- Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton
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The progesterone receptor (PR) plays an important role in various physiological systems, including female reproduction and the central nervous system, and PR antagonists are thought to be effective not only as contraceptive agents and abortifacients but also in the treatment of various diseases, including hormone-dependent cancers and endometriosis. Here, we identified phenanthridin-6(5H)-one derivatives as a new class of PR antagonists and investigated their structure-activity relationships. Among the synthesized compounds, 37, 40, and 46 exhibited very potent PR antagonistic activity with high selectivity for PR over other nuclear receptors. These compounds are structurally distinct from other nonsteroidal PR antagonists, including cyanoaryl derivatives, and should be useful for further studies of the clinical utility of PR antagonists.
- Nishiyama, Yuko,Mori, Shuichi,Makishima, Makoto,Fujii, Shinya,Kagechika, Hiroyuki,Hashimoto, Yuichi,Ishikawa, Minoru
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Read Online
- Benzidine compound and application thereof
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The invention relates to a benzidine compound and application thereof. The benzidine compound has a structure disclosed in the following formula I. The invention also provides the pharmaceutically acceptable salt, the isomer, the raceme, the pro-drug cocrystallization compound, the hydrate and the solvate of the compound, and the application thereof for preparing medicines for treating or preventing ROR (Retinoid-related Orphan nuclear Receptor) gamma regulation and control relevant diseases. More importantly, the class of compound can be used for treating medicines used for treating inflammation, immunological diseases, cancers and neurological diseases.
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Paragraph 0054; 0056-0058
(2019/07/01)
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- Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγInverse Agonist for Treatment of Castration-Resistant Prostate Cancer
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We report the design, optimization, and biological evaluation of nuclear receptor RORγinverse agonists as therapeutic agents for prostate cancer treatment. The most potent compound 27 (designated as XY101) exhibited cellular activity with an IC50/su
- Zhang, Yan,Wu, Xishan,Xue, Xiaoqian,Li, Chenchang,Wang, Junjian,Wang, Rui,Zhang, Cheng,Wang, Chao,Shi, Yudan,Zou, Lingjiao,Li, Qiu,Huang, Zenghong,Hao, Xiaojuan,Loomes, Kerry,Wu, Donghai,Chen, Hong-Wu,Xu, Jinxin,Xu, Yong
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p. 4716 - 4730
(2019/05/08)
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- Novel Compounds
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The present specification provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an RORγ and/or RORγt mediated disease state.
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Paragraph 0639-0640
(2017/07/06)
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- METHODS FOR TREATING CANCER WITH RORGAMMA INHIBITORS
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The present invention provides compositions, methods, and kits comprising one or more compounds of Formula I, such as XY018, alone or in combination with one or more anticancer drugs, such as an anti-androgen drug, that are useful for treating cancer, e.g., prostate cancer, such as castration-resistant prostate cancer (CRPC), and numerous other types of cancer including lung cancer, breast cancer, liver cancer, ovarian cancer, endometrial cancer, bladder cancer, colon cancer, gastric cancer, lymphoma, and glioma.
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Paragraph 0188
(2017/09/02)
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- Modulators of the nuclear hormone receptor ROR
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The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
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Page/Page column 134
(2017/03/28)
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- Synthesis and insecticidal activities of novel analogues of flubendiamide containing a hexafluoroisopropanol moiety
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Ten novel analogues of flubendiamide containing a hexafluoroisopropanol moiety were designed and synthesized. Their insecticidal activities against armyworm (Pseudaletia separata Walker) were examined and compared with the commercial product flubendiamide. Compound 7b showed nearly the same insecticidal activity as flubendiamide against armyworm.
- Wu, Mingxi,Zhao, Wenwen,Jin, Guanyi,Huang, Qingchun,Cao, Song
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experimental part
p. 1310 - 1314
(2012/09/05)
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