[EN] PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE<br/>[FR] COMPOSÉS DE PYRIMIDINE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION
申请人:GENENTECH INC
公开号:WO2010014939A1
公开(公告)日:2010-02-04
Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF
申请人:BARNES David Weninger
公开号:US20120028969A1
公开(公告)日:2012-02-02
The present invention provides compounds of formula (I);
or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
The present invention provides a compound of formula I;
a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists
作者:Zhicai Yang、David J. Fairfax、Jun-Ho Maeng、Liaqat Masih、Alexander Usyatinsky、Carla Hassler、Soshanna Isaacson、Kevin Fitzpatrick、Russell J. DeOrazio、Jianqing Chen、James P. Harding、Matthew Isherwood、Svetlana Dobritsa、Kevin L. Christensen、Jonathan D. Wierschke、Brian I. Bliss、Lisa H. Peterson、Cathy M. Beer、Christopher Cioffi、Michael Lynch、W. Martin Rennells、Justin J. Richards、Timothy Rust、Yuri L. Khmelnitsky、Marlene L. Cohen、David D. Manning
DOI:10.1016/j.bmcl.2010.09.038
日期:2010.11
A new class of 2-substitutedbenzoxazole carboxamides are presented as potent functional 5-HT3 receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT3A receptors. A chemistry optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT3 receptor antagonists with good metabolic stability. These novel analogues possess drug-like
PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
申请人:Bergeron Philippe
公开号:US20100069357A1
公开(公告)日:2010-03-18
Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).