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A reversed sulfonamide series of selective RORc inverse agonists

artículo científico publicado en 2014

Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) i

artículo científico publicado en 2015

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

artículo científico publicado en 2017

Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

artículo científico publicado en 2012

Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability

artículo científico publicado en 2016

Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists

artículo científico publicado en 2015

Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties

artículo científico publicado en 2016

Hepatobiliary disposition of thyroid hormone in Mrp2-deficient TR- rats: reduced biliary excretion of thyroxine glucuronide does not prevent xenobiotic-induced hypothyroidism

artículo científico publicado en 2009

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists

artículo científico publicado en 2015

Identification of tertiary sulfonamides as RORc inverse agonists

artículo científico publicado en 2014

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

artículo científico publicado en 2014

N-phenylphenylglycines as novel corticotropin releasing factor receptor antagonists

artículo científico publicado en 2004

Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold

artículo científico publicado en 2009

Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834

artículo científico publicado en 2015

Presentation, management and outcomes of thrombosis for children with cardiomyopathy

artículo científico publicado en 2006

Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy

artículo científico publicado en 2003

Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists

artículo científico publicado en 2014

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc

artículo científico publicado en 2013