[EN] COMPOSITIONS AND METHODS COMPRISING SUBSTITUTED 2-AMINOIMIDAZOLES<br/>[FR] COMPOSITIONS ET PROCÉDÉS COMPRENANT DES 2-AMINOIMIDAZOLES SUBSTITUÉS
申请人:CURZA GLOBAL LLC
公开号:WO2018184019A1
公开(公告)日:2018-10-04
The present invention presents 2-(acylamino)imidazoles with therapeutic activity, including selective activity against cancer cells, and compositions comprising them. Methods of using and preparing the 2-(acylamino)imidazoles are also presented.
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
The present invention relates to pharmaceutically and/or diagnostically active compounds, in particular peptide analogues (peptidomimetics), which can be reversibly controlled between an active and an inactive state by irradiation with light of different wavelengths. The present invention further relates to an intermediate compound usable in the manufacture of such pharmaceutically and/or diagnostically active compounds, as well as a manufacturing method thereof.
Organocatalytic Stereoconvergent Synthesis of α-CF<sub>3</sub>Amides: Triketopiperazines and Their Heterocyclic Metamorphosis
作者:Robert W. Foster、Eva N. Lenz、Nigel S. Simpkins、Darren Stead
DOI:10.1002/chem.201701548
日期:2017.7.3
The highly enantioselective alkylation of α‐CF3 enolates, generated from triketopiperazines, has been accomplished through use of a bifunctional thiourea organocatalyst to facilitate 1,4‐addition to varied enone acceptors. On treatment with appropriate nitrogen nucleophiles, the chiral triketopiperazine products undergo a metamorphosis, to provide novel fused heterocyclic lactams such as extended pyrazolopyrimidines