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    13-Thia-prostacycline derivatives
    1.
    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。

    Process for making bicyclic lactone derivatives for use as intermediates in the synthesis of prostaglandins
    3.
    发明授权
    Process for making bicyclic lactone derivatives for use as intermediates in the synthesis of prostaglandins 失效
    用于制备前列腺素合成中的二环内酯衍生物的方法

    公开(公告)号：US4204999A

    公开(公告)日：1980-05-27

    申请号：US952950

    申请日：1978-10-20

    申请人： Istvan Tomoskozi ,  Gabor Kovacs ,  Istvan Szekely ,  Vilmos Simonidesz ,  Marianna Lovasz nee Gaspar ,  Borbala Keresztesnee Ordog ,  Julia Remport nee Radoczi ,  Istvan Stadler ,  Zsuzsa Visky nee Gombos ,  Csaba Szantay

    发明人： Istvan Tomoskozi ,  Gabor Kovacs ,  Istvan Szekely ,  Vilmos Simonidesz ,  Marianna Lovasz nee Gaspar ,  Borbala Keresztesnee Ordog ,  Julia Remport nee Radoczi ,  Istvan Stadler ,  Zsuzsa Visky nee Gombos ,  Csaba Szantay

    IPC分类号： C07D307/935 ,  C07D493/04 ,  C07D493/02 ,  C07D307/77

    CPC分类号： C07D307/935 ,  C07D493/04

    摘要： A process for the preparation of optically active or racemic lactone diol derivatives of the formula ##STR1## (for use as intermediates in the Corey prostaglandin synthesis). Optically active or racemic lactone diol derivatives are inclosed, in whichR.sup.3 and R.sup.4 are the same or different and stand for a hydrogen, or a lower alkanoyl optionally substituted with one, two or three halogen atoms, or form together a ##STR2## group, in which R.sup.5 and R.sup.6 are the same or different and stand for a hydrogen, alkyl or aryl, with a process for preparing them.According to the invention the above compound are prepared by reacting optically active or racemic lactone of the formula II with formaldehyde or with a formaldehyde polymerisate, in the presence of the mixture of a strong acid and water or of a lower alkane carboxylic acid optionally substituted with one, two or three halogen atoms, and then optionally subjecting the obtained compound of the general formula I, in which R.sup.3 and/or R.sup.4 stand for an alkanoyl optionally substituted with one, two or three halogen atoms to partial or total hydrolysis or alcoholysis in an acid or alkaline medium and/or reacting it with the oxo-compounds of the formula R.sup.5 --CHO or R.sup.6 --CO--R.sup.5 or with the acetals of the above compounds.The compounds according to the invention are useful intermediates in the Corey prostaglandine synthesis.

    摘要翻译： 制备式（IMAGE）的光学活性或外消旋内酯二醇衍生物的方法（用作Corey前列腺素合成中的中间体）。 光学活性或外消旋内酯二醇衍生物被封闭，其中R3和R4相同或不同，代表氢，或任选被一个，两个或三个卤素原子取代的低级烷酰基，或一起形成一个< 其中R5和R6相同或不同，代表氢，烷基或芳基，具有制备它们的方法。 根据本发明，上述化合物通过使式II的光学活性或外消旋内酯与甲醛或甲醛聚合物在强酸和水的混合物或任选被 一个，两个或三个卤素原子，然后任选地使得到的通式I的化合物，其中R 3和/或R 4代表任选被一个，两个或三个卤素原子取代的烷酰基部分或全部水解或醇解 酸或碱性介质和/或使其与式R5-CHO或R6-CO-R5的氧代化合物或与上述化合物的缩醛反应。 根据本发明的化合物在Corey前列腺素合成中是有用的中间体。

    7-Oxo-PGI.sub.2 -derivatives and process for the preparation thereof and pharmaceutical compositions containing same
    7.
    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

    申请人： Vilmos Simonidesz ,  Agnes Papp nee Behr ,  Gabor Kovacs ,  Jozsef Ivanics ,  Julia Der nee Foldvary ,  Istvan Stadler ,  Istvan Pallagi

    发明人： Vilmos Simonidesz ,  Agnes Papp nee Behr ,  Gabor Kovacs ,  Jozsef Ivanics ,  Julia Der nee Foldvary ,  Istvan Stadler ,  Istvan Pallagi

    IPC分类号： C07D307/937 ,  A61K31/34 ,  A61K31/557 ,  C07D307/935

    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。