865670-67-3Relevant academic research and scientific papers
7-Aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists
Zhang, Puwen,Kern, Jeffrey C.,Terefenko, Eugene A.,Fensome, Andrew,Unwalla, Ray,Zhang, Zhiming,Cohen, Jeffrey,Berrodin, Thomas J.,Yudt, Matthew R.,Winneker, Richard C.,Wrobel, Jay
, p. 6589 - 6600 (2008/12/21)
Novel 7-aryl benzo[1,4]oxazepin-2-ones were synthesized and evaluated as non-steroidal progesterone receptor (PR) modulators. The structure activity relationship of 7-aryl benzo[1,4]oxazepinones was examined using the T47D cell alkaline phosphatase assay. A number of 7-aryl benzo[1,4]oxazepinones such as 10j and 10v demonstrated good in vitro potency (IC50 of 10-30 nM) and selectivity (over 100-fold) at PR over other steroidal receptors such as glucocorticoid and androgen receptors (GR and AR). Several 7-aryl benzo[1,4]oxazepinones were active in the rat uterine decidualization model. In this in vivo model, compounds 10j and 10u were active at 3 mg/kg when dosed orally.
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5′-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators
Kern, Jeffrey C.,Terefenko, Eugene A.,Fensome, Andrew,Unwalla, Ray,Wrobel, Jay,Cohen, Jeffrey,Zhu, Yuan,Berrodin, Thomas J.,Yudt, Matthew R.,Winneker, Richard C.,Zhang, Zhiming,Zhang, Puwen
scheme or table, p. 5015 - 5017 (2009/05/30)
A series of novel 7-(5′-cyanopyrrol-2-yl) substituted benzo[1,4]oxazepin-2-ones were prepared and tested for their progesterone receptor (PR) agonist or antagonist activity in the alkaline phosphatase assay using the human T47D breast carcinoma cell line.
7-aryl 1,5-dihydro-4, 1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators
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Page/Page column 14, (2008/06/13)
This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
