Substituted pyrazinone derivatives as alpha2c-adrenoreceptor antagonists

A technology of pyrazinone and derivatives, applied in the field of substituted pyrazinone derivatives
CN101346368AInactive Publication Date: 2009-01-14JANSSEN PHARMA NV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JANSSEN PHARMA NV
Publication Date
2009-01-14
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereo- chemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having se- lective a2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and / or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and / or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.
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Description

technical field

[0001] The present invention relates to selective α 2C - Adrenergic receptor antagonist activity as well as substituted pyrazinone derivatives having 5-HT reuptake inhibitory activity. The invention also relates to their preparation, pharmaceutical compositions comprising said derivatives and their use as medicaments, in particular for the treatment of diseases of the central nervous system. Background of the invention

[0002] Adrenoceptors form the binding site between the endogenous catecholamines epinephrine and norepinephrine and numerous target cells in the body that mediate the biological effects of the sympathetic nervous system. They are divided into three main subtypes, α 1 、α 2 and beta 3 . So far, nine different subtypes of adrenaline have been cloned from several species: α 1A 、α 1B 、α 1D 、α 2A 、α 2B 、α 2C , β 1 , β 2 and beta 3 . (Hieble, J.P. et al. J. Med. Chem. 1995, 38, 3415-3444). Available α 2 Ligands are only marginally s...

Claims

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