Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
AssigneeSamumed, LLC
InventorsJohn Hood, David Mark Wallace, Sunil Kumar KC
Life of this patent
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Abstract
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Claims20
A compound, or a pharmaceutically acceptable salt thereof, having the structure of Formula Ia:
- wherein:
- R1, R2, R4, R7, and R9 are all H;
- R6 is —(C1-9 alkyl)narylR13;
- R3 is -heteroarylR14R15;
- R10 is independently selected from the group consisting of —C1-9 alkyl and —(C1-9 alkyl)ncarbocyclyl;
- R13 is 1-5 substituents each selected from the group consisting of H, C1-9 alkyl, and halide;
- R14 is NHC(═O)R10;
- R15 is H;
- Y1, Y2, and Y4 are C;
- Y3 is nitrogen and R8 is absent;
- and
- each n is 0 or 1.
A compound, or a pharmaceutically acceptable salt thereof, having the structure of Formula Ia:
- wherein:
- R1, R2, R4, R7, and R9 are all H;
- R6 is -phenylR13;
- R3 is -pyridylR14R15;
- R10 is —C1-9 alkyl;
- R13 is halide;
- R14 is NHC(═O)R10;
- R15 is H;
- Y1, Y2, and Y4 are C;
- and
- Y3 is nitrogen and R8 is absent.
A pharmaceutical composition comprising a therapeutically effective amount of a compound, or pharmaceutically acceptable salt thereof, having the structure of Formula Ia:
- wherein:
- R1, R2, R4, R7, and R9 are all H;
- R6 is —(C1,9 alkyl)narylR13;
- R3 is -heteroarylR14R15;
- R10 is independently selected from the group consisting of —C1-9 alkyl and —(C1-9 alkyl)ncarbocyclyl;
- R13 is 1-5 substituents each selected from the group consisting of H, C1-9 alkyl, and halide;
- R14 is NHC(═O)R10;
- R15 is H;
- Y1, Y2, and Y4 are C;
- Y3 is nitrogen and R8 is absent;
- each n is 0 or 1;
- and
- a pharmaceutically acceptable excipient.
A pharmaceutical composition comprising a therapeutically effective amount of a compound, or pharmaceutically acceptable salt thereof, having the structure of Formula Ia:
- wherein:
- R1, R2, R4, R7, and R9 are all H;
- R6 is -phenylR13;
- R3 is -pyridylR14R15;
- R10 is —C1-9 alkyl;
- R13 is halide;
- R14 is NHC(═O)R10;
- R15 is H;
- Y1, Y2, and Y4 are C;
- and
- Y3 is nitrogen and R8 is absent.
Dependencies are inferred from the claim text.