N-pyridinyl acetamide derivatives as Wnt signalling pathway inhibitors
AssigneeRedx Pharma PLC
InventorsInder Bhamra, Michael Mathieson, Craig Donoghue, Richard Testar
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.
Claims24
A compound of formula (VIa):
- wherein
- het1 represents a substituted or unsubstituted 9 membered bicyclic heteroaryl group comprising a 5 membered ring, wherein the 5 membered ring comprises 1 or 2 nitrogen atoms, and a 6 membered ring, wherein the 6 membered ring comprises 1 or 2 nitrogen atoms, and when substituted the ring system is substituted with 1, 2, or 3 groups independently selected at each occurrence from the group consisting of halo, C1-4 alkyl, C1-4 haloalkyl, —ORA2, —NRA2RB2, —CN, —SO2RA2, and C3-6 cycloalkyl;
- het2 is a 5 or 6 membered heterocyclic ring which may be unsubstituted or substituted, and when substituted the ring is substituted with 1, 2 or 3 groups independently selected at each occurrence from the group consisting of halo, C1-4 alkyl, C1-4 haloalkyl, —ORA1, —NRA1RB1, —CN, —NO2, —NRA1C(O)RB1, —C(O)NRA1RB1, —NRA1SO2RB1, —SO2NRA1RB1, —SO2RA1, —C(O)RA1, —C(O)ORA1 and C3-6 cycloalkyl;
- R3 is selected from the group consisting of H, C1-4 alkyl, C1-4 haloalkyl, and C3-6 cycloalkyl;
- R4 is independently selected at each occurrence from the group consisting of halo, C1-4 alkyl, C1-4 haloalkyl, —CN, —ORA4, —NRA4RB4, —SO2RA4, C3-6 cycloalkyl and C3-6 halocycloalkyl;
- n is 0, 1 or 2;
- and
- RA1, RB1, RA2, RB2, RA4 and RB4 are at each occurrence independently selected from the group consisting of H, C1-4 alkyl, and C1-4 haloalkyl.
A compound of formula (VIb):
- wherein
- het1 represents a substituted or unsubstituted 9 membered bicyclic heteroaryl group comprising a 5 membered ring, wherein the 5 membered ring comprises 1 or 2 nitrogen atoms, and a 6 membered ring, wherein the 6 membered ring comprises 1 or 2 nitrogen atoms, and when substituted the ring system is substituted with 1, 2, or 3 groups independently selected at each occurrence from the group consisting of halo, C1-4 alkyl, C1-4 haloalkyl, —ORA2, —NRA2RB2, —CN, —SO2RA2, and C3-6 cycloalkyl;
- het2 is a 5 or 6 membered heterocyclic ring which may be unsubstituted or substituted, and when substituted the ring is substituted with 1, 2 or 3 groups independently selected at each occurrence from the group consisting of halo, C1-4 alkyl, C1-4 haloalkyl, —ORA1, —NRA1RB1, —CN, —NO2, —NRA1C(O)RB1, —C(O)NRA1RB1, —NRA1SO2RB1, —SO2NRA1RB1, —SO2RA1, —C(O)RA1, —C(O)ORA1 and C3-6 cycloalkyl;
- R3 is selected from the group consisting of H, C1-4 alkyl, C1-4 haloalkyl, and C3-6 cycloalkyl;
- R4 is independently selected at each occurrence from the group consisting of halo, C1-4 alkyl, C1-4 haloalkyl, —CN, —ORA4, —NRA4RB4, —SO2RA4, C3-6 cycloalkyl and C3-6 halocycloalkyl;
- n is 0, 1 or 2;
- and
- RA1, RB1, RA2, RB2, RA4 and RB4 are at each occurrence independently selected from the group consisting of H, C1-4 alkyl, and C1-4 haloalkyl.
Dependencies are inferred from the claim text.