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SUBSTITUTED DIAZA-SPIRO-4.5-DECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS

机译:取代的DIAZA-SPIRO- [4.5]-癸烷衍生物及其作为神经激肽拮抗剂的用途

摘要

This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic 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 rhythm disturbances, pre-eclampsia, nociception, pain, in particular 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, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
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,联合的NK1 / NK2拮抗活性,联合的NK1 / NK3拮抗活性和联合的NK1 / NK2拮抗活性的取代的二氮杂螺-[4.5]-癸烷衍生物。 ,其制剂,包含它们的组合物及其作为药物的用途,特别是用于治疗和/或预防精神分裂症,呕吐,焦虑和抑郁,肠易激综合征(IBS),昼夜节律紊乱,先兆子痫,痛觉,疼痛尤其是内脏和神经性疼痛,胰腺炎,神经源性炎症,哮喘,慢性阻塞性肺疾病(COPD)和排尿障碍(如尿失禁)。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,其中所有取代基定义为在权利要求1中。

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