Pyridopyrimidinone derivatives for use as axl inhibitors
AssigneeOscote Inc.
InventorsJung-Ho KIM, Jang-Sik CHOI, Hee Kyu LEE, Dong-Sik JUNG, Sung-Ho PARK, Yung-Geun CHOI
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Abstract
Pyridopyrimidinone derivatives and pharmaceutical compositions containing the same for use as an Axl inhibitor for the treatment of a disease or condition mediated by Axl such as cancer and metastasis, are disclosed. Also disclosed are methods for treating a Axl-mediated disease or condition by administering to a subject a therapeutically effective amount of the pyridopyrimidinone derivative.
Claims18
1-15. (canceled)
A method of inhibiting Axl in a subject in need thereof, comprising administering an effective amount of a composition comprising a compound of the following Formula (I) or a pharmaceutically acceptable salt thereof:
- wherein
- R1 is C6-C10aryl, C6-C10arylC1-C6alkyl, C5-C6cycloalkyl or C5-C6cycloalkylmethyl, optionally substituted with one or two R3s;
- R3 is independently fluoro, chloro, bromo, iodo, C1-C6alkyl, or trifluoromethyl;
- X is H, fluoro, chloro, bromo, iodo, methyl, or trifluoroethyl;
- Y is chloro, bromo, iodo, C1-C3alkyl, or phenyl;
- R2 is C3-C6cycloalkyl or 4 to 7-membered heterocycloalkyl, wherein the C3-C6cycloalkyl is optionally substituted at carbon atoms with one or two R4s, and wherein the 4 to 7-membered heterocycloalkyl has 1 or 2 heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, sulfone and sulfoxide, and is optionally substituted at carbon atom with R4 or at nitrogen atom with R5;
- R4 is independently hydroxy, hydroxyC1-C6alkyl, amino, aminoC1-C6alkyl, —NH(—C1-C3alkyl), —N(—C1-C3alkyl)2, C1-C3alkyl or halo;
- and
- R5 is H, C1-C3alkyl or —C(═O)(—C1-C3alkyl), wherein the C1-C3alkyl is optionally substituted with 1 to 3 fluoros,
- wherein the subject suffers from a disease or condition mediated by Axl.
Dependencies are inferred from the claim text.