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US 8,263,624 B2Granted
Aryl-substituted heterocycles, and use thereof
AssigneeBayer Intellectual Property GmbH
InventorsMichael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan Heitmeier
Life of this patent
Estimating the term…
Abstract
The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
Claims14
A compound of the formula
- in which
- E represents a group of the formula
- where
- R1 represents hydrogen, hydroxy, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkylamino, C3-C6-cycloalkyl, C3-C6-cycloalkyloxy, C3-C6-cycloalkylamino, C1-C4-alkylcarbonylamino or C1-C4-alkoxycarbonylamino,
- where
- alkyl, alkoxy, alkylamino may be substituted by a substituent, the substituent being selected from the group consisting of hydroxy, amino, C1-C4-alkoxy, C1-C4-alkylamino, C3-C6-cycloalkylamino and a 4- to 7-membered saturated heterocyclyl bound via an N atom which may contain a ring member from the group consisting of N—R5 or O,
- where
- R5 represents hydrogen or C1-C4-alkyl,
- and
- R10 represents hydrogen, C1-C4-alkyl, C1-C4-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkyloxy or —NR11R12,
- where
- R11 represents C1-C4-alkyl or C3-C6-cycloalkyl,
- and
- R12 represents C1-C4-alkyl,
- A represents a 5-membered heteroaryl or partially unsaturated 5-membered heterocyclyl,
- where heteroaryl and heterocyclyl are attached in the 1- or 2-position to the phenyl ring and heteroaryl and heterocyclyl for their part have a 1,3-attachment to the phenyl ring and the carbonylaminomethyl group,
- and
- where heteroaryl and heterocyclyl are substituted by a substituent R6,
- where R6 is attached to the neighbouring atom of the atom to which the carbonylaminomethyl group is attached and has a 1,4-attachment to the phenyl ring
- and
- where the atom to which R6 is attached is a nitrogen or carbon atom
- and
- where
- R6 represents phenyl or a 5- or 6-membered heteroaryl, where phenyl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxy, hydroxymethyl, hydroxyethyl, amino, aminomethyl, aminoethyl, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxymethyl, C1-C4-alkylamino, C1-C4-alkylaminomethyl, hydroxycarbonyl, hydroxy-carbonylmethyl, aminocarbonyl, aminocarbonylmethyl, C1-C4-alkoxycarbonyl, C1-C4-alkoxycarbonylmethyl, C1-C4-alkylaminocarbonyl, C1-C4-alkylaminocarbonylmethyl, aminosulphonyl, C1-C4-alkylaminosulphonyl and C1-C4-alkylsulphonyl,
- R2 represents hydrogen, fluorine, chlorine, cyano, hydroxy, amino, trifluoromethyl, trifluoromethoxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxymethyl, C1-C4-alkylamino, C3-C6-cycloalkyl, aminocarbonyl, C1-C4-alkoxycarbonyl or C1-C4-alkylaminocarbonyl,
- R3 represents hydrogen, fluorine, chlorine, cyano, hydroxy, amino, trifluoromethyl, trifluoromethoxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxymethyl, C1-C4-alkylamino, C3-C6-cycloalkyl, aminocarbonyl, C1-C4-alkoxycarbonyl or C1-C4-alkylaminocarbonyl,
- R4 represents a group of the formula
- where
- * is the point of attachment to the carbonyl group,
- R7 represents hydrogen, fluorine, chlorine, cyano, ethynyl, C1-C4-alkyl, C1-C4-alkoxy or C3-C6-cycloalkyl,
- R8 represents hydrogen, amino, C1-C4-alkyl, C1-C4-alkylamino or C3-C6-cycloalkyl,
- and
- R9 represents hydrogen, fluorine, chlorine, amino or C1-C4-alkyl,
- or one of its salts, its solvates or the solvates of its salts.
31 more elements
Dependencies are inferred from the claim text.