[EN] SUBSTITUTED N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3- DIOXYGENASE<br/>[FR] N-HYDROXYAMIDINOHÉTÉROCYCLES SUBSTITUÉS EN TANT QUE MODULATEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE
申请人:PHENEX DISCOVERY VERWALTUNGS GMBH
公开号:WO2018083241A1
公开(公告)日:2018-05-11
The invention provides modulators of indoleamine 2,3-dioxygenase (IDO1) and their use in the prophylaxis and/or treatment of IDO1-mediated diseases. Specifically, the present invention provides compounds according to Formula (I) an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof.
Synthesis of trifluoromethyl-substituted 1,2,6-thiadiazine 1-oxides from sulfonimidamides under mechanochemical conditions
作者:Marco Thomas Passia、Jan-Hendrik Schöbel、Niklas Julian Lentelink、Khai-Nghi Truong、Kari Rissanen、Carsten Bolm
DOI:10.1039/d1ob01912k
日期:——
TBS-protected or NH-sulfonimidamides react with β-alkoxyvinyl trifluoromethylketones under solvent-free mechanochemical conditions to give 3-trifluoromethyl-substituted three-dimensional 1,2,6-thiadiazine 1-oxides. C4-Functionalized products can be obtained by starting from cyclic enones and brominations of the initially formed heterocycles. The stability of the products was investigated by varying the pH value
[EN] HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS<br/>[FR] DÉRIVÉS HÉTÉROARYLDIHYDROPYRIMIDINE ET MÉTHODES DE TRAITEMENT D'INFECTIONS PAR LE VIRUS DE L'HÉPATITE B
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2019001420A1
公开(公告)日:2019-01-03
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
The present invention relates to compounds of Formula (I), wherein R1, R2, R3, R4 and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants.
A convenient synthetic route to sulfonimidamides from sulfonamides
作者:Yantao Chen、James Gibson
DOI:10.1039/c4ra14056g
日期:——
Sulfonimidamides were prepared in a one-pot transformation from sulfonamides, through nucleophilic substitution of sulfonimidoyl chlorides formed in situ with different amines. This methodology represents a convenient, safe, and easily accessible synthetic route to sulfonimidamides.