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US 10,336,729 B2Granted
4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
AssigneeBoehringer Ingelheim International GmbH
InventorsFrank Himmelsbach, Andreas Blum, Stefan Peters
Life of this patent
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Abstract
The invention relates to new benzonitrile derivatives of the formula (I) wherein R1 to R3 and A are as defined in the description and Claims, to their medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Claims13
A compound of formula (I)
- wherein
- R1 is H or halogen;
- R2 is H or halogen;
- R3 is H or halogen;
- with the proviso that not more than one of R1, R2 and R3 is halogen;
- A is selected from the group consisting of:
- R4 is selected from the group consisting of:
- pyrrolidinyl, piperidinyl, piperazinyl, tetrahydropyranyl, oxazolidinyl, C3-8-cycloalkyl, phenyl, pyridinyl, pyrazinyl, pyridazinyl, pyrimidinyl, [1,3,5]triazinyl, triazolyl, thiazolyl, imidazo[1,2-a]pyridin-2-yl, oxazolyl and oxadiazolyl,
- wherein each R4 is optionally substituted with one or more groups independently of each other selected from the group consisting of halogen, OH, CO2H, CN, CF3, C1-3-alkyl, C1-3-alkyl-O—, (RN)2N—, C1-3-alkyl-C(═O)—, C1-4-alkyl-O—C(═O)—, (RN)2N—C(═O)—, (RN)2N—C1-3-alkyl-, C3-6-cycloalkyl-C1-3-alkyl-O—, C1-3-alkyl-SO2—, (RN)2N—SO2— and C1-3-alkyl-C(═O)—(RN)N—C1-3-alkyl-;
- and
- wherein a —CH2— group of the pyrrolidinyl, oxazolidinyl, piperidinyl or piperazinyl group of R4 is optionally replaced with a —C(═O)— group;
- RN is H or C1-4-alkyl;
- R5 is CN or OH;
- or, R4 and R5 groups together with the carbon atom, to which they are attached, may form the following group:
- wherein each of the above-mentioned alkyl and —O-alkyl groups may be linear or branched and are optionally substituted by one or more F;
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.