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N-substituted benzenepropanamide or benzenepropenamide for use in the treatment of pain and inflammation

A technology of -OR6, a compound, applied in the field of N-substituted phenylalanamide or phenylacrylamide for the treatment of pain and inflammation, capable of solving problems such as side effects

Active Publication Date: 2012-12-12
NOVAREMED LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although widely used, NSAIDs can have side effects, sometimes serious ones, including digestive problems, bleeding problems, problems related to retaining fluid, and increased risk of heart and blood vessel disorders

Method used

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  • N-substituted benzenepropanamide or benzenepropenamide for use in the treatment of pain and inflammation
  • N-substituted benzenepropanamide or benzenepropenamide for use in the treatment of pain and inflammation
  • N-substituted benzenepropanamide or benzenepropenamide for use in the treatment of pain and inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0191] Antinociceptive effects of compound 2 and compound 3

[0192] The purpose of this study was to evaluate the antinociceptive activity of test items in the mouse hot plate test when administered subchronically. The lapse of response time to paw licking or jumping was measured following placement on a heated surface (hot plate) to determine a potential antinociceptive effect in mice.

[0193] A total of 42 Balb / c mice (12 weeks old) were used. At study initiation, mice were approximately 25 g, male. The minimum and maximum weights in the group were within ±10% of the group mean weight.

[0194] and (Perigo) compared to test compounds 2 and 3. Use DMSO solution. Six groups of mice (n=7 or n=8 mice each) were tested, the last group receiving

[0195]

[0196] Formulations prepared according to the table below were used for administration to groups of mice.

[0197]

[0198]

[0199] All groups received the drug orally daily for 16 days. Hot plate experime...

Embodiment 2

[0208] Nociceptin activity using compound 2

[0209] Using the procedure outlined in Example 1, 40 male mice (Balb / c, 9 weeks old, untested) were divided into 5 groups (8 mice each) and treated daily with the formulations shown in the table below ( 0 minutes, orally).

[0210]

[0211] Animals were assayed on a hot plate at: -60, 0, 120, 240, 360, 420 and 480 minutes. The average temperature of the hot plate is 52±1 degrees.

[0212] Figure 2a and 2b Data for these tests are presented.

Embodiment 3

[0214] Nociceptin activity using compound 2

[0215] Using the procedure outlined in Example 1, 40 male mice (Balb / c, 9 weeks old, untested) were divided into 5 groups (8 mice each) and treated daily with the formulations shown in the table below ( 0 minutes, orally).

[0216]

[0217] Animals were assayed on a hot plate at: -60, 0, 60, 120, 180, 240, 300 and 360 minutes. The average temperature of the hot plate is 52±1 degrees.

[0218] Figure 3a , 3b and 3c present the data for this test.

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PUM

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Abstract

Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula (I), in which: the dotted line represents a single or a double bond; and R5 and R5' are independently -H, -OH or -OR6, where R6 is a linear or branched C1-C4 alkyl; X is -CH2O-,; Z is -CH2CH2O-CH(CH3)CH2O- or -CH2CH(CH3)O-; m is 1; and n is an integer of 1- 5. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.

Description

technical field [0001] The present invention relates to the treatment or prevention of pain and provides methods of treatment or prevention of pain and the use of certain compounds in the manufacture of medicaments for the treatment or prevention of pain in humans and non-human animals. Background technique [0002] Pain is a multilevel, or multidimensional, experiential response to various stimulus conditions. Pain is defined by the International Society for the Study of Pain (IASP) as "an unpleasant sensory and emotional experience associated with, or described in light of, acute or underlying tissue damage". [0003] Pain in animals is often the result of nociception (ie, nervous system activity caused by stimulation of nociceptors). Neuropathic pain differs from nociceptive pain in that it involves damage to the nerves that lead to the sensation of pain. In certain pains, the pain results from some form of damage in the brain. Pain can occasionally be psychogenic, ie,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61P29/00
CPCA61K31/165A61P25/04A61P29/00
Inventor E·卡普兰
Owner NOVAREMED LTD
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