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NSAID and sigma receptor ligand combinations

A technology of synergistic composition and ligand, which is applied in the field of pain prevention and/or treatment, and can solve problems such as the incomplete understanding of the mechanism of action of Analgin

Inactive Publication Date: 2016-05-25
LAB DEL DR ESTEVE SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Likewise, the mechanism of action of Analgin is not fully understood

Method used

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  • NSAID and sigma receptor ligand combinations
  • NSAID and sigma receptor ligand combinations
  • NSAID and sigma receptor ligand combinations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0245] Example 1: Synthesis of 4-{2-[5-methyl-1-(naphthalene-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (compound 63) and its hydrochloric acid Salt

[0246]

[0247] Compound 63 can be prepared according to the method disclosed in the previous application WO2006 / 021462. Its hydrochloride can be prepared according to the following steps:

[0248] Compound 63 (6.39 g) was dissolved in ethanol saturated with hydrochloric acid, then stirred for several minutes to obtain a mixture, which was evaporated to dryness. The residue was crystallized from isopropanol. The mother liquor of the first crystallization is subjected to the second crystallization by concentration. A total of 5.24 g (63%) of the corresponding hydrochloride (m.p. = 197-199° C.) were obtained through two crystallizations.

[0249] 1 H-NMR (DMSO-d 6 )δppm: 10, 85 (bs, 1H), 7, 95 (m, 4H), 7, 7 (dd, J = 2, 2, 8, 8Hz, 1H), 7, 55 (m, 2H), 5 ,9(s,1H),4,55(m,2H),3,95(m,2H),3,75(m,2H),3,55-3,4(m,4H),3, 2(m,2H),2,...

Embodiment 2

[0251] Example 2: Evaluation of analgesic effect in the treatment of postoperative pain

[0252] 2.1 General experimental plan

[0253] Rat's anesthesia induction Performed with 3% veterinary isoflurane, Ohmeda vaporizer and anesthesia room. Anesthesia was maintained by isoflurane vapor through the nose of the animal during the surgical procedure. Once the rat is anesthetized, the rat is laid flat in the prone position and its right hind paw is cleaned with alcohol.

[0254] Then, an approximately 10 mm skin incision was made with a scalpel on the rat's hind paw, starting approximately 5 mm from the heel and extending toward the toes. Locate the fascia and elevate the muscle with curved scissors, making a longitudinal incision of approximately 5 mm, leaving the muscle origin and insert intact. The skin of the paw was closed using a suture needle and silk thread (3.0) and the wound was cleaned with povidone.

[0255] Evaluations were performed 30 minutes after product adm...

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PUM

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Abstract

The invention refers to a synergistic combination comprising a sigma ligand, particularly a Sigma ligand of general formula (I), and NSAID compound, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and / or treatment of pain.

Description

technical field [0001] The present invention relates to an active substance composition especially useful for the prophylaxis and / or treatment of pain. Background technique [0002] The treatment of pain symptoms has important significance in the field of medicine. Currently, there is a high demand for pain therapy worldwide. The large amount of scientific work that has recently emerged in the field of applied analgesics also demonstrates the urgent need for specific treatments for pain symptoms. [0003] The International Association for the Study of Pain (IASP) defines pain as "an unpleasant sensory and emotional experience related to actual or potential tissue damage or described in terms of such damage" (IASP, Classification of chronic pain, second edition, IASP Press( 2002), 210). Although pain is a complex process influenced by physiological and psychological factors and is often subjective, it can be classified according to its cause or syndrome. Pain can be class...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/415A61K31/167A61K31/196A61K31/4152A61K45/06A61K31/4523A61K31/4725A61K31/496A61K31/5377A61P29/00
CPCA61K45/06A61K31/167A61K31/196A61K31/415A61K31/4152A61K31/4523A61K31/4725A61K31/496A61K31/5377A61P25/02A61P25/04A61P29/00A61P43/00A61K2300/00A61K31/192A61K31/635
Inventor 丹尼尔·赞马尼罗·卡斯坦尼杜恩里克·波蒂略·萨利多恩里克·何塞·科沃斯·莫拉尔
Owner LAB DEL DR ESTEVE SA
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