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Use of amygdalin analogues for the treatment of psoriasisUse of amygdalin analogues for the treatment of psoriasis description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20080125378, Use of amygdalin analogues for the treatment of psoriasis. Brief Patent Description - Full Patent Description - Patent Application Claims
The present disclosure relates to the field of therapy and prophylaxis of psoriasis and other inflammatory and/or allergic dermopathies. BACKGROUNDInflammatory or allergic dermopathies may be a cause of physical and psychological problems for human beings and animals. For some of these diseases, such as psoriasis, there is no cure yet. Psoriasis is a chronic and recurrent disease. The cause of the accelerated cell growth of psoriasis is unknown, but immune mechanisms are thought to play an important role. Peptide T is an octapeptide of sequence ASTTTNYT corresponding to a gp120 protein sequence segment of the human immunodeficiency virus. The analysis of its pharmacological profile shows that peptide T is effective in the treatment of psoriasis (cf. E. M. Faber et al., Proc. Natl. Acad. Sci. 1991, vol. 25, p. 658; T. Talme et al., Proc. Natl. Acad. Sci. 1995, vol. 287, p. 553). However, the use of peptide T as a medication is not advisable because of its low absorption, metabolic instability and immunogenic effects. As there is not yet a completely satisfactory treatment for psoriasis, it is of great interest to develop new antipsoriasis drugs. From structure-activity studies based on the chemotactic properties of peptide T analogues (cf. M. Marastoni et al., Int. J. Pept. Proetin Res. 1993, vol. 41, pp. 441-454), a model of the bioactive conformation of peptide T was proposed (cf. N. B. Centeno et al., J. Comp.-Aided Mol. Design 1998, vol. 12, p. 7-14). In addition, this study has led to define a pharmacophore as well as its required positions for a good chemotactic activity of monocytes (cf. O. Llorens et al., Left. Pent. Sci. 1998, vol. 5, pp. 179-182). This pharmacophore was later used for in silico assays of different databases for compounds, which led to the natural product amygdalin (VII) as peptidomimetic of peptide T. Subsequent chemotaxis studies have demonstrated that amygdalin (VII) exhibits a chemotactic profile similar to that of peptide T and, consequently, a presumable similar antipsoriatic activity (cf. O. Llorens et al., Bioorg. Med. Chem. Left. 1998, vol. 8, pp. 781-786). Nevertheless, amygdalin (VII) is a natural product having a toxic profile. Its toxicity is known to be due to the release of cyanide ions in vivo. DESCRIPTION SUMMARY Disclosed here is a finding that a group of structural analogue compounds of amygdalin possess a chemotactic profile similar to that of amygdalin, which makes them be potentially useful for the prophylactic and/or curative treatment of inflammatory and/or allergic dermopathies and, particularly, for the treatment of psoriasis. Nothing in the art suggests that the compounds of formula (I) (set forth below) have the activity associated with that which is presently disclosed. An aspect hereof relates to the use of a compound of formula (I) or its enantiomers or the mixtures thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable solvates thereof, wherein n is an integer from 0 to 4; R1 is a radical selected from the group consisting of H, CH3, CH2-CH3, C(CH3)3, COOH, CONH2 and C≡CH; R2, R3, R4 and R5 are radicals independently selected from the group consisting of H, F, Cl, Br, (C1-C3-alkoxyl and (C1-C4)-alkyl; and R6 is a radical selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkoxyl, (C1-C4)-alkyl, R7, CH=CH-R7 and O-CH2-R7; wherein R7 is phenyl or phenyl mono- or independently di-substituted with F, Cl, Br, (C1-C3)-alkoxyl or (C1-C4)-alkyl. Such compounds may be used for the prophylactic and/or curative treatment of an inflammatory and/or allergic dermopathy, particularly psoriasis, and/or used in the preparation of a medicament thereof. Moreover, the present disclosure also relates to a prophylactic and/or curative method for treating a patient suffering from an inflammatory and/or allergic dermopathy, particularly psoriasis, which may include administering (particularly in some implementations by oral, parenteral or topical route) a pharmaceutically effective amount of a compound of formula (I) or its enantiomers or the mixtures thereof, or their pharmaceutically acceptable salts, or their pharmaceutically acceptable solvates, together with pharmaceutically acceptable excipients or carriers. An advantage of the compounds of formula (I) over amygdalin may lie on a much lower toxicity.
In a preferred implementation here, n is an integer from 0 and 2. Also preferred is the use of compounds (I) wherein R2, R3, R4 and R5 are radicals independently selected from the group consisting of H, F, Cl, Br, methoxyl and methyl; and R6 is a radical selected from the group consisting of H, F, Cl, Br, methoxyl, methyl, 2-phenylvinyl and phenyl. And it is especially preferred the use of the following particular compounds, the preparation of which is described in the examples disclosed herein:
4-methoxybenzyl 6-O-(β-D-glucopyranosyl)-β-D-glucopyranoside;
benzyl-6-O-(β-D-glucopyranosyl)-β-D-glucopyranoside;
(1 RS)-1-phenylethyl-6-O-(β-D-glucopyranosyl)-β-D-glucopiranoside;
(1 RS)-1-phenylpropyl-6-O-(β-D-glucopyranosyl)-β-D-glucopyranoside;
(1 RS)-1-phenyl-2,2-dimethylpropyl-6-O-(β-D-glucopyranosyl)-β-D-glucopyranoside;
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