JANSSENS, FRANS EDUARD,SOMMEN, FRANCOIS MARIA,DE BOECK, BENOIT CHRISTIAN ALBERT GHISLAIN,LEENAERTS, JOSEPH ELISABETH
申请号：
CA2509088
公开号：
CA2509088C
申请日:
2003.12.17
申请国别(地区):
CA
年份:
2012
代理人:
摘要：
This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particularNK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and acombined NK1/NK2/NK3 antagonistic activity, their preparation, compositionscomprising them and their use as a medicine, in particular for the treatmentof schizophrenia, emesis, anxiety and depression, irritable bowel syndrom(IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation,asthma, micturition disorders such as urinary incontinence and nociception.The compounds according to the invention can be represented by general Formula(I) and comprises also the pharmaceutically acceptable acid or base additionsalts thereof, the stereochemically isomeric forms thereof, the N-oxide formthereof and prodrugs thereof, wherein all substituents are defined as in Claim1. In view of their capability to antagonize the actions of tachykinins byblocking the neurokinin receptors, and in particular antagonizing the actionsof substance P, Neurokinin A and Neurokinin B by blocking the NK1, NK2 and NK3receptors, the compounds according to the invention are useful as a medicine,in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particularschizoaffective disorders, depression, anxiety disorders, stress-relateddisorders, sleep disorders, cognitive disorders, personality disorders, eatingdisorders, neurodegenerative diseases, addiction disorders, mood disorders,sexual dysfunction, pain and other CNS-related conditions； inflammation；allergic disorders； emesis； gastrointestinal disorders, in particularirritable bowel syndrome (IBS)； skin disorders； vasospastic diseases；fibrosing and collagen diseases； disorders related to immune enhancement orsuppression and rheumatic diseases and body weight control.
