- 专利标题： HIGHLY SELECTIVE AKR1C3 INHIBITORS AND METHODS OF USE THEREOF
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申请号： PCT/US2018/017986申请日： 2018-02-13
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公开(公告)号： WO2018148721A1公开(公告)日： 2018-08-16
- 发明人: TRIPPIER, Paul , VERMA, Kshitij , PENNING, Trevor, M. , ZHANG, Tianzhu
- 申请人： TEXAS TECH UNIVERSITY SYSTEM , THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
- 申请人地址： Office Of Research Commercialization P.O. Box 42007 Lubbock, TX 79409-2007 US
- 专利权人： TEXAS TECH UNIVERSITY SYSTEM,THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
- 当前专利权人： TEXAS TECH UNIVERSITY SYSTEM,THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
- 当前专利权人地址： Office Of Research Commercialization P.O. Box 42007 Lubbock, TX 79409-2007 US
- 代理机构： CHALKER, Daniel, J. et al.
- 优先权： US62/458,267 20170213
- 主分类号： C07C233/55
- IPC分类号： C07C233/55 ; C07C69/612 ; C07C233/54 ; C07C235/38 ; C07C235/84 ; C07C69/94 ; C07C69/616 ; C07C69/608 ; C07C69/035 ; C07D213/79 ; C07F5/02 ; C07F5/04 ; A61K31/166 ; A61K31/167 ; A61K31/215 ; A61K31/216 ; A61K31/222 ; A61K31/235 ; A61K31/4409 ; A61P35/00 ; A61P35/02
摘要：
The present invention includes methods and compositions that inhibit AKR1C3 enzymatic activity and consequently reduces androgen receptor (AR) transactivation, AR and prostate specific antigen (PSA) expression levels in, for example, prostate cancer, castration-resistant prostate cancer, breast cancer, acute myeloid leukemia (AML), T-cell acute lymphoblastic leukemia (T-ALL), or a leukemia.
