Search Results - "Zhang, Rosemary F"
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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-07-2017)“…[Display omitted] A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of…”
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Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases
Published in Journal of medicinal chemistry (23-09-2010)“…The discovery and characterization of 7k (BMS-582949), a highly selective p38α MAP kinase inhibitor that is currently in phase II clinical trials for the…”
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Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis
Published in ACS medicinal chemistry letters (14-03-2019)“…The four members of the Janus family of nonreceptor tyrosine kinases play a significant role in immune function. The JAK family kinase inhibitor, tofacitinib…”
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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2014)“…A new class of Janus kinase (JAK) inhibitors was discovered using a rationally designed pyrrolo[1,2-b]pyridazine-3-carboxamide scaffold. Preliminary studies…”
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Benzothiazole based inhibitors of p38α MAP kinase
Published in Bioorganic & medicinal chemistry (15-03-2008)“…The rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38α MAP kinase are described. Rational design,…”
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5-Cyanopyrimidine Derivatives as a Novel Class of Potent, Selective, and Orally Active Inhibitors of p38α MAP Kinase
Published in Journal of medicinal chemistry (06-10-2005)“…A novel class of 5-cyanopyrimidine-based inhibitors of p38α MAP kinase has been investigated. Analogues optimized through SAR iterations display low nanomolar…”
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7
Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38[alpha] MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases
Published in Journal of medicinal chemistry (20-11-2013)“…The discovery and characterization of 7k (BMS-582949), a highly selective p38{alpha} MAP kinase inhibitor that is currently in phase II clinical trials for the…”
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8
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase
Published in Journal of medicinal chemistry (06-10-2005)“…A novel class of 5-cyanopyrimidine-based inhibitors of p38alpha MAP kinase has been investigated. Analogues optimized through SAR iterations display low…”
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9
Benzothiazole based inhibitors of p38alpha MAP kinase
Published in Bioorganic & medicinal chemistry letters (15-03-2008)“…Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38alpha MAP kinase are described. The issue of metabolic…”
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