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    Benzopyran derivatives and processes for the preparation thereof
    23.
    发明授权
    Benzopyran derivatives and processes for the preparation thereof 失效
    苯并吡喃衍生物及其制备方法

    公开(公告)号：US5236935A

    公开(公告)日：1993-08-17

    申请号：US886986

    申请日：1992-05-21

    申请人： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    发明人： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    IPC分类号： C07D405/04

    CPC分类号： C07D405/04

    摘要： The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.E is a hydrogen atom, or a C.sub.1-6 alkyl, cyclopropyl, cyclopropylmethyl or benzyl group; R.sup.F is --COR.sup.A or --CSR.sup.A ; X is O, S or NR.sup.C, and n is an integer from 0 to 3, wherein R.sup.A and R.sup.C have the same meanings as defined above;R.sub.3 is a C.sub.1-4 straight or branched alkyl group; andR.sub.4 is ##STR4## wherein R.sup.G and R.sup.H are, each independently, a C.sub.-16 alkyl group or an optionally substituted phenyl group; A and B are, each independently, S or O; and Z is a C.sub.1-3 straight or branched alkyl group.

    摘要翻译： 本发明涉及新型的式（I）的苯并吡喃衍生物，其通过降低血压以及对血管平滑肌的松弛活性而在治疗高血压方面具有优异的选择性。 本发明还涉及制备这些化合物的方法; 以及含有这些化合物作为活性成分的药物组合物。 （I）其中：R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，-SO2RC或-SO2NRCRD，其中X1，X2和X3各自独立地是氟，氯或氢 原子; RA和RB各自独立地为氨基，C 1-6烷氧基，C 1-6烷基或任选取代的苯基; 和RC和RD是氢原子，或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是 其中RE是氢原子或C1-6烷基，环丙基，环丙基甲基或苄基; RF是-CORA或-CSRA; X是O，S或NRC，n是0-3的整数，其中RA和RC具有与上述相同的含义; R3是C1-4直链或支链烷基; 并且R 4是，其中RG和RH各自独立地是C 16-16烷基或任选取代的苯基; A和B各自独立地为S或O; Z为直链或支链的C1-3烷基。