Tylosin derivatives, processes for their production and...

C - Chemistry – Metallurgy – 07 – H

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260/230.35

C07H 17/08 (2006.01)

Patent

CA 1241952

- 1 - A b s t r a c t TYLOSIN DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM This invention relates to novel 23-demycinosyltylosin- derivatives possessing potent and broad spectrum anti- bacterial activity, processes for their preparation and pharmaceutical compositions containing them. The compounds are of the general formula Image - 2 - wherein R1 is hydrogen or acyl; R2 is acyl; R3 is hydrogen or acyl; or R2 and R3 are together a carbonyl group linking the 3"-and 4"-hydroxyl groups; R4 is hydrogen or acyl; R6 is methyl, hydroxymethyl, fluoromethyl, chloromethyl, bromomethyl, iodomethyl, di-(C1-C6)alkylaminomethyl, acyloxymethyl, CHO or a group of the formula CH=R5 wherein R5 is as hereinbelow defined; and Z is an iminogroup R5 or, when R6 is fluoromethyl, chloromethyl, bromomethyl, iodomethyl, acyloxymethyl, CHO, di(C1-C6)a1kylaminomethyl, Z can also be oxo; and the pharmaceutically acceptable salts thereof.

431296

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