首页> 外国专利> In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

机译:考虑到它们通过阻断神经激肽受体来拮抗神经激肽的作用,特别是通过阻断NK1受体来拮抗P物质的作用的能力,根据本发明的化合物可用作药物,特别是在预防和治疗中。治疗神经激肽介导的疾病,例如中枢神经系统疾病,尤其是抑郁症,焦虑症,与压力有关的疾病,睡眠障碍,认知障碍,人格障碍,精神分裂性障碍,进食障碍,神经退行性疾病,成瘾障碍,情绪疾病,性功能障碍,疼痛和其他中枢神经系统相关疾病;炎;过敏性疾病呕吐胃肠道疾病,特别是肠易激综合症(IBS);皮肤疾病;血管痉挛性疾病;纤维化和胶原蛋白疾病;与免疫增强或抑制,风湿性疾病和体重控制有关的疾病。

摘要

The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS. 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.In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
机译:本发明涉及具有神经激肽拮抗活性,特别是NK1拮抗活性的取代的1,4-二哌啶-4-基-哌嗪衍生物,它们的制备,包含它们的组合物以及它们作为药物的用途,特别是用于治疗呕吐,焦虑,抑郁,疼痛,胰腺炎和IBS。本发明的化合物可以由通式(I)表示,并且还包含其药学上可接受的酸或碱加成盐,其立体化学异构体形式,其N-氧化物形式以及其前药,其中所有取代基均被定义如权利要求1所述,考虑到它们通过阻断神经激肽受体来拮抗神经激肽的作用,特别是通过阻断NK1受体来拮抗P物质的作用的能力,本发明的化合物可用作药物。特别是在神经激肽介导的疾病的预防和治疗中,例如中枢神经系统疾病,特别是抑郁症,焦虑症,与压力有关的疾病,睡眠障碍,认知障碍,人格障碍,分裂情感障碍,进食障碍,神经退行性疾病,成瘾障碍,情绪障碍,性功能障碍,疼痛和其他与CNS相关的疾病意图炎;过敏性疾病呕吐胃肠道疾病,特别是肠易激综合症(IBS);皮肤疾病;血管痉挛性疾病;纤维化和胶原蛋白疾病;与免疫增强或抑制,风湿性疾病和体重控制有关的疾病。

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