JANSSENS, FRANS EDUARD,严森,嚴森,SCHOENTJES, BRUNO,布鲁诺,布魯諾,COUPA, SOPHIE,柯帕,PONCELET, ALAIN PHILIPPE,彭思特,SIMONNET, YVAN RENE FERDINAND,史孟特
申请号：
TW094110661
公开号：
TWI389901B
申请日:
2005.04.04
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
This invention concerns substituted diaza－spiro－[5.5]－undecane derivatives having neurokinin antagonistic activity, in particular NK1antagonistic activity, a combined NK1/NK2antagonistic activity, a combined NK1/NK3antagonistic activity and a combined NK1/NK2/NK3antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythmdisturbances, pre－eclampsia, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence.The compounds according to the invention can be represented by general Formula (I)and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N－oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.本發明係有關具有神經激肽拮抗劑活性，特定言之NK1拮抗劑活性、組合之NK1/NK2拮抗劑活性、組合之NK1/NK3拮抗劑活性及組合之NK1/NK2/NK3拮抗劑活性之經取代之二氮雜－螺－[5.5]－十一烷衍生物，及其製法、含其之組合物及其作為醫藥之用途，特定言之用於治療與/或預防精神分裂症、嘔吐、焦慮症與抑鬱症、應激性腸部症候群(IBS)、生理時鐘紊亂、子癲前期、傷害感受、疼痛，特定言之內臟與神經病變性疼痛、胰炎、神經發炎、氣喘、COPD與排尿障礙如：尿失禁。根據本發明化合物可由通式(I)代表且亦包括其醫藥上可接受之酸或鹼加成鹽、其立體化學異構型、其N－氧化物型與其前藥，其中所有取代基均如申請專利範圍第1項之定義。
