174485-71-3Relevant articles and documents
RORγ MODULATORS
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Page/Page column 22-23; 58; 62, (2018/04/13)
The invention provides an RORγ receptor agonist comprising a compound of formula (I), wherein the variables are as defined herein. These compounds are analogous to known RORγ receptor antagonists. The invention further provides a method of activating -the nuclear receptor RORγ, comprising -contacting the RORγ with an effective amount or concentration of a compound of the invention; and a method of treating cancer in a patient, comprising administering to the patient an effective dose of a compound of the invention.
A convergent, scalable synthesis of HIV protease inhibitor PNU-140690
Fors, Kristina S.,Gage, James R.,Heier, Richard F.,Kelly, Robert G.,Perrault, William R.,Wicnienski, Nancy
, p. 7348 - 7356 (2007/10/03)
PNU-140690, an inhibitor of the HIV protease enzyme undergoing clinical evaluation as a chemotherapeutic agent for treatment of AIDS, was synthesized by a convergent approach amenable to large-scale preparation in a pilot plant environment. The key step is the aldol addition of nitroaromatic ester (+)-8 to aldehyde 19e. The two stereocenters present in the target molecule were each set independently by resolution of enantiomers. Intermediates along the synthetic routes were chosen to maximize opportunities for isolation and purification by crystallization.
