US 2012/0083528 A1 · NOVEL PROTEIN KINASE MODULATORS AND THERAPEUTIC USES THEREOF

Abstract

The present invention provides new tyrphostin derivatives acting as protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, and/or which directly or indirectly affect proteins in the PTK-mediated signal transduction pathway, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.

Claims20

Dependent claims

A method of inhibiting signal transduction pathways mediated by a protein tyrosine kinase (PTK), comprising the step of contacting a cell comprising said PTK with an effective inhibitory amount of a compound represented by the structure of formula 1:

wherein
R1, R2, R5 and R6 are independently selected from H, C1-C4 alkyl, acyl and a functional group that gives rise to hydroxyl upon hydrolysis;
R3 and R7 are independently selected from H, halogen, haloalkyl and OR8 wherein R8 is H, C1-C4 alkyl, acyl or a functional group that gives rise to hydroxyl upon hydrolysis;
R4 is H or CN,
including salts, hydrates, solvates, polymorphs, optical isomers, geometrical isomers, enantiomers, diastereomers, and mixtures thereof;
or a pharmaceutical composition comprising said compound, and a pharmaceutically acceptable carrier.

3 more elements

Dependencies are inferred from the claim text.

Novel protein kinase modulators and therapeutic uses thereof

Life of this patent

Novel protein kinase modulators and therapeutic uses thereof

Life of this patent

Abstract

Claims20