Patent ID: 6790830
Filing Date: 2004-09-14
Classification: A61K,A61P,A61Q,C07K

Abstract:
A method for treating alopecia and promoting hair growth which comprises treating a patient in need thereof with a pharmaceutical composition containing a 3-position analog of cyclosporin represented by Formula 1, as an active ingredient: in which A represents N-methyl-(4R)-4-[(E)-2-butenyl]-4-methyl-L-threonine, (2S,3R,4R,6E)-3-sulfhydryl-4-methyl-2-(methylamino)-6-octenoic acid or (2S,4R,6E)-3-oxo-4-methyl-2-(methylamino)-6-octenoic acid; B represents L-aminobutyric acid (Abu), L-alanine (Ala), L-threonine (Thr), L-valine (Val) or L-norvaline (Nva); C represents a D-amino acid represented by the general formula 1, CH3NHâ€”CH(R1)â€”COOHâ€ƒâ€ƒ[General formula 1]â€ƒin which, R1 is one selected from the group consisting of C1-C6 straight or branched alkyl, alkenyl or alkynyl moieties, substituted or unsubstituted with one or more selected from the group consisting of amino, hydroxy, halo, haloalkyl, ester, alkoxy, cyano, nitro, alkylamino, and dialkylamino, and â€”Xâ€”R2 represented by the general formula 2 below, â€ƒâ€”Xâ€”R2â€ƒâ€ƒ[General formula 2]â€ƒin which, X is oxygen or sulfur, and R2 is one selected from the group consisting of hydrogen, and C1-C6 straight or branched alkyl, alkenyl or alkynyl moieties, substituted or unsubstituted with one or more selected from the group consisting of amino, hydroxy, halo, haloalkyl, ester, alkoxy, cyano, nitro, alkylamino, and dialkylamino, with the proviso that when X is sulfur, R2 is one selected from the group consisting of hydrogen, and C2-C6 straight or branched alkyl, alkenyl or alkynyl moieties, substituted or unsubstituted with one or more selected from the group consisting of amino, hydroxy, halo, haloalkyl, ester, alkoxy, cyano, nitro, alkylamino, and dialkylamino; D represents N-methyl-L-leucine, &ggr;-hydroxy N-methyl-L-leucine or L-valine; E represents L-valine or L-norvaline; F represents N-methyl-L-leucine, &ggr;-hydroxy N-methyl-L-leucine or L-leucine; G represents L-alanine or L-alanine thioamide ([7&psgr;8 CSâ€”NH], NHâ€”CHCH3â€”CSâ€”); H represents a D-amino acid represented by the general formula 3, â€”NHâ€”CH(CH2R3)â€”COOHâ€ƒâ€ƒ[General formula 3]â€ƒin which, R3 is hydrogen or â€”Xâ€”R4 represented by the general formula 4, â€”Xâ€”R4â€ƒâ€ƒ[General formula 4]â€ƒin which, X is oxygen or sulfur, and R4 is one selected from the group consisting of hydrogen, and C1-C6 straight or branched alkyl, alkenyl or alkynyl moieties, substituted or unsubstituted with one or more selected from the group consisting of amino, hydroxy, halo, haloalkyl, ester, alkoxy, cyano, nitro, alkylamino, and dialkylamino; I represents N-methyl-L-leucine, &ggr;-hydroxy-N-methyl-L-leucine or L-leucine; J represents N-methyl-L-leucine, &ggr;-hydroxy-N-methyl-L-leucine or L-leucine; and, K represents N-methyl-L-valine or L-valine.