- 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
[作者:LIU CHUNJIAN; LIN JAMES; WROBLESKI STEPHEN T; LIN SHUQUN; HYNES JOHN JR; WU HONG; DYCKMAN ALARIC J; LI TIANLE; WITYAK JOHN; GILLOOLY KATHLEEN M; PITT SIDNEY; SHEN DING REN; ZHANG ROSEMARY F; MCINTYRE KIM W; SALTERCID LUISA; SHUSTER DAVID J; ZHANG HONGJIAN; MARATHE PUNIT H; DOWEYKO ARTHUR M; SACK JOHN S; KIEFER SUSAN E; KISH KEVIN F; NEWITT JOHN A; MCKINNON MURRAY; DODD JOHN H; BARRISH JOEL C; SCHIEVEN GARY L; LEFTHERIS KATERINA,期刊:Journal of Medicinal Chemistry, 页码:6629-6639 , 文章类型: Article,,卷期:2010年53-18]
- The discovery and characterization of 7k (BMS-582949), a highly selective p38 alpha, MAP kinase inhibitor that is currently in phase H clinical trials for the treatment of rheumatoid arthritis, is described, A key to the...
- Nonsteroidal Dissociated Glucocorticoid Agonists Containing Azaindoles as Steroid A-Ring Mimetics
[作者:RIETHER DORIS; HARCKEN CHRISTIAN; RAZAVI HOSSEIN; KUZMICH DANIEL; GILMORE THOMAS; BENTZIEN JOERG; PACK EDWARD J JR; SOUZA DONALD; NELSON RICHARD M; KUKULKA ALISON; FADRA TAZMEEN N; ZUVELAJELASKA LJILJANA; PELLETIER JOSEPHINE; DINALLO ROGER; PANZENBECK MARK; TORCELLINI CAROL; NABOZNY GERALD H; THOMSON DAVID S,期刊:Journal of Medicinal Chemistry, 页码:6681-6698 , 文章类型: Article,,卷期:2010年53-18]
- Syntheses and structure activity relationships (SA R) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in v...
- Design, Synthesis, and Biological Evaluation of Halogenated N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: Discovery of an Isoform-Selective Small Molecule Phospholipase D2 Inhibitor
[作者:LAVIERI ROBERT R; SCOTT SARAH A; SELVY PAIGE E; KIM KWANGHO; JADHAV SATYAWAN; MORRISON RYAN I; DANIELS J SCOTT; BROWN H ALEX; LINDSLEY CRAIG W,期刊:Journal of Medicinal Chemistry, 页码:6706-6719 , 文章类型: Article,,卷期:2010年53-18]
- Phospholipase D (PLD) catalyzes the conversion of phosphatidylcholine to the lipid second messenger phosphatidic acid. Two mammalian isoforms of PLD have been identified, PLD I and PLD2, which share 53% sequence identity...
|