Claims for Patent: 9,902,714

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. ##STR00001##
Inventor(s):	Vermeulen; Wim (Vosselaar, BE), Hostyn; Steven Anna (Hove, BE), Cuyckens; Filip Albert Celine (Aartselaar, BE), Jones; Russell Mark (Binningen, CH), Broggini; Diego Fernando Domenico (Zurich, CH)
Assignee:	ASTEX THERAPEUTICS LTD (Cambridge, GB)
Application Number:	15/128,345
Patent Claims:	1. A compound selected from the group consisting of a compound of formula (I): ##STR00039## a tautomeric form, and stereochemically isomeric form thereof, wherein n represents an integer equal to 1 or 2; R.sub.1 represents hydrogen, C.sub.1-6alkyl, hydroxyC.sub.1-6alkyl, C.sub.1-6alkyl substituted with --C(.dbd.O)NHCH.sub.3, or C.sub.1-6alkyl substituted with --S(.dbd.O).sub.2-- C.sub.1-4alkyl; R.sub.2a represents hydrogen, fluoro or chloro; R.sub.2b or R.sub.2c each independently represent methoxy or hydroxyl; R.sub.3 represent hydrogen, C.sub.1-6alkyl, C.sub.3-6cycloalkyl, or C.sub.1-2alkyl substituted with C.sub.3-6cycloalkyl; R.sub.4 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 ##STR00040## or a pharmaceutically acceptable salt thereof or a solvate thereof. 3. A compound according to claim 1 wherein R.sub.2a represents hydrogen or fluoro, or a pharmaceutically acceptable salt thereof or a solvate thereof. 4. A compound according to claim 3 wherein R.sub.2a 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 ##STR00041## 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 R.sub.3 represents hydrogen, or a pharmaceutically acceptable salt thereof or a solvate thereof. 8. A compound according to claim 1 wherein R.sub.3 represents C.sub.1-6alkyl, in particular C.sub.1-4alkyl, or a pharmaceutically acceptable salt thereof or a solvate thereof. 9. A compound according to claim 1, wherein the compound has the following structure ##STR00042## or a pharmaceutically acceptable salt thereof or a solvate thereof. 10. A compound according to claim 1 wherein R.sub.1 represents hydrogen or C.sub.1-6alkyl, or a pharmaceutically acceptable salt thereof or a solvate thereof. 11. A compound according to claim 10 wherein R.sub.1 represents C.sub.1-6alkyl, or a pharmaceutically acceptable salt thereof or a solvate thereof. 12. A compound according to claim 11 wherein R.sub.1 represents methyl, or a pharmaceutically acceptable salt thereof or a solvate thereof. 13. A compound according to claim 1 wherein R.sub.2b represents methoxy, or a pharmaceutically acceptable salt thereof or a solvate thereof. 14. A compound according to claim 1 wherein R.sub.2b represents hydroxy, or a pharmaceutically acceptable salt thereof or a solvate thereof. 15. A compound according to claim 1 wherein R.sub.2c represents methoxy, or a pharmaceutically acceptable salt thereof or a solvate thereof. 16. A compound according to claim 1 wherein R.sub.2c represents hydroxy, or a pharmaceutically acceptable salt thereof or a solvate thereof. 17. The compound ##STR00043## or a pharmaceutically acceptable salt or solvate thereof. 18. A compound according to claim 17 wherein the compound is ##STR00044## 19. A compound selected from ##STR00045## 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) ##STR00046## with formaldehyde in the presence of a suitable solvent, at a suitable temperature, wherein R.sub.1, R.sub.2a, R.sub.2b, R.sub.2c, R.sub.3, R.sub.4 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.