AGENT IN COSMETIC OR PHARMACEUTICAL COMPOSITION FOR TREATMENT OF DISORDERS ASSOCIATED WITH SUPERREGULATION OF RRA RECEPTORS AND/OR HYPERVITAMINOSIS A, AND COMPOUNDS EXHIBITING THIS ACTIVITY Russian patent published in 2000 - IPC

Abstract RU 2157361 C2

FIELD: pharmaceutical chemistry. SUBSTANCE: invention provides retinoid- type agent corresponding to general formula I: (I), wherein R1 is methyl, hydroxymethyl, radical -O-R3, or radical -CO-R4; R2 is one of the radicals -(X)-(CH2)q-R6, -(X)n-(CH2)q-R7, -CH=CH-(CH2)3-R6, or -CH=CH-(CH2)t-R7; Ar is radical depicted by formulas II (a-d): (II); in which definition, in turn, R3 is hydrogen atom, lower alkyl, or radical -(CH2)m-(CO)n-R8; R4 is hydrogen atom, lower alkyl, amino radical of the formula -NR'R", or radical OR9; R5 is hydrogen or halogen atom, linear or branched C1-C20-alkyl, hydroxyl, radical -OR10 or OCOR10; R6 is hydrogen atom, linear or branched C1-C20-alkyl, or alkenyl; R7 is aryl, mono- or polyhydroxylic radical, in which hydroxyl groups are optionally protected by methoxy or acetoxy groups or by radical -COR4, provided that R7 is not polyether radical containing oxygen atom in alpha position to carbon atom in sixth position of naphthyl radical; R8 is lower alkyl or saturated heterocyclic radical; R9 is hydrogen, linear or branched C1-C20- alkyl, alkenyl, mono- or polyhydroxyalkyl, aryl, or arylalkyl radical optionally substituted by a sugar, amino acid or peptide residue; R10/ is lower alkyl; X is oxygen atom or -S(O)2 radical; R' and R", identical or different, are hydrogen atom, lower alkyl, mono- or polyhydroxyalkyl optionally substituted by aryl radical, amino acid, peptide or sugar residue, or R' and R" form together saturated heterocycle; m is integer from 1 to 3, n is 0 or 1; p integer from 5 to 12, q from 0 to 12, n from 0 to 2, s from 3 to 10, and t from 0 to 10; and also salts of the above-defined compounds or their chiral analogs. EFFECT: increased assortment of drugs. 23 cl, 43 ex

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RU 2 157 361 C2

Authors

Zhan-Mishel' Bernardon

Dates

2000-10-10Published

1996-04-30Filed