公开(公告)号：US20080312276A1

公开(公告)日：2008-12-18

申请号：US12136986

申请日：2008-06-11

申请人： Josephus H.M. Lange ,  Hendrik C. Wals ,  Bernard J. Vliet Van ,  Mahmut Yildirim

发明人： Josephus H.M. Lange ,  Hendrik C. Wals ,  Bernard J. Vliet Van ,  Mahmut Yildirim

IPC分类号： A61K31/4709 ,  C07D231/06 ,  C07D401/12 ,  A61P25/28 ,  A61K31/415

CPC分类号： C07D231/06 ,  C07D401/12 ,  C07D409/04

摘要： The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders.Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.

摘要翻译： 本发明涉及作为大麻素CB1受体调节剂的4,5-二氢 - （1H） - 吡唑（吡唑啉）衍生物，包含这些化合物的药物组合物，其合成方法，制备用于其合成的新中间体的方法， 以及制备组合物的方法。 本发明还涉及施用于患者的化合物和组合物在多发性硬化，创伤性脑损伤，疼痛，包括慢性疼痛，神经性疼痛，急性疼痛和炎性疼痛，骨质疏松症，食欲障碍，癫痫，阿尔茨海默病中的治疗效果的用途 ，Tourette综合征，脑缺血，呕吐，恶心和胃肠道疾病。 本公开的化合物涉及式（I）：其中取代基具有说明书中给出的定义。