Quinazoline derivatives and pharmaceutical compositions...

Details Quinazoline derivatives and pharmaceutical compositions... Quinazoline derivatives and pharmaceutical compositions...

2011-05-10

2011-05-10

Wilson, James O (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C544S284000, C544S293000

Reissue Patent

active

RE042353

ABSTRACT:
The invention relates to quinazoline derivatives of formula (1)wherein m is an integer from 1 to 2; R1represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6(wherein R5and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10and R11each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

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