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US 2006/0052416 A1Published application
2-Amido-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
AssigneeGenentech, Inc.
InventorsJohn Dickson, Carl Hodge, Jose Mendoza, Ke Chen
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Abstract
2-Amido-4-substituted-aryl-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.
Claims60
At least one chemical entity chosen from compounds of Formula I:
- and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof, wherein
- R3 is chosen from hydroxy, alkoxy, amino, substituted amino, and Ar;
- Ar is chosen from cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl;
- L is chosen from C0-C4alkylene, substituted C1-C4alkylene, —(C0-C4alkylene)-NH—(C═O)—;
- and —(C0-C4alkylene)(C═O)—;
- W is chosen from hydrogen, halo, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl;
- Q is chosen from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl;
- and
- Z is chosen from alkyl, and substituted alkyl,
- with the provisos that
- when Q is optionally substituted pyridin-3-yl, L is a covalent bond, W is 3-methylphenyl, R3 is optionally substituted pyridin-4-yl, then Z is not methyl;
- when Ar is pyridin-4-yl, W is hydrogen, and Q is chosen from benzyl, substituted benzyl, phenethyl, and substituted phenethyl, then Z is not chosen from lower alkyl and substituted lower alkyl;
- when Ar is 2-oxo-(3-hydroquinolyl), W is hydrogen, Z is methyl, then Q is not phenyl;
- when W is chosen from 2-(cyclohexylamino)pyridin-4-yl and 2-(cyclopentylamino)pyridin-4-yl, Ar is 3-methylphenyl, Z is methyl, then Q is not pyridin-3-yl or 6-methylpyridin-3-yl;
- Ar is not substituted pyridone or benzoyloxypyridine;
- when either R1 or R2 is hydrogen, then Ar is not 4-pivaloyloxyphenyl;
- Q is not a heteroaryl, substituted heteroaryl, heterocycloalkyl or substituted heterocycloalkyl comprising one or more heteroatoms chosen from S and N, fused with an aryl, substituted aryl, heteroaryl, or substituted heteroaryl ring;
- when Z is lower alkyl or 3-morpholinopropyl, then Ar is not phenyl, 4-methoxyphenyl, or 2,5-dimethoxyphenyl;
- when Ar is pyridinyl, L is a covalent bond, Z is hydrogen or methyl, and W is phenyl substituted with one methoxy, methyl, chloro, fluoro, chloroor t-butyl, then Q is not methyl;
- and
- when Ar is 4-t-butylphenyl, L is a covalent bond, Z is propyl and Q is 1-cyano-2-hydroxy-prop-1-enyl, then W is not hydrogen.
18 more elements
-63. (canceled)
Dependencies are inferred from the claim text.