FIELD: organic chemistry, medicine. SUBSTANCE: invention relates to novel retinoid compounds of general formulas (I) , (II) , (III) and (IV) eliciting retinoid negative hormonal biological activity and/or similar activity of antagonist of retinoids based on thereof, method of assay of antagonists of retinoid hormones, method of treatment of pathological state in mammal showing sensitivity to treatment with retinoid antagonist or negative hormone by administration of compound of the formula (I) or (II). In indicated compounds of formulas (I), (II), (III) and (IV) X is taken among oxygen, sulfur atom, [C(R1)2]n′, respectively; R1 means hydrogen atom or alkyl with number of carbon atoms from 1 to 6; R2 means hydrogen atom pr lower alkyl with number of carbon atoms from 1 to 6, fluorine, chlorine, bromine, iodine atoms, CF3, fluorosubstituted alkyl with number of carbon atoms from 1 to 6, hydroxygroup, SH-group, alkoxy-group with number of carbon atoms from 1 to 6 or alkylthio-group with number of carbon atoms from 1 to 6; R3 means hydrogen atom or lower alkyl with number of carbon atoms from 1 to 6 or fluorine atom; m means whole number from 0 to 3; o means whole number from 0 to 3; Z means -C≡C-, -CO-NH, -COO-, -CSNH-, -CH=CH-, -(CR1=CR1)n′ where n' means whole number from 0 to 5 or Z is absent; Y means phenyl or naphthyl group or heteroaryl taken among group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyranozyl, thiazolyl, oxazolyl, imidazolyl and pyrazolyl. EFFECT: improved method of assay and treatment, valuable properties of compounds. 167 cl, 18 tbl, 20 dwg
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Authors
Dates
2003-05-10—Published
1996-08-23—Filed