Claims for Patent: 9,062,029

Summary for Patent: 9,062,029

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 GmbH (Darmstadt, DE)
Application Number:	14/149,110
Patent Claims:	1. A pharmaceutical formulation, comprising a pharmaceutically acceptable carrier, and an active ingredient 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)pyrimidi- n-2-yl]- benzyl}-2H-pyridazin-3-one, sulfate "A2" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)pyrimidi- n-2-yl]- benzyl}-2H-pyridazin-3-one, mesylate "A3" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)pyrimidi- n-2-yl]- benzyl}-2H-pyridazin-3-one, besylate "A4" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)pyrimidi- n-2-yl]- benzyl}-2H-pyridazin-3-one, p-tosylate "A5" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)pyrimidi- n-2-yl]- benzyl}-2H-pyridazin-3-one, fumarate "A6" 6-(1-Methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)pyrimidi- n-2-yl]- benzyl}-2H-pyridazin-3-one, maleate "A7" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-ox- o-1,6- dihydropyridazin-3-yl)benzonitrile, hydrochloride monohydrate "A8" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-ox- o-1,6- dihydropyridazin-3-yl)benzonitrile, hydrobromide "A9" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-ox- o-1,6- dihydropyridazin-3-yl)benzonitrile, mesylate "A10" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-o- xo-1,6- dihydropyridazin-3-yl)benzonitrile, besylate "A11" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-o- xo-1,6- dihydropyridazin-3-yl)benzonitrile, malate "A12" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-o- xo-1,6- dihydropyridazin-3-yl)benzonitrile, fumarate "A13" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-o- xo-1,6- dihydropyridazin-3-yl)benzonitrile, maleate and "A14" 3-(1-{3-[5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-o- xo-1,6- dihydropyridazin-3-yl)benzonitrile, p-tosylate or a tautomer or stereoisomer thereof, wherein the pharmaceutical formulation is in the form of one or more dosage units, which is provided either as a single dose per day or in a series of doses of two or more per day so that the total daily dose would be the same as for the single dose per day, and wherein said single or series of daily doses comprise 0.5 mg to 1 g of said active ingredient, or 0.1 to 100 mg of said active ingredient per kg of body weight of the intended recipient mammal. 2. A pharmaceutical formulation according to claim 1, wherein said single or series of daily doses comprise 1 mg to 700 mg of said active ingredient, or 1 to 10 mg of said active ingredient per kg of body weight of the intended recipient mammal. 3. A pharmaceutical formulation according to claim 1, wherein said single dose comprises 5 mg to 100 mg of said active ingredient. 4. A pharmaceutical formulation according to claim 1, which contains 3-(1-{3- [5-(1-Methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl } -6-oxo-1,6-dihydro-pyridazin-3-yl)benzonitrile, hydrochloride monohydrate.