Abbott Gmbh & Co Kg

Abb Vie Deutschland Gmbh & Co. Kg

Abbvie Deutschland Gmbh and Co Kg

Armin Beyerbach

Gisela Backfisch

Liliane Unger

Andreas Haupt

Wilfried Martin Braje

Karla Drescher

Sean Colm Turner

Wilfried Lubisch

Roland Grandel

Christophe Henry

Wilfried Hornberger

Andreas Kling

Helmut Mack

Achim Moeller

Juergen Delzer

Barbara Vogg

John Darbyshire

Jürgen Delzer

The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.  

Carboxamide compounds and their use as calpain inhibitors

The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CHor CHR; Ris H, C,-C-alkyl, C,-C-alkyl substituted by C-C-cycloalkyl, C-C-hydroxyalkyl, fluorinated C,-C-alkyl, C-C-cycloalkyl, fluorinated C-C-cycloalkyl, C-Calkenyl, fluorinated C-C-alkenyl, formyl, acetyl or propionyl; R, Rand Rare, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF; E is NRor CH, wherein Ris H or C-C-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR, where Ris H, C-C-alkyl, fluorinated C-C-alkyl, C-Calkylcarbonyl or fluorinated C-C-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents R, wherein the variable Rhas the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand. 

Heterocyclic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor

The invention relates to compounds of the formula I: wherein The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine Dreceptor antagonists or dopamine Dagonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

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The invention relates to compounds of the formula (I). The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

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Bad Dürkheim, Germany

Armin Beyerbach