N-[1-(4-Amino-6,7-dialkoxy-2-quinazolinyl)-4-piperidy
l]-oxazolidine-2,4-diones
    1.
    发明授权
    N-[1-(4-Amino-6,7-dialkoxy-2-quinazolinyl)-4-piperidy l]-oxazolidine-2,4-diones 失效
    N- [1-(4-氨基-6,7-二烷氧基-2-喹唑啉基)-4-哌啶基] - 恶唑烷-2,4-二酮

    公开(公告)号:US4539323A

    公开(公告)日:1985-09-03

    申请号:US531842

    申请日:1983-09-14

    CPC分类号: C07D413/04 C07D413/14

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 8 carbon atoms or arylmethyl; orR.sub.1 and R.sub.2, together with each other, are --(CH.sub.2).sub.4 or --(CH.sub.2).sub.5 --; andR.sub.3 and R.sub.4, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 4 carbon atoms or arylmethyl; orR.sub.3 and R.sub.4, together with each other, are --CH.sub.3 -- or --CH.sub.2 --CH.sub.2 --;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of cardiovascular diseases, especially hypertension.

    摘要翻译: 其中R 1和R 2可以相同或不同,各自独立地为氢,1至8个碳原子的直链或支链烷基或芳基甲基; 或R 1和R 2彼此一起为 - (CH 2)4或 - (CH 2)5 - ; 并且可以相同或不同的R 3和R 4各自独立地为氢,1至4个碳原子的直链或支链烷基或芳基甲基; 或R 3和R 4彼此一起为-CH 3 - 或-CH 2 -CH 2 - ; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用于治疗心血管疾病,特别是高血压。

    3,1 Benzoxazin-2-ones and use thereof
    2.
    发明授权
    3,1 Benzoxazin-2-ones and use thereof 失效
    3,苯并恶嗪-2-酮及其用途

    公开(公告)号:US4341778A

    公开(公告)日:1982-07-27

    申请号:US280349

    申请日:1981-07-06

    CPC分类号: C07D265/18

    摘要: The invention relates to compounds of general formula I ##STR1## (wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group;R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen, fluorine or chlorine atom or a hydroxy, methyl, ethyl or (C.sub.1 -C.sub.4) alkoxy group, or R.sub.3 together with R.sub.4 represents a methylenedioxy group;R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or a methyl group;R.sub.7 represents a group of formula ##STR2## R represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group; R.sub.8 represents a fluorine or chlorine atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkylthio, hydroxymethyl, CONHR.sub.11, SO.sub.2 NHR.sub.11, OR.sub.12, methoxycarbonyl, ethoxycarbonyl or NHSO.sub.2 CH.sub.3 group;R.sub.9 represents a hydrogen, fluorine or chlorine atom or a OR.sub.12 group;R.sub.10 represents a hydrogen or chlorine atom or an amino, methyl or methoxy group;R.sub.11 represents a hydrogen atom or a methyl, ethyl or hydroxyethyl group;R.sub.12 represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkyl-CO, aryl-CH.sub.2 or aryl-CO group; andn represents 1, 2 or 3) and acid addition salts thereof as well as to processes for their preparation and pharmaceutical compositions containing them. The compounds of the invention possess interesting pharmacological properties in particular displaying hypotensive and selective tocolytic effects.

    摘要翻译: 本发明涉及通式I(I)的化合物(其中R 1和R 2可以相同或不同,各自表示氢原子或(C 1 -C 4)烷基; R 3和R 4可以 相同或不同,各自表示氢,氟或氯原子或羟基,甲基,乙基或(C1-C4)烷氧基,或R3与R4一起代表亚甲二氧基; R5和R6可以相同 或不同的,各自表示氢原子或甲基; R 7表示下式的基团:R表示氢原子或(C 1 -C 4)烷基; R 8表示氟或氯原子或(C 1 -C 4) )烷基,(C1-C4)烷硫基,羟甲基,CONHR11,SO2NHR11,OR12,甲氧基羰基,乙氧基羰基或NHSO2CH3基; R9表示氢,氟或氯原子或OR12基团; R10表示氢或氯原子或氨基, 甲基或甲氧基; R11表示氢原子或甲基,乙基或羟乙基; R12表示a 氢原子或(C 1 -C 4)烷基,(C 1 -C 4)烷基-CO,芳基-CH 2或芳基-CO基团; 和n表示1,2或3)及其酸加成盐以及其制备方法和含有它们的药物组合物。 本发明的化合物具有特别显示降血压和选择性溶瘤作用的有趣的药理学性质。

    Pyrrolo[2,3-C]pyridines and their use as anti-hypertensive agents
    4.
    发明授权
    Pyrrolo[2,3-C]pyridines and their use as anti-hypertensive agents 失效
    吡咯并[2,3-C]吡啶及其作为抗高血压药的用途

    公开(公告)号:US4766129A

    公开(公告)日:1988-08-23

    申请号:US47417

    申请日:1987-05-06

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.3 is hydrogen or alkyl of 1 to 6 carbon atoms;n and m are each independently 0, 1 or 2, the sum of n and m being 1 or 2;X, Y and Z are each independently oxygen, sulfur, --NR.sub.4 --, .dbd.CR.sub.5 --, --CHR.sub.5 --, ##STR2## provided that only one of X, Y and Z is O, S, ##STR3## and one or two of X, Y and Z are --R.sub.4 --; R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms; andR.sub.5 is hydrogen or, together with a vicinal radical R.sub.5, a phenyl ring, or when m and n are both 1, the dihydro form with its double bond in conjugation with the C-terminal carboxylic group;or a non-toxic, pharmacologically acceptable salt thereof. The compounds as well as their salts are useful as antihypertensives.

