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Ketolides from the class of 15-membered lactams

Patent 6110965 Issued on August 29, 2000. Estimated Expiration Date: Icon_subject July 31, 2018. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

8a-aza-8a-homoerythromycin lactams Patent #: 5202434
Issued on: 04/13/1993
Inventor: Wilkening

Inventors

Assignee

Application

No. 127764 filed on 07/31/1998

US Classes:

514/459, Nitrogen containing540/454Chalcogen in the hetero ring

Examiners

Primary: Raymond, Richard L.
Assistant: Coleman, Brenda

Attorney, Agent or Firm

International Classes

A61K 031/35
C07D 267/00
A61P 031/04

Foreign Application Priority Data

1998-04-06 HR

Abstract

The present invention relates to the new 15-membered ketoazalides from the class of 6-O-methyl-8a-aza-8a-homo-and 6-O-methyl-9a-aza-9a-homoerythromycin A with the general formula (I) ##STR1## wherein A represents NH group and B at the same time represents C=O group, orA represents C=O group and B at the same time represents NH group,R1 represents OH group, L-cladinosyl group of the formula (II) ##STR2## or together with R2 represents ketone, R2 represents hydrogen or together with R1 represents ketone,R3 represents hydrogen or C1 -C4 alkanoyl group,to intermediates and a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions, as well as to the use of pharmaceutical compositions for treating bacterial infections.

Other References

  • Waddell et al., Synthesis and Antibacterial Activity of O-methyl Derivatives of Azalide Antibiotics, Bioorganic & Medicinal Chemisty Letters, vol. 8, No. 11, pp. 1321-1326, Jun. 199
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