摘要:
PROBLEM TO BE SOLVED: To provide a compound having a strong and selective antagonistic activity against an oxytocin receptor, and to provide a medicine composition which contains the compound as an active ingredient and is used for preventing and treating threatened premature delivery. SOLUTION: This peptide compound is represented by chemical formula (I) or its pharmacologically acceptable salt. And, a medicine composition for preventing and treating threatened premature delivery contains the peptide compound or its pharmacologically acceptable salt as an active ingredient. COPYRIGHT: (C)2004,JPO
摘要:
PROBLEM TO BE SOLVED: To obtain a peptide derivative, for example, for the prevention of premature miscarriage, which has the low anti-vasopressin action but the anti-oxytocin action, by removing protecting groups of a specific peptide having a plurality of protected SH groups, followed by the oxidation in an acidic aqueous medium. SOLUTION: The peptide derivative (or its salt) shown by formula VII is obtained by the first dehydration condensation between a compound shown by formula I (R is H or a protecting group for the guanidino group of Arg; R is a protecting group for the imino group of Pro) and a compound shown by formula II (R is a protecting group for the thiol group; R is a protecting group for the amino group), the second dehydration condensation with a compound shown by formula III (R is a protecting group for the amino group), the third dehydration condensation with a compound shown by formula IV (R is H or a protecting group for the indolyl group; R is the same as R ), the fourth dehydration condensation with a compound shown by formula V to give a compound shown by formula VI (MBzl is 4-methoxybenzyl), the removal of two MBzl groups, followed by the oxidation in an aqueous medium at pH 4.0-6.0 to form the intramolecular disulfide bond(s).
摘要:
The invention relates to an immunogenic principle containing a specific antigen determinant of a predetermined native antigen. This immunogenic principle is constituted by a conjugate between a hapten bearing said antigenic site and a muramyl-peptide, essentially in the absence of supporting macromolecules, this conjugate having an immunogenic effect not only against itself, but also with respect to the native antigen carrying said antigenic site.