3-(4'-aminobutylamino)propylaminobleomycin derivatives, and...

C - Chemistry – Metallurgy – 07 – K

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530/9

C07K 9/00 (2006.01) C07H 15/26 (2006.01) A61K 37/00 (1985.01)

Patent

CA 1270600

26053-48 ABSTRACT OF THE DISCLOSURE Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula [BX]-NH-(CH2)3-A-(CH2)4-B wherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula Image or Image in which R1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl group or a methyl group substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms,which substituents may be unsubstituted or further substituted in more than one position by one or more substituents selected from the group consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula Image in which R3 and R4 each represents (i) a hydrogen atom, (ii) an alkyl group having 5 to 10 carbon atoms, or (iii) a methyl group or a methyl group substituted by at least one of a phenyl group and a cycloalkyl group, which substituents may be unsubstituted or further substituted in more than one position by one or more substituents selected from the group consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms and a benzyloxy group, with the proviso that at least one of R3 and R4 is a group other than a hydrogen atom, and the pharmaceutically acceptable salts thereof.

457427

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