[EN] QUINOLINONE-PYRAZOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS<br/>[FR] COMPOSÉS DE QUINOLÉINONE-PYRAZOLONE MODULATEURS ALLOSTÉRIQUES POSITIFS DU RÉCEPTEUR M1
申请人:MERCK SHARP & DOHME
公开号:WO2011049731A1
公开(公告)日:2011-04-28
The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Therapeutic pyrazoloquinoline derivatives
申请人:Helicon Therapeutics, Inc.
公开号:US07872002B2
公开(公告)日:2011-01-18
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms:
The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).