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US 2004/0006118 A1Published application
Nf-kb inhibitors
OwnerJames F Callahan, Amy K Roshakinventors
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Abstract
The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-β phosphorylation of IκB.
Claims18
A method of inhibiting IKK-β phosphorylation and the subsequent degradation of IκB comprising administering to a patient in need thereof an effective amount of a compound of Formula I:
- 8
- wherein:
- R1 is NR4R5;
- R2 is CONH2, or SO2NH2;
- R3 is aryl, or heteroaryl;
- R4 is H, or alkyl;
- R5 is selected from the group consisting of H, CO-C1-6alkyl, SO2-C1-6alkyl, CONH-R6, CONH-R7, CSNH-R6, CSNH-R7, SO2NH-R7, and SO2NH-R8;
- R6 is H or alkyl;
- except when R2 is CONH2, R4 is H;
- R7 is H or alkyl;
- provided that when R2 is CONH2 and R5 is H, R7 is not H;
- R8 is H, or alkyl
- and pharmaceutically acceptable salts, hydrates and solvates thereof.
10 more elements
A compound according to Formula (I) wherein:
- R1 is NR4R5;
- R2 is SO2NH2;
- R3 is aryl, or heteroaryl;
- R4 is H, or alkyl;
- R5 is selected from the group consisting of H, CO—C1-6alkyl, CONH-R6, CONH-R7, CSNH-R6, CSNH-R7, SO2NH-R7, and SO2NH-R8;
- R6 is H, or alkyl;
- R7 is aryl, or heteroaryl;
- and
- R8 is H, or alkyl.
6 more elements
A compound according to formula (I) wherein:
- R1 is NR4R5;
- R2 is CONH2;
- R3 is aryl, or heteroaryl;
- R4 is alkyl;
- R5 is selected from the group consisting of H, CO—Cl 1-6alkyl, CONH-R6, CONH-R7, CSNH-R6, CSNH-R7, SO2NH-R7, and SO2NH-R8;
- R6 is H, or alkyl;
- R7 is aryl, or heteroaryl;
- and
- R8 is H, or alkyl.
6 more elements
A compound according to formula (I) wherein:
- R1 is NR4R5;
- R2 is CONH2;
- R3 is aryl, or heteroaryl;
- R4is H;
- R5 is selected from the group consisting of CONH-R6, CONH-R7, CSNH—
- R6, and CSNH-R7,
- R6 is alkyl;
- and
- R7 is aryl, and heteroaryl.
6 more elements
A compound according to formula (I) wherein:
- R1 is NR4R5;
- R2 is CONH2;
- R3 is aryl, or heteroaryl;
- R4 is H, or alkyl;
- R5 is SO2NH-R7, or SO2NH-R8;
- R7 is aryl, or heteroaryl;
- and
- R8 is H, or alkyl.
5 more elements
Dependencies are inferred from the claim text.