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    Novel 20 benzcylamino pregnene derivatives and process for preparing same
    5.
    发明授权
    Novel 20 benzcylamino pregnene derivatives and process for preparing same 失效
    新型20苄基氨基孕烯衍生物及其制备方法

    公开(公告)号：US4668437A

    公开(公告)日：1987-05-26

    申请号：US775347

    申请日：1985-09-11

    申请人： Sandor Solyom ,  Lajos Toldy ,  Katalin Szilagyi nee Farago

    发明人： Sandor Solyom ,  Lajos Toldy ,  Katalin Szilagyi nee Farago

    IPC分类号： C07J5/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J

    CPC分类号： C07J33/007 ,  C07J41/005 ,  C07J43/003 ,  C07J5/0015

    摘要： The invention relates to new pregnene derivatives of the general formula (I), ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for a hydrogen atom or a C.sub.2-4 alkanoyl group;R.sup.3 stands for a hydrogen atom, a hydroxyl group or a C.sub.2-4 alkanoyloxy group;A represents a ring of the general formula (1) ##STR2## or a ring of the general formula (2), ##STR3## wherein R.sup.4 means a hydrogen atom or a methyl group;R.sup.5 stands for a hydroxyl group, a C.sub.2-4 alkanoyloxy group or a C.sub.1-3 alkoxy group;R.sup.6 means a hydroxyl group, a C.sub.2-4 alkanoyloxy group, a C.sub.1-3 alkoxy group, an oxo group or a C.sub.2-3 alkylenedithio group; the dotted line optionally represents one or more additional valence bonds, with the proviso that, when the dotted line between C.sub.9 and C.sub.11 represents an additional valence bond, then R.sup.3 stands for a hydrogen atom; and the wavy line shows that the given substituent can be bound to the carbon atom in two alternative spatial arrangements,as well as to their stereoisomers and the mixture of these stereoisomers.The compounds of the general formula (I) are valuable intermediates for the synthesis of known biologically active 21-hydroxyprogesterone derivatives.

    摘要翻译： 本发明涉及通式（I）的新孕烯衍生物，其中R1代表C1-4烷基; R2代表氢原子或C2-4烷酰基; R3代表氢原子，羟基或C2-4烷酰氧基; A表示通式（1）的环，（1）或通式（2）的环，其中R 4表示氢原子或甲基; R5代表羟基，C2-4烷酰氧基或C1-3烷氧基; R6表示羟基，C2-4烷酰氧基，C1-3烷氧基，氧代基或C2-3亚烷基二硫基; 虚线可选地表示一个或多个另外的价键，条件是当C9和C11之间的虚线表示另外的价键时，则R3代表氢原子; 并且波浪线表示给定的取代基可以以两种可选的空间排列结合于碳原子，以及它们的立体异构体和这些立体异构体的混合物。 通式（I）的化合物是合成已知生物活性的21-羟孕酮衍生物的有价值的中间体。

    Steroid-spiro-oxathiazolidine derivatives and a process for the preparation thereof
    8.
    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。

    Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof
    9.
    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。