Pyrimidylaminobenzamide Derivatives For Sytemic Mastocytosis
OwnerLeila Alland, Doriano Fabbro +2inventors
InventorsLeila Alland, Doriano Fabbro, Jurgen Mestan, Paul W. Manley
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Abstract
The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis.
Claims10
A method for the treatment or prevention of systemic mastocytosis comprising administration of a pyrimidylaminobenzamide derivative of formula (I):
- wherein
- R1 represents hydrogen, lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, carboxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, or phenyl-lower alkyl;
- R2 represents hydrogen, lower alkyl, optionally substituted by one or more identical or different radicals R3, cycloalkyl, benzcycloalkyl, heterocyclyl, an aryl group, or a mono- or bicyclic heteroaryl group comprising zero, one, two or three ring nitrogen atoms and zero or one oxygen atom and zero or one sulfur atom, which groups in each case are unsubstituted or mono- or polysubstituted;
- and R3 represents hydroxy, lower alkoxy, acyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amino, mono- or disubstituted amino, cycloalkyl, heterocyclyl, an aryl group, or a mono- or bicyclic heteroaryl group comprising zero, one, two or three ring nitrogen atoms and zero or one oxygen atom and zero or one sulfur atom, which groups in each case are unsubstituted or mono- or polysubstituted;
- or wherein R1 and R2 together represent alkylene with four, five or six carbon atoms optionally mono- or disubstituted by lower alkyl, cycloalkyl, heterocyclyl, phenyl, hydroxy, lower alkoxy, amino, mono- or disubstituted amino, oxo, pyridyl, pyrazinyl or pyrimidinyl;
- benzalkylene with four or five carbon atoms;
- oxaalkylene with one oxygen and three or four carbon atoms;
- or azaalkylene with one nitrogen and three or 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, carboxy, phenyl, substituted phenyl, pyridinyl, pyrimidinyl, or pyrazinyl;
- R4 represents hydrogen, lower alkyl, or halogen;
- and a N-oxide or a pharmaceutically acceptable salt of such a compound.
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A method for treating mammals suffering from systemic mastocytosis comprising administering to a mammal in need of such treatment a FIP1L1-PDGFRα-induced inhibiting amount of a compound of formula (II):
- or an N-oxide or pharmaceutically acceptable salts thereof.
A pharmaceutical preparation for the treatment of FIP1L1-PDGFRα-induced systemic mastocytosis comprising a compound of formula (II):
- or an N-oxide or pharmaceutically acceptable salts thereof.
A method for treating mammals, including man, suffering from systemic mastocytosis comprising administering to a mammal in need of such treatment a compound of formula (II):
Dependencies are inferred from the claim text.