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Treating neuropathic pain with neuropeptide FF receptor 2 agonists

A receptor agonist, receptor technology, applied in the field of compounds that selectively interact with this receptor subtype, can solve the problems of onset and inefficiency in all patients

Inactive Publication Date: 2006-12-06
ACADIA PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, existing treatments for neuralgia are not designed for these types of pain, so it is not surprising that these drugs are ineffective and do not work in all patients

Method used

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  • Treating neuropathic pain with neuropeptide FF receptor 2 agonists
  • Treating neuropathic pain with neuropeptide FF receptor 2 agonists
  • Treating neuropathic pain with neuropeptide FF receptor 2 agonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0255] Example 1: 1-(4-fluorobenzylideneamino)guanidine hydrochloride (2001)

[0256] Application of 4-fluorobenzaldehyde (5.0 mmol, 621 mg) gave the title compound (2001 ) (534 mg, 49%) as a white powder according to GP1. 1 H NMR (CD 3 OD) δ8.13(s, 1H), 7.85(m, 2H), 7.17(m, 2H); HPLC-MS (ammonium acetate) [M+H]+ = 181.1.

Embodiment 2

[0257] Example 2: 1-[(trifluoromethyl)benzylideneamino]guanidine hydrochloride (2002)

[0258] Application of 3-(trifluoromethyl)benzaldehyde (5.0 mmol, 871 mg) gave the title compound (2002) (643 mg, 48%) as a white powder according to GP1. 1 H NMR (CD 3 OD) δ8.22(s, 1H), 8.17(m, 1H), 8.05(m, 1H), 7.74(m, 1H), 7.65(m, 1H); HPLC-MS (ammonium acetate) [M+H ] + = 231.1.

Embodiment 3

[0259] Example 3: 1-[1-(3-bromophenyl)ethylideneamino]guanidine hydrochloride (2003)

[0260] According to GP1, the title compound (2003) (977 mg, 67%) was obtained as a white powder using 3'-bromoacetophenone (5.0 mmol, 995 mg). 1 H NMR (CD 3 OD) δ8.12 (ap.t, J=1.7Hz, 1H), 7.84 (ddd, J=8.0, 1.7, 1.0Hz, 1H), 7.59 (ddd, J=7.8, 2.0, 1.0Hz, 1H), 7.35(ap.t, J=8.0Hz, 1H), 2.36(s, 3H); HPLC-MS (ammonium acetate) [M+H] + = 255.1, 257.1.

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Abstract

The invention described below relates to the discovery of the neuropeptide FF receptor subtype that mediates acute nociception and chronic neuropathic pain, compounds that selectively interact with this receptor subtype and methods for treating acute pain and chronic neuropathic pain.

Description

[0001] related application [0002] This application claims priority to U.S. Provisional Application No. 60 / 506,130, filed September 25, 2003, by Scully et al., entitled "Treatment of Neuralgia with Neuropeptide FF Receptor 2 Agonists," and Scully et al., 2003 Priority to U.S. Provisional Application No. 60 / 508,008, entitled "Treatment of Neuralgia with Neuropeptide FF Receptor 2 Agonists," filed October 2, 2010, which is incorporated herein by reference in its entirety, including all drawings. field of invention [0003] Aspects of the invention described below relate to methods of treating acute pain and chronic neuralgia using compounds that modulate the activity of neuropeptide FF receptor subtypes that mediate acute nociception and chronic neuralgia. Aspects of the invention also relate to compounds that selectively interact with such receptor subtypes and methods of identifying said compounds. Background of the invention [0004] Pain is a common human experience. It...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N33/14G01N33/94C07C279/36A61K31/155
Inventor 奥德拉·L·斯库利罗伯特·E·戴维斯金伯利·E·瓦努韦尔路易斯·罗伯托·加德尔耶尔韦和·拉梅赫尼古拉斯·迈克尔·凯利法布里奥·贝尔托齐弗拉迪米尔·舍伯克基
Owner ACADIA PHARMA INC
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