发明公开
EP3116861A1 SMALL MOLECULES FOR INHIBITING MALE FERTILITY
审中-公开
KLEINMOLEKÜLEZUR HEMMUNG DERMÄNNLICHENFRUCHTBARKEIT
- 专利标题: SMALL MOLECULES FOR INHIBITING MALE FERTILITY
- 专利标题(中): KLEINMOLEKÜLEZUR HEMMUNG DERMÄNNLICHENFRUCHTBARKEIT
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申请号: EP15761799.4申请日: 2015-03-13
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公开(公告)号: EP3116861A1公开(公告)日: 2017-01-18
- 发明人: O'RAND, Michael
- 申请人: The University of North Carolina at Chapel Hill
- 申请人地址: 100 Europa Drive Suite 430 Chapel Hill, NC 27517 US
- 专利权人: The University of North Carolina at Chapel Hill
- 当前专利权人: The University of North Carolina at Chapel Hill
- 当前专利权人地址: 100 Europa Drive Suite 430 Chapel Hill, NC 27517 US
- 代理机构: Schütte, Gearoid
- 优先权: US201461953293P 20140314
- 国际公布: WO2015138919 20150917
- 主分类号: C07D251/52
- IPC分类号: C07D251/52 ; C07D253/07 ; C07D253/075 ; C07D487/04 ; C07D498/04 ; A61K31/53 ; A61P15/16
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.
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