US 2011/0033453 A1Published application

Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members

OwnerCarlos Garcia-Echeverria, Sauveur-Michel Mariainventors

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Abstract

The present invention relates to the use of compounds of formula (I) in the treatment of Epidermal Growth Factor Receptor (EGFR) family members dependent diseases or diseases that have acquired resistance to agents that target EGFR family members, use of said compounds for the manufacture of pharmaceutical compositions for the treatment of said diseases, combinations of said compounds with EGFR modulators for said use, methods of treating said diseases with said compounds and pharmaceutical preparations for the treatment of said diseases comprising said compounds alone or in combination, especially with an EGFR modulator.

A method of treating a patient suffering from an EGFR dependent disease comprising administering an effective amount of a compound of formula I,

or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein, W is CRW, or N, wherein RW is selected from the group consisting of
(1) hydrogen,
(2) cyano,
(3) halogen,
(4) methyl,
(5) trifluoromethyl,
(6) sulfonamido;
R1 is selected from the group consisting of
(1) hydrogen,
(2) cyano,
(3) nitro,
(4) halogen,
(5) substituted and unsubstituted alkyl,
(6) substituted and unsubstituted alkenyl,
(7) substituted and unsubstituted alkynyl,
(8) substituted and unsubstituted aryl,
(9) substituted and unsubstituted heteroaryl,
(10) substituted and unsubstituted heterocyclyl,
(11) substituted and unsubstituted cycloalkyl,
(12) —COR1a,
(13) —CO2R1a,
(14) —CONR1aR1b,
(15) —NR1aR1b,
(16) —NR1aCOR1b,
(17) —NR1aSO2R1b,
(18) —OCOR1a,
(19) —OR1a,
(20) —SR1a,
(21) —SOR1a,
(22) —SO2R1a, and
(23) —SO2NR1aR1b,
wherein R1a, and R1b are independently selected from the group consisting of
(a) hydrogen,
(b) substituted or unsubstituted alkyl,
(c) substituted and unsubstituted aryl,
(d) substituted and unsubstituted heteroaryl,
(e) substituted and unsubstituted heterocyclyl, and
(f) substituted and unsubstituted cycloalkyl;
R2 is selected from the group consisting
(1) hydrogen,
(2) cyano,
(3) nitro,
(4) halogen,
(5) hydroxy,
(6) amino,
(7) substituted and unsubstituted alkyl,
(8) —COR2a, and
(9) —NR2aCOR2b,
wherein R2a, and R2b are independently selected from the group consisting of
(a) hydrogen, and
(b) substituted or unsubstituted alkyl;
R3 is selected from the group consisting of
(1) hydrogen,
(2) cyano,
(3) nitro,
(4) halogen,
(5) substituted and unsubstituted alkyl,
(6) substituted and unsubstituted alkenyl,
(7) substituted and unsubstituted alkynyl,
(8) substituted and unsubstituted aryl,
(9) substituted and unsubstituted heteroaryl,
(10) substituted and unsubstituted heterocyclyl,
(11) substituted and unsubstituted cycloalkyl,
(12) —COR3a,
(13) —NR3aR3b,
(14) —NR3aCOR3b,
(15) —NR3aSO2R3b,
(16) —OR3a,
(17) —SR3a,
(18) —SOR3a,
(19) —SO2R3a, and
(20) —SO2NR3aR3b,
wherein R3a, and R3b are independently selected from the group consisting of
(a) hydrogen,
(b) substituted or unsubstituted alkyl,
(c) substituted and unsubstituted aryl,
(d) substituted and unsubstituted heteroaryl,
(e) substituted and unsubstituted heterocyclyl, and
(f) substituted and unsubstituted cycloalkyl;
and
R4 is selected from the group consisting of
(1) hydrogen, and
(2) halogen.

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Abstract

Claims16