C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/9
C07K 9/00 (2006.01)
Patent
CA 1244824
ABSTRACT OF THE DISCLOSURE An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity: [BX]-NH-(CH2)3-A-)CH2)3-B wherein [BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid; A represents a group of the general formula Image wherein R1 is a lower alkyl or benzyl, R2 is a lower alkyl or benzyl, R is a lower alkylene, and n is 0 or 1; and B represents a group of the formula Image wherein R3 and R4 are independently (1) a hydrogen atom, or (2) an alkyl group, which may be substituted by one or more phenyl, naphthyl, anthranyl, furyl, thiophene, norbornene, or cycloalkyl groups [these substituent groups may be further substituted by one or more halogen atoms or lower alkyl, lower alkoxy, cyano, halomethyl, or benzyloxy groups (the benzyloxy group may be substituted by one or more halogen atoms or lower alkoxy, benzyloxy or cycloalkylmethyloxy groups)], provided that at least either one of R3 and R4 groups is a group other than hydrogen atom; and a process for the preparation thereof. -2-
417731
Fujii Akio
Fukuoka Takeyo
Muraoka Yasuhiko
Nakatani Tokuji
Takahashi Katsutoshi
Gowling Lafleur Henderson Llp
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
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