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首页> 外国专利> Pharmaceutical composition comprising trans-4 - 1 - 3,5-bis (trifluoromethyl) benzoyl - 2 - 4 - (phenylmethyl) - piperidinil - N - (2,6-dimethylphenyl) - 1 - piperazinilcetamida and an opioid Analgesic such as codeine,Morphine, Fentanyl, and use for the Prevention and / or treatment of Pain and / or emesis in nociception and opioid treatments.

Pharmaceutical composition comprising trans-4 - 1 - 3,5-bis (trifluoromethyl) benzoyl - 2 - 4 - (phenylmethyl) - piperidinil - N - (2,6-dimethylphenyl) - 1 - piperazinilcetamida and an opioid Analgesic such as codeine,Morphine, Fentanyl, and use for the Prevention and / or treatment of Pain and / or emesis in nociception and opioid treatments.

机译：药物组合物，其包含反式-4- [1- [3,5-双（三氟甲基）苯甲酰基] 2-4-（苯基甲基）-哌啶子] -N-（2,6-二甲基苯基）-1-哌嗪类烟酰胺和阿片类镇痛药用作可待因，吗啡，芬太尼，并在伤害感受和阿片类药物治疗中用于预防和/或治疗疼痛和/或呕吐。

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摘要

This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives having neurokinin antagonistic activity, in particular NKSUB1 /SUBantagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NKSUB1/SUB-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise NKSUB1/SUB-antagonists according to the general Formula (I) 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. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.
机译：本发明涉及用于基于阿片样物质的疼痛和/或伤害感受的新型制剂，其包含阿片样物质镇痛药和具有神经激肽拮抗活性，特别是NK 1 的1-（1,2-二取代哌啶基）-4-取代哌嗪衍生物。拮抗活性，所述制剂在制备用于预防和/或治疗呕吐，疼痛和/或伤害感受的药物中的用途，特别是在急性和慢性疼痛治疗中，更特别地在炎性，术后，急诊室（ER），突破性，神经性和癌症性疼痛治疗以及NK 1 受体拮抗剂在制备用于预防和/或治疗阿片类药物呼吸抑制和耐受性的药物中的用途基础的疼痛治疗。本发明的药物制剂包含通式（I）的NK 1 -拮抗剂，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-氧化物形式和其前药，其中所有取代基如权利要求1所定义。根据本发明的药物组合物在很大程度上减少了与阿片类镇痛药相关的许多不良副作用，特别是呼吸抑制和耐受性，从而增加了阿片类药物的总耐受性。说阿片类药物在疼痛治疗中。

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