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US 10,292,985 B2Granted
TGF beta receptor antagonists
AssigneeBristol-Myers Squibb Company
InventorsRobert M. Borzilleri, Brian E. Fink, Lalgudi S. Harikrishnan, Jayakumar Sankara Warrier
Life of this patent
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Abstract
The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Claims12
A compound of the formula
- wherein:
- A is —NH-bicyclic heteroaryl or bicyclic heteroaryl, optionally substituted with 1-2 R2 groups;
- R1 is aryl or heteroaryl, optionally substituted with 1-3 R6;
- R2 is halogen, optionally substituted (C1-C6)alkyl, optionally substituted (C1-C6)alkoxy, —CHF2, CF3, optionally substituted (C3-C8)cycloalkyl, —NH2 or NHSO2(C1-C6)alkyl;
- R4 is hydrogen, halogen, optionally substituted (C1-C6)alkyl, CH2N7CR8 or —CONR7R8;
- R5 is hydrogen, halogen, —CONHR9, —CH2 NHR10R11 or —NHR10R11;
- R6 is hydrogen, halogen, optionally substituted (C1-C6)alkyl, optionally substituted (C1-C6)alkoxy, —CHF2, CF3, optionally substituted (C3-C8)cycloalkyl, —NH2 or NHSO2(C1-C6)alkyl;
- R7 is hydrogen, amino(C1-C6)alkyl or hydroxy(C1-C6)alkyl;
- R8 is hydrogen, amino(C1-C6)alkyl or hydroxy(C1-C6)alkyl;
- or
- R7 and R8 are taken together with the nitrogen to which they are attached to form a heterocyclic group;
- R9 is hydrogen or optionally substituted (C1-C6)alkyl;
- R10 is hydrogen or optionally substituted (C1-C6)alkyl
- R11 is hydrogen or optionally substituted (C1-C6)alkyl;
- or
- R10 and R11 are taken together with the nitrogen to which they are attached to form a heterocyclic group;
- and/or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.
14 more elements
Dependencies are inferred from the claim text.