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    13-Thia-prostacycline derivatives
    8.
    发明授权
    13-Thia-prostacycline derivatives 失效
    13-前列环素衍生物

    公开(公告)号：US4425358A

    公开(公告)日：1984-01-10

    申请号：US370503

    申请日：1982-04-21

    申请人： Csaba Szantay ,  Lajos Novak ,  Jozsef Aszodi ,  Vilmos Simonidesz ,  Geza Galambos ,  Gabor Kovacs ,  Sandor Virag ,  Istvan Stadler ,  Peter Kormoczy

    发明人： Csaba Szantay ,  Lajos Novak ,  Jozsef Aszodi ,  Vilmos Simonidesz ,  Geza Galambos ,  Gabor Kovacs ,  Sandor Virag ,  Istvan Stadler ,  Peter Kormoczy

    IPC分类号： C07D307/935 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  C07C405/00 ,  C07D307/937 ,  C07D407/12

    CPC分类号： C07D307/937 ,  C07C405/0033 ,  C07D407/12 ,  Y10S514/822

    摘要： The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.

    摘要翻译： 本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物，其中R1是氢，可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - ， - CH = CH-或-C 3 D C-; 符号X和Y之一是氢，甲基或乙基，另一个是羟基，四氢吡喃基氧基，1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。 式I的化合物可以通过使式III的13-前 - 前列腺素（III）反应来制备。

    Vasodilative 4-thia-PGI.sub.1 and 4-sulfinyl-PGI.sub.1 and derivatives thereof
    9.
    发明授权
    Vasodilative 4-thia-PGI.sub.1 and 4-sulfinyl-PGI.sub.1 and derivatives thereof 失效
    血管扩张型4-thia-PGI1和4-亚磺酰基-PGI1及其衍生物

    公开(公告)号：US4379164A

    公开(公告)日：1983-04-05

    申请号：US314433

    申请日：1981-10-23

    申请人： Istvan Tomoskozi ,  Peter Gyory ,  Gabor Kovacs ,  Sandor Virag ,  Peter Kormoczy ,  Istvan Stadler

    发明人： Istvan Tomoskozi ,  Peter Gyory ,  Gabor Kovacs ,  Sandor Virag ,  Peter Kormoczy ,  Istvan Stadler

    IPC分类号： C07D307/935 ,  A61K31/557 ,  A61K31/5575 ,  A61P1/04 ,  A61P9/08 ,  A61P11/08 ,  C07C405/00 ,  C07D307/937 ,  A61K31/335

    CPC分类号： C07D307/937

    摘要： A compound having vasodilative, bronchodilative, stomach-mucosa-protective and platelet-aggregation-inhibiting activity has the formulaA 4-thia- or 4-sulfinyl-PGI.sub.1 -compound of the formula I ##STR1## wherein Q stands for --S-- or --SO--,A stands for C.sub.1-6 straight or branched chain alkylene,B stands for ethylene, vinylene or ethinylene,R.sup.1 represents hydrogen or C.sub.1-4 alkyl,R.sup.2 represents C.sub.1-8 straight or branched chain alkyl or mono-substituted aryl-oxy-methyl,R.sup.3 stands for hydrogen or acetyl, andZ represents --COOH, --CN, --CH.sub.2 OH or --COOW, wherein W stands for an equivalent of a pharmacologically acceptable cation or C.sub.1-4 alkyl.

    摘要翻译： 具有血管扩张性，支气管扩张性，胃粘膜保护性和血小板聚集抑制活性的化合物具有式I的4-硫杂或4-亚磺酰基-GlyI化合物，其中Q代表 - S-或-SO-，A代表C 1-6直链或支链亚烷基，B代表亚乙基，亚乙烯基或亚乙烯基，R 1代表氢或C 1-4烷基，R 2代表C1-8直链或支链烷基或单 - 取代的芳氧基 - 甲基，R3代表氢或乙酰基，Z代表-COOH，-CN，-CH2OH或-COOW，其中W代表药理学上可接受的阳离子或C 1-4烷基的当量。