Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-08-04
1995-02-07
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514349, 514350, 514351, 514352, 514354, 514355, 514357, 514441, 514438, 514445, 514447, 514471, 514472, 514473, 514510, 514532, 514534, 514535, 514561, 514562, 514563, 514569, 424401, 424428, 549 63, 549 64, 549 69, 549 72, 549479, 549480, 549483, 549491, 549498, 560 10, 560 12, 560 17, 560 18, 560 37, 560 38, 560 42, 560 46, 560 47, 560 48, 562426, 562430, 562442, 562451, 562453, 562455, 562456, 562457, 562458, A61K 31235, A61K 3134, A61K 3138, C07D33366
Patent
active
053875940
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to new di(aromatic) compounds, to a process for preparing them and to their use in human and veterinary medicine and in cosmetics.
These new di(aromatic) compounds find application in the topical and systemic treatment of dermatological conditions linked to a disorder of keratinization (differentiation/proliferation) and dermatological or other conditions having inflammatory and/or immunoallergic components, and in degenerative diseases of connective tissue, and possess antitumour activity. In addition, these compounds may be used in the treatment of atopy, both cutaneous and respiratory, and of rheumatoid psoriasis.
They also find application in the ophthalmological field, in particular in the treatment of corneopathies.
The di(aromatic) compounds according to the invention may be represented by the following general formula: ##STR4## in which: Ar represents either a radical ##STR5## with n=1 or 2 or a radical ##STR6## R.sub.3 and R.sub.5 representing a hydrogen atom, an OH group, an alkoxy radical having from 1 to 6 carbon atoms, an .alpha.-substituted alkyl radical having from 3 to 12 carbon atoms or an .alpha.,.alpha.-disubstituted alkyl radical having from 4 to 12 carbon atoms, a cycloalkyl radical having from 3 to 12 carbon atoms or a mono-or polycyclic cycloalkyl radical having from 5 to 12 carbon atoms in which the carbon having the free valence is trisubstituted, from 1 to 6 carbon atoms, an .alpha.-substituted alkyl radical having from 3 to 12 carbon atoms, an .alpha.,.alpha.-disubstituted alkyl radical having from 4 to 12 carbon atoms, a cycloalkyl radical having from 3 to 12 carbon atoms, a mono- or polycyclic cycloalkyl radical having from 5 to 12 carbon atoms in which the carbon having the free valence is trisubstituted, a monohydroxyalkyl radical, a polyhydroxyalkyl radical, a fluorine atom, a chlorine atom, an SH group, a group SR.sub.6, a group SOR.sub.6, a group SO.sub.2 R.sub.6, an alkenyl radical having from 2 to 6 carbon atoms or an alkenyloxy radical having from 2 to 6 carbon atoms, --CH.sub.2 OH radical, a radical --COR.sub.7, a --CH(OH)CH.sub.3 radical, a radical --CH.sub.2 OCOR.sub.8, a radical --SO.sub.2 R.sub.9, a radical --SOR.sub.9 or a radical --SR.sub.9, radical --N(r'r"), a lower alkyl radical, a monohydroxyalkyl radical, a polyhydroxyalkyl radical or a sugar residue,
1 to 12 carbon atoms or an alkenyl radical having from 2 to 12 carbon atoms, atom, a lower alkyl radical, an aryl radical, an aralkyl radical, an amino acid residue, a sugar residue, an amino sugar residue or a heterocycle, or r' and r" taken together form a heterocycle, radical having from 1 to 20 carbon atoms or a sugar residue, (r'r"), alkoxy radical having from 1 to 6 carbon atoms, a fluorine atom, a chlorine atom, a CF.sub.3 group, a group COR.sub.7, a CH.sub.2 OR group or a group CH.sub.2 OR.sub.6, --CH.dbd.CR.sub.11 --, a divalent radical --N.dbd.CH-- or a divalent radical --N.dbd.CR.sub.6 --, an alkoxy radical having from 1 to 6 carbon atoms, a fluorine atom, a chlorine atom or a CF.sub.3 group, selected from the group consisting of: ##STR7## R' representing a hydrogen atom or a --CH.sub.3 radical, W representing an oxygen or sulphur atom or a group --NR', represents a group --NR', ##STR8## Q representing an oxygen atom or --NR', Y representing an oxygen atom or alternatively a sulphur atom when Q represents a group --NR', ##STR9## R" representing a hydrogen atom, a --CH.sub.3 radical, an OH group, a fluorine atom or a chlorine atom, or R' and R" taken together form a methano radical (.dbd.CH.sub.2) or
an oxo radical (=0 ), ##STR10## Y representing an oxygen atom or a sulphur atom, with the proviso that, when simultaneously X represents ##STR11## Z represents --CH.dbd.CH-- and R.sub.2 represents a hydrogen atom, when Ar represents a radical of formula (III) in which R.sub.3 and R.sub.5 are other than a hydrogen atom and other than an .alpha.-substituted or .alpha.,.alpha.-disubstituted alkyl radical having from 3 to 5 carbon atoms, and the salts of the compounds of formula
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Bernardon Jean-Michel
Pilgrim William R.
Centre International de Recherches Dermatologiques Galderma (Cir
Raymond Richard L.
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