Pharmaceutical composition for the treatment of pathologies caused by the general response of the immune system
First Claim
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1. A pharmaceutical composition comprising one or more amides of mono- and di-carboxylic acids and one or more polyphenols belonging to the hydroxystilbene family, wherein:
- said one or more amides of mono- and di-carboxylic acids are the N-acylderivatives of formula (I);
X—
R1—
C(O)—
Y1
(I) wherein X—
R1—
C(O) is selected from the group consisting of;
a) a monocarboxylic acid acyl residue, wherein X—
R1 is a saturated or unsaturated alkyl radical having from 1 to 23 carbon atoms, and from 1 to 6 double bonds, or an araliphatic, or aromatic, or heterocyclic, or heteroaromatic radical;
the saturated or unsaturated alkyl radical is optionally substituted with one or more hydroxy, amino, carbonyl, carboxyl, cycloalkyl, aryl, heterocyclic, heteroaromatic group or condensed polycyclic groups. b) the acyl residue of an aromatic, or araliphatic, or heterocyclic, or heteroaromatic, or saturated or unsaturated aliphatic dicarboxylic acid, with from 2 to 20 carbon atoms, optionally substituted with a hydroxy, amino, aromatic, heterocyclic or heteroaromatic group, wherein X is a residue of formula C(O)Y2 and Y2 is -OH or has the same meaning as described for Y1;
when Y2 is —
OH the resulting carboxyl group is optionally salified with a biologically acceptable organic or inorganic cation, preferably sodium, potassium, magnesium, calcium or zinc;
Y1 is selected from the group consisting of;
e) NH2;
f) NR2R3, an amine residue of a mono or bifunctional aminoalcohol, wherein R2 is an alcohol residue selected from a linear or branched C1-C20 mono or dihydroxyalkyl, optionally substituted in the alkyl chain with one or more aromatic groups, or a hydroxyaryl, optionally substituted with one or more linear or branched alkyl radicals with from 1 to 20 carbon atoms;
or an amine residue of an aminoalkylaryl substituted in the aromatic ring with a methoxy group and an —
OH group;
the hydroxyl groups of such aminoalcohols are optionally substituted with a phosphate or glycerophosphate group to form —
OPO3H2 or —
OPO2H—
O—
CH2—
CH(OH)—
CH2—
OH, or with a glycoxy radical to form an O-glycoside, preferably D- and L-glucose, D- and L-galactose, D- and L-mannose, D- and L-ribose, D- and L-fructose, D- and L-glucosamine, D-galactosamine, D-mannosamine, D-glucuronic acid and sialic acid;
wherein said 0-glycosides are α
- or β
-glycosides;
R3 is H, —
CH3 or the same as R2;
g) an amino residue of an optically active or inactive aminoacid, wherein R2, together with the nitrogen atom to which it is bound, forms an alpha-aminoacid, optionally carrying a side chain optionally substituted with —
OH, —
OPO3H2, —
OPO2H—
O—
CH2—
CH(OH)-CH2—
OH, —
SH, S—
CH3;
R3 is —
H or —
CH3;
h) the amino residue of a glycosamine of formula (II);
wherein one of the groups P, Y and Z is —
N(H)—
or —
N(CH3)— and
the remaining groups are —
H or —
OH.
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Abstract
The present invention relates to a pharmaceutical composition consisting of amides of mono- and di-carboxylic acids and hydroxystilbenes, and may be used for the treatment of pathologies caused, sustained and/or characterised by an abnormal general response of the immune system, in both humans and animals.
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Citations
19 Claims
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1. A pharmaceutical composition comprising one or more amides of mono- and di-carboxylic acids and one or more polyphenols belonging to the hydroxystilbene family, wherein:
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said one or more amides of mono- and di-carboxylic acids are the N-acylderivatives of formula (I);
X—
R1—
C(O)—
Y1
(I)wherein X—
R1—
C(O) is selected from the group consisting of;
a) a monocarboxylic acid acyl residue, wherein X—
R1 is a saturated or unsaturated alkyl radical having from 1 to 23 carbon atoms, and from 1 to 6 double bonds, or an araliphatic, or aromatic, or heterocyclic, or heteroaromatic radical;
the saturated or unsaturated alkyl radical is optionally substituted with one or more hydroxy, amino, carbonyl, carboxyl, cycloalkyl, aryl, heterocyclic, heteroaromatic group or condensed polycyclic groups.b) the acyl residue of an aromatic, or araliphatic, or heterocyclic, or heteroaromatic, or saturated or unsaturated aliphatic dicarboxylic acid, with from 2 to 20 carbon atoms, optionally substituted with a hydroxy, amino, aromatic, heterocyclic or heteroaromatic group, wherein X is a residue of formula C(O)Y2 and Y2 is -OH or has the same meaning as described for Y1;
when Y2 is —
OH the resulting carboxyl group is optionally salified with a biologically acceptable organic or inorganic cation, preferably sodium, potassium, magnesium, calcium or zinc;
Y1 is selected from the group consisting of;
e) NH2;
f) NR2R3, an amine residue of a mono or bifunctional aminoalcohol, wherein R2 is an alcohol residue selected from a linear or branched C1-C20 mono or dihydroxyalkyl, optionally substituted in the alkyl chain with one or more aromatic groups, or a hydroxyaryl, optionally substituted with one or more linear or branched alkyl radicals with from 1 to 20 carbon atoms;
or an amine residue of an aminoalkylaryl substituted in the aromatic ring with a methoxy group and an —
OH group;
the hydroxyl groups of such aminoalcohols are optionally substituted with a phosphate or glycerophosphate group to form —
OPO3H2 or —
OPO2H—
O—
CH2—
CH(OH)—
CH2—
OH, or with a glycoxy radical to form an O-glycoside, preferably D- and L-glucose, D- and L-galactose, D- and L-mannose, D- and L-ribose, D- and L-fructose, D- and L-glucosamine, D-galactosamine, D-mannosamine, D-glucuronic acid and sialic acid;
wherein said 0-glycosides are α
- or β
-glycosides;
R3 is H, —
CH3 or the same as R2;
g) an amino residue of an optically active or inactive aminoacid, wherein R2, together with the nitrogen atom to which it is bound, forms an alpha-aminoacid, optionally carrying a side chain optionally substituted with —
OH, —
OPO3H2, —
OPO2H—
O—
CH2—
CH(OH)-CH2—
OH, —
SH, S—
CH3;
R3 is —
H or —
CH3;
h) the amino residue of a glycosamine of formula (II);
wherein one of the groups P, Y and Z is —
N(H)—
or —
N(CH3)— and
the remaining groups are —
H or —
OH. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)
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Specification