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    Acylaminoquinazoline derivatives and a pharmaceutical composition containing them
    5.
    发明授权
    Acylaminoquinazoline derivatives and a pharmaceutical composition containing them 失效
    酰氨基喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：US4495188A

    公开(公告)日：1985-01-22

    申请号：US324425

    申请日：1981-11-24

    申请人： Yasunobu Sato ,  Hiroshi Fukumi ,  Hiroyuki Koike ,  Nobuaki Kitahara

    发明人： Yasunobu Sato ,  Hiroshi Fukumi ,  Hiroyuki Koike ,  Nobuaki Kitahara

    IPC分类号： C07D413/14 ,  A61K31/505 ,  A61K31/55 ,  A61P9/12 ,  C07D207/16 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14

    CPC分类号： C07D207/16

    摘要： Acylaminoquinazoline derivatives of formula ##STR1## (in which: R.sup.1 represents a lower alkoxy group, a substituted or unsubstituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a vinyl group having an optionally substituted phenyl or furyl substituent, an optionally substituted phenyl group, a furyl group, an oxazolyl group, a methylthiooxadiazolyl group or a tetrahydrofuryl group;R.sup.2 represents a hydrogen atom or a lower alkyl group;R.sup.3 represents a lower alkyl group or an optionally substituted phenyl group;R.sup.4 represents a hydrogen atom or an acyloxy-substituted phenyl group;X represents a methylene group or a sulphur atom; andn is 2 or 3)and pharmaceutically acceptable acid addition salts thereof are valuable antihypertensive agents and inhibit the activity of the angiotension I-converting enzyme. They may be prepared by reacting a 4-aminoquinazoline derivative with a carboxylic acid or reactive derivative thereof corresponding to the amide group which it is desired to introduce at the 4- position of said compound of formula (I). The compounds of the invention may be formulated with conventional pharmaceutically acceptable carriers or diluents to provide a pharmaceutical composition.

    摘要翻译： 式（I）的酰氨基喹唑啉衍生物（其中：R1表示低级烷氧基，取代或未取代的低级烷基，环烷基，低级烯基，具有任意取代的苯基或呋喃基取代基的乙烯基， 任选取代的苯基，呋喃基，恶唑基，甲硫基二唑基或四氢呋喃基; R 2表示氢原子或低级烷基; R 3表示低级烷基或任意取代的苯基; R 4表示氢 原子或酰氧基取代的苯基; X表示亚甲基或硫原子; n为2或3）及其药学上可接受的酸加成盐是有价值的抗高血压药，并且抑制血管紧张素I转化酶的活性。 它们可以通过4-氨基喹唑啉衍生物与其中所需的引入式（I）化合物的4-位的酰胺基的羧酸或其反应性衍生物反应来制备。 本发明的化合物可以与常规的药学上可接受的载体或稀释剂配制以提供药物组合物。