1-溴-3-(4-氯苯基)丙酮 、 硫脲 在
乙酸乙酯 、 Brine 、 magnesium sulfate 、 ethyl acetate hexanes 作用下,
以
乙醇 为溶剂,
反应 2.0h,
以to give 19.9 grams of the title compound as a tan powder (86% yield)的产率得到2-Amino-4-(p-chlorbenzyl)thiazol
[EN] 2-AMINOTHIAZOLE COMPOUNDS USEFUL AS ASPARTYL PROTEASE INHIBITORS<br/>[FR] COMPOSES DE 2-AMINOTHIAZOLE UTILES EN TANT QU'INHIBITEURS DE L'ASPARTYLE-PROTEASE
申请人:MERCK & CO INC
公开号:WO2005097767A1
公开(公告)日:2005-10-20
The present invention is directed to 2-aminothiazole compounds which are aspartyl protease inhibitors, and are inhibitors of both the beta-secretase enzyme and HIV protease, and that are useful in the treatment of diseases in which the beta-secretase enzyme and HIV are involved, such as Alzheimer's disease, HIV Infection and AIDS. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme and HIV protease are involved.
2-Aminothiazole Compounds Useful As Aspartyl Protease Inhibitors
申请人:Coburn A. Craig
公开号:US20070203147A1
公开(公告)日:2007-08-30
The present invention is directed to 2-aminothiazole compounds which are aspartyl protease inhibitors, and are inhibitors of both the beta-secretase enzyme and HIV protease, and that are useful in the treatment of diseases in which the beta-secretase enzyme and HIV are involved, such as Alzheimer's disease, HIV Infection and AIDS. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme and HIV protease are involved.
This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof:
wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.