    摘要翻译: 其中R 1是氢,1至6个碳原子的烷基或苯基(1至6个碳原子的烷基)的式 R2是氢,1至4个碳原子的烷基或苯基(1至6个碳原子的烷基); R3是氢或1至6个碳原子的烷基; n和m各自独立地为0,1或2,n和m的和为1或2; X,Y和Z各自独立地为氧,硫,-NR4-,= CR5-,-CHR5-,,条件是X,Y和Z中只有一个是O,S,,一个或两个 X,Y和Z为-R4-; R4是氢或1-4个碳原子的烷基; 并且R 5是氢或与连位基R5一起为苯环,或者当m和n均为1时,与C末端羧基共轭的双键形式的二氢形式; 或其无毒的药理学上可接受的盐。 化合物及其盐可用作抗高血压药。

    1-aryloxypropanolamines
    5.
    发明授权
    1-aryloxypropanolamines 失效
    1-芳氧基丙醇胺

    公开(公告)号:US4594344A

    公开(公告)日:1986-06-10

    申请号:US755044

    申请日:1985-07-15

    CPC分类号: C07D285/30

    摘要: Disclosed are novel compounds having the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, a lower alkyl, lower alkoxy, lower alkoxy lower alkyl, lower alkenyl, lower alkenyl oxy, cyano, hydroxy, trifluoromethyl, nitro, amino, aminocarbonylmethyl, lower monoalkylamino, lower dialkylamino group;R.sub.2 is a hydrogen or halogen atom, cyano, lower alkyl or lower alkoxy or acylamino group;R.sub.3 is a hydrogen or halogen atom, a lower alkyl or lower alkoxy group, while R.sub.2 and R.sub.3 together can also be a butadienyl or methylene dioxy group;R.sub.4 is a hydrogen atom or a lower alkyl group;R.sub.5 is a chlorine atom or a trifluoromethyl group;X is an alkylene group;and the non-toxic, pharmaceutically acceptable acid addition salts thereof.The compounds are suitable for treatment and prophylaxis of hypertension.

    摘要翻译: 公开了具有下式的新化合物:其中R1是氢或卤原子,低级烷基,低级烷氧基,低级烷氧基低级烷基,低级烯基,低级烯基氧基,氰基,羟基,三氟甲基,硝基,氨基,氨基羰基甲基, 低级单烷基氨基,低级二烷基氨基; R2是氢或卤素原子,氰基,低级烷基或低级烷氧基或酰氨基; R3是氢或卤素原子,低级烷基或低级烷氧基,R2和R3一起也可以是丁二烯基或亚甲基二氧基; R4是氢原子或低级烷基; R5是氯原子或三氟甲基; X是亚烷基; 和其无毒的药学上可接受的酸加成盐。 该化合物适用于治疗和预防高血压。

    2,3,4,9-tetrahydro beta carboline derivatives, useful as
antihypertensive agents
    10.
    发明授权
    2,3,4,9-tetrahydro beta carboline derivatives, useful as antihypertensive agents 失效
    2,3,4,9-四氢β-咔啉衍生物,可用作抗高血压药

    公开(公告)号:US4683238A

    公开(公告)日:1987-07-28

    申请号:US749473

    申请日:1985-06-27

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.3 is hydrogen or alkyl of 1 to 6 carbon atoms;n and m are each independently 0, 1 or 2, the sum of n and m being 1 or 2;X, Y and Z are each independently oxygen, sulfur, --NR.sub.4 --, .dbd.CR.sub.5 --, --CHR.sub.5 --, ##STR2## provided that only one of X, Y and Z is O, S ##STR3## and one or two of X, Y and Z are --NR.sub.4 --; R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms; andR.sub.5 is hydrogen or, together with a vicinal radical R.sub.5, a phenyl ring, or when m and n are both 1, the dihydro form with its double bond in conjugation with the C-terminal carboxylic group;or a non-toxic, pharmacologically acceptable salt thereof. The compounds as well as their salts are useful as antihypertensives.

    摘要翻译: 其中R 1是氢,1至6个碳原子的烷基或苯基(1至6个碳原子的烷基)的式 R2是氢,1至4个碳原子的烷基或苯基(1至6个碳原子的烷基); R3是氢或1至6个碳原子的烷基; n和m各自独立地为0,1或2,n和m的和为1或2; X,Y和Z各自独立地为氧,硫,-NR4-,= CR5-,-CHR5-,,条件是X,Y和Z中只有一个是O,S 和X中的一个或两个 ,Y和Z是-NR 4 - ; R4是氢或1-4个碳原子的烷基; 并且R 5是氢或与连位基R5一起为苯环,或者当m和n均为1时,与C末端羧基共轭的双键形式的二氢形式; 或其无毒的药理学上可接受的盐。 化合物及其盐可用作抗高血压药。