Macrolide compositions

C - Chemistry – Metallurgy – 07 – H

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167/185, 260/230

C07H 17/08 (2006.01) A61K 31/70 (2006.01)

Patent

CA 1328257

Abstract Pharmaceutical compositions comprising as an active ingredient a compound of the formula Image I wherein R1 is -N(CH3)2 or -[N(CH3)2R]+X-; R is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, benzyl or benzyl substituted by from 1 to 3 substituents selected from fluoro, chloro, C1-C4- alkyl, C1-C4-alkoxy, nitro, C1-C4-alkoxycarbonyl, -N(C1- C4-alkyl)2 or cyano; R2 and R3 each are H or together form a bond; R4 and R5 independently are H or C1-C4-acyl, or together with a carbonyl group form a five-membered cyclic carbonate; R6 is H or C1-C4-acyl; and X- is halide, hydroxide, carboxylate, sulfate, phosphate, nitrate, C1-C3-alkylsulfonate or arylsulfonate; or, when R1 is -N(CH3)2, a pharmaceutically acceptable salt thereof. These macrolides, some of which are novel compounds, enhance gastrointestinal motility.

596863

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