Oxazole- and thiazole-alkanoic acid compounds
    121.
    发明授权
    Oxazole- and thiazole-alkanoic acid compounds 失效
    恶唑和噻唑 - 链烷酸化合物

    公开(公告)号:US4175130A

    公开(公告)日:1979-11-20

    申请号:US889073

    申请日:1978-03-22

    CPC classification number: C07D263/46 C07D263/42 C07D277/34 C07D277/36

    Abstract: Oxazole- and thiazole-alkanoic acid compounds useful as drugs for the treatment of atherosclerosis with lipid metabolism disorder, and having the formula: ##STR1## wherein R is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group, a pyridylmethyl group or a tocopheryl group; each of R.sup.1 and R.sup.2 is a hydrogen atom or a halogen atom; R.sup.3 is a hydrogen atom, a halogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.4 is a hydrogen atom, a halogen atom, a nitro group, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a trifuloromethyl group; each of X and Y is an oxygen atom or a sulfur atom; and A is a straight or branched alkylene group having 1 to 4 carbon atoms, and pharmaceutically acceptable salts thereof are disclosed.

    Abstract translation: 恶唑和噻唑 - 链烷酸化合物可用作用于用脂质代谢紊乱治疗动脉粥样硬化的药物,并具有下式:其中R是氢原子,具有1至4个碳原子的烷基,芳烷基, 吡啶基甲基或生育酚基; R1和R2各自为氢原子或卤素原子; R3是氢原子,卤原子或碳原子数1〜4的烷基。 R4是氢原子,卤素原子,硝基,碳原子数1〜4的烷基,碳原子数1〜4的烷氧基或三氟甲基; X和Y各自为氧原子或硫原子; A是具有1至4个碳原子的直链或支链亚烷基,并且其药学上可接受的盐被公开。

    Thiazole cardiovascular agents
    124.
    发明授权
    Thiazole cardiovascular agents 失效
    噻唑心血管药

    公开(公告)号:US4064258A

    公开(公告)日:1977-12-20

    申请号:US706342

    申请日:1976-07-19

    CPC classification number: C07D277/56 C07C31/137 C07D277/36 C07C2102/18

    Abstract: 1-Alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanol; 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene-N-alkyloxazolidine and/or 2-substituted oxazolidine derivatives thereof, and methods of making such compounds. The compounds exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The compounds are also useful in the treatment of hypertension in mammals. The 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidines and derivatives are also intermediates for the 1-alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanols. The 1-alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanols can be prepared by base or acid hydrolysis of the corresponding 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine or derivative; or by treatment of the corresponding 3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2,3-epoxypropane with the desired alkylamine. Similarly the 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine or derivative can be prepared from the corresponding 1-alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanols via treatment with an aldehyde or ketone.

    Abstract translation: 1-烷基氨基-3-(5-碳代环烷基氨基羰基噻唑-2-基氧基)-2-丙醇; 5-(5-碳代环烷基氨基羰基噻唑-2-基氧基亚甲基-N-烷基氮杂环丁烷和/或其2-取代的恶唑烷衍生物及其制备方法,该化合物表现出心血管活性,可用于治疗哺乳动物异常心脏病。 5-(5-碳代环烷基氨基羰基噻唑-2-基氧基亚甲基)-N-烷基噻唑啉及其衍生物也是1-烷基氨基-3-(5-碳代环烷基氨基羰基噻唑-2-基) 1-烷基氨基-3-(5-碳代环烷基氨基羰基噻唑-2-基氧基)-2-丙氧基甲醇可以通过碱或水解相应的5-(5-碳代环烷基氨基羰基噻唑-2-基氧基亚甲基) )-N-烷氧基唑烷或衍生物;或通过用所需的烷基胺处理相应的3-(5-碳代环烷基氨基羰基噻唑-2-基氧基)-2,3-环氧丙烷。类似地,5-(5-碳环烷基氨基羰基硫 唑烷-2-基氧基亚甲基)-N-烷氧基唑烷或衍生物可以通过用醛或酮处理由相应的1-烷基氨基-3-(5-碳代环烷基氨基羰基噻唑-2-基氧基)-2-丙醇的惰性醇制备。

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