2-pyridinyl[7-(substituted-pyridin-4-yl)...

A - Human Necessities – 01 – N

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A01N 43/00 (2006.01) A61K 31/33 (2006.01)

Patent

CA 2559295

The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5~- a]pyrimidin-3-yl]methanones with at least one substituent on the 4-pyridinyl ring having the chemical structure of formula (I): The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4- yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula: (I) in to modulate GABA and GABA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and/or GABA receptors.

Nouvelles 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]méthanones présentant au moins un substituant sur le noyau 4-pyridinyle, dont la structure chimique correspond à la formule (I). La présente invention concerne en outre des compositions et méthodes reposant sur l'utilisation de ces nouvelles 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]méthanones de formule (I) pour moduler les fonctions de GABA et du récepteur GABA et provoquer des réactions thérapeutiques chez des sujets mammaliens pour soulager des troubles neurologiques ou psychiatriques, y compris l'accident vasculaire cérébral, le traumatisme cérébral, l'épilepsie, la douleur, la migraine, les troubles de l'humeur, l'anxiété, les troubles liés au stress post-traumatique, les troubles obsessionnels-compulsifs, la manie, la psychose maniaco-dépressive, la schizophrénie, les crises d'épilepsie, les convulsions, l'acouphène, les troubles neurodégénératifs dont la maladie d'Alzheimer, la maladie de Charcot et la maladie de Parkinson, la chorée de Huntington, la dépression, les troubles obsessionnels-compulsifs, la manie, la névralgie faciale et autres névralgies, la douleur neuropathique, l'hypertension, l'ischémie cérébrale, l'arythmie cardiaque, la myotonie, la toxicomanie, la myoclonie, le tremblement permanent, la dyskinésie et d'autres troubles des mouvements, l'hémorragie cérébrale néonatale et l'hypertonie spastique, ainsi que d'autres troubles psychiatriques et neurologiques médiés par GABA et / ou les récepteurs GABA.

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