VANILLOID ANALOGUES CONTAINING RESINIFERATOXIN PHARMACOPHORES AS POTENT VANILLOID RECEPTOR AGONISTS AND ANALGESICS, COMPOSITION AND USES THEREOF

摘要

PURPOSE: Provided is a vanilloid analogue which contains resiniferatoxin pharmacophores so as to be useful as a potent vanilloid receptor agonists and analgesics. Also, a pharmaceutical composition is provided which contains an effective amount of the same, as an active ingredient and a pharmaceutically acceptable carrier, and which is used for treating bladder hypersensitivity. CONSTITUTION: A vanilloid analogue is represented by the formula (1) wherein, X is an oxygen atom or a sulfur atom; A is -NHCH2- or -CH2; R1 is a substituted or unsubstituted alkylaryl group having 1-4 carbons, or R4CO-(in which, R4 is an alkyl group having 1-18 carbons, an alkenyl group having 2-18 carbons, or a substituted or unsubstituted aryl group having 6-10 carbons); R2 is a hydrogen atom, an alkyl group having 1-6 carbons, an alkoxy group having 1-6 carbons, a haloalkyl group having 1-6 carbons or a halogen atom; R3 is a hydrogen atom, an alkyl group having 1-4 carbons, an amino alkyl group, a diacid monoester group, or an alpha-alkylacid group; and * represents a chiral carbon atom.