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US 2006/0135561 A1Published application
4-Aminopiperidine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsMarkus Boehringer, Daniel Hunziker, Bernd Kuhn, Bernd Loeffler, Thomas Luebbers, Fabienne Ricklin
Life of this patent
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Abstract
The present invention relates to compounds of the formula (I) wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or β-cell protection.
Claims18
A compound of the formula I:
- wherein:
- R1 is selected from the group consisting of
- phenyl, unsubstituted or mono-, di-, or trisubstituted, independently, by lower alkyl, lower alkoxy, phenyl, phenoxy, halogen, or lower halogenalkyl;
- naphthyl, unsubstituted or mono-, di-, or trisubstituted, independently, by lower alkyl, halogen, lower halogenalkyl, lower alkoxy, phenyl or phenoxy;
- tetrahydronaphthyl;
- C3-7-cycloalkyl;
- —(CHR3)m-phenyl, wherein m is 1, 2, or 3 and phenyl being unsubstituted or mono-, di, or trisubstituted, independently, by lower alkyl, halogen,
- lower halogenalkyl, lower alkoxy, phenyl or phenoxy and wherein
- R3 is hydrogen, lower alkyl or phenyl;
- —(CH2)n-heteroaryl, wherein n is 1, 2 or 3;
- —(CH2)n-heteroaryl, wherein n is 1, 2, 3 and heteroaryl is mono-, di-, or trisubstituted, independently, by lower alkyl, halogen, lower halogenalkyl, or lower alkoxy;
- —C(O)—CH2-phenyl, with phenyl being unsubstituted or mono-, di-, or trisubstituted, independently, by lower alkyl, halogen, lower halogenalkyl, lower alkoxy, phenyl or phenoxy;
- —C(O)—CH2-heteroaryl;
- and
- —C(O)—CH2-heteroaryl, wherein heteroaryl is mono-, di-, or trisubstituted, independently, by lower alkyl, halogen, lower halogenalkyl, or lower alkoxy;
- R2 is selected from the group consisting of lower alkyl, lower halogenalkyl;
- phenyl, unsubstituted or mono-, di-, or trisubstituted, independently,
- by lower alkyl, halogen, lower halogenalkyl, or lower alkoxy;
- naphthyl, unsubstituted or mono-, di-, or trisubstituted, independently, by lower alkyl, halogen, lower halogenalkyl, or lower alkoxy;
- heteroaryl, unsubstituted or mono-, di-, or trisubstituted, independently, by lower alkyl, halogen, lower halogenalkyl, or lower alkoxy;
- —COOH;
- —C(O)—NR4R5;
- wherein
- R4 and R5 are lower alkyl or together with the nitrogen atom to which they are attached form a
- 4-, 5- or 6-membered heterocycle which may contain a further heteroatom selected from O, N or S;
- and pharmaceutically acceptable salts thereof.
23 more elements
Dependencies are inferred from the claim text.