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US 11,691,970 B2Granted
Pyrazolopyridinone compounds
AssigneeJanssen Pharmaceutica NV
InventorsHaibing Guo, Zhao-Kui Wan, Luoheng Qin, Qian Liu, Wing Shun Cheung
Life of this patent
Estimating the term…
Abstract
Pyrazolopyridinone compounds, the pharmaceutical compositions comprising said compounds, and the use of said compounds as FGFR (fibroblast growth factor receptor) inhibitors and their use in the treatment of diseases, e.g. cancer.
Claims45
A compound of formula (I):
- or a tautomeric or stereochemically isomeric form thereof, wherein:
- A1, A2 and A3 each independently are CH, CRa or N, provided that maximum two of A1, A2 and A3 are CRa;
- C1 is hydrogen or C1-4alkyl;
- C2 is hydrogen, C1-4alkyl, hydroxyl or C1-4alkoxy;
- or C1 and C2 are taken together to form a C3-6cycloalkyl together with the carbon atom to which they are attached;
- Y is a direct bond, —O—, C(═O), NRy, S(═O)2, or C1-4alkyl;
- Ry is hydrogen or C1-4alkyl;
- each Ra independently is C1-6alkyl, haloC1-6alkyl, halo, C1-6alkoxy, carboxyl, C1-6alkyl-oxycarbonyl, C2-6alkenyl, C2-6alkynyl, cyano, cyanoC1-6alkyl, hydroxyC1-6alkyl, —C(═O)—NH2, —C(═O)—NH(C1-4alkyl), —C(═O)—N(C1-4alkyl)2, or a 3 to 6 membered monocyclic saturated heterocyclyl containing at least one heteroatom that is N, O or S;
- Rb is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy, C1-6alkyloxycarbonyl, C2-6alkenyl, C2-6alkynyl, cyanoC1-6alkyl, hydroxyC1-6alkyl, —C(═O)—NH2, —C(═O)—NH(C1-4alkyl), —C(═O)—N(C1-4alkyl)2, C3-6cycloalkyl, phenyl, a 3 to 6 membered monocyclic heterocyclyl containing at least one heteroatom that is N, O or S, or C1-6alkyl substituted with C3-6cycloalkyl or with phenyl or with a 3 to 6 membered monocyclic heterocyclyl containing at least one heteroatom that is N, O or S;
- D is a 3 to 12 membered heterocyclyl containing at least one heteroatom that is N, O or S, wherein said heterocyclyl is optionally substituted with 1 to 5 Rc substituents;
- each Rc independently is oxo, halo, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyl, haloC1-6alkyl, haloC1-6alkyloxy, carboxyl, HOOC—C1-6alkyl-, C1-6alkyl substituted with —C(═O)—O—C1-6alkyl, C1-6alkyl-O—C(═O)—, cyano, cyanoC1-6alkyl, C1-6alkyl-C(═O)—, —SO2—C1-6alkyl, C3-6cycloalkyl, phenyl, a 3 to 6 membered monocyclic saturated heterocyclyl containing at least one heteroatom that is N, O or S, or a 5 or 6 membered monocyclic aromatic heterocyclyl containing at least one heteroatom that is N, O or S;
- B is a 3 to 12 membered carbocyclyl or a 3 to 12 membered heterocyclyl containing at least one heteroatom that is N, O or S, wherein said carbocyclyl and heterocyclyl are each optionally substituted with 1 to 5 R substituents;
- each R independently is C1-6alkyl, cyano, halo, C1-6alkoxy, haloC1-6alkoxy, hydroxyl, hydroxyC1-6alkyl, haloC1-6alkyl, oxo, —SO2—NH2, —SO2—NH(C1-4alkyl), —SO2—N(C1-4alkyl)2, —NH—C(═O)—C2-6alkenyl, —C(═O)—C1-6alkyl, —C(═O)—C2-6alkenyl, C1-6alkyl-O—C(═O)—, C3-6cycloalkyl, phenyl, or a 3 to 6 membered monocyclic heterocyclyl containing at least one heteroatom that is N, O or S;
- or a pharmaceutically acceptable salt thereof or a solvate thereof.
11 more elements
Dependencies are inferred from the claim text.