PURPOSE: To provide the subject new compounds showing an inhibitory effect on depression of Ca-concentration or collagen fiber content in bone and useful as a medicine for preventing and improving bone-absorption diseases such as malignant hypercalcemia, bone Paget's disease and osteoporosis.
CONSTITUTION: Compounds of formula I (R is aliphatic acyl or benzyloxycarbonyl which may be respectively substituted with halogen; R2 is lower alkyl or aralkyl; R3 is lower alkyl, methylthioethyl, etc.; R4 is aliphatic acyl, hydroxyiminomethyl, etc.) e.g. N-benzyloxy-carbonyl-L-leucin-(1-ethoxalyl) pentylamide. The compound of formula I, in the case of R = benzyloxycarbonyl and R4=-CO-COOR5 (R5 is lower alkyl), can be obtained by saponifying a compound of formula II (R6 is R5) in an aqueous alkaline solution, subsequently converting the resultant compound into its anhydride, then reacting the anhydride with methoxymethylamine and ethyl vinyl ether in order and subsequently carrying out ozone oxidation.
SAITO MASAYUKI
NIWADA SHINJIRO
KISO YOSHINOBU
HAYASHI YASUHIRO
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