Tetracycline derivatives and their use as antibiotic agents

摘要

A compound of formula (I) and their use for the treatment of Gram-positive, Gram-negative and community acquired infections
<Chemistry id="chema01" num="0001"><Image id="ia01" he="35" wi="105" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>R represents hydrogen, halogen, C<Sub>1-6</Sub>alkyl or NRaRb;</ListItem><ListItem>R<Sup>1</Sup> represents hydrogen, C<Sub>1-6</Sub>alkyl or together R<Sup>1</Sup> and R<Sup>3</Sup> represent a CH<Sub>2</Sub> moiety;</ListItem><ListItem>R<Sup>2</Sup> represents hydrogen, -OC<Sub>1-6</Sub>alkyl, -O(O)C<Sub>1-6</Sub>alkyl or hydroxy;</ListItem><ListItem>R<Sup>3</Sup> represents hydrogen, hydroxy or together R<Sup>3</Sup> and R<Sup>1</Sup> represent a CH<Sub>2</Sub> moiety;</ListItem><ListItem>R<Sup>4</Sup> represents hydrogen or C<Sub>1-6</Sub>alkyl;</ListItem><ListItem>R<Sup>5</Sup> represents hydrogen, C<Sub>1-6</Sub>alkyl or C<Sub>1-6</Sub>alkoxycarbonyl;</ListItem><ListItem>X represents NRxRY or -OC<Sub>1-6</Sub>alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, amino and trifluoromethyl;</ListItem><ListItem>Rx and Ry independently represent hydrogen, benzyl, C<Sub>3-6</Sub>cycloalkyl,C<Sub>3-6</Sub>alkenyl, C<Sub>3-6</Sub>alkynyl, C<Sub>1-6</Sub>alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, NRaRb and trifluoromethyl, -C<Sub>1-6</Sub>alkylcycloalkyl, -C<Sub>1-6</Sub>alkylheterocycle, -C<Sub>1-6</Sub>alkylamino and -C<Sub>1-6</Sub>alkylthio or together Rx and Ry form a heterocycle;</ListItem></UnorderedLists> and pharmaceutically acceptable derivatives and solvates thereof.