[EN] HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS<br/>[FR] COMPOSÉS D'HÉTÉROARYLOXYHÉTÉROCYCLYLE CONVENANT COMME INHIBITEURS DE LA PDE10
申请人:AMGEN INC
公开号:WO2011143495A1
公开(公告)日:2011-11-17
Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof:
wherein, each of R
1
and R
2
independently represents a group such as a hydrogen atom or a halogen atom; R
3
represents a group such as a hydrogen atom; each of R
4
and R
5
independently represents a group such as a hydrogen atom, a halogen atom or a C
1-4
alkyl group; each of R
6
and R
7
independently represents a hydrogen atom or a C
1-4
alkyl group; X represents a group such as a C
3-10
cycloalkyl group, C
6-10
aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group α; Y represents a group such as —CO—, —O— or —NRa—, and Ra represents a group such as a hydrogen atom or a C
1-4
alkyl group.
The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.