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US 7,888,364 B2Granted
Pyridyl inhibitors of hedgehog signalling
AssigneeCuris, Inc.
InventorsJanet L. Gunzner, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
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Abstract
The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Claims55
A compound of formula I:
- wherein
- A is substituted benzene;
- X is NR4C(O) or NR4C(S);
- Y is absent;
- R1 is aryl or heteroaryl, each of which is optionally substituted;
- R2 is halogen, or alkyl substituted with halogen and an R2 is in the o-position on said A benzene relative to pyridyl;
- R3 is halogen, hydroxyl, carboxyl, alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, a carbocycle or a heterocycle wherein each alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, carbocycle and heterocycle is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, sulfonyl or alkoxy;
- R4 is H or alkyl;
- m is 0-3;
- n is 1-3;
- or a salt or solvate thereof.
8 more elements
A compound of formula Ib
- wherein R3 is H or methyl,
- R8 is halogen or alkyl substituted with halogen;
- X is NR4C(O),
- m is 0-3,
- R4 is H or alkyl, and
- R1 is aryl or heteroaryl, each of which is optionally substituted.
3 more elements
The compound of the formula
Dependencies are inferred from the claim text.