Inhibitors of tyrosine kinases

3:

• A compound of formula I according to claim 1 wherein
• R1 and R2 together represent alkylene with four or five carbon atoms, optionally mono- or disubstituted by lower alkyl, cycloalkyl, heterocyclyl, phenyl, hydroxy, lower alkoxy, amino, mono- or disubstituted amino, pyridyl, pyrazinyl or pyrimidinyl;
• benzalkylene with four or five carbon atoms in the alkylene group;
• oxyalkylene with one oxygen and four carbon atoms;
• or azaalkylene with one nitrogen and four carbon atoms wherein nitrogen is unsubstituted or substituted by lower alkyl, phenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, carboxy-lower alkyl, carbamoyl-lower alkyl, N-mono- or N,N-disubstituted carbamoyl-lower alkyl, cycloalkyl, lower alkoxycarbonyl, phenyl, substituted phenyl, pyridinyl, pyrimidinyl, or pyrazinyl;
• R4 represents hydrogen, lower alkyl, or halogen;
• or a N-oxide or a pharmaceutically acceptable salts thereof.

4:

• A compound of formula I according to claim 1 wherein
• R1 and R2 together represent alkylene with four or five carbon atoms, optionally mono- or disubstituted by lower alkyl, cycloalkyl, phenyl, hydroxy, lower alkoxy, amino, benzoylamino, piperidino, pyridyl, pyrazinyl or pyrimidinyl;
• benzalkylene with four or five carbon atoms in the alkylene group;
• oxyalkylene with one oxygen and four carbon atoms;
• or azaalkylene with one nitrogen and four carbon atoms wherein nitrogen is unsubstituted or substituted by lower alkyl, phenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, carboxy-lower alkyl, carbamoyl-lower alkyl, carbamoyl-lower alkyl N-mono- or N,N-disubstituted by lower alkyl, phenyl, lower alkylene or oxa-lower alkylene, cycloalkyl, lower alkoxycarbonyl, phenyl, methoxyphenyl, trifluoromethylphenyl, trifluoromethoxyphenyl, pyridinyl, pyrimidinyl, or pyrazinyl;
• R4 represents hydrogen or lower alkyl;
• or a N-oxide or a pharmaceutically acceptable salts thereof.

5:

• A compound of formula I according to claim 1 wherein
• R1 and R2 together represent alkylene with four or five carbon atoms, optionally mono- or disubstituted by phenyl, hydroxy, amino, benzoylamino, or piperidino;
• benzalkylene with four or five carbon atoms in the alkylene group;
• oxyalkylene with one oxygen and four carbon atoms;
• or azaalkylene with one nitrogen and four carbon atoms wherein nitrogen is unsubstituted or substituted by lower alkyl, phenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, carbamoyl-lower alkyl, pyrrolidinocarbonyl-lower alkyl, morpholinocarbonyl-lower alkyl, cyclopentyl, lower alkoxycarbonyl, phenyl, methoxyphenyl, trifluoromethylphenyl, pyridinyl;
• pyrimidinyl, or pyrazinyl;
• R4 represents hydrogen or methyl;
• or a N-oxide or a pharmaceutically acceptable salts thereof.

11:

• A process for the synthesis of a compound of the formula
• or an N-oxide or a salt thereof, wherein the symbols R1, R2 and R4 are as defined in claim 1, characterized in that a compound of formula II
• wherein R4 is as defined for a compound of formula I, wherein the carboxy group —COOH is in activated form, is reacted with an amine of the formula III
• R1—NH—R2 (III)
• wherein R1 and R2 are as defined for a compound of the formula I, optionally in the presence of a dehydrating agent and an inert base and/or a suitable catalyst, and optionally in the presence of an inert solvent;
• where the above starting compounds II and III may also be present with functional groups in protected form if necessary and/or in the form of salts, provided a salt-forming group is present and the reaction in salt form is possible;
• any protecting groups in a protected derivative of a compound of the formula I are removed;
• and, if so desired, an obtainable compound of formula I is converted into another compound of formula I or a N-oxide thereof, a free compound of formula I is converted into a salt, an obtainable salt of a compound of formula I is converted into the free compound or another salt, and/or a mixture of isomeric compounds of formula I is separated into the individual isomers.