TRPV1 agonists, formulations containing them and uses thereof

Details TRPV1 agonists, formulations containing them and uses thereof TRPV1 agonists, formulations containing them and uses thereof

2005-07-06

2008-09-30

Witherspoon, Sikarl A (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

C560S106000, C560S110000, C514S561000, C514S563000

Reexamination Certificate

active

07429673

ABSTRACT:
The compounds of the general formula (I) in which X is represents two hydrogen atoms, a π-bond, oxygen or methylene: R2 is a C6-C12aryl, or arylalkyl residue: R3 is hydrogen, 2-hydroxyethyl or 2-aminoethyl are useful for the treatment of pathologies mediated by vanilloid receptors type I.

REFERENCES:
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patent: 1 426 047 (2004-06-01), None
patent: WO 00/16756 (2000-03-01), None
Appendino, Giovanni et al: “N-Acylvanillamides: Development of an Expeditious Synthesis and Discovery of New Acyl Templates for Powerful Activation of the Vanilloid Receptor” Journal of Medicinal Chemistry, 45(17), 3739-3745 CODEN: JMCMAR; ISSN: 0022-2623, 2002, XP002346966 cited in the application p. 3742; compound 1Q, p. 3742, col. 1, last paragraph—p. 3742, col. 2, paragraph 1.
Janusz J M et al: “Vanilloids. 1. Analogs of Capsaicin With Antinociceptive and Antiinflammatory Activity” Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 36, No. 18, 1993, pp. 2595-2604, XP001008868 ISSN: 0022-2623 table III; compound 36.
Appendino, Giovanni et al: “Development of the first ultra-potent “capsaicinoid” agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential” Journal of Pharmacology and Experimental Therapeutics, 312(2), 561-570 CODEN: JPETAB; ISSN: 0022-3565, 2005, XP008053161, p. 566, col. 1, line 30-line 35 p. 566; table 1.

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