PURPOSE: To obtain a new compound having low toxicity, chemical stability and excellent immunosuppressive action.
CONSTITUTION: A compound of the formula GU-X1-(CH2)a-CONH-X2- CONH-(CH2)4-NH-(CH2)3-NH-Y [Gu is guanidino; X1 is (CH2)5 or phenylene; (a) is 4-13; (X2 is (CH2)0-2-CH(R00)0-2; R00 is H, OH, OCH3 or CH2OH; Y is H or a residue after removal of OH from carboxyl of an amino acid or a peptide] or its salt such as 10-{N-(11-guanidinoundecanoyl)-r-amino-β- hydroxybutanoyl}-1,5,10-triazadecane. The compound is obtained by removing a protecting group of a compound of the formula Gu-X1-(CH2)a-CONH-X2- CONH-(CH2)4-NR1-(CH2)3-NH-R2-R2 by reduction, acidolysis, hydrolysis, etc. The compound is useful for suppressing rejection in organ transplantation and skin graft and treating autoimmune diseases such as multiple sclerosis, hemolytic anemia, etc.
NEMOTO KYUICHI
ITO JUNPEI
KOBAYASHI FUMIKO
TAKESAKO KAZUTADA
TAKARA SHUZO CO