7-methoxy-6-thiatetracyclines and their preparation

C - Chemistry – Metallurgy – 07 – D

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C07D 335/04 (2006.01) C07D 335/06 (2006.01)

Patent

CA 1066710

ABSTRACT OF THE DISCLOSURE 7-Methoxy-6-thiatetracyclines of the formula Image wherein R1, R2, R3 and R4 each are H or alkyl of 1 to 4 carbon atoms, and the physiologically acceptable acid addition salts thereof are provided herein by specified reactions with solvolyzing, hydrogenolyzing or hydroxy- lating agents. Such compounds and their physiologically acceptable acid salts possess valuable pharmacologicaly properties with good toleration. For example, they exhibit a broad spectrum of antibacterial activity against both Gram-positive and Gram-negative bacteria, including tetracycline-re- sistant Gram-positive and Gram-negative organisms. Acoordingly, these movel tetracyclines can be used as medicines, especially as broad spectrum antibiotics for cambating bacterial infections.

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