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US 2008/0177068 A1Published application
Quinazole derivatives
OwnerWenlin Huang, Xiaohong Zhouinventors
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Abstract
The present invention relates to quinazoline derivatives represented by general formula (I): wherein X, Y, Z, R1, R2, R3, and R4 are as defined herein. The invention also relates to a method of preparing these compounds, and use of these compounds for inhibiting tumor growth.
Claims19
A method of preparing a compound of formula (I):
- wherein
- X represents H, methyl, or C1-4 alkyl;
- Y represents
- wherein n is 1, 2, 3, or 4, and R5, being the same or different groups, is H, methyl, trifluoromethyl, nitro, cyano, C2-C4 alkyl, C2-C4 alkoxyl, N—(C2-C4)alkylamino, enzyme, hydroxyl, NN-triaza(C1-C4) alkylamino, C2-C4 alkylthio or C2-C4 alkylsulfonyl;
- Z is
- —O, —S or —NH;
- R1 represents methyl or C1-C4 alkyl;
- R2 represents C1-C5 alkyl-R6, C2-C6 alkenyl-R6, or C2-C6 alkynyl-R6, in which the alkyl, alkenyl, and alkynyl are optionally substituted with one or more alkynyl, enzyme or amino;
- and R6 is piperidin-4-yl, optionally substituted with one or more substituents of alkynyl, enzyme or amino;
- R3 and R4 represent H, methyl, C1-C4 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, or heterocycloalkyl;
- the method comprising reacting a compound of formula (III):
- wherein L1 represents halogen, alkoxyl, aryloxy, or sulfonoxy;
- R1 represents methyl or C1-C4 alkyl;
- R3 and R4, independently, represent H, C2-C4 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, or isocycloalkyl;
- X represents H, methyl or C1-C4 alkyl;
- and
- Y represents
- wherein n is 1, 2, 3, or 4, and R5, being the same or different groups, is H, methyl, trifluoromethyl, nitro, cyano, C2-C4 alkyl, C2-C4 alkoxyl, N-(C2-C4)alkylamine, enzyme, hydroxyl, NN-triaza(C1-C4) alkylamino, C2-C4 alkylthio or C2-C4 alkylsulfonyl;
- with a compound of formula (IV):
- R2-Z-H (IV)
- wherein R2 represents C1-C5 alkyl-R6, C2-C6 alkenyl-R6, C2-C6 alkynyl-R6, in which the alkyl, alkenyl, and alkynyl are optionally substituted with one or more alkynyl, enzyme or amino;
- and R6 is piperidin-4-yl, optionally substituted with one or more substituents of alkynyl, enzyme or amino;
- and
- Z represents —O, —NH,
- or —S.
22 more elements
Dependencies are inferred from the claim text.