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US 2011/0212950 A1Published application
4,4-disubstituted piperidines
AssigneeNovartis AG
InventorsDirk Behnke, Peter Herold, Stjepan Jelakovic, Nathalie Jotterand, Isabelle Lyothier, Robert Mah, Stefan Stutz, Vincenzo Tschinke
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Abstract
The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R2, has the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
Claims9
Compound of the general formula (I)
- or a pharmaceutically acceptable salt thereof, in which R2 is phenyl, which is substituted by 1-3 radicals, one of which is located in the para-position relative to the bond from the phenyl ring to the remainder of the molecule, selected independently from the group consisting of
- C1-6-alkanoyloxy-C1-6-alkyl,
- C2-6-alkenyl,
- C2-6alkenyloxy,
- C2-6-alkenyloxy-C1-6-alkyl,
- C1-6alkoxy,
- C1-6-alkoxy-C1-6-alkoxy,
- C1-6-alkoxy-C1-6-alkoxy-C1-6-alkoxy,
- C1-6-alkoxy-C1-6-alkoxy-C1-6-alkoxy-C1-6-alkyl,
- C1-6-alkoxy-C1-6-alkoxy-C1-6-alkyl,
- C1-6-alkoxy-C1-6-alkyl,
- C1-6-alkoxy-C1-6-alkylamino-C1-6-alkyl,
- C1-6-alkoxy-C1-6-alkylsulfanyl,
- C1-6-alkoxy-C1-6-alkylsulfanyl-C1-8-alkyl,
- C1-6-alkoxycarbonyl,
- C1-6-alkoxycarbonyloxy-C1-8-alkyl,
- C1-6-alkyl,
- C1-8-alkylsulfanyl,
- C1-6-alkylsulfanyl-C1-6-alkoxy,
- C1-6-alkylsulfanyl-C1-6-alkoxy-C1-6-alkyl,
- C1-6-alkylsulfanyl-C1-6-alkyl,
- C1-6-alkylsulfonyl-C1-6-alkoxy-C1-6-alkyl,
- C1-6-alkylsulfonyl-C1-6-alkyl,
- C2-8-alkynyl,
- optionally N-mono- or N,N-di-C1-6-alkylated amino-C1-6-alkoxy,
- optionally N-mono- or N,N-di-C1-6-alkylated amino-carbonyl-C1-6-alkyl,
- aryl-pyrrolidinyl-C0-8-alkoxy,
- heterocyclyl-pyrrolidinyl-C0-6-alkoxy,
- aryl-C0-6-alkoxy-C1-6-alkoxy,
- aryl-C0-6-alkoxy-C1-6-alkoxy-C1-6-alkyl,
- carboxy-C1-6-alkyl,
- cyano,
- cyano-C1-6-alkyl,
- C3-8-cycloalkyl-C0-6-alkoxy-C1-6-alkoxy,
- C3-8-cycloalkyl-C0-6-alkoxy-C1-6-alkoxy-C1-6-alkyl,
- C3-8-cycloalkyl-C0-6-alkoxy-C1-6-alkyl,
- C3-8-cycloalkyl-C0-6-alkylamino-C1-6-alkyl,
- heterocyclyl-carbonyl-C1-6-alkyl,
- heterocyclyl-sulfanyl-C1-6-alkoxy-C1-6-alkyl and
- heterocyclyl-C2-6-alkoxy-C1-6-alkyl;
- and may, in addition to the aforementioned substituents, also be substituted by a maximum of 2 halogens, the maximum total number of substituents on the phenyl radical of R2 being 3.
38 more elements
6-7. (canceled)
Dependencies are inferred from the claim text.