Aminocycloalkanes as DPP-IV inhibitors
AssigneeHoffman-La Roche Inc.
InventorsMarkus Boehringer, Daniel Hunziker, Bernd Kuhn, Bernd Loeffler, Hans Marty, Patrizio Mattei, Robert Narquizian
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Abstract
The present invention relates to compounds of formula (I) wherein R1 is 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, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
Claims17
A compound of the formula (I):
- wherein:
- R1 is selected from
- R2,R 3, R4, R5 and R6 are each independently selected from hydrogen, lower alkyl, halogenated lower alkyl, lower alkoxy or halogen;
- provided that R2, R3, R4, R5 and R6 are not all hydrogen;
- R7is lower alkyl;
- R8is lower alkyl;
- X is >C═O or >SO2;
- R9 and R11 are hydrogen or together form a double bond;
- R10 and R12 are independently selected from hydrogen or lower alkyl;
- m is 1 or 2;
- n is 0, 1, or 2;
- and pharmaceutically acceptable salts thereof for the use in therapy.
A compound according to formula (I):
- wherein:
- R1 is selected from
- R2, R3, R4, R5 and R6 are each independently selected from hydrogen, lower alkyl, halogenated lower alkyl or halogen;
- provided that R2, R3, R4, R5 and R6 are not all hydrogen;
- R7 is lower alkyl;
- R8 is lower alkyl;
- X is >C═O or >SO2;
- R9 and R11 are hydrogen or together form a double bond;
- R10 and R12 are independently selected from hydrogen or lower alkyl;
- m is 1 or 2;
- n is 0, 1, or 2;
- and pharmaceutically acceptable salts thereof,
- with the further proviso that the following compounds are excluded
- 2-(m-tolyl)-cyclohexylamine, 2-(p-tolyl)-cyclohexylamine, 2-(o-tolyl)-cyclohexylamine, 2-(2-chlorophenyl)-cyclohexylamine, 2-(3-chlorophenyl)-cyclohexylamine, 2-(p-chlorophenyl)-cyclohexylamine, 2-(2-bromophenyl)-cyclohexylamine, 2-(o-tolyl)-cyclopentylamine, 2-(p-tolyl)-cyclopentylamine,
- 2-(4-chlorophenyl)-cyclopentylamine, 2-(3,5-difluorophenyl)-cyclopentylamine, 2-(3-fluorophenyl)-cyclopentylamine, 2-(4-fluorophenyl)-cyclopentylamine,
- 2-(4-bromophenyl)-cyclopentylamine, and
- 2-(4-tert-butylphenyl)-cyclopentylamine.
A pharmaceutical composition, comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is selected from
- R2, R3, R4, R5 and R6 are each independently selected from hydrogen, lower alkyl, halogenated lower alkyl, lower alkoxy or halogen;
- provided that R2, R3, R4, R5 and R6 are not all hydrogen;
- R7 is lower alkyl;
- R8 is lower alkyl;
- X is >C═O or >SO2;
- R9 and R11 are hydrogen or together form a double bond;
- R10 and R12 are independently selected from hydrogen or lower alkyl;
- m is 1 or 2;
- and
- n is 0, 1, or 2;
- or a pharmaceutically acceptable salt thereof;
- and a pharmaceutically acceptable carrier and/or adjuvant.
Dependencies are inferred from the claim text.