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Last Updated: December 12, 2025

Claims for Patent: 9,902,714


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Summary for Patent: 9,902,714
Title:Quinoxaline derivatives useful as FGFR kinase modulators
Abstract:The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Inventor(s):Wim Vermeulen, Steven Anna HOSTYN, Filip Albert Celine CUYCKENS, Russell Mark JONES, Diego Fernando Domenico BROGGINI
Assignee:Janssen Pharmaceutica NV, Astex Therapeutics Ltd
Application Number:US15/128,345
Patent Claims: 1. A compound selected from the group consisting of a compound of formula (I): a tautomeric form, and stereochemically isomeric form thereof, wherein n represents an integer equal to 1 or 2; R1 represents hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyl substituted with —C(═O)NHCH3, or C1-6alkyl substituted with —S(═O)2— C1-4alkyl; R2a represents hydrogen, fluoro or chloro; R2b or R2c each independently represent methoxy or hydroxyl; R3 represent hydrogen, C1-6alkyl, C3-6cycloalkyl, or C1-2alkyl substituted with C3-6cycloalkyl; R4 represents hydrogen, methyl or ethyl; or a pharmaceutically acceptable salt thereof or a solvate thereof.

2. A compound according to claim 1, wherein the compound has the following structure or a pharmaceutically acceptable salt thereof or a solvate thereof.

3. A compound according to claim 1 wherein R2a represents hydrogen or fluoro, or a pharmaceutically acceptable salt thereof or a solvate thereof.

4. A compound according to claim 3 wherein R2a represents fluoro, or a pharmaceutically acceptable salt thereof or a solvate thereof.

5. A compound according to claim 1, wherein the compound has the following structure or a pharmaceutically acceptable salt thereof or a solvate thereof.

6. A compound according to claim 1 wherein n represents an integer equal to 1, or a pharmaceutically acceptable salt thereof or a solvate thereof.

7. A compound according to claim 1 wherein R3 represents hydrogen, or a pharmaceutically acceptable salt thereof or a solvate thereof.

8. A compound according to claim 1 wherein R3 represents C1-6alkyl, in particular C1-4alkyl, or a pharmaceutically acceptable salt thereof or a solvate thereof.

9. A compound according to claim 1, wherein the compound has the following structure or a pharmaceutically acceptable salt thereof or a solvate thereof.

10. A compound according to claim 1 wherein R1 represents hydrogen or C1-6alkyl, or a pharmaceutically acceptable salt thereof or a solvate thereof.

11. A compound according to claim 10 wherein R1 represents C1-6alkyl, or a pharmaceutically acceptable salt thereof or a solvate thereof.

12. A compound according to claim 11 wherein R1 represents methyl, or a pharmaceutically acceptable salt thereof or a solvate thereof.

13. A compound according to claim 1 wherein R2b represents methoxy, or a pharmaceutically acceptable salt thereof or a solvate thereof.

14. A compound according to claim 1 wherein R2b represents hydroxy, or a pharmaceutically acceptable salt thereof or a solvate thereof.

15. A compound according to claim 1 wherein R2c represents methoxy, or a pharmaceutically acceptable salt thereof or a solvate thereof.

16. A compound according to claim 1 wherein R2c represents hydroxy, or a pharmaceutically acceptable salt thereof or a solvate thereof.

17. The compound or a pharmaceutically acceptable salt or solvate thereof.

18. A compound according to claim 17 wherein the compound is

19. A compound selected from or a pharmaceutically acceptable salt or solvate thereof.

20. A process for the preparation of a compound of formula (I) as claimed in claim 1, or a pharmaceutically acceptable salt thereof or a solvate thereof, which process comprises: reacting a compound of formula (II) with formaldehyde in the presence of a suitable solvent, at a suitable temperature, wherein R1, R2a, R2b, R2c, R3, R4 and n are as defined in claim 1; and optionally thereafter converting one compound of the formula (I) into another compound of the formula (I).

21. A pharmaceutical composition comprising a compound as defined in claim 1, or a pharmaceutically acceptable salt thereof or a solvate thereof and a pharmaceutically acceptable carrier.

22. A pharmaceutical composition comprising a compound as defined in claim 18, and a pharmaceutically acceptable carrier.

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