[EN] PEPTIDOMIMETIC N5-METHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE DERIVATIVES, TRIAZASPIRO[4.14]NONADECANE DERIVATIVES AND SIMILAR COMPOUNDS AS INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION [FR] DÉRIVÉS DE N5-MÉTHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE PEPTIDOMIMÉTIQUES, DÉRIVÉS DE TRIAZASPIRO[4.14]NONADÉCANE ET COMPOSÉS SIMILAIRES UTILISÉS EN TANT QU'INHIBITEURS DE RÉPLICATION DE NOROVIRUS ET DE CORONAVIRUS
Continuous Chemoselective Methylation of Functionalized Amines and Diols with Supercritical Methanol over Solid Acid and Acid−Base Bifunctional Catalysts
bifunctional catalysts (Cs-P-Si mixed oxide and gamma-alumina) was investigated in a continuous-flow, fixed-bed reactor. The use of scCH(3)OH in the reaction of 2-aminoethanol with methanol (amine/CH(3)OH = 1/10.8) over the solid catalysts led to a significant improvement in the chemoselectivity of the N-methylation. Among the catalysts examined, the Cs-P-Si mixed oxide provided the most efficient catalyst
TRICYCLIC PYRIDONE COMPOUNDS AS JAK2 V617F INHIBITORS
申请人:Incyte Corporation
公开号:US20220002299A1
公开(公告)日:2022-01-06
The present application provides tricyclic pyridone compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
[EN] 4 -MORPHOLINO-PYRIDO [3, 2 -D] PYRIMIDINES ACTIVE ON PI3K<br/>[FR] 4-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES
申请人:MERCK SERONO SA
公开号:WO2010037765A3
公开(公告)日:2010-07-15
Novel Calcium Antagonists with Both Calcium Overload Inhibition and Antioxidant Activity. 1. 2-(3,5-Di-<i>tert-</i>butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones
作者:Tatsuya Kato、Tomokazu Ozaki、Kazuhiko Tamura、Yoshiyuki Suzuki、Michitaka Akima、Nobuhiro Ohi
DOI:10.1021/jm980335f
日期:1998.10.1
A series of 2-(3,5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones was synthesized in order to explore novel calcium antagonists with potent antiischemic activity. These compounds were designed to have, in addition to Ca2+ antagonistic activity, both Ca2+ overload prevention and antioxidant activity in one molecule. These three kinds of activity were evaluated by using a K+-depolarized rat aorta, a veratridine-induced Ca2+ overload model of rat cardiomyocytes, and a soybean lipoxygenase-induced lipid peroxidation model of rabbit low-density lipoprotein, respectively. In particular, 2-(3,5-di-tert-butyl-4-hydroxyphenyl)-3-[3-[N-methyl-N-[2-[3,4-(methylenedioxy)phenoxy]ethyl]amino]propyl]-1,3-thiazolidin-4-one (7o) was found to be highly potent and possessed a well-balanced combination of these actions in vitro.