16-membered macrolide derivatives and process for producing the

Details 16-membered macrolide derivatives and process for producing the 16-membered macrolide derivatives and process for producing the

1993-10-29

1995-04-18

Lilling, Herbert J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

435 76, 536 71, C12P 1962, C12P 1960, C07H 1708, A61K 3170

Patent

active

054079187

ABSTRACT:
16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 represents a straight-chain alkyl group having 1 to 3 carbon atoms; R.sup.2 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.3 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.4 represents a straight-chain alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted allyl group; and R.sup.5 represents a substituted or unsubstituted, straight-chain or branched alkyl, alkenyl or aralkyl group having 1 to 10 carbon atoms; and pharmaceutically acceptable salts thereof are disclosed. These compounds show excellent and long-acting antimicrobial activities. A novel process for producing these 16-membered macrolide derivatives is further disclosed.

REFERENCES:
S. Omura et al., J. Antibiotics, 20(4), 234 (1967).
Y. Matsuhashi et al., ibid., 32(7), 777 (1979).
S. Omura et al., ibid., 33 (8), 911 (1980).
H. Sakakibara et al., ibid., 34(12), 1577 (1981).
K. Tsuzuki et al., ibid., 39(12), 1787 (1986).

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