2-amino-6,7-dihydroxy-4-thiaheptanoic acid derivatives, production and use thereof
AssigneeTakeda Chemical Industries, Ltd.
InventorsSeiichi Tanida, Tsuneaki Hida, Mitsuhiro Wakimasu, Setsuo Harada, Koichi Yukishige
Life of this patent
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Abstract
A compound of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen or aliphatic acyl, A is amino which may be protected, X is an amino acid sequence consisting of 1 to 10 amino acid residues which contain at least one amino acid residue having a water-solubility enhancing group, or a salt thereof has an activity of remarkably improving hematopoietic disorder and is useful as an immuno-stimulating agent or an agent for treating thrombocytopenia.
Claims39
A compound having the formula:
- ##STR8## wherein each of R.sup.1 and R.sup.2 is hydrogen or aliphatic acyl, A is amino which may be protected by a protective group selected from the group consisting of formyl, C.sub.6-14 arylcarbonyl, substituted oxycarbonyl, C.sub.7-19 aralkyl-carbonyl, trityl and phthaloyl, X is an amino acid sequence consisting of 1 to 10 amino acid residues which contain at least one acidic amino acid residue, or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glutamyl -glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexade canoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glutamyl-glycy l-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexade canoyloxy)-4-thiaheptanoyl-glycyl-D-glutamic acid or a salt thereof.
The immuno-stimulating composition according to claim 14, wherein at least one of R.sup.1 and R.sup.2 is aliphatic acyl.
(2R,6S)-2-amino-6,7-bis(he xadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-glutamyl-threonyl-threo nine or a salt thereof.
(2R,6R)-2-amino-6,7 -bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-glutamyl-threony l-threonine or a salt thereof.
(2R,6R)-2-amino-6,7-bis(he xadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-glutamyl-threonine or a salt thereof.
(2R,6R)-2- amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-glutami c acid or a salt thereof.
(2R,6R)-2-amino-6,7-b is(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-D-glutamic acid or a salt thereof.
(2R,6S)-2-am ino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-glutamic acid or a salt thereof.
(2R,6S)-2-amino-6,7- bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-D-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glutamic acid or a salt thereof.
(2R,6R)-2-amino -6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glutamyl-glycyl-D-glutamic acid or a salt thereof.
(2R,6R)-2-amino -6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glutamyl-glycyl-glutamyl-glycyl-D -glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexad ecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-D-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glutamyl-D-glu tamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(h exadecanoyloxy)-4-thiaheptanoyl-glutamyl-glutamyl-D-glutamic acid or a salt thereof.
(2R,6 R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glutamyl-D-gluta mic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis (hexadecanoyloxy)-4-thiaheptanoyl-glutamyl-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glutamyl-gluta myl-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadeca noyloxy)-4-thiaheptanoyl-glycyl-glycyl-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiaheptanoyl-glycyl-D-gluta mic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis (hexadecanoyloxy)-4-thiaheptanoyl-glycyl-glycyl-glycyl-aspartic acid or a salt thereof.
(2R,6R)-2- (9-fluorenylmethyloxycarbonylamino)-6,7-bis(hexadecanoyloxy)-4-thiaheptanoy l-glutamyl-glycyl-D-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(hexadecanoyloxy)-4-thiah eptanoyl-glutamyl-glycyl-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(octadecanoyloxy)-4-thiaheptan oyl-glycyl-glutamyl-glutamic acid or a salt thereof.
(2R,6R)-2-amino-6,7-bis(tetradecanoyloxy)-4-thia heptanoyl-glycyl-glutamyl-glutamic acid or a salt thereof.
Dependencies are inferred from the claim text.