Simplified resiniferatoxin analogues as vanilloid receptor...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

Reexamination Certificate

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C560S255000

Reexamination Certificate

active

06872748

ABSTRACT:
The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions that have such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for preventing, alleviating or treating pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neutopathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease or urgent urinary incontinence.

REFERENCES:
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The Cloned Capsaicin Receptor Integrates Multiple Pain-Producing Stimuli, M.Tominaga et al., Neuron, vol. 21, 531-543, Sep. 1998.
Impaired Nociception & Pain Sensation in Mice Lacking the Capsaicin Receptor, MJ Caterina et al., Apr. 14, 2000, vol. 288 Science, pp. 306-313.
Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia, Letters to Nature, vol. 405, May 11, 2000, pp. 183-187.
3-Acyloxy-2-phenalkylpropyl Amides & Esters of Homovanillic Acid as Novel Vanilloid Receptor Agonists, Bioorganic & Medicinal Chemistry Letters 9 (1999) 2909-2914.
Capsaicin-like agonists, R. Wrigglesworth et al., Drugs of the Future 1998, 23(5): 531-538.

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