Branca ,  Roland Jaunin ,  Hans P. Maki ,  Franzi Marti ,  Henri Ramuz

    发明人： Quirico Branca ,  Roland Jaunin ,  Hans P. Maki ,  Franzi Marti ,  Henri Ramuz

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/55 ,  A61K31/551 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/14 ,  C07D235/26 ,  C07D243/14 ,  C07D277/62 ,  C07D277/64 ,  C07D401/06 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07D413/06

    CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D235/14 ,  C07D235/26 ,  C07D243/14 ,  C07D249/08 ,  C07D277/64 ,  C07D401/06 ,  C07D471/04 ,  C07D487/04

    摘要： Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof. The compounds of formual I have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias, high blood pressure and cardiac insufficiency.

    摘要翻译： 其中R为低级烷基，R 1为卤素，R 2为C 1 -C 12 - 烷基，R 3为羟基，低级烷氧基，低级烷基 - 羰基氧基，低级烷氧基 - 低级 - 烷基羰基氧基，低级 烷基氨基羰基氧基，芳基氨基羰基氧基或芳基 - 低级烷基氨基羰基氧基，X是C1-C18-亚烷基，其任选可以被1,4-亚苯基中断或被1,4-亚环己基中断或延长，A是二或三取代的2-咪唑基 经由亚乙基或取代或未取代的选自苯并咪唑基，苯并咪唑啉酮，咪唑并[4,5-c]吡啶基，咪唑并[4,5-c]吡啶基，苯并噻唑基，苯并二氮杂-2,5-二 -1-基和吡咯并[2,1-c] - [1,4]苯并二氮杂-5,11-二酮-10-基，n为0或1，以外消旋体和光学对映体的形式，以及 作为N-氧化物及其可药用的酸加成盐。 形式I的化合物具有显着的钙拮抗和抗心律不齐活性，因此可以用作药物，特别是用于控制或预防心绞痛，局部缺血，心律失常，高血压和心脏功能不全。

    Benzodiazepine derivatives
    10.
    发明授权
    Benzodiazepine derivatives 失效
    苯并二氮杂衍生物

    公开(公告)号：US4327026A

    公开(公告)日：1982-04-27

    申请号：US283711

    申请日：1981-07-16

    申请人： Quirico Branca ,  Albert E. Fischli ,  Andre' Szente

    发明人： Quirico Branca ,  Albert E. Fischli ,  Andre' Szente

    IPC分类号： A61K31/55 ,  A61K31/551 ,  A61P5/38 ,  C07D243/16 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  C07D243/28

    CPC分类号： C07D243/24

    摘要： There is presented benzodiazepine derivatives of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is lower alkyl, R.sup.2 and R.sup.3 each are hydrogen or lower alkyl, R.sup.4 is the group ##STR3## R.sup.5 is hydrogen or halogen, R.sup.8 is hydrogen or lower alkyl, R.sup.9 is lower alkyl or lower alkoxyalkyl, R.sup.10 is lower alkyl, R.sup.11 is hydrogen, lower alkyl or lower hydroxyalkyl, R.sup.12 is hydrogen or lower alkyl and R.sup.14 is lower alkyl or aryl, and either R.sup.6 is hydrogen or lower alkyl and R.sup.7 is lower alkyl or lower hydroxyalkyl or R.sup.6 and R.sup.7 together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N-R.sup.13, in which R.sup.13 is hydrogen or lower alkyl, and either R.sup.6 ' is hydrogen or lower alkyl and R.sup.7 ' is lower alkyl or R.sup.6 ' and R.sup.7 ' together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula > N-R.sup.13 ', in which R.sup.13 ' is lower alkyl, with the proviso that R.sup.4 is the group R.sup.6 ' R.sup.7 ' N--CO--NH--CH(R.sup.8)-- when A is the group (c),and pharmaceutically acceptable acid addition salts thereof.The compounds exhibit aldosterone-antagonistic properties and are suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.

    摘要翻译： 呈现下式的苯并二氮杂衍生物其中A是下列基团：R 1是低级烷基，R 2和R 3各自是氢或低级烷基，R 4是基团 + TR R5是氢或卤素，R8是氢或低级烷基，R9是低级烷基或低级烷氧基烷基，R10是低级烷基，R11是氢，低级烷基或低级羟烷基，R12是氢或低级烷基，R14是低级烷基或芳基， 并且R 6是氢或低级烷基，且R 7是低级烷基或低级羟基烷基，或者R 6和R 7与氮原子一起是3-至7-元杂环，当它至少为5元时，它可以含有一个环 成员为氧或硫原子或式> N-R13的基团，其中R13为氢或低级烷基，R6'为氢或低级烷基，R7'为低级烷基或R6'和R7'以及 氮原子是3-至7-元杂环，当其为至少5元时，其可以含有作为环成员的氧 或硫原子或式“N-R13”的基团，其中R13'为低级烷基，条件是R4为R6'R7'N-CO-NH-CH（R8） - 当A为 （c）组及其药学上可接受的酸加成盐。 该化合物显示醛固酮拮抗性质，适用于控制或预防心力衰竭，肝腹水，原发性醛固酮增多症和特发性高血压。