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US 7,678,814 B2Granted
Aroyl-piperidine derivatives
AssigneeNovartis AG
InventorSiem Jacob Veenstra
Life of this patent
Estimating the term…
Abstract
The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(quinoloy-lamino)-piperidines of the formula . . . wherein Y and R each are as defined above and the ring A is unsubstituted or mono- or polysubstituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts thereof, to the use thereof, to processes for the preparation thereof and to pharmaceutical compositions comprising a compound according to the invention.
Claims7
A compound of the formula
- wherein Y is ═N— or ═N(O)—, R is OH when Y is ═N— and R is H when Y is ═N(O)— and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl, provided that when R is OH and Y is ═N— the ring A is not unsubstituted, and pharmaceutically acceptable salts thereof.
A compound selected from:
- 1-oxy-quinoline-4-carboxylic acid [(2R,4S)-1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-chloro-benzyl)piperidin-4-yl]-amide or a pharmaceutically acceptable salt thereof, or 2-hydroxy-quinoline-4-carboxylic acid [(2R,4S)-1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-chloro-benzyl)-piperidin-4-yl]-amide or a pharmaceutically acceptable salt thereof.
A process for the preparation of a compound of Formula I, comprising:
- oxidising a compound of formula II;
- optionally separating a mixture of isomers obtainable by the process;
- and isolating the desired isomer of the resulting oxidized compound.
Dependencies are inferred from the claim text.