A compound of the following formula or a pharmacologically acceptable salt thereof:
1
wherein A represents a phenyl group or the like, B represents an aryl group or the like, X represents an oxygen atom or the like, and n represents 0 or 1. The compound is a PPAR &ggr; modulator which is a therapeutic agent for retrograde osteoporosis in which excessive differentiation of adipocytes is inhibited and formation and differentiation of osteoblasts from stem cells is facilitated, and for diabetes mellitus without characteristics such as excessive adipogenesis, liver dysfunction, vascular disorders, heart diseases and the like.
Synthesis of monosubstituted thioureas by vapour digestion and mechanochemical amination of thiocarbamoyl benzotriazoles
作者:Mateja Đud、Oxana V. Magdysyuk、Davor Margetić、Vjekoslav Štrukil
DOI:10.1039/c6gc00089d
日期:——
Thiocarbamoyl benzotriazoles, as safe and easy-to-handle isothiocyanate equivalents, were quantitatively converted to N-monosubstituted thioureas by vapour digestion synthesis in ammonia atmosphere. This simple, but timely process provided a synthetic platform...
[EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF THE ANDROGEN RECEPTOR<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DU RÉCEPTEUR DES ANDROGÈNES
申请人:ARVINAS INC
公开号:WO2016118666A1
公开(公告)日:2016-07-28
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.