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US 2004/0167337 A1Published application
2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl}-amino}-alkylboronic acid derivatives
AssigneeNovartis AG
InventorsPascal Furet, Vito Guagnano, Patricia Imbach, Marc Lang
Life of this patent
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Abstract
The present invention relates to compounds of formula (I) their synthesis and pharmaceutical compositions thereof for the therapeutic treatment of a proliferative diseases in warm-blooded animals, including humans. 1
Claims20
A compound of the formula I
- 29
- wherein
- R1 is unsubstituted or substituted aryl;
- arylalkylcarbonyl, wherein the aryl moiety is unsubstituted or substituted;
- unsubstituted or substituted heterocyclyl;
- or heterocyclylalkylcarbonyl, wherein the heterocyclyl moiety is unsubstituted or substituted;
- R2 is unsubstituted or substtuted aryl or unsubstituted or substituted heteroaryl;
- R3 is hydrogen, unsubstitued or substituted aryl or alkyl which is unsubstituted or substituted by
- unsubstituted or substituted cycloalkyl,
- unsubstituted or substituted aryl, or
- unsubstituted or substituted heteroaryl comprising at least one nitrogen atom;
- R4 is a moiety of the formula IA,
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- wherein A1 and A2 are hydroxy or substituted hydroxy, or together with the binding boron atom and the two binding oxygen atoms form a ring of the formula IA*,
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- wherein W is alkylene, substituted alkylene, unsubstituted or substituted cycloalkylene, unsubstituted or substituted bicycloalkylene or unsubstituted or substituted tricycloalkylene;
- and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, or unsubstituted or substituted cycloalkyl;
- or a salt thereof.
15 more elements
Dependencies are inferred from the claim text.