The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer.
[EN] INHIBITORS OF FATTY ACID SYNTHASE (FAS)<br/>[FR] INHIBITEURS DE LA SYNTHASE D'ACIDES GRAS (FAS)
申请人:MERCK & CO INC
公开号:WO2007089634A2
公开(公告)日:2007-08-09
[EN] The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer. [FR] La présente invention concerne des composés qui comprennent des 3-aryl-4-hydroxyquinolin-2(1H)-ones substituées qui inhibent l'activité de la FAS. L'invention concerne également des compositions qui comprennent de tels composés d'inhibition et des procédés d'inhibition de l'activité de la FAS par l'administration du composé à un patient ayant besoin d'un traitement contre le cancer.
Solvent-free microwave synthesis of 4-hydroxy-3-phenylquinolin-2(1H)-ones and variants using activated arylmalonates
作者:Alexey Rivkin、Bruce Adams
DOI:10.1016/j.tetlet.2006.01.148
日期:2006.4
The disclosure herein describes the rapid synthesis of 4-hydroxy-3-phenylquinolin-2(1H)-ones and variants via a solvent-freemicrowave cyclocondensation reaction using di-(2,4,6-trichlorophenyl)-2-phenylmalonate, which improves the general scope of this reaction.