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US 2003/0232831 A1Published application
Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
AssigneeBristol-Myers Squibb Company
InventorsAlaric Dyckman, Katerina Leftheris, John Hynes
Life of this patent
Estimating the term…
Abstract
Compounds having the formula (I), 1 and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are surprisingly advantageous as p38 kinase inhibitors, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, NH2, or NH(CH3), preferably methyl; X is N or CH; and R1 through R6 are as described in the specification.
Claims16
A compound of formula (I),
- 34
- or a pharmaceutically-acceptable salt, prodrug, or solvate thereof, wherein:
- X1, X2 and X3 are independently selected from N and CH, wherein when X1, X2 and/or X3 is CH, the hydrogen atom of said X1, X2 and/or X3 is optionally replaced with a substituent R5 or a bond joining ring W to C*;
- R1 and R4 are independently selected from hydrogen, alkyl, substituted alkyl, —OR8, —SR8, —OC(═O)R8, —CO2R8, —C(═O)NR8R9, —NR8R9, —S(═O)R8, —SO2R8, —SO2NR8R9, —NR10SO2NR8R9, —NR10SO2R8, —NR8C(═O)R9, —NR8CO2R9, —NR10C(═O)NR8R9, halogen, nitro, and cyano;
- R2 is hydrogen or C1-4alkyl;
- R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, NH2, or NH(CH3);
- R5 is attached to any available carbon atom of the aryl or heteroaryl ring W and at each occurrence is independently selected from alkyl, halogen, trifluoromethoxy, trifluoromethyl, hydroxy, alkoxy, alkanoyl, alkanoyloxy, amino, alkylamino, aralkylamino, dialkylamino, alkanoylamino, thiol, alkylthio, ureido, nitro, cyano, carboxy, carboxyalkyl, carbamyl, alkoxycarbonyl, alkylthiono, arylthiono, arylsulfonylamine, alkylsulfonylamine, sulfonic acid, alkylsulfonyl, sulfonamido, phenyl, benzyl, aryloxy, and benzyloxy, and/or two of the R5 groups may be taken together to form a five or six membered fused carbocyclic, heterocyclic, or heteroaryl ring, wherein each R5 group and/or each fused ring formed by two R5 groups in turn optionally may be substituted with up to two R11;
- R6 is attached to any available carbon atom of the phenyl ring A and at each occurrence is independently selected from alkyl, halogen, trifluoromethoxy, trifluoromethyl, hydroxy, alkoxy, alkanoyl, alkanoyloxy, amino, alkylamino, aralkylamino, dialkylamino, alkanoylamino, thiol, alkylthio, ureido, nitro, cyano, carboxy, carboxyalkyl, carbamyl, alkoxycarbonyl, alkylthiono, arylthiono, arylsulfonylamine, alkylsulfonylamine, sulfonic acid, alkylsulfonyl, sulfonamido, phenyl, benzyl, aryloxy, and benzyloxy, wherein each R6 group in turn optionally may be substituted by up to two R12;
- R8, R9 and R10 are independently selected from hydrogen, alkyl, substituted alkyl, aryl, heteroaryl, cycloalkyl and heterocyclo;
- R11 and R12 are independently selected from hydroxy, alkyl, substituted alkyl, alkoxy, aryl, aralkyl, and aryl substituted with zero to three of C1-4alkyl, C2-6alkenyl, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, C1-4alkylamino, aminoC1-4alkyl, hydroxy, hydroxyC1-4alkyl, alkoxy, and C1-4alkylthio;
- and
- m and n are 0, 1, 2 or 3.
9 more elements
Dependencies are inferred from the claim text.