Vascular hypertrophy suppressor
    61.
    发明授权
    Vascular hypertrophy suppressor 失效
    血管肥大抑制因子

    公开(公告)号:US5736561A

    公开(公告)日:1998-04-07

    申请号:US588240

    申请日:1996-01-18

    申请人: Kohei Nishikawa

    发明人: Kohei Nishikawa

    摘要: This invention relates to a method for the prophylaxis or treatment of vascular hypertropy in a mammal by administering a pharmaceutically effective amount of a compound represented by the formula (I): ##STR1## wherein ring W is a nitrogen-containing heterocyclic ring residue which may be substituted; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue which optionally binds through a hetero-atom; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic length of two or less; n denotes 1 or 2; a and b forming the heterocyclic ring residue are independently one or two optionally substituted carbon or hetero atoms; c is an optionally substituted carbon or hetero atom; provided that, when the ring W is a condensed ring, R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue which binds through a hetero atom, or a salt thereof to a mammal in need thereof.

    摘要翻译: 本发明涉及通过施用药学有效量的式(I)表示的化合物来预防或治疗哺乳动物的血管肥大的方法:其中环W是含氮杂环残基,其可以是 被替代 R1是氢或任选取代的烃残基,其任选地通过杂原子结合; R3表示能够形成阴离子或能够改变的基团的基团; X表示亚苯基和苯基直接或通过原子长度为2或更小的间隔物彼此结合; n表示1或2; 形成杂环残基的a和b独立地是一个或两个任选取代的碳或杂原子; c是任选取代的碳或杂原子; 条件是当环W是稠环时,R 1是氢或任选取代的通过杂原子结合的烃残基或其盐与有需要的哺乳动物结合。

    Method for the treatment of sclerosis of the glomeruli
    62.
    发明授权
    Method for the treatment of sclerosis of the glomeruli 失效
    治疗肾小球硬化症的方法

    公开(公告)号:US5719173A

    公开(公告)日:1998-02-17

    申请号:US696475

    申请日:1996-08-14

    摘要: This invention relates to prophylactic or therapeutic drug for diabetic nephropathy or glomerulonephritis, comprising, as an active ingredient, a compound or salt thereof represented by general formula (I) ##STR1## wherein R.sup.1 stands for H or an optionally substituted hydrocarbon residue; R.sup.2 stands for an optionally esterified carboxyl group; R.sup.3 stands for a group actually or potentially capable of forming an anion; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic chain length of two or less; n stands for 1 or 2; ring A stands for a benzene ring having an optional substituent in addition to R.sup.2 ; Y stands for a bond, --O--, --S(O).sub.m -- (wherein m stands for 0, 1 or 2), or --N(R.sup.4)-- (wherein R.sup.4 stands for H or an optionally substituted alkyl group).

    摘要翻译: 本发明涉及用于糖尿病性肾病或肾小球肾炎的预防或治疗药物,其包含作为活性成分的由通式(I)表示的化合物或其盐,其中R1代表H或任选取代的烃残基 ; R2代表任选酯化的羧基; R3代表实际上或潜在能够形成阴离子的组; X表示亚苯基和苯基直接或通过原子链长度为2或更小的间隔物彼此结合; n代表1或2; 环A代表除R2之外具有任选取代基的苯环; Y代表键,-O - , - S(O)m-(其中m代表0,1或2)或-N(R 4) - (其中R 4表示H或任选取代的烷基)。

    Piperidine derivatives, their production and use
    65.
    发明授权
    Piperidine derivatives, their production and use 失效
    哌啶衍生物,其生产和使用

    公开(公告)号:US4954625A

    公开(公告)日:1990-09-04

    申请号:US400680

    申请日:1989-08-30

    IPC分类号: A61K38/00 C07K5/02

    CPC分类号: C07K5/0222 A61K38/00

    摘要: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

    1,4-benzoxazine derivatives and pharmaceutical use
    67.
    发明授权
    1,4-benzoxazine derivatives and pharmaceutical use 失效
    1,4-苯并恶嗪衍生物和药物用途

    公开(公告)号:US4789675A

    公开(公告)日:1988-12-06

    申请号:US13441

    申请日:1987-02-10

    摘要: 1,4-Benzoxazine derivatives representable by the general formula; ##STR1## wherein R.sup.1 and R.sup.2 independently stand for hydrogen, halogen atom, nitro group, an optionally substituted lower alkyl group, an optionally substituted amino group, an optionally substituted hydroxyl group, a lower alkoxycarbonyl group, or when R.sup.1 and R.sup.2 are adjacent to each other,R.sup.1 and R.sup.2 combinedly stand for a ring representable by --CH.sub.2).sub.m (wherein m denotes an integer of 3 to 5) or --O--CH.sub.2).sub.n O-- (wherein n denotes an integer of 1 to 3),R.sup.3 stands for hydrogen or a lower alkyl group,R.sup.4 and R.sup.5 independently stand for hydrogen, halogen atom, an optionally substituted lower alkyl group or an optionally substituted hydroxyl group, andA stands for an alkylene groupor acid addition salts thereof, are useful as prophylactic or therapeutic drugs for, among others, hypertension or ischemic dieases.

    摘要翻译: 由通式表示的1,4-苯并恶嗪衍生物; 其中R 1和R 2独立地代表氢,卤素原子,硝基,任选取代的低级烷基,任选取代的氨基,任选取代的羟基,低级烷氧基羰基,或当R 1和R 2相邻时 相互之间,R 1和R 2组合​​地代表-CH 2)m(其中m表示3至5的整数)或-O-CH 2)n O-(其中n表示1至3的整数)表示的环,R 3表示 对于氢或低级烷基,R4和R5独立地代表氢,卤素原子,任选取代的低级烷基或任选取代的羟基,A代表亚烷基或其酸加成盐,可用作预防或 治疗药物,尤其是高血压或缺血性坏死。

    Condensed, seven-membered ring compounds and their use
    68.
    发明授权
    Condensed, seven-membered ring compounds and their use 失效
    浓缩的七元环化合物及其用途

    公开(公告)号:US4564612A

    公开(公告)日:1986-01-14

    申请号:US599187

    申请日:1984-04-11

    摘要: Novel condensed, seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 each represent hydrogen, halogen, trifluoromethyl, lower alkyl or alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or alkyl, aralkyl or cycloalkylalkyl which may be substituted; X is a group represented by the formula S(O).sub.n (where n is an integer of 0 to 2); Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of hypertension.

    摘要翻译: 新颖的下式的缩合的七元环化合物:其中R 1和R 2各自代表氢,卤素,三氟甲基,低级烷基或烷氧基,或两者共同形成三 - 或四亚甲基; R3是氢,低级烷基或芳烷基; R4是氢或可以被取代的烷基,芳烷基或环烷基烷基; X为由式S(O)n(n为0〜2的整数)表示的基团。 Y是可被酯化或酰胺化的羧基; m为1或2]及其盐。 这些化合物对血管紧张素转换酶等具有抑制活性,作为高血压的诊断,预防和治疗药物具有价值。