发明申请
US20080070924A1 Novel Formulations For Opioid-Based Treatments Of Pain Comprising 1-(1,2-Disubstituted Piperidinyl)-4-Substituted Piperazine Derivatives
审中-公开
用于基于阿片样物质治疗包含1-(1,2-二取代的哌啶基)-4-取代的哌嗪衍生物的疼痛的新型制剂
- 专利标题: Novel Formulations For Opioid-Based Treatments Of Pain Comprising 1-(1,2-Disubstituted Piperidinyl)-4-Substituted Piperazine Derivatives
- 专利标题(中): 用于基于阿片样物质治疗包含1-(1,2-二取代的哌啶基)-4-取代的哌嗪衍生物的疼痛的新型制剂
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申请号: US10560482申请日: 2004-06-07
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公开(公告)号: US20080070924A1公开(公告)日: 2008-03-20
- 发明人: Frans Eduard Janssens , Francois Maria Sommen , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck , Theo Frans Meert
- 申请人: Frans Eduard Janssens , Francois Maria Sommen , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck , Theo Frans Meert
- 优先权: EPPCT/EP03/06118 20030610
- 国际申请: PCT/EP04/51050 WO 20040607
- 主分类号: A61K31/496
- IPC分类号: A61K31/496 ; A61P25/04
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 NK1 antagonistic 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 NK1-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 NK1-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.
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