Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.-论文-万方医学网

第一作者： John,Hynes

第一单位： Research and Development, Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, NJ 08543, USA. Electronic address: john.hynes@bms.com.

作者： John,Hynes ^[1] ; Hong,Wu ^[2] ; James,Kempson ^[2] ; James J-W,Duan ^[2] ; Zhonghui,Lu ^[2] ; Bin,Jiang ^[2] ; Sylwia,Stachura ^[2] ; John S,Tokarski ^[2] ; John S,Sack ^[2] ; Javed A,Khan ^[2] ; Jonathan S,Lippy ^[2] ; Rosemary F,Zhang ^[2] ; Sidney,Pitt ^[2] ; Guoxiang,Shen ^[2] ; Kate,Gillooly ^[2] ; Kim,McIntyre ^[2] ; Percy H,Carter ^[2] ; Joel C,Barrish ^[2] ; Steven G,Nadler ^[2] ; Luisa M,Salter-Cid ^[2] ; Aberra,Fura ^[2] ; Gary L,Schieven ^[2] ; William J,Pitts ^[2] ; Stephen T,Wrobleski ^[2]

作者单位： Research and Development, Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, NJ 08543, USA. Electronic address: john.hynes@bms.com. ^[1] Research and Development, Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, NJ 08543, USA. ^[2]

主题词动物(Animals);结合部位(Binding Sites);催化域(Catalytic Domain);细胞系(Cell Line);结晶学, X线(Crystallography, X-Ray);疾病模型, 动物(Disease Models, Animal);药物评价, 临床前(Drug Evaluation, Preclinical);半衰期(Half-Life);人类(Humans);炎症(Inflammation);半数抑制浓度(Inhibitory Concentration 50);Janus激酶1(Janus Kinase 1);Janus激酶2(Janus Kinase 2);Janus激酶3(Janus Kinase 3);小鼠(Mice);小鼠, 近交BALB C(Mice, Inbred BALB C);分子构象(Molecular Conformation);分子动力学模拟(Molecular Dynamics Simulation);蛋白激酶抑制剂(Protein Kinase Inhibitors);哒嗪类(Pyridazines);吡咯类(Pyrroles);大鼠(Rats);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);构效关系(Structure-Activity Relationship);TYK2激酶(TYK2 Kinase)

DOI 10.1016/j.bmcl.2017.05.043

PMID 28539220

发布时间 2017-11-25

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Bioorganic & medicinal chemistry letters

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Bioorganic & medicinal chemistry letters

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Bioorganic & medicinal chemistry letters

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Bioorganic & medicinal chemistry letters

相关期刊

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