Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity
摘要:
Activation of protease activated receptor 2 (PAR2) has been implicated in inflammatory and metabolic disorders and its inhibition may yield novel therapeutics. Here, we report a series of PAR2 antagonists based on C-terminal capping of 5-isoxazolyl-L-cyclohexylalanine-L-isoleucine, with benzylamine analogues being effective new PAR2 antagonists. 5-Isoxazolyl-L-cyclohexylalanine-L-isoleucine-2-methoxy-benzylamine (10) inhibited PAR2-, but not PAR1-, induced release of Ca2+ (IC50 0.5 mu M) in human colon cells, IL-6 and TNF alpha secretion (IC50 1-5 mu M) from human kidney cells, and was anti-inflammatory in acute rat paw inflammation (ED50 5 mg/kg sc). These findings show that new benzylamide antagonists of PAR2 have anti-inflammatory activity. (C) 2015 Elsevier Ltd. All rights reserved.
[EN] BIARYL PYRAZOLES AS NRF2 REGULATORS<br/>[FR] BIARYL PYRAZOLES UTILISÉS COMME RÉGULATEURS DE NRF2
申请人:GLAXOSMITHKLINE IP DEV LTD
公开号:WO2017060854A1
公开(公告)日:2017-04-13
The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING ALPHA-V-BETA-3
申请人:Hoffmann-La Roche Inc.
公开号:US20150038523A1
公开(公告)日:2015-02-05
The invention relates to compounds of formula (I): wherein R
1
, R
2
, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.
METHOD FOR PRODUCING CYCLOPLATINIZED PLATINUM COMPLEXES, PLATINUM COMPLEXES PRODUCED BY SAID METHOD, AND THE USE THEREOF
申请人:Englert Ullrich
公开号:US20100267977A1
公开(公告)日:2010-10-21
The present invention relates to a process for preparing cycloplatinated platinum(II) complexes, platinum(II) complexes prepared by this process and the use thereof for the treatment of tumor diseases and/or hemo blastoses.