Derivatives of fortimicin b and process for preparing same

C - Chemistry – Metallurgy – 07 – H

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260/360.3, 260/3

C07H 15/22 (2006.01) C07H 15/224 (2006.01)

Patent

CA 1128057

ABSTRACT OF THE DISCLOSURE 4,2'-di-N-Substitued derivatives of fortimicin B, represented by the formula: Image wherein R1 represents a -?-R, or -CH,-R, group, and R2 represents a Image or -CH2-R4 group and wherein R4 represents an aminoalkyl group having 1 to 8 carbon atoms, hydroxyalkyl group having 1 to 8 carbon atoms carbamoylaminoalkyl group having 2 to 9 carbon atoms or .omega.-aminohydroxyalkyl group having 2 to 9 carbon atoms wherein the amino group and hydroxy group are bonded to different carbon atoms, and R3 represent a carbamoylaminoalkyl group having 2 to 9 carbon atoms, and the pharmaceutically acceptable non-toxic acid addition salts thereof. The derivatives, which display good stability under strongly alkaline conditions and enhanced antibacterial activity, are prepared by chemically modifying fortimicin B.

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