10-AZA-9-deoxo-11-deoxy-erythromycin A and derivatives thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540480, 540482, 540454, A61K 3133, C07D41314

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active

052159809

ABSTRACT:
Compounds of the formula: ##STR1## where R is hydrogen, C.sub.1 -C.sub.10 alkylcarbonyl, or C.sub.1 -C.sub.10 alkyl which can be substituted by amino or cyano, R.sup.1 and R.sup.2 are independently hydrogen, hydroxyl or amino, and the pharmaceutically aceptable salts and esters thereof. Pharmaceutical compositions and methods of their use are also provided for.

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patent: 4517359 (1985-05-01), Kobrehel et al.
patent: 4518590 (1985-05-01), Hauske et al.
patent: 4886792 (1989-12-01), Djokic
patent: 4957905 (1990-09-01), Hunt et al.
patent: 5526889 (1985-06-01), Bright et al.
Fernandes, P., The Macrolide Revival, The Antimicrobic Newsleter, vol. 4, No. 4, pp. 25-36, Apr., 1987, U.S.A.
Djokic, et al., Erythromycin Series Part 13: Synthesis and Structure Elucidation of 10-Dihydro-10-Dihydro-10-deoxo-11-methyl-11-azaerythromycin A. J. Chem. Research(s), 1988, pp. 152-153, U.K.
Bright, et al., Synthesis, In Vitro and In Vivo Activity of Novel 9-Oeoxo-9a-Aza-9a-Homoerythromycin A Derivatives; A New Class of Macrolide Antibiotics, the azalides, J. of Antibio. vol. 41, No. 8, Aug. 1988, pp. 1029-1047 USA.

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