1,4-benzothiazine derivatives, compositions containing them and method
of use
    33.
    发明授权
    1,4-benzothiazine derivatives, compositions containing them and method of use 失效
    1,4-苯并噻嗪衍生物,含有它们的组合物和使用方法

    公开(公告)号:US4640916A

    公开(公告)日:1987-02-03

    申请号:US803217

    申请日:1985-11-27

    摘要: 1,4-Benzothiazine derivatives of the formula; ##STR1## wherein R.sup.1 and R.sup.2 independently stand for hydrogen, halogen, a lower alkyl group, a lower alkoxy group or trifluoromethyl group, or R.sup.1 and R.sup.2, taken together, form a 5-7 membered ring represented by ##STR2## wherein n is an integer of 3 to 5 or a 5-6 membered ring represented by ##STR3## wherein m is 1 or 2, R.sup.3 and R.sup.4 independently stand for hydrogen, halogen, a lower alkyl group, a lower alkoxy group or trifluoromethyl group, R.sup.5 stands for hydrogen or a lower alkyl group, and A stands for an alkylene group or pharmaceutically acceptable salts thereof, are useful as prophylactic or therapeutic drugs for, among others, hypertension and ischemic cardiovascular diseases.

    摘要翻译: 式的1,4-苯并噻嗪衍生物; 其中R 1和R 2独立地代表氢,卤素,低级烷基,低级烷氧基或三氟甲基,或者R 1和R 2一起形成由表示的5-7元环,其中n是 3〜5的整数或由下式表示的5-6元环,其中m为1或2,R3和R4分别代表氢,卤素,低级烷基,低级烷氧基或三氟甲基,R5代表 对于氢或低级烷基,A表示亚烷基或其药学上可接受的盐,可用作高血压和缺血性心血管疾病等预防或治疗药物。

    Quinoline derivatives, their production and use as ACAT inhibitors
    35.
    发明授权
    Quinoline derivatives, their production and use as ACAT inhibitors 失效
    喹啉衍生物,其生产和用作ACAT抑制剂

    公开(公告)号:US5523407A

    公开(公告)日:1996-06-04

    申请号:US280664

    申请日:1994-07-27

    摘要: A quinoline derivative of the formula (I): ##STR1## wherein each phenyl ring of A and B can have one or more substituents; X is ##STR2## (R.sup.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group) or ##STR3## (R.sup.2 is a hydrogen atom or a lower alkyl group); Y is --(CH.sub.2).sub.m --(m is 0, 1 or 2) or --CH.dbd.CH--, Z is a group of the formula: ##STR4## wherein each phenyl ring of C and D can have one or more substituents, R.sup.3 and R.sup.4 are each a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, N,N-di-lower alkylcarbamoyloxy, optionally esterified carboxy or hydroxyl group, R.sup.5 is a halogen atom, or a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, N,N-di-lower alkylcarbamoyloxy, optionally esterified carboxy or hydroxyl group, R.sup.6 and R.sup.7 are each a hydrogen atom or a lower alkyl group, and n, o and p are each 1 or 2; l is 0 or 1; or its salt, which is useful as a drug for atherosclerosis.

    摘要翻译: 式(I)的喹啉衍生物:其中A和B的每个苯环可以具有一个或多个取代基; X为(R 1为氢原子,低级烷基或低级烷氧基)或者(R 2为氢原子或低级烷基)。 Y是 - (CH 2)m - (m是0,1或2)或-CH = CH-,Z是下式的基团:其中C和D的每个苯环可以具有一个或 更多的取代基,R 3和R 4各自为氢或卤素原子,或低级烷基,低级烷氧基,低级酰氧基,低级烷氧基羰基氧基,N,N-二低级烷基氨基甲酰氧基,任意酯化的羧基或羟基,R5为卤素原子, 或低级烷基,低级烷氧基,低级酰氧基,低级烷氧基羰基氧基,N,N-二低级烷基氨基甲酰氧基,任意酯化的羧基或羟基,R6和R7各自为氢原子或低级烷基,n,o和p 分别为1或2; l为0或1; 或其盐,其可用作动脉粥样硬化的药物。

    Tricyclic heterocyclic compounds, their production and use
    36.
    发明授权
    Tricyclic heterocyclic compounds, their production and use 失效
    三环杂环化合物,其生产和使用

    公开(公告)号:US5418239A

    公开(公告)日:1995-05-23

    申请号:US117950

    申请日:1993-09-08

    摘要: Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

    摘要翻译: 新颖的通式如下的杂环化合物:其中环A和环B各自表示取代或未取代的苯环; X表示下式的基团:其中R 2为氢,烷基或烷氧基; m为0或1,式为:其中R 3为氢或烷基,或下式:-O-CO-; Y表示键,-NH-,C1或2亚烷基或-CH = CH-; R1表示取代或未取代的烃基; n表示具有优异酰基辅酶A:胆固醇酰基转移酶抑制活性的整数3〜6或其盐,及其制备方法及其用途。

    Thienopyridine derivatives which are intermediates
    38.
    发明授权
    Thienopyridine derivatives which are intermediates 失效
    作为中间体的噻吩并吡啶衍生物

    公开(公告)号:US5256782A

    公开(公告)日:1993-10-26

    申请号:US886081

    申请日:1992-05-20

    CPC分类号: C07D495/04

    摘要: Thienopyridine derivatives of the formula (I): ##STR1## wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: ##STR2## (wherein R.sup.1 is hydrogen, alkyl or alkoxy; and n is 0 or 1) or a group of the formula: ##STR3## (wherein R.sup.2 is hydrogen or alkyl); Y is a single bond, --NH--, alkylene having 1 or 2 carbon atoms or --CH.dbd.CH--; and R.sup.3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.

    摘要翻译: 式(I)的噻吩并吡啶衍生物:其中环A是任选取代的苯环; 环B是任选取代的噻吩环:X是下式的基团:其中R 1是氢,烷基或烷氧基,n是0或1)或下式的基团:其中 R2是氢或烷基); Y是单键,-NH-,具有1或2个碳原子的亚烷基或-CH = CH-; 并且R 3是任选取代的烃基,或其盐。 他们表现出强烈的ACAT抑制活性。

    Thienopyridine derivatives and their pharmaceutical use
    39.
    发明授权
    Thienopyridine derivatives and their pharmaceutical use 失效
    噻吩吡啶衍生物及其药物用途

    公开(公告)号:US5143919A

    公开(公告)日:1992-09-01

    申请号:US744492

    申请日:1991-08-13

    IPC分类号: C07D495/04

    CPC分类号: C07D495/04

    摘要: Thienopyridine derivatives of the formula (I): ##STR1## wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: ##STR2## (wherein R.sup.1 is hydrogen, alkyl or alkoxy; and n is 0 or 1) or a group of the formula: ##STR3## (wherein R.sup.2 is hydrogen or alkyl); Y is a single bond, --NH--, alkylene having 1 or 2 carbon atoms or --CH.dbd.CH--; and R.sup.3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.