Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
3-METHYL-2- ( (2S) -2- (4- (3-METHYL-L, 2, 4-0XADIAZ0L-5-YL) PHENYL) MORPHOLINO) -6- (PYRIM-IDIN-4-YL) PYRIMIDIN-4 (3H) -ONE AS TAU PROTEIN KINASE INHIBITOR
申请人:Sakai Daiki
公开号:US20110003988A1
公开(公告)日:2011-01-06
A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof:
which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
Asymmetrichydrogenation of unsaturated morpholines has been developed by using a bisphosphine-rhodium catalyst bearing a large bite angle. With this approach, a variety of 2-substituted chiral morpholines could be obtained in quantitative yields and with excellent enantioselectivities (up to 99% ee). The hydrogenated products could be transformed into key intermediates for bioactive compounds.