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Use of sigma receptor ligands for prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (ic/bps)

A technique for bladder pain and cystitis, which is applied in the application field of sigma receptor ligands in the prevention and treatment of pain associated with interstitial cystitis/bladder pain syndrome (IC/BPS), and can solve the problem of no treatment, etc. question

Inactive Publication Date: 2016-03-02
LAB DEL DR ESTEVE SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] In conclusion, since IC / BPS-related pain also represents a visceral neuropathic pain syndrome characterized by hyperalgesia for which no standard treatment is known, it is necessary to provide a treatment for IC / BPS-related pain, especially for patients with IC / BPS New forms of treatment for neuropathic pain, allodynia, hyperalgesia, and peripheral neuropathy that develop during and / or after BPS

Method used

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  • Use of sigma receptor ligands for prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (ic/bps)
  • Use of sigma receptor ligands for prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (ic/bps)
  • Use of sigma receptor ligands for prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (ic/bps)

Examples

Experimental program
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Effect test

Embodiment 1

[0195] Example 1: Synthesis of 4-{2-[5-methyl-1-(naphthalene-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine hydrochloride (compound 63.HCl )

[0196]

[0197] 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:

[0198] Compound 63 (6.39 g) was dissolved in ethanol saturated with hydrochloric acid. The mixture was then stirred for several minutes and 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.

[0199] 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), 2,35(s,3H).

[0200] H...

Embodiment 2

[0201] Example 2: Role of the sigma-1 receptor in cyclophosphamide-induced cystitis

[0202] Existing animal models of visceral pain in mice have limited practical utility because they are not viscera specific. The animal model of cyclophosphamide-induced cystitis maintains an inflammatory feature confined to the bladder, resulting in an ideal model for studying the genetic and physiological basis of visceral pain as interstitial inflammation / bladder pain syndrome (IC / PBS) (Elsa Anton, 2002; Bon et al., 2003; JUrol. Sep; 170(3):1008-12).

[0203] 2.1 Materials and methods

[0204] 2.1.1 Animals

[0205] The mice used in the experiment were female CD-1 mice, which were divided into wild type (Spain, Barcelona, ​​Charles River, wild type WT) and σ-1 receptor knockout type (Spain, Barcelona, ​​Esteve laboratory, σ 1 -KO), the mouse body weight was 25-30g. The above σ 1 -KO mice were generated in the CD-1 background as described previously (Entrena et al., 2009). Before the ...

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Abstract

The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and / or treat pain associated to interstitial cystitis / bladder pain syndrome (IC / BPS).

Description

technical field [0001] The present invention relates to the use of sigma receptor ligands, especially certain pyrazole derivatives and pharmaceutical compositions thereof in the treatment and / or prevention of pain associated with interstitial cystitis / bladder pain syndrome (IC / BPS) application. 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 influence...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/415A61K31/4155A61K31/485A61K31/5377A61P13/10A61P29/00
CPCA61K31/415A61K31/4155A61K31/485A61K31/5377A61P13/10A61P25/00A61P25/02A61P29/00A61P43/00A61K2300/00A61K45/06
Inventor 何塞-米格尔·维拉-赫内恩德斯曼纽尔·梅尔洛斯-罗卡何塞-曼纽尔·贝延斯-卡夫雷拉克鲁兹-米格尔·C-马丁内斯
Owner LAB DEL DR ESTEVE SA
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