Claims for Patent: 8,329,692

Summary for Patent: 8,329,692

Title:	Pyrimidinyl pyridazinone derivatives
Abstract:	Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
Inventor(s):	Schadt; Oliver (Rodenbach, DE), Dorsch; Dieter (Ober-Ramstadt, DE), Stieber; Frank (Heidelberg, DE), Blaukat; Andree (Schriesheim, DE)
Assignee:	Merck Patent Gesellschaft mit beschrankter Haftung (Darmstadt, DE)
Application Number:	12/668,491
Patent Claims:	1. A compound selected from the group consisting of TABLE-US-00006 No. Name and/or structure "A1" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)- pyrimidin-2-yl]benzyl}-2H-pyridazin-3-one, sulfate "A2" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)- pyrimidin-2-yl]benzyl}-2H-pyridazin-3-one, mesylate "A3" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)- pyrimidin-2-yl]benzyl}-2H-pyridazin-3-one, besylate "A4" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)- pyrimidin-2-yl]benzyl}-2H-pyridazin-3-one, p-tosylate "A5" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)- pyrimidin-2-yl]benzyl}-2H-pyridazin-3-one, fumarate "A6" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)- pyrimidin-2-yl]benzyl}-2H-pyridazin-3-one, maleate "A7" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, hydrochloride monohydrate "A8" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, hydrobromide "A9" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, mesylate "A10" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, besylate "A11" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, malate "A12" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, fumarate "A13" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, maleate "A14" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2- yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, p-tosylate or a tautomers or stereoisomer thereof. 2. A pharmaceutical composition comprising a compound according to claim 1 or a tautomers or stereoisomer thereof and one or more pharmaceutically acceptable excipients and/or adjuvants. 3. A pharmaceutical composition comprising at least one compound according to claim 1 or a tautomers or stereoisomer thereof, and at least one pharmaceutically active ingredient other than the compound of claim 1. 4. A kit comprising separate packs of (a) an effective amount of a compound according to claim 1 or a tautomers or stereoisomer thereof, and (b) an effective amount of a pharmaceutically active ingredient other than the compound of claim 1. 5. A compound according to claim 1, which is TABLE-US-00007 "A1" 6-(1-Methyl-1H-pyrazol-4-y1)-2-{3-[5-(2-morpholin-4- ylethoxy)pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one, sulfate. 6. A compound according to claim 1, which is TABLE-US-00008 "A2" 6-(1-Methy1-1H-pyrazol-4-y1)-2-{3-[5-(2-morpholin-4- ylethoxy)pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one, mesylate. 7. A compound according to claim 1, which is TABLE-US-00009 "A3" 6-(1-Methy1-1H-pyrazol-4-y1)-2-{3-[5-(2-morpholin-4- ylethoxy)pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one, besylate. 8. A compound according to claim 1, which is TABLE-US-00010 "A4" 6-(1-Methy1-1H-pyrazol-4-y1)-2-{3-[5-(2-morpholin-4- ylethoxy)pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one, p-tosylate. 9. A compound according to claim 1, which is TABLE-US-00011 "A5" 6-(1-Methy1-1H-pyrazol-4-y1)-2-{3-[5-(2-morpholin-4- ylethoxy)pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one, fumarate. 10. A compound according to claim 1, which is TABLE-US-00012 "A6" 6-(1-Methy1-1H-pyrazol-4-y1)-2-{3-[5-(2-morpholin-4- ylethoxy)pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one, maleate. 11. A compound according to claim 1, which is TABLE-US-00013 "A7" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, hydrochloride monohydrate. 12. A compound according to claim 1, which is TABLE-US-00014 "A8" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, hydrobromide. 13. A compound according to claim 1, which is TABLE-US-00015 "A9" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, mesylate. 14. A compound according to claim 1, which is TABLE-US-00016 "A10" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, besylate. 15. A compound according to claim 1, which is TABLE-US-00017 "A11" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, malate. 16. A compound according to claim 1, which is TABLE-US-00018 "A12" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, fumarate. 17. A compound according to claim 1, which is TABLE-US-00019 "A13" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, maleate. 18. A compound according to claim 1, which is TABLE-US-00020 "A14" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}- 6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile, p-tosylate.