Modulators of p38 MAP kinase
AssigneeIconix Pharmaceuticals, Inc.
InventorsDavid J. Morgans JR., Silke Thode, Dongxu Sun
Life of this patent
Estimating the term…
Abstract
Compounds of formula I are effective modulators of p38 MAP kinase. 1 wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-pipelidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl; R2 is H or lower alkyl; R3 is aryl substituted with 1-3 R6 substituents; R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl; and A is —CH— or —N—; and pharmaceutically acceptable salts thereof.
Claims14
A compound of formula 1:
- 7
- wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-piperidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl;
- R2 is H or lower alkyl;
- R3 is aryl substituted with 1-3 R6 substituents;
- R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl;
- and
- A is —CH— or —N—;
- and pharmaceutically acceptable salts thereof.
A method for modulating p38 activity, comprising:
- Administering to a subject cell that expresses p38 an effective amount of a compound of formula 1:
- 8
- wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-piperidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl;
- R2 is H or lower alkyl;
- R3 is aryl substituted with 1-3 R6 substituents;
- R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl;
- and
- A is —CH— or —N—;
- and pharmaceutically acceptable salts thereof.
A pharmaceutical composition, comprising:
- A compound of formula 1,
- 9
- wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-piperidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl;
- R2 is H or lower alkyl;
- R3 is aryl substituted with 1-3 R6 substituents;
- R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl;
- and
- A is —CH— or —N—;
- and pharmaceutically acceptable salts thereof;
- and
- A pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.