The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1,
the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds.
The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
The present invention relates to non-steroidal progesterone receptor modulators of the general formula I,
the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds.
The compounds according to the invention are suitable for the therapy and prophylaxis of gynecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
Synthesis of biaryl-styrene monomers by microwave-assisted Suzuki coupling
作者:Hazit A. Zayas、Michael C. Bowyer、Christopher P. Gordon、Clovia I. Holdsworth、Adam McCluskey
DOI:10.1016/j.tetlet.2009.07.117
日期:2009.10
Biaryl-styrenic monomers are prepared via Suzukicoupling as functional monomers in the synthesis of molecularly imprinted polymers. Traditional thermal Suzuki approaches are hampered by competition between Suzuki, Heck and homo-coupling reactions. Microwave-assisted approaches facilitated rapid access to the desired Suzuki products whilst suppressing both Heck and homo-couplings of 4-vinylboronic
Novel amphiphilic homopolymers containing <i>meta-</i>
and <i>para-</i>
pyridine moieties with living characteristics and their self-assembly
作者:Yoon-Hyung Hur、Nam-Goo Kang、Beom-Goo Kang、Yong-Guen Yu、Mohammed Changez、Jae-Suk Lee
DOI:10.1002/pola.26743
日期:2013.8.15
Amphiphilic monomers containing the isomeric pyridinemoieties 3‐(4‐vinylphenyl)pyridine (3VPPy) and 4‐(4‐vinylphenyl)pyridine (4VPPy) were synthesized using the Suzuki coupling reaction. A living anionic polymerization of 3VPPy and 4VPPy was successfully performed under various conditions to overcome the limitations of anionic polymerization and to compare their properties with those of poly(2‐(4
C3-Selective Trifluoromethylthiolation and Difluoromethylthiolation of Pyridines and Pyridine Drugs via Dihydropyridine Intermediates
作者:Xin-Yue Zhou、Ming Zhang、Zhong Liu、Jia-Hao He、Xiao-Chen Wang
DOI:10.1021/jacs.2c06776
日期:2022.8.17
difluoromethylthiolation of pyridines. The method relies on borane-catalyzed pyridine hydroboration for generation of nucleophilic dihydropyridines; these intermediates react with trifluoromethylthio and difluoromethylthio electrophiles to form functionalized dihydropyridines, which then undergo oxidative aromatization. The method can be used for late-stage functionalization of pyridine drugs for the generation