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17 条记录 (耗时 0.027 秒)

    Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof
    5.
    发明授权
    Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof 失效
    取代的类固醇 - 螺恶唑烷酮衍生物及其制备方法

    公开(公告)号：US4218446A

    公开(公告)日：1980-08-19

    申请号：US25080

    申请日：1979-03-29

    申请人： Sandor Solyom ,  Lajos Toldy ,  Katalin Szilagyi nee Farago ,  Inge Schafer ,  Eleonora Szondy ,  Janos Borvendeg ,  Ilona Hermann nee Szente

    发明人： Sandor Solyom ,  Lajos Toldy ,  Katalin Szilagyi nee Farago ,  Inge Schafer ,  Eleonora Szondy ,  Janos Borvendeg ,  Ilona Hermann nee Szente

    IPC分类号： C07J31/00 ,  A61K31/58 ,  A61P5/38 ,  C07J43/00

    CPC分类号： C07J43/006 ,  Y10S514/869

    摘要： Diuretic pharmaceutically active steroid-spiro-oxazolidinone compounds of the formula (I), ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is C.sub.1-4 alkyl,R.sup.3 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl,Z.sup.1 and Z.sup.2 each are hydrogen or together form a second valence bond, or Z.sup.1 is hydrogen and Z.sup.2 is R.sup.4 --S--,Z.sup.3 and Z.sup.4 each are hydrogen or together form a second valence bond, or Z.sup.3 is hydrogen and Z.sup.4 is R.sup.4 --S--, with at least one of the pairs Z.sup.1 -Z.sup.2 and Z.sup.3 -Z.sup.4 representing hydrogen and an R.sup.4 --S-- group, andR.sup.4 is hydrogen or alkyl, alkenyl, aralkyl or acyl with up to 7 carbon atoms, provided that when Z.sup.1 and Z.sup.2 together form a valence bond, or Z.sup.1 represents a hydrogen atom and Z.sup.2 and R.sup.4 --S-- group then R.sup.1 is methyl.

    摘要翻译： 式（I）的利尿药物活性类固醇 - 螺恶唑烷酮化合物，其中R 1是氢或甲基，R 2是C 1-4烷基，R 3是氢，C 1-4烷基或C 2-4链烯基， Z1和Z2各自为氢或一起形成第二价键，或Z1为氢，Z2为R4-S-，Z3和Z4各自为氢或一起形成第二价键，或Z3为氢，Z4为R4-S - ，其中至少一对Z1-Z2和Z3-Z4代表氢和R4-S-基团，R4是氢或具有至多7个碳原子的烷基，烯基，芳烷基或酰基，条件是当Z1和 Z2一起形成价键，或Z1表示氢原子，Z2和R4-S-基团，则R1为甲基。

    Pyrazole derivatives with an ergoline skeleton, their acid addition salts, and a process for the preparation thereof
    8.
    发明授权
    Pyrazole derivatives with an ergoline skeleton, their acid addition salts, and a process for the preparation thereof 失效
    具有麦角无骨骨架的吡唑衍生物及其酸加成盐及其制备方法

    公开(公告)号：US4632928A

    公开(公告)日：1986-12-30

    申请号：US615387

    申请日：1984-05-30

    申请人： Tivadar Rettegi ,  Erzsebet Mago nee Karacsony ,  Lajos Toldy ,  Jozsef Borsy ,  Ilona Berzetei ,  Andras Ronai ,  Aliz Druga ,  Gyorgy Cseh

    发明人： Tivadar Rettegi ,  Erzsebet Mago nee Karacsony ,  Lajos Toldy ,  Jozsef Borsy ,  Ilona Berzetei ,  Andras Ronai ,  Aliz Druga ,  Gyorgy Cseh

    IPC分类号： A61K31/48 ,  A61P1/00 ,  A61P9/12 ,  A61P11/00 ,  A61P43/00 ,  C07D457/02

    CPC分类号： C07D457/02

    摘要： The invention relates to novel pyrazole derivatives with an ergoline skeleton of the general formula I, ##STR1## wherein x . . . y stands for a ##STR2## R is a hydrogen atom or methyl group, R.sub.1 stands for a hydrogen atom, C.sub.1-4 alkyl, carbethoxy or pyridyl-group,R.sub.2 stands for a hydrogen atom, C.sub.1-4 alkyl, allyl, C.sub.2-4 oxoalkyl-, C.sub.2-4 hydroxyalkyl or C.sub.2-4 hydroxyiminoalkyl group,R.sub.3 stands for a hydrogen atom, C.sub.1-4 alkyl, hydroxy or pyridyl group, furthermoreR.sub.2 and R.sub.3 may stand together for a group of general formula (II), ##STR3## wherein Z stands for a methylene, carbonyl, hydroxymethylene or hydroxyiminomethylene group,R.sub.4 stands for a hydrogen atom or one or two C.sub.1-4 alkyl group(s), andn is 1 or 2,and pharmaceutically acceptable salts thereof.Furthermore the invention relates to a process for the preparation of these compounds.The novel compounds are potent PGF.sub.2.alpha. receptor antagonists.

    摘要翻译： 本发明涉及具有通式I的麦角灵骨架的新型吡唑衍生物，其中x。 。 。 y表示氢原子或甲基，R1表示氢原子，C1-4烷基，乙氧基或吡啶基，R2表示氢原子，C1-4烷基，烯丙基，C2- 4个氧代烷基 - ，C2-4羟基烷基或C2-4羟基亚氨基烷基，R3代表氢原子，C1-4烷基，羟基或吡啶基，此外R2和R3可以连在一起为通式（II） 图像II其中Z表示亚甲基，羰基，羟基亚甲基或羟基亚氨基亚甲基，R4表示氢原子或一个或两个C1-4烷基，n为1或2，及其药学上可接受的盐。 此外，本发明涉及一种制备这些化合物的方法。 新型化合物是有效的PGF2α受体拮抗剂。