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    13-Thia-prostacycline derivatives
    4.
    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
    5.
    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。

    2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation
    8.
    发明授权
    2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation 失效
    2,3,4-三硝基间亚苯基前列腺素衍生物及其抑制血小板聚集的组合物和方法

    公开(公告)号：US4451483A

    公开(公告)日：1984-05-29

    申请号：US367068

    申请日：1982-04-09

    申请人： Istvan Szekely ,  Krisztina Kekesi ,  Mariann Lovasz nee Gaspar ,  Sandor Botar ,  Pal Hadhazy ,  Istvan Rakoczi ,  Laszlo Muszbek ,  Judit Skopal ,  Istvan Stadler ,  Karoly Horvath ,  Gabor Kovacs ,  Peter Kormoczy

    发明人： Istvan Szekely ,  Krisztina Kekesi ,  Mariann Lovasz nee Gaspar ,  Sandor Botar ,  Pal Hadhazy ,  Istvan Rakoczi ,  Laszlo Muszbek ,  Judit Skopal ,  Istvan Stadler ,  Karoly Horvath ,  Gabor Kovacs ,  Peter Kormoczy

    IPC分类号： A61K31/5575 ,  C07C405/00 ,  C07D307/937 ,  A61K31/34 ,  C07D307/935

    CPC分类号： C07D307/937 ,  C07C405/00 ,  C07C405/0041 ,  Y10S514/822

    摘要： 2,3,4-trinor-1,5-inter-m-phenylene-prostacycline derivatives of the formula (I), ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1-4 alkyl group, an alkali metal cation or a primary, secondary, tertiary or quaternary ammonium cation,R.sup.2 and R.sup.3 each represent hydrogen or a C.sub.1-4 alkanoyl, benzoyl, substituted benzoyl, tetrahydropyranyl, ethoxyethyl or tri-(C.sub.1-4 alkyl)-silyl group,R.sup.4 is hydrogen or a C.sub.1-4 alkyl group, andR.sup.5 is a hexyl, heptyl, phenoxymethyl or m-trifluoromethylphenoxymethyl group, orR.sup.5 represents a group of the general formula ##STR2## and in this latter formula Z is an amino group or an optionally halo-substituted C.sub.1-4 alkanoylamino, benzoylamino or tosylamino group, andR.sup.6 is a C.sub.4-6 alkyl, phenyl or benzyl group,are prepared by reacting a bicyclic lactol of the formula (II), ##STR3## with a reactive phosphorane prepared from a triphenyl-m-carbobenzylphosphonium halide and a strong base, optionally esterifying the resulting prostaglandin derivative and, whenever it contains a free amino group, protecting this amino group by acylation, reacting then the prostaglandin derivative with an electrophilic reagent of the formula E-X, wherein X is halogen atom and E is halogen atom or an acetyl, trifluoroacetyl or N-succinimido group, and subjecting the resulting halogenated PGI.sub.1 derivative to hydrogen halide elimination. The compounds of the formula (I) possess valuable biological effects and can be applied in therapy primarily as blood platelet aggregation inhibiting agents.

    摘要翻译： 式（I）的2,3,4-三硝基-1,5-间 - 间 - 亚苯基 - 前列环素衍生物，其中R 1是氢，C 1-4烷基，碱金属阳离子或 伯，仲，叔或季铵阳离子，R2和R3各自表示氢或C1-4烷酰基，苯甲酰基，取代的苯甲酰基，四氢吡喃基，乙氧基乙基或三（C1-4烷基） - 甲硅烷基，R4是氢或 C 1-4烷基，R 5为己基，庚基，苯氧基甲基或间三氟甲基苯氧基甲基，或R 5表示通式“IMAGE”的基团，在后一式中Z为氨基或任意卤素取代的C1 -4烷酰基氨基，苯甲酰氨基或甲苯磺酰氨基，R6是C4-6烷基，苯基或苄基，是通过使式（II）的双环内酰醇与式（II）的双环内酰醇与由 三苯基-m-苄基苄基卤化鏻和强碱，任选地酯化所得的前列腺素衍生物，并且每当其含有时 游离氨基，通过酰化保护该氨基，然后将前列腺素衍生物与式EX的亲电试剂反应，其中X是卤素原子，E是卤素原子或乙酰基，三氟乙酰基或N-琥珀酰亚胺基，并使 得到的卤化PGI1衍生物消除卤化氢。 式（I）化合物具有有价值的生物学效应，可用作主要作为血小板聚集抑制剂的治疗。