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    SMALL MOLECULES FOR INHIBITING MALE FERTILITY
    91.
    发明公开
    SMALL MOLECULES FOR INHIBITING MALE FERTILITY 审中-公开
    KLEINMOLEKÜLEZUR HEMMUNG DERMÄNNLICHENFRUCHTBARKEIT

    公开(公告)号：EP3116861A1

    公开(公告)日：2017-01-18

    申请号：EP15761799.4

    申请日：2015-03-13

    申请人： The University of North Carolina at Chapel Hill

    发明人： O'RAND, Michael

    IPC分类号： C07D251/52 ,  C07D253/07 ,  C07D253/075 ,  C07D487/04 ,  C07D498/04 ,  A61K31/53 ,  A61P15/16

    CPC分类号： C07D251/52 ,  A61K31/53 ,  C07D253/07 ,  C07D253/075 ,  C07D487/04 ,  C07D498/04

    摘要： Compounds suitable for use in providing male contraception, an assay method for identifying such compounds, and methods of providing contraception using the compounds, are provided. In one embodiment, the compounds described herein mimic the binding of anti-EPPIN antibodies to EPPIN, and thus inhibit the forward motility of sperm in humans and other primates. In another embodiment, the compounds described herein inhibit or enhance EPPIN-semenogelin binding, and inhibit forward motility of sperm. The assays described herein identify compounds which inhibit sperm motility, and can be carried out in a high throughput manner, using labeled recombinant EPPIN and semenogelin. The compounds can be used in oral or transdermal compositions to temporarily and reversibly inhibit male fertility. They can also be used in addition to, or in place of, spermicides in spermicidal compositions, such as those used in conjunction with condoms, diaphragms, and spermicidal jellies.

    摘要翻译： 提供了适用于提供男性避孕的化合物，用于鉴定这些化合物的测定方法以及使用该化合物提供避孕方法。 在一个实施方案中，本文所述的化合物模拟抗EPPIN抗体与EPPIN的结合，并因此抑制精子在人和其他灵长类动物中的向前运动。 在另一个实施方案中，本文所述的化合物抑制或增强EPPIN-精液素结合，并抑制精子的向前运动。 本文描述的测定法使用标记的重组EPPIN和精液蛋白来鉴定抑制精子活力的化合物，并且可以以高通量的方式进行。 这些化合物可用于口服或透皮组合物中以暂时和可逆地抑制雄性生育力。 除了杀精组合物中的杀精剂外，还可以使用它们，例如与避孕套，隔膜和杀精胶冻结合使用的杀精剂。

    TRIAZINE DERIVATIVES
    100.
    发明公开
    TRIAZINE DERIVATIVES 有权
    三嗪衍生物

    公开(公告)号：EP2016059A2

    公开(公告)日：2009-01-21

    申请号：EP07728693.8

    申请日：2007-05-02

    申请人： Ciba Holding Inc.

    发明人： EHLIS, Thomas ,  BORSOS, Elek

    IPC分类号： C07D251/52 ,  C07D251/70 ,  A61Q17/04

    CPC分类号： C07D251/52 ,  C07D251/70

    摘要： Disclosed are triazine derivatives of formula (1), wherein X1 is a bivalent radical of formula (1a) -NR9-A-NR9-; (1b); or (1c) *-O-A-O-* A and A' independently from each other are unsubstituted or substituted, straight-chain or branched C1-C12alkylene, which is optionally interrupted by C5-C12cycloalkylene, N, O or S; C5-C12cycloalkylene; biphenylene; C6-C10arylene; or C5-C10arylene-(C1-C12alkylene); R1 is a radical of formula (1d); (1e); (1f); (1g); or (1h); R2 and R3 independently from each other are hydrogen; C1-C12alkyl; OR7; NR7R8; C6-C10aryl; X2 is O, or NH; W1 is C1-C20alkyl; or a group Sp-Sil; Sp is a straight-chain or branched saturated or single or multiple unsaturated C3-C12 hydrocarbon; Sil is a silane; an oligosiloxane; or a polysiloxane moiety; and R4, R5 R6, R7, R8 and R9 independently from each other are hydrogen; C1-C12alkyl; or C3-C12cycloalkyl.