Aromatic and polycyclic compounds and their use in human or vete

Details Aromatic and polycyclic compounds and their use in human or vete Aromatic and polycyclic compounds and their use in human or vete

1994-08-22

1996-08-20

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514543, 514563, 514568, 514569, 424 60, 344172, 549447, 549561, 560 56, 560 42, 560 37, 560256, 562452, 562455, 562467, 568646, C07C 6526, C07C 6517, C07C 6344

Patent

active

055479839

DESCRIPTION:

BRIEF SUMMARY
This application a 371 of PCT/FR 92/00404 filed May 4, 1992.
The subject of the present invention is new aromatic polycyclic derivatives, process for preparing them and their use in human and veterinary medicine and in cosmetics.
These new compounds find application in the topical and systemic treatment of dermatological conditions linked to a keratinization disorder (differentiation-proliferation) and of dermatological conditions, or the like, with inflammatory and/or immunoallergic components and in connective tissue degeneration diseases, and they have an antitumour activity. In addition, these compounds can be used in the treatment of atopy, whether cutaneous or respiratory, and of rheumatoid psoriasis. They also find application in the ophthalmological field, especially in the treatment of corneopathies.
The compounds according to the invention may be represented by the following general formula: ##STR2## in which: R.sub.1 represents atom or a lower alkyl radical, ##STR3## R.sub.10 representing: a) a hydrogen atom, ##STR4## r' and r" representing a hydrogen atom, a lower alkyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl radical or an amino acid or sugar residue or alternatively, taken together, form a heterocycle, or branched alkyl radical having 1 to 20 carbon atoms, a mono- or polyhydroxyalkyl radical, an aryl or aralkyl radical which is (are) optionally substituted or a sugar residue or an amino acid residue, and defined above, a lower alkyl radical optionally substituted by a hydroxyl, by a lower alkoxy or by a radical ##STR5## R.sub.12 representing a hydrogen atom, a low alkyl radical, a hydroxyl radical, a lower alkoxy radical or a radical ##STR6## r' and r" having the same meanings as above, or R.sub.2 and R.sub.3, taken together, form, with the benzene nucleus, a naphthalene nucleus, atoms or a cycloaliphatic radical, --CH.dbd.CH--(CH.sub.2).sub.n --R.sub.13', or the radical --O(CH.sub.2).sub.m --R.sub.14 ##STR7## a monohydroxyalkyl radical or a polyhydroxyalkyl radical whose hydroxyls are optionally protected in methoxy or acetoxy form, an epoxidized lower alkyl radical or the radical ##STR8## R.sub.15 representing the radical OR.sub.16 or the radical ##STR9## R.sub.16 representing a hydrogen atom, a lower alkyl radical, an aryl radical or an aralkyl radical, radical, a polyhydroxyalkyl radical, the radical ##STR10## the radical ##STR11## a mono- or polyhydroxylated alkenyl radical having 2 to 10 carbon atoms, or when R.sub.2 and R.sub.3 are not taken together, m may be 0 and/or R.sub.14 may represent a hydrogen atom or a lower alkyl radical,
R.sub.6 and R.sub.7 represent a hydrogen atom, a halogen atom, a lower alkyl radical or the radical --OR.sub.16,
R.sub.5 and R.sub.6 may, in addition, form a methylenedioxy ring when R.sub.6 is in the 3-position of the benzene nucleus, and the salts of the compounds of formula (I) when R.sub.1 or R.sub.13 represent a carboxylic acid functional group or when R.sub.14 represents an amine functional group and the chiral analogues of the said compounds of formula (I) and the geometric isomers of the said compounds when R.sub.2 and R.sub.3 are not taken together.
When the compounds according to the invention exist in the form of salts, when R.sub.1 or R.sub.13 represent a carboxylic functional group, in this case, these are salts of an alkali or alkaline-earth metal or alternatively of zinc or of an organic amine.
When R.sub.14 represents an amine functional group, in this case, they are pharmaceutically or cosmetically acceptable salts formed by addition of an organic or inorganic acid, in particular hydrochloric, sulphuric, acetic, citric, fumaric, hemisuccinic, maleic and mandelic acid.
Lower alkyl radical is understood to mean a radical having 1 to 6 carbon atoms and preferably methyl, ethyl, isopropyl, butyl and tert-butyl radicals.
Lower alkoxy radical should be understood to mean radicals having 1 to 4 carbon atoms, especially methoxy, ethoxy, isopropoxy or butoxy radicals.
Cycloaliphatic radical should be understood to

REFERENCES:
patent: 4801616 (1989-01-01), Gapinski
Lehman, Cancer Res. 51(18) 4804 (1991).

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