Anthranilic acid amides and pharmaceutical use thereof

摘要

The invention relates to anthranilic acid amide derivatives of formula I
<Chemistry id="chema01" num="0001"><Image id="ia01" he="44" wi="82" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry>
wherein Ar is represented by the subformula I<Sub>a</Sub><Chemistry id="chema02" num="0002"><Image id="ia02" he="43" wi="63" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry>
wherein R<Sub>a</Sub> represents H or lower alkyl, and R<Sub>1</Sub> represents H or perfluoro lower alkyl, R<Sub>2</Sub> represents H, halogen, C<Sub>2</Sub>-C<Sub>7</Sub>alkyl, C<Sub>2</Sub>-C<Sub>7</Sub>alkenyl or lower alkynyl;
or Ar is represented by the subformula I<Sub>b</Sub>, and
<Chemistry id="chema03" num="0003"><Image id="ia03" he="23" wi="43" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry>
R<Sub>1</Sub> represents perfluoro lower alkyl, and R<Sub>2</Sub> represents bromo, iodo, C<Sub>2</Sub>-C<Sub>7</Sub>alkyl, C<Sub>2</Sub>-C<Sub>7</Sub>alkenyl or lower alkynyl, or R<Sub>1</Sub> represents H, and R<Sub>2</Sub> represents fluoro, bromo, indo, ethyl, C<Sub>5</Sub>-C<Sub>7</Sub>alkyl, C<Sub>2</Sub>-C<Sub>7</Sub>alkenyl or lower alkynyl;
to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; to a method for the treatment of such diseases in animals; and to the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.