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US 8,569,306 B2Granted
JNK modulators
AssigneeHoffmann-La Roche Inc.
InventorsBernd Buettelmann, Bindu Goyal, Wylie Solang Palmer
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH—R2 Or N—SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
Claims14
A compound of formula I:
- wherein
- R1 is —OH, —OR, or hydroxy-lower alkyl, where R is lower alkyl, benzyl, aryl-lower alkyl, or methylsulfonyl-lower alkyl;
- R2 is —OH, —NH2, —CH2SO2R4, —SO2R4—NHSO2R4, —CO2R5, or
- where R3 is H, lower acyl, or an amino acid;
- R4 is lower alkyl, —NH2, lower alkyl-amino, or di(lower alkyl)amino;
- R5 is H or lower alkyl;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A pharmaceutical composition for treating inflammation, comprising:
- an effective amount of a compound of Formula I:
- wherein
- R1 is —OH, —OR, or hydroxy-lower alkyl, where R is lower alkyl, benzyl, aryl-lower alkyl, or methylsulfonyl-lower alkyl;
- R2 is —OH, —NH2, —SO2R4, —NHSO2R4, —CO2R5, or
- where R3 is H, lower acyl, or an amino acid;
- R4 is lower alkyl, —NH2, lower alkyl-amino, or di(lower alkyl)amino;
- R5 is H or lower alkyl;
- or a pharmaceutically acceptable salt thereof;
- and a pharmaceutically acceptable excipient.
6 more elements
A method of treating a subject for inflammation, said method comprising:
- administering to a subject in need thereof an effective amount of a compound of formula I:
- wherein
- R1 is —OH, —OR, or hydroxy-lower alkyl, where R is lower alkyl, benzyl, aryl-lower alkyl, or methylsulfonyl-lower alkyl;
- R2 is —OH, —NH2, —SO2R4, —NHSO2R4, —CO2R5, or
- where R3 is H, lower acyl, or an amino acid;
- R4 is lower alkyl, —NH2, lower alkyl-amino, or di(lower alkyl)-amino;
- R5 is H or lower alkyl;
- or a pharmaceutically acceptable salt thereof.
5 more elements
A method of inhibiting the activity of JNK, comprising:
- contacting said JNK with an effective concentration of a compound of formula I:
- wherein
- R1 is —OH, —OR, or hydroxy-lower alkyl, where R is lower alkyl, benzyl, aryl-lower alkyl, or methylsulfonyl-lower alkyl;
- R2 is —OH, —NH2, —SO2R4, —NHSO2R4, —CO2R5, or
- where R3 is H, lower acyl, or an amino acid;
- R4 is lower alkyl, —NH2, lower alkyl-amino, or di(lower alkyl)-amino;
- R5 is H or lower alkyl;
- or a pharmaceutically acceptable salt thereof.
5 more elements
Dependencies are inferred from the claim text.