304876-16-2Relevant academic research and scientific papers
Compound serving as thyroid hormone beta receptor agonist and use thereof
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Paragraph 0297-0301, (2021/02/10)
The invention relates to a compound serving as a thyroid hormone beta receptor agonist and use thereof, and further relates to a pharmaceutical composition containing the compound. The compound or thepharmaceutical composition can be used for preparing a
CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES
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Paragraph 0203, (2020/03/28)
A chemoselective and reactive Mn(CF3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)- 1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348)
Fensome, Andrew,Adams, William R.,Adams, Andrea L.,Berrodin, Tom J.,Cohen, Jeff,Huselton, Christine,Illenberger, Arthur,Kern, Jeffrey C.,Hudak, Valerie A.,Marella, Michael A.,Melenski, Edward G.,McComas, Casey C.,Mugford, Cheryl A.,Slayden, Ov D.,Yudt, Matthew,Zhang, Zhiming,Zhang, Puwen,Zhu, Yuan,Winneker, Richard C.,Wrobel, Jay E.
, p. 1861 - 1873 (2008/12/20)
We have continued to explore the 3,3-dialkyl-5-aryloxindole series of progesterone receptor (PR) modulators looking for new agents to be used in female healthcare: contraception, fibroids, endometriosis, and certain breast cancers. Previously we reported
Thio-oxindole derivatives
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Page column 46, (2010/11/30)
This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1and R2are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl;1-propynyl; or3-propynyl; or R1and R2are joined to form an alkyl, alkenyl or heterocyclic ring; or R1and R2together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3is H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, alkynyl, substituted alkynyl, or CORA; RAis H, C1to C3alkyl, substituted C1to C3alkyl, C1to C3alkoxy, substituted C1to C3alkoxy, C1to C3aminoalkyl, or substituted C1to C3aminoalkyl; R4is H, halogen, CN, NH2, NO2, C1to C6alkyl, or substituted C1to C6alkyl, C1to C6alkoxy, substituted C1to C6alkoxy, C1to C6aminoalkyl, or substituted C1to C6aminoalkyl; R5is optionally substituted and selected from a benzene ring, a five or six membered heterocyclic ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2or NR6; or an indol-4-yl, indol-7-yl or benzo-2-thiophene moiety; Q1is S, NR7, CR8R9; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.
Fensome, Andrew,Bender, Reinhold,Cohen, Jeffrey,Collins, Mark A,Mackner, Valerie A,Miller, Lori L,Ullrich, John W,Winneker, Richard,Wrobel, Jay,Zhang, Puwen,Zhang, Zhiming,Zhu, Yuan
, p. 3487 - 3490 (2007/10/03)
A new series of 3,3-disubstituted-5-aryloxindoles has been synthesized and evaluated for progesterone receptor antagonist (PR) activity in a T47D cell alkaline phosphatase assay and for their ability to bind PR in competition binding studies. In this comm
