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US 2008/0293756 A1Published application
4,4-disubstituted piperidine derivatives
AssigneeHoffman-La Roche Inc.
InventorsAndreas D. Christ, Rainer E. Martin, Peter Mohr
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Abstract
This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
Claims21
A compound of formula I:
- wherein
- R1 is selected from the group consisting of C2-7-alkyl, C2-7-alkenyl, C3-7-alkinyl, C3-7-cycloalkyl, halogen-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl and benzyl;
- R2 is selected from the group consisting of hydrogen, C1-7-alkyl,
- hydroxy, C1-7-alkoxy, C2-7-alkenyloxy,
- hydroxy-C1-7-alkoxy, C1-7-alkoxy-C1-7-alkoxy,
- —O-benzyl, —O—C3-7-cycloalkyl,
- halogen, halogen-C1-7-alkyl, halogen-C1-7-alkoxy,
- amino, pyrrolyl, imidazolyl,
- —C(O)OR6, wherein R6 is C1-7-alkyl, and
- unsubstituted phenyl or phenyl substituted by one to three groups independently selected from C1-7-alkyl, halogen and C1-7-alkoxy;
- R3 is hydrogen or C1-7-alkoxy;
- R4 is —NH—CO—R7, wherein R7 is a ring selected from phenyl or pyridyl, said ring being unsubstituted or substituted by one or two groups selected from C1-7-alkyl or halogen;
- R5 is —CO—NH2 or —CN;
- or R4 and R5 are bonded to each other to form a ring together with the carbon atom to which they are attached, and R4 and R5 together are:
- —NH—C(O)—NH—C(O)—,
- —C(O)—NR8—CH2—CH2—, wherein R8is phenyl, or
- —N═CR9—NH—C(O)—, wherein R9 is phenyl;
- and pharmaceutically acceptable salts thereof.
15 more elements
Dependencies are inferred from the claim text.