Derivatives of erythromycylamine

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 72, 536 74, A61K 3170, C07H 1708

Patent

active

051108003

ABSTRACT:
Three new groups of 9-N-substituted derivatives of erythromycylamine with superior oral activity against Gram-positive pathogens, new processes for preparing derivatives of erythromycylamine and aliphatic aldehydes by controlling the pH of the reaction and by catalytic hydrogenation, and pharmaceutical compositions and methods using the new compounds are provided.

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patent: 4048306 (1977-09-01), Maier et al.
patent: 4256738 (1981-03-01), Woitun et al.
Massey et al. "Erythromycylamine", Tetrahedron Letters 1970 (2), 157-160.
Ryden et al., "N-Substituted Derivatives of Erythromycylamine," J. Med. Chem. 16 (9), 1059-1060 (1973).
Cockerill et al., "Substituent Effects on the pKa Values and Rates of Hydrolysis of Aryl-methylene-erythromycylamines," J. Chem. Soc. Perkin, II 1973, 173-179.
Massey et al., "Antibacterial Activity of 9(S)-erythromycylamine-Aldehyde Condensation Products," J. Med. Chem. 17, 105-107 (1974).
Vince et al., "Binding of N-Substituted Erythromycylamine to Ribosomes," Antimicrobial Agents and Chemotherapy 9 (1), 131-136 (1976).

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