7-Oxo-PGI.sub.2 -derivatives and process for the preparation thereof and
pharmaceutical compositions containing same
    3.
    发明授权
    7-Oxo-PGI.sub.2 -derivatives and process for the preparation thereof and pharmaceutical compositions containing same 失效
    7-氧代-PGI2-衍生物及其制备方法和含有它们的药物组合物

    公开(公告)号:US4330553A

    公开(公告)日:1982-05-18

    申请号:US205292

    申请日:1980-11-10

    CPC分类号: C07D307/937

    摘要: New PGI.sub.2 derivatives and a process for their preparation are disclosed of the formula (I) ##STR1## wherein Q is hydrogen, a pharmacologically acceptable cation, or lower alkyl;A is cis or trans --CH.dbd.CH--, --C.tbd.C--, or --CH.sub.2 --CH.sub.2 --;R.sup.13 is hydrogen or a C.sub.1 to C.sub.4 alkanoyl or is a blockinggroup of the formula R.sup.7 R.sup.8 R.sup.9 Si or ##STR2## wherein R.sup.7, R.sup.8 and R.sup.9 are the same or different and can be straight or branched chain alkyl groups having 1 to 4 carbon atoms and R.sup.10 and R.sup.11 are the same or different and can be hydrogen or methyl, and R.sup.12 represents methyl or ethyl, or is tetrahydropyran-2-yl;R.sup.4 is hydrogen or lower alkyl inthe .alpha. or .beta. steric position;R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;Y is methylene, oxygen or an --NH-- group; andR.sup.3 is lower alkyl or phenyl which can be monosubstituted phenyl. The compounds are useful as antiaggregation or thrombus-dissolving agents, stomach juice secretion inhibiting agents and antiasthmatic agents.

    摘要翻译: 公开了新的PGI 2衍生物及其制备方法,式(I)其中Q为氢,药理学可接受的阳离子或低级烷基; A是顺式或反式-CH = CH - , - C 3BOND C - 或-CH 2 -CH 2 - ; R 13是氢或C 1至C 4烷酰基或是式R 7 R 8 R 9 Si或其中R 7,R 8和R 9相同或不同并且可以是具有1至4个碳原子的直链或支链烷基和R 10和 R 11相同或不同,可以是氢或甲基,R 12表示甲基或乙基,或是四氢吡喃-2-基; R4是氢或在α或β位置的低级烷基; R1和R2各自为氢或低级烷基; Y是亚甲基,氧或-NH-基团; 并且R 3是可以是单取代的苯基的低级烷基或苯基。 该化合物可用作抗凝聚剂或血栓溶解剂,胃液分泌抑制剂和抗哮喘剂。