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首页> 外国专利> Substituted 1,4-di-piperidin-4-yl-piperazine derivative combined with an opioid analgesic and their use for the treatment of pain and side-effects associated with opioid-based treatments

Substituted 1,4-di-piperidin-4-yl-piperazine derivative combined with an opioid analgesic and their use for the treatment of pain and side-effects associated with opioid-based treatments

机译：取代的1,4-二哌啶-4-基-哌嗪衍生物与阿片类镇痛药的组合及其在治疗与阿片类药物相关的疼痛和副作用中的用途

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This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-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 opioid-based 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 in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise a pharmaceutically acceptable carrier and, as active ingredients, a therapeutically effective amount of an opioid analgesic and 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 emesis, 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/或伤害感受治疗的新制剂，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1，4-二哌啶-4-基-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，特别是在基于阿片样物质的急性和慢性疼痛治疗中，尤其是在炎症，手术室，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/或治疗阿片类药物性呼吸抑制的药物中的用途基础的疼痛治疗。根据本发明的药物制剂包含药学上可接受的载体以及作为活性成分的治疗有效量的根据通式（I）的阿片类镇痛药和NK 1 拮抗剂，药学上可接受的酸或其碱加成盐，其立体化学异构体形式，其N-氧化物形式及其前药，其中所有取代基均如权利要求1所定义。根据本发明的药物组合物在很大程度上减少了许多不需要的侧-与阿片类镇痛药有关的副作用，尤其是呕吐，呼吸抑制和耐受性，从而增加了所述阿片类药物在疼痛治疗中的总耐受性。

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