JANSSENS, FRANS EDUARD,严森,嚴森,SOMMEN, FRANCOIS MARIA,宋门,宋門,DE BOECK, BENOIT CHRISTIAN ALBERT GHISLAIN,柏艾克,LEENAERTS, JOSEPH ELISABETH,李纳兹,李納茲
申请号：
TW094110941
公开号：
TWI358298B
申请日:
2005.04.07
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
The invention concerns substituted 4－alkyl－and 4－alkanoyl－piperidine derivatives having neurokinin antagonistic activity, in particular NK1antagonistic activity and a combined NK1/NK3antagonistic activity, 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 rhythm disturbances, pre－eclampsia, nociception, pain, in particuIar visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (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, theN－oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.本發明係關於具有神經激肽拮抗活性之經取代之4-烷基-及4-烷醯基-六氫吡啶衍生物，特別是NK1拮抗活性及結合的NK1/NK3拮抗活性，含彼之組成物及其作為藥劑之用途，特別是用於治療及/或預防精神分裂症、嘔吐、焦慮及憂鬱、應激性腸徵候群(IBS)、晝夜節律紊亂、子癇前期、疼痛感受、疼痛尤其是內臟及神經變性痛、胰腺炎、神經性發炎、氣喘、慢性阻塞性肺病(COPD)及排尿障礙例如尿失禁。；根據本發明之化合物可用通式(I)代表且也包括其藥學上可接受的酸或鹼加成鹽，其立體化學異構物形式、其N-氧化物形式及其前驅藥，其中全部的取代基係根據申請專利範圍第1項定義。
