- Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors
[作者:LAZERWITH SCOTT E; BAHADOR GINA; CANALES EDA; CHENG GUOFENG; CHONG LEE; CLARKE MICHAEL O; DOERFFLER EDWARD; EISENBERG EUGENE J; HAYES JACLYN; LU BING; LIU QI; MATLES MIKE; MERTZMAN MICHAEL; MITCHELL MICHAEL L; MORGANELLI PHILIP; MURRAY BERNARD P; ROBINSON MARGARET; STRICKLEY ROBERT G; TESSLER MEGAN; TIRUNAGARI NEERAJ; WANG JIANHONG; WANG YUJIN; ZHANG JENNIFER R; ZHENG XUBIN; ZHONG WEIDONG; WATKINS WILLIAM J,期刊:ACS Medicinal Chemistry Letters, 页码:715-719 , 文章类型: Article,,卷期:2011年2-10]
- A novel series of HCV replication inhibitors based on a pyrido[3,2-d]primidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exp...
- Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility
[作者:JIA LANQI; SIMPSON ROBERT D; YUAN JING; XU ZHENRONG; ZHAO WEI; CACATIAN SALVACION; TICE COLIN M; GUO JOAN; ISHCHENKO ALEXEY; SINGH SURESH B; WU ZHONGREN; MCKEEVER BRIAN M; BUKHTIYAROV YURI; JOHNSON JUDITH A; DOE CHRISTOPHER P; HARRISON RICHARD K; MCGEEHAN GERARD M; DILLARD LAWRENCE W; BALDWIN JOHN J; CLAREMON DAVID A,期刊:ACS Medicinal Chemistry Letters, 页码:747-751 , 文章类型: Article,,卷期:2011年2-10]
- Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the c-yclohexylmethyl group occupying the SI pock...
- The Discovery of VX-745: A Novel and Selective p38 alpha Kinase Inhibitor
[作者:DUFFY JOHN P; HARRINGTON EDMUND M; SALITURO FRANCESCO G; COCHRAN JOHN E; GREEN JEREMY; GAO HUAI; BEMIS GUY W; EVINDAR GHOTAS; GALULLO VINCENT P; FORD PAMELLA J; GERMANN URSULA A; WILSON KEITH P; BELLON STEVEN F; CHEN GUANGING; TASLIMI PAUL; JONES PETER; HUANG CASSEY; PAZHANISAMY S; WANG YOWMING; MURCKO MARK A; SU MICHAEL S S,期刊:ACS Medicinal Chemistry Letters, 页码:758-763 , 文章类型: Article,,卷期:2011年2-10]
- The synthesis of novel, selective, orally active 2,5-disubstituted 6H-pyrimido[1,6-b]pyridazin-6-one p38 alpha inhibitors is described. Application of structural information from enzyme-ligand complexes guided the select...
- Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer
[作者:BURGER MATTHEW T; PECCHI SABINA; WAGMAN ALLAN; NI ZHIJIE; KNAPP MARK; HENDRICKSON THOMAS; ATALLAH GORDANA; PFISTER KEITH; ZHANG YANCHEN; BARTULIS SARAH; FRAZIER KELLY; NG SIMON; SMITH AARON; VERHAGEN JOELLE; HAZNEDAR JOSHUA; HUH KAY; IWANOWICZ ED; XIN XIAOHUA; MENEZES DANIEL; MERRITT HANNE; LEE ISABELLE; WIESMANN MARION; KAUFMAN SUSAN; CRAWFORD KENNETH; CHIN MICHAEL; BUSSIERE DIRKSEN; SHOEMAKER KEVIN; ZAROR ISABEL; MAIRA SAUVEURMICHEL; VOLIVA CHARLES F,期刊:ACS Medicinal Chemistry Letters, 页码:774-779 , 文章类型: Article,,卷期:2011年2-10]
- Phosphoinositide-3-kinases (PI3Ks) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein we describe the structure guided optimization of a series of ...
- Identification of Inhibitors of NOD1-Induced Nuclear Factor-kappa B Activation
[作者:KHAN PASHA M; CORREA RICARDO G; DIVLIANSKA DANIELA B; PEDDIBHOTLA SATYAMAHESHWAR; SESSIONS E HAMPTON; MAGNUSON GAVIN; BROWN BROCK; SUYAMA EIGO; YUAN HONGBIN; MANGRAVITANOVO ARIANNA; VICCHIARELLI MICHAEL; SU YING; VASILE STEFAN; SMITH LAYTON H; DIAZ PAUL W; REED JOHN C; ROTH GREGORY P,期刊:ACS Medicinal Chemistry Letters, 页码:780-785 , 文章类型: Article,,卷期:2011年2-10]
- NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specif...
- Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable gamma-Secretase Modulator
[作者:PENG HAIRUO; TALREJA TINA; XIN ZHILI; CUERVO J HERNAN; KUMARAVEL GNANASAMBANDAM; HUMORA MICHAEL J; XU LIN; ROHDE ELLEN; GAN LAWRENCE; JUNG MIYOUNG; SHACKETT MELANIE N; CHOLLATE SOWMYA; DUNAH ANTHONE W; SNODGRASSBELT PAMELA A; ARNOLD H MOORE; TAVERAS ARTHUR G; RHODES KENNETH J; SCANNEVIN ROBERT H,期刊:ACS Medicinal Chemistry Letters, 页码:786-791 , 文章类型: Article,,卷期:2011年2-10]
- We have investigated a novel series of acid-derived gamma-secretase modulators as a potential treatment of Alzheimer's disease. Optimization based on cellular potency and brain pharmacodynamics after oral dosing led to t...
|