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Serving hundreds of leading biopharmaceutical companies globally:

Express Scripts
Boehringer Ingelheim
US Department of Justice

Generated: June 23, 2018

DrugPatentWatch Database Preview

Details for Patent: 8,586,608

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Title:Quinazoline derivatives and pharmaceutical compositions containing them
Abstract: A compound of general formula I ##STR00001## wherein: R.sub.a is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; R.sub.b is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and R.sub.c is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
Inventor(s): Himmelsbach; Frank (Mittelbiberach, DE), Langkopf; Elke (Warthausen, DE), Blech; Stefan (Warthausen, DE), Jung; Birgit (Laupheim, DE), Baum; Anke (Vienna, AT), Solca; Flavio (Vienna, AT)
Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG (Ingelheim am Rhein, DE)
Filing Date:Sep 21, 2009
Application Number:12/563,340
Claims:1. A compound of formula I ##STR00006## wherein: R.sub.a is a benzyl or 1-phenylethyl group; R.sub.b is bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and R.sub.c is a cyclopropylmethoxy, cyclobutyloxy or cyclopentyloxy group, or a stereoisomer, or physiologically acceptable salt thereof.

2. A compound selected from the group consisting of: (c) 4-[(R)-(1-phenylethyl)amino]-6-{[4-(N,N-bis(2-methoxyethyl)amino)-1-oxo-2- -buten-1-yl]amino}-7-cyclopropylmethoxyquinazoline; (f) 4-[(R)-(1-phenylethyl)amino]-6-({4-[N-(tetrahydropyran-4-yl)-N-methylamin- ol]-1-oxo-2-buten-1-yl}amino)-7-cyclopropylmethoxyquinazoline; and (g) 4-[(R)-(1-phenylethyl)amino]-6-({4-[N-(tetrahydrofuran-3-yl)-N-methylamin- ol]-1-oxo-2-buten-1-yl}amino)-7-cyclopropylmethoxyquinazoline; or a stereoisomer, or physiologically acceptable salt thereof.

3. A pharmaceutical composition comprising a compound according to one of claim 1 or 2, and one or more inert carriers and/or diluents.

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