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145 条记录 (耗时 0.02 秒)

    Novel D-homosteroids
    17.
    发明授权
    Novel D-homosteroids 失效
    新型D-类固醇激素

    公开(公告)号：US4578475A

    公开(公告)日：1986-03-25

    申请号：US573983

    申请日：1984-01-26

    申请人： Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： A61K31/15 ,  A61K31/275 ,  C07J63/00 ,  C07J71/00 ,  C07D211/70 ,  C07D307/94

    CPC分类号： C07J71/001 ,  C07J63/008 ,  C07J71/0047 ,  C07J71/0063

    摘要： The novel D-homosteroids of the formula ##STR1## wherein R.sup.1 represents a --CN, .dbd.NOH or .dbd.CH--NHOH group; R.sup.2 represents oxo or, where R.sup.1 represents a --CN group, R.sup.2 represents oxo or a --OAc group; or R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 of the steroid skeleton represents a [2,3-d]-fused isoxazole ring, a [3,2-c]-fused pyrazole ring, a [3,2-c]-fused N-acylated pyrazole ring or a [2,3-c]-fused furazan ring; Ac represents an acyl group; R.sup.3 and R.sup.4 represent methyl and R.sup.5 and R.sup.6 together represent an additional bond between carbon atoms 5 and 6 of the steroid skeleton; or R.sup.4 and R.sup.5 together represent --O--, R.sup.3 represents hydrogen or methyl, and R.sup.6 represents hydrogen; R.sup.7 represents hydrogen, lower-alkyl or ethynyl; R.sup.8 represents hydroxy or acyloxy; or R.sup.7 and R.sup.8 together represent a spiroether group of the formula ##STR2## or a spirolactone group of the formula ##STR3## the dotted 16,17-bond is an optional additional carbon-carbon bond; and the dotted 2,3-bond is an additional carbon-carbon bond when R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 form the isoxazole or pyrazole ring or when R.sup.2 represents a --OAc group,inhibit the synthesis of progesterone in organisms and can be used for fertility control. The novel D-homosteroids can be manufactured by molecular modifications of other D-homosteroids.

    摘要翻译： 式中，R1表示-CN，= NOH或= CH-NHOH基团的新型D-类固醇类化合物。 R 2表示氧代，或其中R 1表示-CN基，R 2表示氧代或-OCc基; 或R 1和R 2与类固醇骨架的碳原子2和3一起代表[2,3-d] - 稠合的异恶唑环，[3,2-c] - 引入的吡唑环，[3,2-c] - 引入的N-酰化吡唑环或[2,3-c] - 呋喃环; Ac表示酰基; R3和R4表示甲基，R5和R6一起代表类固醇骨架的碳原子5和6之间的附加键; 或R 4和R 5一起表示-O-，R 3表示氢或甲基，R 6表示氢; R7表示氢，低级烷基或乙炔基; R8表示羟基或酰氧基; 或者R 7和R 8一起表示式Ia的螺醚基或式Ia的螺内酯基团，点缀的16,17-键是任选的另外的碳 - 碳键; 当R 1和R 2与碳原子2和3一起形成异恶唑或吡唑环时，或当R 2表示-OAc基团时，虚线的2,3-键是另外的碳 - 碳键，抑制生物体中孕酮的合成， 用于生育控制。 新型D-类固醇可以通过其他D-类固醇激素的分子修饰来制造。

    D-homo-19-norsteroids
    18.
    发明授权
    D-homo-19-norsteroids 失效
    D-homo-19-降胆固醇

    公开(公告)号：US3984476A

    公开(公告)日：1976-10-05

    申请号：US621850

    申请日：1975-10-14

    申请人： Andor Furst ,  Marcel Muller ,  Jurg Albert Walter Gutzwiller ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Andor Furst ,  Marcel Muller ,  Jurg Albert Walter Gutzwiller ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： C07J63/00 ,  C07C49/45

    CPC分类号： C07J63/008 ,  Y10S514/843

    摘要： D-Homosteroids of the formula ##SPC1##Wherein R.sup.3 .alpha. is hydrogen, R.sup.3 .beta. is hydrogen, lower alkanoyloxy or aroyloxy and R.sup.3 .alpha. and R.sup.3 .beta. taken together are oxo; R.sup.13 is lower alkyl; R.sup.17a .beta. is hydrogen, lower alkanoyl, aroyl or lower alkyl; R.sup.17a .alpha. is hydrogen, lower alkyl, ethynyl, 1-propynyl, vinyl, chloroethynyl, butadiynyl or propadienyl and the dotted line in the A-ring denotes an additional carbon bond in either the 4,5- or 5(10)-position and processes for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as contraceptives and regulators of the female menstrual cycle.

    摘要翻译： 式中的D-类固醇，其中R3为氢，R3为氢，低级烷酰氧基或芳酰基，R3和R3为一起为氧代; R 13是低级烷基; R17aβ是氢，低级烷酰基，芳酰基或低级烷基; R17aa是氢，低级烷基，乙炔基，1-丙炔基，乙烯基，氯乙炔基，丁二炔基或丙二烯基，A环中的虚线表示在4,5-或5（10） - 位中的另外的碳键， 公开了其制备方法。

    D-Homo-19-norsteroids
    19.
    发明授权
    D-Homo-19-norsteroids 失效
    D-Homo-19-诺贝星

    公开(公告)号：US4057561A

    公开(公告)日：1977-11-08

    申请号：US770433

    申请日：1977-02-22

    申请人： Andor Furst ,  Jurg Gutzwiller ,  Marcel Muller ,  Rudolf Wiechert ,  Ulrich Eder ,  Gunter Neef

    发明人： Andor Furst ,  Jurg Gutzwiller ,  Marcel Muller ,  Rudolf Wiechert ,  Ulrich Eder ,  Gunter Neef

    IPC分类号： C07J63/00 ,  C07C49/48 ,  C07C69/02 ,  C07D309/22

    CPC分类号： C07J63/008

    摘要： D-homosteroids of the formula ##STR1## WHEREIN R.sup.3.alpha. is hydrogen, R.sup.3.beta. is hydroxy, lower alkanoyloxy or aroyloxy and R.sup.3.alpha. and R.sup.3.beta. taken together are oxo; R.sup.17a.alpha. is hydrogen, lower alkyl, ethynyl, vinyl, allyl, methallyl, propadienyl, 1-propynyl, butadiynyl or chloroethynyl; R.sup.17a.beta. is hydrogen, alkanoyl, aroyl, lower alkyl, cycloalkyl-lower-alkyl, benzyl, furfuryl or tetrahydropyranyl; R.sup.18 is hydrogen or methyl and the dotted line in the C-ring denotes an additional carbon to carbon bond in the 11,12-position andProcesses for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as ovulation inhibitors and androgenic/anabolic agents.

    摘要翻译： 式中的β-均质甾族化合物，其中R3a是氢，R3β是羟基，低级烷酰氧基或芳酰氧基，R3a和R3β一起是氧代; R17a是氢，低级烷基，乙炔基，乙烯基，烯丙基，甲代烯丙基，丙炔基，1-丙炔基，丁二炔基或氯乙炔基; R17aβ是氢，烷酰基，芳酰基，低级烷基，环烷基 - 低级 - 烷基，苄基，糠基或四氢吡喃基; R18是氢或甲基，C环中的虚线表示11,12位中的另外的碳 - 碳键，并且其制备方法被公开。