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US 2006/0217369 A1Published application
ATP competitive kinase inhibitors
AssigneeBristol-Myers Squibb Company
InventorsAshvinikumar Gavai, Ping Chen, Yufen Zhao
Life of this patent
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Abstract
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
Claims19
A compound of the formula I
- wherein
- R1 and R2 are independently selected from the group consisting of hydrogen, halogen, —OH, alkyl, substituted alkyl, —CN, —NH2, —CONHR3, —OCONHR3, —CONHSO2R3, —NHCONHR3, —CH2OR3, —CH2CH2OH, alkoxy, substituted alkoxy, aryl, substituted aryl, aryloxy, substituted aryloxy, —CF3 and —OCF3 two of which may be attached to the same ring carbon atom provided that the resultant compound is chemically stable;
- R3 is hydrogen or C1-C4 alkyl;
- R4 is an optionally substituted aryl or heteroaryl group;
- said substituents on the substituted aryl or substituted heteroaryl group are selected from the group consisting of one or more hydrogen, halogen, alkyl, substituted alkyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, aralkyl, substituted aralkyl, aryloxy and substituted aryloxy;
- R5 is halogen, C1-C6 alkyl or C1-C6 alkoxy;
- X is a direct bond or —CH—;
- n=0, 1, 2;
- or a pharmaceutically acceptable salt or stereoisomer thereof.
6 more elements
A compound of the formula
- R1 and R2 are independently selected from the group consisting of hydrogen, halogen, —OH, alkyl, substituted alkyl, —CN, —NH2, —CONHR3, —OCONHR3, —CONHSO2R3, —NHCONHR3, —CH2OR3, —CH2CH2OH, alkoxy, substituted alkoxy, aryl, substituted aryl, aryloxy, substituted aryloxy, —CF3 and —OCF3 two of which may be attached to the same ring carbon atom provided that the resultant compound is chemically stable;
- R3 is hydrogen or C1-C4 alkyl;
- R4 is an optionally substituted aryl or heteroaryl group;
- said substituents on the substituted aryl or substituted heteroaryl group are selected from the group consisting of one or more hydrogen, halogen, alkyl, substituted alkyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, aralkyl, substituted aralkyl, aryloxy and substituted aryloxy;
- R5 is halogen, C1-C6 alkyl or C1-C6 alkoxy;
- X is a direct bond or —CH—;
- or a pharmaceutically acceptable salt or stereoisomer thereof.
4 more elements
A compound of the formula
- wherein
- R1 and R2 are independently selected from the group consisting of hydrogen, halogen, —OH, alkyl, substituted alkyl, —CN, —NH2, —CONHR3, —OCONHR3, —CONHSO2R3, —NHCONHR3, —CH2OR3, —CH2CH2OH, alkoxy, substituted alkoxy, aryl, substituted aryl, aryloxy, substituted aryloxy, —CF3 and —OCF3 two of which may be attached to the same ring carbon atom provided that the resultant compound is chemically stable;
- R3 is hydrogen or C1-C4 alkyl;
- R4 is an optionally substituted aryl or heteroaryl group;
- said substituents on the substituted aryl or substituted heteroaryl group are selected from the group consisting of one or more hydrogen, halogen, alkyl, substituted alkyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, aralkyl, substituted aralkyl, aryloxy and substituted aryloxy;
- R5 is halogen, C1-C6 alkyl or C1-C6 alkoxy;
- or a pharmaceutically acceptable salt or stereoisomer thereof.
4 more elements
A compound selected from the group consisting of
- (3R,4R)-4-amino-1-((4-(3-methoxyphenylamino) quinazolin-5-yl)methyl)-N-methylpiperidine-3-carboxamide,
- (3R,4R)-4-amino-1-[[4-[(3-chlorophenyl)amino]-5-quinazolinyl]methyl]-3-piperidinol,
- (3R,4R)-4-amino-1-[[4-[(3-ethynylphenyl)amino]-5-quinazolinyl]methyl]-3-piperidinol,
- N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-5-((4-aminopiperidin-1-yl)methyl)quinazolin-4-amine,
- (3R,4R)-1-((4-(1-(3-fluorobenzyl)-1H-indazole-5-ylamino)quinazolin-5-yl)methyl)-4-aminopiperidin-3-ol,
- (3R,4R)-4-amino-1-((4-(3-methoxyphenylamino)quinazolin-5-yl)methyl)-3-piperidinol,
- 5-[(4-amino-1-piperidinyl)methyl]-N-(3-methoxyphenyl)-4-quinazolinamine,
- ((3R,4R)-4-amino-1-((4-(3-ethynylphenylamino)quinazolin-5-yl)methyl)piperidin-3-yl)methanol,
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.