| abstract |
The present invention relates to substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives antagonistic to neurokinin activity, in particular those having NK1 antagonist activity, a combination of NK1 / NK3 antagonist activity and a combination of NK1 / NK2 / NK3 antagonistic action, the process of their preparation, preparations containing them and their use in medicine, especially in the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disorders, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the present invention can be represented by general formula (I) and also include their pharmaceutically acceptable acid and base addition salts, their stereochemically isomeric forms, their N-oxide form and their prodrugs, in which all substituents are as defined. of Claim 1. Due to their ability to antagonize tachykinins by neurokinin receptor blockade, in particular by antagonizing the action of substance P, neurokinin A and neurokinin B by blocking NK1, NK2 and NK3 receptors, the compounds of the present invention are useful drugs, especially in the prophylaxis and treatment of tachykinin-mediated conditions such as, for example, CNS diseases, especially schizoaffective diseases, depression, anxiety, stress disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction, mood disorders, sexual dysfunction, pain and other related conditions. with and CNS; inflammation; allergic diseases; emeze; gastrointestinal diseases, especially irritable bowel syndrome (IBS); skin diseases; vasospastic diseases, fibrin diseases and collagenosis; disorders associated with enhanced immune function or suppression of the immune system and rheumatic diseases, as well as weight control. |