SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
申请人:OOST Thorsten
公开号:US20140057916A1
公开(公告)日:2014-02-27
This invention relates to substituted 4-pyridones of formula 1
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
Selective Intramolecular CH Amination through the Metalloradical Activation of Azides: Synthesis of 1,3-Diamines under Neutral and Nonoxidative Conditions
作者:Hongjian Lu、Huiling Jiang、Lukasz Wojtas、X. Peter Zhang
DOI:10.1002/anie.201005552
日期:2010.12.27
N2 is the only by‐product in a stereospecific and highly diastereoselective intramolecularCH amination of sulfamoyl azides with a cobalt(II)‐based metalloradical catalyst (see scheme). The catalytic system has an unusual capacity for the efficient amination of strong primary CH bonds, as well as secondary and tertiary CH bonds, and functional‐group tolerance is excellent owing to the neutral and
Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3′-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2′epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.
BENZIMIDAZOLE AND IMADAZOPYRIDINE CARBOXIMIDAMIDE COMPOUNDS
申请人:Gilead Sciences, Inc.
公开号:US20160333009A1
公开(公告)日:2016-11-17
The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I:
or pharmaceutically acceptable salts thereof, in which X, L, n, m, R
1
, R
2a
, R
2b
, R
n
, R
m
, and R
t
are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
本公开提供了式I的吲哌酮2,3-二氧化酶1(IDOL)抑制剂:
或其药学上可接受的盐,其中X、L、n、m、R
1
、R
2a
、R
2b
、R
n
、R
m
和R
t
如本文所定义,以及包括式I化合物的药物组合物,或其药学上可接受的盐,并使用这些方法来治疗由IDO1介导的疾病。