Syk inhibitors with high potency in presence of blood
摘要:
We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic assays, cellular assays and in primary cells in the presence of blood. Introduction of a 7-aminoindole substituent led to derivatives with good kinase selectivity and little or no hERG channel inhibition (3b, 10c). (C) 2014 Elsevier Ltd. All rights reserved.
[EN] PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS<br/>[FR] PYRAZOLO[1,5-A]PYRIMIDINES EN TANT QU'AGENTS ANTIVIRAUX
申请人:GILEAD SCIENCES INC
公开号:WO2011163518A1
公开(公告)日:2011-12-29
The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
[EN] ANTIBACTERIAL AGENTS: N(ALPHA)-AROYL-N-ARYL-PHENYLALANINAMIDES<br/>[FR] AGENTS ANTIBACTÉRIENS : N (ALPHA)-AROYL-N-ARYL-PHÉNYLALANINAMIDES
申请人:UNIV RUTGERS
公开号:WO2015120320A1
公开(公告)日:2015-08-13
The invention provides compounds having activity as bacterial RNA polymerase inhibitors and antibacterial agents, as well as compositions comprising the compounds and methods for their use. Specifically, phenylalanineamide and tyrosinamide compounds are disclosed that have inhibitory activity toward mycobacterium tuberculosis RNA polymerase. Use of these compounds in the treatment o prevention of M. tuberculosis infections in a mammal, is disclosed.
One-Step Synthesis of Diverse Pyridine-Containing Heterocycles with 3-Ethoxycyclobutanones at Room Temperature
作者:Yun Lin、Xinglin Yang、Weidong Pan、Yu Rao
DOI:10.1021/acs.orglett.6b01027
日期:2016.5.6
An efficient and convenient approach toward a diversity-oriented synthesis of bioactive pyridine-containing fused heterocycles is described. Through a Lewis acid catalyzed union of 3-ethoxycyclobutanones with various heterocyclic amines, a broad range of heterocycliccompounds were prepared readily at ambient temperature with excellent regioselectivity.
[EN] HIGHLY ACTIVE SELF-SUFFICIENT NITRATION BIOCATALYSTS<br/>[FR] BIOCATALYSEURS DE NITRATION AUTO-SUFFISANTS HAUTEMENT ACTIFS
申请人:UNIV FLORIDA
公开号:WO2018081456A1
公开(公告)日:2018-05-03
The disclosure relates to the field of fusion proteins. In some aspects, the disclosure relates to artificial fusion proteins comprising cytochrome P450 enzymes linked to reductase enzymes and uses thereof. In some aspects, the disclosure relates to compounds produced by artificial cytochrome P450 enzymes.
[EN] PIPERIDINE DERIVATIVES AS CCR5 INHIBITORS<br/>[FR] DERIVES DE LA PIPERIDINE, INHIBITEURS DU CCR5
申请人:NOVARTIS AG
公开号:WO2004031172A1
公开(公告)日:2004-04-15
Disclosed are compounds of formula (I) wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.