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Use of spiro imidazolidine-4, 3'-indole-2, 2', 5' (1H) triones for treatment of conditions associated with vanilloid receptor 1

A vanilloid receptor and imidazolidine technology, which can be used in medical preparations containing active ingredients, bone diseases, respiratory diseases, etc., and can solve problems such as irritation, neurotoxicity, hypothermia, etc.

Inactive Publication Date: 2009-04-22
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although VR1 receptor agonists can be used as analgesics by destroying nociceptors, the use of agonists such as capsaicin and its analogs is limited because of their irritation, neurotoxicity and low induction. body temperature

Method used

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  • Use of spiro imidazolidine-4, 3'-indole-2, 2', 5' (1H) triones for treatment of conditions associated with vanilloid receptor 1
  • Use of spiro imidazolidine-4, 3'-indole-2, 2', 5' (1H) triones for treatment of conditions associated with vanilloid receptor 1
  • Use of spiro imidazolidine-4, 3'-indole-2, 2', 5' (1H) triones for treatment of conditions associated with vanilloid receptor 1

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0246] The invention will be illustrated by the following non-limiting examples.

[0247] usual method

[0248] The invention will be illustrated by the following examples, in which, in general:

[0249] (i) Unless otherwise indicated, the operation is carried out at normal or room temperature, that is, 17-25°C and an atmosphere of an inert gas such as argon;

[0250] (ii) Evaporation is carried out by rotary evaporation under vacuum, followed by work-up procedures after removal of residue by filtration;

[0251] (iii) 1 H NMR spectra were measured by Brucker at 400 MHz. Mass spectrometry was performed using electrospray (LC-MS; LC: Waters2790, column XTerra MS C 8 2.5μm 2.1X30mm, buffer gradient H 2 O+0.1%TFA:CH 3 CN+0.04%TFA, MS: micromass ZMD / / ammonium acetate buffer) ionization technique;

[0252] (iii) if there is a yield, it is not necessarily the maximum obtainable;

[0253] (v) use the following abbreviations:

[0254] alloc allyloxycarbonyl

[0255] DCE D...

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PUM

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Abstract

The invention relates to use of spiro [imidazolidine-4,3-indole]2,2',5'(1H) Triones for treatment of conditions accociated with vanilloid receptor 1. Furthermore, the present invention relates to a new use of spiro-hydantoin derivatives of formula (I), or salts, solvates or solvated salts thereof, as well as to new compounds, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

Description

technical field [0001] The present invention relates to the novel use of the spiro-hydantoin derivative of formula I or its salt, solvate or solvate salt, and relates to the novel compound, its preparation method and the novel compound used in its preparation Intermediates, to pharmaceutical compositions containing said therapeutically active compounds, and to the use of said active compounds in therapy. Background technique [0002] Compounds of general formula I below are disclosed in EP66378 and EP28906. EP66378 and EP28906 further describe the use of these compounds to inhibit the enzyme aldose reductase. [0003] It has now been found that the spiro-hydantoin derivatives disclosed in EP 66378 and EP 28906 are more suitable for inhibiting the vanilloid receptor 1 (VR1). These inhibitors are suitable for the treatment of disorders associated with vanilloid receptor 1 in the central and peripheral nervous system. In particular, the compounds of the invention are useful ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/10A61K31/4188A61P25/02
CPCC07D487/10A61K31/4188A61P1/00A61P1/04A61P1/08A61P1/18A61P9/10A61P11/00A61P13/00A61P13/10A61P19/02A61P25/00A61P25/02A61P25/04A61P29/00A61P43/00
Inventor 露西·霍罗斯佐克卡曼·利昂米洛斯劳·托马斯泽夫斯基克里斯托弗·沃尔波尔
Owner ASTRAZENECA AB