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    Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof
    2.
    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。

    Steroid-spiro-oxathiazolidine derivatives and a process for the preparation thereof
    3.
    发明授权
    Steroid-spiro-oxathiazolidine derivatives and a process for the preparation thereof 失效
    类固醇 - 螺 - 恶噻唑烷衍生物及其制备方法

    公开(公告)号：US4342754A

    公开(公告)日：1982-08-03

    申请号：US242711

    申请日：1981-03-11

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

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

    IPC分类号： A61K31/58 ,  A61P7/10 ,  C07J41/00 ,  C07J43/00

    CPC分类号： C07J41/0088 ,  C07J43/006 ,  Y10S514/869

    摘要： New steroid-spiro-oxathiazolidine derivatives pharmaceutical compositions containing the same, and to a process for the preparation thereof are disclosed.The new compounds have antimineral corticoide effects and have the following formula (I), ##STR1## wherein R.sub.1 is a C.sub.1-3 alkyl or a C.sub.2-4 alkenyl group, andZ is a group of the formulae (II) to (VI), ##STR2## wherein R.sub.2 is methyl or ethyl,R.sub.3 is hydrogen or methylR.sub.4 is hydrogen, a C.sub.1-3 alkyl group, a di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl group, a C.sub.2-4 alkylcarbonyl group, a C.sub.2-4 alkoxycarbonyl group or a C.sub.3-6 carboxyalkylcarbonyl group, andthe dotted lines may represent additional valence bonds, with the proviso that if Z is a group of the formula (VI), a double bond exists between the carbon atoms in positions 4 and 5 or 5 and 6, andif R.sub.4 is a di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl group or a C.sub.3-6 carboxyalkylcarbonyl group, the compounds may also be formed as their salts.

    摘要翻译： 公开了新的类固醇 - 螺 - 恶唑烷衍生物药物组合物及其制备方法。 新化合物具有抗皮质素的作用，具有下式（I），其中R 1为C 1-3烷基或C 2-4链烯基，Z为式（II）〜 （VI），其中R2是甲基或乙基，R3是氢或甲基R4是氢，（VI）其中R2是甲基或乙基， C 1-3烷基，二（C 1-4烷基） - 氨基-C 1-4烷基，C 2-4烷基羰基，C 2-4烷氧基羰基或C 3-6羧基烷基羰基，虚线 可以代表额外的价键，条件是如果Z是式（VI）的基团，则在4位和5位或5位和6位之间的碳原子之间存在双键，如果R4是二 - （C1- 4烷基） - 氨基-C 1-4烷基或C 3-6羧基烷基羰基，化合物也可以形成为其盐。

    6-Amino-5.beta.,19-cycloandrostane derivatives
    5.
    发明授权
    6-Amino-5.beta.,19-cycloandrostane derivatives 失效
    6-氨基-5 {62,19-环戊二烯衍生物

    公开(公告)号：US4028348A

    公开(公告)日：1977-06-07

    申请号：US658863

    申请日：1976-02-17

    申请人： Pal Bite ,  Imre Moravcsik ,  Inge Schafer ,  Gyula Horvath ,  Zsuzsanna Mehesfalvi nee Vajna ,  Janos Borvendeg ,  Ilona Hermann nee Szente

    发明人： Pal Bite ,  Imre Moravcsik ,  Inge Schafer ,  Gyula Horvath ,  Zsuzsanna Mehesfalvi nee Vajna ,  Janos Borvendeg ,  Ilona Hermann nee Szente

    IPC分类号： C07J53/00 ,  C07J41/00 ,  C07J43/00

    CPC分类号： C07J53/00

    摘要： Novel 6-amino-5.alpha.,19-cycloandrostane derivatives of formula I and their pharmaceutically acceptable addition salts ##STR1## wherein X denotes any of the groups of the formula =CH(OR), =CO or =C=N-OR.sub.1,Y denotes any of the groups of the formula =CO, =CH(OR.sub.1), =C=N-OR.sub.1, =C(OR.sub.1)-C.tbd.CH or ##STR2## wherein R denotes a hydrogen atom, a C.sub.1-4 alkyl group or a C.sub.2-5 acyl group, andR.sub.1 denotes a hydrogen atom, a straight-chained or branched C.sub.1-5 alkyl group, a straight-chained or branched C.sub.1-5 hydroxyalkyl group, a C.sub.3-8 cycloalkyl group, an allyl group, or a benzyl group, andR.sub.3 has the same meaning as R.sub.2 but if R.sub.2 is a sec. or tert. alkyl group or an alicyclic group, then R.sub.3 can only be a hydrogen atom; and if R.sub.2 is a benzyl group then R.sub.3 can only be a hydrogen atom or a primary alkyl group, furtherR.sub.2 and R.sub.3 may denote together with the adjcacent nitrogen atom a piperidine, a morpholine, or an N-methylpiperazine group. These compounds have exhibited an aldosterone-antagonistic effect on rats.

    摘要翻译： 式I的新型6-氨基-5α，19-环戊二烯衍生物及其药学上可接受的加成盐（I）其中X表示式= CH（OR），= CO或= C = N -OR1，Y表示式= CO，= CH（OR1），= C = N-OR1，= C（OR1）-C3ONDCH或者其中R表示氢原子，C1 -4-烷基或C 2-5酰基，R 1表示氢原子，直链或支链C 1-5烷基，直链或支链C 1-5羟基烷基，C 3-8环烷基， 烯丙基或苄基，R3与R2具有相同的含义，但如果R2为秒。 或叔。 烷基或脂环基，那么R 3只能是氢原子; 并且如果R 2是苄基，那么R 3只能是氢原子或伯烷基，R 2和R 3可以与相邻的氮原子一起表示哌啶，吗啉或N-甲基哌嗪基。 这些化合物对大鼠表现出醛固酮拮抗作用。