| 摘要 |
<p>PROBLEM TO BE SOLVED: To provide the subject new derivative consisting of a specific bile acid derivative, having extremely high solubility in a solvent of an acidic pH region, giving little damage on the mucosa and useful as a nasal absorbefacient to improve the absorbability of a physiologically active peptide for the treatment of diabetes, osteoporosis, etc. SOLUTION: This new bile acid derivative is expressed by the formula R<2> -CO- A-R<1> [R<1> is a basic amino acid residue (the residue is bonded to A through nitrogen atom in the basic amino acid residue); R<2> is a group of the formula I (R<3> and R<4> are each H or OH) or the formula II; A is single bond or a group of the formula NHCH2 CO] (e.g. 2-amino-5- N'-[4-(3,7,12-trihydroxy-10,13- dimethylhexadecahydrocyclopenta [a] phenanthren-17-yl)pentanoyl] guanidino}pentanoic acid) and is useful e.g. as a nasal absorbefacient. The compound can be produced by reacting a glycine ester with a compound of the formula R<2> -COOH, removing the carboxyl protecting group, reacting with a basic amino acid ester and removing the protecting group.</p> |
