Discovery of 1-{4-[3-Fluoro-4-((3S,6R)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist was written by Fauber, Benjamin P.;Rene, Olivier;Deng, Yuzhong;DeVoss, Jason;Eidenschenk, Celine;Everett, Christine;Ganguli, Arunima;Gobbi, Alberto;Hawkins, Julie;Johnson, Adam R.;La, Hank;Lesch, Justin;Lockey, Peter;Norman, Maxine;Ouyang, Wenjun;Summerhill, Susan;Wong, Harvey. And the article was included in Journal of Medicinal Chemistry in 2015.Category: alcohols-buliding-blocks This article mentions the following:
Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. Using the previously reported tertiary sulfonamide as a starting point, the authors engineered structural modifications that significantly improved human and rat metabolic stabilities while maintaining a potent and highly selective RORc inverse agonist profile. The most advanced δ-sultam compound I possessed favorable RORc cellular potency with 75-fold selectivity for RORc over other ROR family members and >200-fold selectivity over 25 addnl. nuclear receptors in a cell assay panel. The favorable potency, selectivity, in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in a PK/PD model support the evaluation of I in preclin. studies. In the experiment, the researchers used many compounds, for example, 3-Amino-3-methylbutan-1-ol (cas: 42514-50-1Category: alcohols-buliding-blocks).
3-Amino-3-methylbutan-1-ol (cas: 42514-50-1) belongs to alcohols. Alcohols are weak acids. The most acidic simple alcohols (methanol and ethanol) are about as acidic as water, and most other alcohols are somewhat less acidic. Under carefully controlled conditions, simple alcohols can undergo intermolecular dehydration to give ethers. This reaction is effective only with methanol, ethanol, and other simple primary alcohols.Category: alcohols-buliding-blocks
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts