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US 8,618,303 B2Granted
Pyrrolidine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsHenner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian
Life of this patent
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Abstract
The invention provides compounds of formula wherein R1, R2, R3, R4, R5, and R6 are as defined herein or a pharmaceutically suitable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
Claims17
A compound of formula I
- wherein
- R1 is
- or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl are each optionally substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl;
- X is NR or O;
- R is —C(O)-lower alkyl, —C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl are each optionally substituted by lower alkyl, lower alkoxy, cyano, —C(O)-lower alkyl, halogen or lower alkyl substituted by halogen;
- R2 is hydrogen or lower alkyl;
- R3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen;
- R4 is hydrogen or lower alkyl;
- wherein R2 and R4 are not simultaneously hydrogen or lower alkyl;
- R5 is lower alkyl;
- and
- R6 is halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O)2-lower alkyl or cyano;
- or a pharmaceutically active salt, sterioisomer or racemic or non-racemic mixture thereof.
10 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is
- or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl are each optionally substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl;
- X is NR or O;
- R is —C(O)-lower alkyl, —C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl are each optionally substituted by lower alkyl, lower alkoxy, cyano, —C(O)-lower alkyl, halogen or lower alkyl substituted by halogen;
- R2 is hydrogen or lower alkyl;
- R3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen;
- R4 is hydrogen or lower alkyl;
- wherein R2 and R4 are not simultaneously hydrogen or lower alkyl;
- R5 is lower alkyl;
- and
- R6 is halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O)2-lower alkyl or cyano;
- or a pharmaceutically active salt, sterioisomer or racemic or non-racemic mixture thereof and a pharmaceutically acceptable carrier.
10 more elements
Dependencies are inferred from the claim text.