[EN] 2-PYRIDINYL[7-(SUBSTITUTED-PYRIDIN-4-YL) PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]METHANONES<br/>[FR] 2-PYRIDINYL[7-(PYRIDIN-4-YLE SUBSTITUE)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]METHANONES
申请人:DOV PHARMACEUTICAL INC
公开号:WO2005084439A1
公开(公告)日:2005-09-15
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.
本发明提供了具有化学结构式(I)的新型2-吡啶基[7-(吡啶-4-基)吡唑并[1,5-a]嘧啶-3-基]甲酮,其中4-吡啶基环上至少有一个取代基。该发明还提供了应用化学式(I)的新型2-吡啶基[7-(吡啶-4-基)吡唑并[1,5-a]嘧啶-3-基]甲酮的组合物和方法,用于调节GABA和GABA受体生理,以引发哺乳动物主体中的治疗反应,以缓解神经系统或精神障碍,包括中风、头部创伤、癫痫、疼痛、偏头痛、情绪障碍、焦虑、创伤后应激障碍、强迫性障碍、躁狂、双相障碍、精神分裂症、癫痫发作、抽搐、耳鸣、包括阿尔茨海默病、肌萎缩侧索硬化和帕金森病在内的神经退行性疾病、亨廷顿舞蹈症、抑郁症、双相障碍、躁狂、三叉神经痛和其他神经痛、神经痛、高血压、脑缺血、心律失常、肌张力过高、物质滥用、肌阵挛、本体震颤、运动障碍和其他由GABA和/或GABA受体介导的新生儿脑出血、痉挛性瘫痪以及痉挛性瘫痪,以及其他精神和神经障碍的方法。