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    Anti-androgen compounds
    4.
    发明授权
    Anti-androgen compounds 失效
    抗雄激素化合物

    公开(公告)号：US4081458A

    公开(公告)日：1978-03-28

    申请号：US800673

    申请日：1977-05-26

    申请人： Michael E. Flaugh

    发明人： Michael E. Flaugh

    IPC分类号： C07C45/54 ,  C07C45/65 ,  C07C45/74 ,  C07C49/603 ,  C07C49/623 ,  C07D493/04

    CPC分类号： C07D493/04 ,  C07C45/54 ,  C07C45/65 ,  C07C45/74 ,  C07C49/603 ,  C07C49/623 ,  Y10S514/859

    摘要： Compounds of the formula ##STR1## in which each R is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, cyano, or halo, and both R groups are identical and are symmetrically located; R.sub.1 is C.sub.1 -C.sub.3 alkyl and R.sub.2 is methyl, or R.sub.1 and R.sub.2 taken together are (CH.sub.2 --.sub.n in which n is an integer from 4 to 6; and (1) X.sub.c and X.sub.d are hydrogen, and the combination of X.sub.a and Y.sub.a and of X.sub.b and Y.sub.b each represents a double bond, subject to the limitation that, when R.sub.1 is C.sub.1 -C.sub.3 alkyl and is other than methyl, X.sub.c, X.sub.d, and R.sub.1 are all in an .alpha.-configuration; or (2) X.sub.a, X.sub.b, X.sub.c, X.sub.d, Y.sub.a, and Y.sub.b are hydrogen, subject to the limitation that both X.sub.c and X.sub.d are in an .alpha.-configuration, both X.sub.a and X.sub.b are in an .alpha.-configuration or in a .beta.-configuration, and, R.sub.1, when it is C.sub.1 -C.sub.3 alkyl, is in an .alpha.-configuration, are useful in inhibiting the action of androgens or are intermediates to such anti-androgen compounds.

    摘要翻译： 其中每个R是氢，C 1 -C 4烷基，C 1 -C 4烷氧基，羟基，氰基或卤素，和两个R基团的式“IMAGE”的化合物是相同的并且对称地定位; R1是C1-C3烷基，R2是甲基，或者R1和R2一起是（CH2-n，其中n是4-6的整数;和（1）Xc和Xd是氢，Xa和Ya的组合 并且Xb和Yb各自表示双键，但受限于当R 1为C 1 -C 3烷基且不同于甲基时，X c，X d和R 1均为α-构型;或（2）Xa， Xb，Xc，Xd，Ya和Yb是氢，Xc和Xd都是α构型的限制，Xa和Xb都是α构型或β构型，R1， 当它是C1-C3烷基时，是α-构型，可用于抑制雄激素的作用或者是这种抗雄激素化合物的中间体。

    Process for the preparation of alkylated cyclopentenones
    7.
    发明授权
    Process for the preparation of alkylated cyclopentenones 失效
    烷基化环戊烯酮的制备方法

    公开(公告)号：US4499297A

    公开(公告)日：1985-02-12

    申请号：US552462

    申请日：1983-11-16

    申请人： Valentin Rautenstrauch

    发明人： Valentin Rautenstrauch

    IPC分类号： C07C69/02 ,  B01J31/00 ,  C07B61/00 ,  C07C45/00 ,  C07C45/54 ,  C07C49/597 ,  C07C49/623 ,  C07C67/00 ,  C07C69/145 ,  C11B9/00 ,  C07C45/48

    CPC分类号： C11B9/003 ,  C07C45/54 ,  C07C69/145

    摘要： Cyclopentenones of formula ##STR1## wherein each of symbols R.sup.1 and R.sup.2, when taken separately, represents an alkyl radical of C.sub.1 to C.sub.6, or a hydrogen atom, or, when taken together, they represent a polymethylene, or one of them designates a hydrogen atom and the other an alkyl radical of C.sub.1 to C.sub.6, are prepared starting from compounds having formula ##STR2## wherein R stands for a C.sub.1 to C.sub.6 alkyl radical or a phenyl group, via a catalytic reaction promoted by a metallo-organic compound of formulaMeX.sub.2 (R.sup.3 CN).sub.2 (III)wherein Me represents palladium or platinum, R.sup.3 represents a C.sub.1 to C.sub.3 alkyl radical or a phenyl group and X defines a halogen atom.

    摘要翻译： 式（I）的环戊烯酮，其中符号R1和R2各自单独表示C1至C6的烷基或氢原子，或者当它们一起表示聚亚甲基或其中之一时， 表示氢原子，另一个为C 1〜C 6的烷基，由具有式（II）的化合物开始制备，其中R表示C1至C6烷基或苯基，通过由 式MeX2（R3CN）2（Ⅲ）的金属有机化合物，其中Me表示钯或铂，R3表示C1至C3烷基或苯基，X表示卤素原子。