Patent ID: 6313162
Filing Date: 2001-11-06
Classification: A61P,C07C

Abstract:
A propynyl biaromatic compound, having the general formula (I) below: ##STR7##in which:R.sub.1 is(i) the --CH.sub.3 radical(ii) the radical --CH.sub.2 --O--R.sub.6(iii) the radical --O--R.sub.6, or(iv) the radical --CO--R.sub.7R.sub.6 and R.sub.7 having the meanings given below,Ar is a radical selected from the group consisting of (a)-(e) below: ##STR8##R.sub.5 and R.sub.6 have the meanings given below,X is a radical of formula: ##STR9##R.sub.8 and R.sub.9 have the meanings given below,R.sub.2 and R.sub.3, which may be identical or different, are selected from the following:(i) a hydrogen atom,(ii) a linear or branched alkyl radical having from 1 to 20 carbon atoms,(iii) a radical --OR.sub.6,(iv) a radical --SR.sub.6,R.sub.6 is defined below,wherein R.sub.2 and R.sub.3, taken together, may form, with the adjacent aromatic ring, a 5- or 6-membered ring optionally substituted with methyl groups and/or optionally interrupted by an oxygen or sulfur atom,wherein R.sub.2 and R.sub.3 cannot simultaneously have the meanings (i), (iii) and (iv) mentioned above,R.sub.4 and R.sub.5, which may be identical or different, are hydrogen atom, a halogen atom, a linear or a branched alkyl radical having from 1 to 20 carbon atoms or a radical --OR.sub.6,wherein if R.sub.4 is a hydroxyl radical, then R.sub.2 and R.sub.3 form, with the adjacent aromatic ring, a 5- or 6-membered ring which optionally is substituted with methyl groups and/or optionally interrupted by an oxygen or a sulfur atom,R.sub.6 is a hydrogen atom, a lower alkyl radical or a radical --COR.sub.10R.sub.10 is defined below,R.sub.7 is selected from the following:(a) a hydrogen atom(b) a lower alkyl radical(c) a radical of formula: ##STR10##wherein R' and R"" are defined below,(d) a radical --OR.sub.11,(e) a radical --NHOR.sub.6,R.sub.11 is defined below,R.sub.8 and R.sub.9, if considered separately, are the same and are either a hydrogen atom or a radical --OR.sub.10, or R.sub.8 and R.sub.9 are different, and one of them is a hydrogen atom and the other is a lower alkyl radical, or, R.sub.8 and R.sub.9 together form a ring --Y--(CH.sub.2).sub.n --Y--, with Y representing an oxygen or a sulfur atom and with n equal to 2 or 3,R.sub.10 is a lower alkyl radical,R.sub.11 is a hydrogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, an alkenyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl or aralkyl radical, a sugar residue or an amino acid or peptide residue,R' and R"", which may be identical or different, are selected from 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 a salt or optical or geometric isomer of said compound.