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US 2004/0176380 A1Published application
New dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsMatthias Hoffmann, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Juergen Quant, Flavio Solca, Florian Colbatzky
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Abstract
The present invention relates to new dihydropteridinones of general formula (I) 1 wherein the groups L and R1- R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
Claims13
1) A Compound of the formula (I),
- 978
- wherein
- R1, R2 which are identical or different, denote hydrogen or optionally substituted C1-C6-alkyl, or
- R1 and R2 together denote a 2- to 5-membered alkyl bridge which optionally contain 1 to 2 heteroatoms,
- R3 denotes hydrogen or a group selected from among optionally substituted C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkynyl and C6-C14-aryl, or a group selected from among optionally substituted and/or bridged C3-C12-cycloalkyl, C3-C12-cycloalkenyl, C7-C12-polycycloalkyl, C7-C12-polycycloalkenyl, C5-C12-spirocycloalkyl, C3-C12-heterocycloalkyl which contains 1 to 2 heteroatoms, and C3-C12-heterocycloalkenyl which contains 1 to 2 heteroatoms, or
- R1 and R3 or R2 and R3 together denote a saturated or unsaturated C3-C4-alkyl bridge which optionally contain 1 heteroatom,
- R4 denotes a group selected from among hydrogen, —CN, hydroxy, —NR6R7 and halogen, or a group selected from among optionally substituted C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C5-alkyloxy, C2-C5-alkenyloxy, C2-C5-alkynyloxy, C1-C6-alkylthio, C1-C6-alkylsulphoxo and C1-C6-alkylsulphonyl,
- L denotes a linker selected from among optionally substituted C2-C10-alkyl, C2-C10-alkenyl, C6-C14-aryl, -C2-C4-alkyl-C6-C14-aryl, -C6-C14-aryl-C1-C4-alkyl,
- optionally bridged C3-C12-cycloalkyl and heteroaryl which contains 1 or 2 nitrogen atoms,
- n denotes 0 or 1
- m denotes 1 or 2
- R5 denotes a group selected from among optionally substituted morpholinyl, piperidinyl, piperazinyl, piperazinylcarbonyl, pyrrolidinyl, tropenyl, R8-diketomethylpiperazinyl, sulphoxomorpholinyl, sulphonylmorpholinyl, thiomorpholinyl, —NR8R9 and azacycloheptyl,
- R6, R7 which are identical or different, denote hydrogen or C1-C4-alkyl, and
- R8, R9 denote unsubstituted nitrogen substituents at R5, which are identical or different, denote either hydrogen or a group selected from among C1-C6-alkyl, —C1-C4-alkyl-C3-C10-cycloalkyl, C3-C10-cycloal kyl, C6-C14-aryl, -C1-C4-alkyl-C6-C14-aryl, pyranyl, pyridinyl, pyrimidinyl, C1-C4-alkyloxycarbonyl, C6-C14-arylcarbonyl, C1-C4-alkylcarbonyl, C6-C14-arylmethyloxycarbonyl, C6-C14-arylsulphonyl, C1-C4-alkylsulphonyl and C6-C14-aryl-C1-C4-alkylsulphonyl,
- optionally in the form of the tautomers, the racemates, the enantiomers, the diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts thereof.
12 more elements
11) Compound of formula (II),
- 983
- wherein
- R1, R2 which are identical or different, denote hydrogen or optionally substituted C1-C6-alkyl, or
- R1 and R2 together denote a 2- to 5-membered alkyl bridge which optionally contain 1 to 2 heteroatoms,
- R3 denotes hydrogen or a group selected from among optionally substituted C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkynyl and C6-C14-aryl, or a group selected from among optionally substituted and/or bridged C3-C12-cycloalkyl, C3-C12-cycloalkenyl, C7-C12-polycycloalkyl, C7-C12-polycycloalkenyl, C5-C12-spirocycloalkyl, C3-C12-heterocycloalkyl which contains 1 to 2 heteroatoms, and C3-C12-heterocycloalkenyl which contains 1 to 2 heteroatoms, or
- R1 and R3 or R2 and R3 together denote a saturated or unsaturated C3-C4-alkyl bridge which optionally contain 1 heteroatom,
- and A is a leaving group.
4 more elements
Dependencies are inferred from the claim text.