RETINOID COMPOUNDS (VARIANTS), COMPOSITION, METHOD FOR ASSAY OF RETINOID HORMONE ANTAGONISTS, METHOD OF TREATMENT AND INTERMEDIATE SUBSTANCES Russian patent published in 2003 - IPC

Abstract RU 2203884 C2

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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RU 2 203 884 C2

Authors

Klejn Ehlliott S.

Dzhonson Alan T.

Stehndiven Ehndrju M.

Biard Richard L.

Gillett Sehmjuel Dzh.

Duong Tien T.

Nehgpehl Sanil

Valigonda Vid'Jasagar

Teng Min

Chandraratna Roshanta A.

Dates

2003-05-10Published

1996-08-23Filed