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The present invention is directed to a compound of the formula (A): or a pharmaceutically acceptable salt thereof; and also to compounds of formula (I): or a pharmaceutically acceptable salt thereof.
Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using s...
The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors alpha and beta (ERalpha and ERbeta, respectively) and is a potent uterine antagonist with minimal effects on the ovaries as determined by serum biomarkers...
A readily automated solid-phase approach to the synthesis of diverse benzimidazoles is described. The procedure utilizes polymer supported 4-fluoro-3-nitrobenzoic acid and a wide range of commercially available amines and aldehydes. The key heterocyclization step is achieved under mild conditions and was found to be general for a large number of di...
Substituted 4(3H)-quinazolinones were synthesized under acidic conditions from polymer supported anthranilamide precursors and aldehyde inputs. Dehydrogenation using potassium permanganate followed by trifluoroacetic acid cleavage afforded the desired compounds in acceptable yields and purities. Additional diversity at the 3 position was realized b...
Thiol ligands are capable of partially displacing cyanide from Au(CN) 2-, demonstrating that their affinity for gold(I) is very high. Raman and 13C NMR evidence for the formation in solution of mixed-ligand complexes, RSAuCN -, which disproportionate to Au(CN)2 - and (RS) 2Au -, is presented. With use of literature values for reduction potentials,...