Tricyclic compounds and intermediates thereof
    4.
    发明公开
    Tricyclic compounds and intermediates thereof 失效
    Tricyclische Verbindungen und ihre Zwischenprodukte。

    公开(公告)号:EP0497201A1

    公开(公告)日:1992-08-05

    申请号:EP92101012.0

    申请日:1992-01-22

    摘要: Disclosed is a tricyclic compound represented by the formula (I):

    wherein each of R¹, R², R³ and R⁴ independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR⁹R¹⁰CO₂R¹¹ (wherein each of R⁹, R¹⁰ and R¹¹ independently represents hydrogen or C1-6 alkyl) or CONR¹²R¹³ (wherein each of R¹² and R¹³ independently represents hydrogen or C1-6 alkyl); R⁵ represents hydrogen or C1-6 alkyl; each of R⁶, R⁷ and R⁸ independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y¹-Y² represents CH₂-O, CH₂-S(O) n , (wherein n represents 0, 1, or 2), CH₂CH₂, CH=CH or CON(R¹⁴) (wherein R¹⁴ represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

    摘要翻译: 公开了由式(I)表示的三环化合物:其中R 1,R 2,R 3和R 4各自独立地表示氢,C 1-6烷基,C 1-6 烷氧基,C 1-6烷硫基,氨基,C 1-6烷基氨基,卤代C 1-6烷基,卤代C 1-6烷氧基,卤素,硝基,氰基,羧基,C 1-6烷氧基羰基,羟甲基,CR 9 R 1, (其中R 9,R 1,O和R 1各自独立地表示氢或C 1-6烷基)或CONR 1 2 R 1(3)其中R 1和R 2各自独立地表示氢或C 1-6烷基)。 R 5表示氢或C 1-6烷基; R 6,R 7和R 8各自独立地表示氢,C 1-6烷基,羟基,C 1-6烷氧基,C 1-6烷酰氧基,C 1-6烷硫基,氰硫基或卤素; X表示CH或N; Y 1 -Y 2表示CH 2 -O,CH 2 -S(O)n,(其中n表示0,1或2),CH 2 CH 2,CH = CH或CON(R 1 4) (其中R 1 4代表氢或C 1-6烷基),Z代表氧或硫,或其药学上可接受的盐。 该化合物具有酰基辅酶A:胆固醇酰基转移酶抑制活性,因此预期对高脂血症和动脉硬化具有预防和治疗作用。

    1,4-Dihydropyridine derivatives
    10.
    发明公开
    1,4-Dihydropyridine derivatives 失效
    1,4-二氢吡啶衍生物

    公开(公告)号:EP0093945A3

    公开(公告)日:1984-09-12

    申请号:EP83104076

    申请日:1983-04-26

    摘要: Compounds having effects to dilate coronary artery and peripheral blood vessels and to depress the blood pressure, and useful as drugs for cardiovascular disease are represented by the following general formula:
    wherein R, represents a hydrogen atom, an alkyl group having 1-5 carbon atoms, an alkenyl group having 2-5 carbon atoms, an aralkyl group having 7-13 carbon atoms or an acyl group having 1-7 carbon atoms, R. and R 3 are the same or different groups and each represents a substituted or unsubstituted alkyl group having 1-5 carbon atoms, an alkenyl group having 2-5 carbon atoms, a disubstituted aminoalkyl group having 1-5 carbon atoms or a substituted or unsubstituted heterocyclic group, R 4 and R 5 are the same or different groups and each represents a hydrogen atom, a halogen atom or a nitro group, and R 6 and R 7 are the same or different groups and each represents an alkyl group having 1-5 carbon atoms; the pharmaceutically acceptable acid addition salt thereof are also effective therapeutic compounds.

    摘要翻译: 具有扩张冠状动脉和外周血管并降低血压的作用的化合物可用作心血管疾病的药物,其由下列通式表示:其中R 1代表氢原子,具有1-5个碳原子的烷基 具有2-5个碳原子的烯基,具有7-13个碳原子的芳烷基或具有1-7个碳原子的酰基,R和R3是相同或不同的基团并且各自表示取代或未取代的烷基 具有1-5个碳原子的链烯基,具有2-5个碳原子的链烯基,具有1-5个碳原子的二取代氨基烷基或取代或未取代的杂环基,R 4和R 5是相同或不同的基团并且各自表示氢原子 卤素原子或硝基,R6和R7是相同或不同的基团,每个代表具有1-5个碳原子的烷基; 其药学上可接受的酸加成盐也是有效的治疗化合物。