- Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990
-
Utilizing structure-based drug design, a novel dihydropyridopyrimidinone series which exhibited potent Hsp90 inhibition, good pharmacokinetics upon oral administration, and an excellent pharmacokinetic/pharmacodynamic relationship in vivo was developed from a commercial hit. The exploration of this series led to the selection of NVP-HSP990 as a development candidate.
- McBride, Christopher M.,Levine, Barry,Xia, Yi,Bellamacina, Cornelia,Machajewski, Timothy,Gao, Zhenhai,Renhowe, Paul,Antonios-Mccrea, William,Barsanti, Paul,Brinner, Kristin,Costales, Abran,Doughan, Brandon,Lin, Xiaodong,Louie, Alicia,McKenna, Maureen,Mendenhall, Kris,Poon, Daniel,Rico, Alice,Wang, Michael,Williams, Teresa E.,Abrams, Tinya,Fong, Susan,Hendrickson, Thomas,Lei, Dachuan,Lin, Julie,Menezes, Daniel,Pryer, Nancy,Taverna, Pietro,Xu, Yongjin,Zhou, Yasheen,Shafer, Cynthia M.
-
-
Read Online
- OXIM DERIVATIVES AS HSP90 INHIBITORS
-
The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
- -
-
Page/Page column 181-182
(2009/09/05)
-
- 2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-D] PYRIMIDIN-5-ONES
-
Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nevous system diseases.
- -
-
Page/Page column 37
(2010/11/26)
-