Methyl-pyrrolidine ether derivatives
AssigneeHoffmann-La Roche Inc.
InventorsMatthias Nettekoven, Hasane Ratni, Walter Vifian
Life of this patent
Estimating the term…
Abstract
The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
Claims10
A compound of formula I
- wherein
- A is selected from the groups (a), (b) or (c):
- or is cycloalkyl, optionally substituted by lower alkyl (c);
- Ar1 is phenyl or a six membered heteroaryl;
- X1 is N or CH;
- X2 is N—R1 or O;
- R1 is S(O)2-lower alkyl, C(O)-cycloalkyl substituted by lower alkyl, or is C(O)-lower alkyl, lower alkyl, cyano, cycloalkyl or is a six membered heteroaryl substituted by lower alkyl, cyano, C(O)-lower alkyl, halogen, lower alkyl substituted by halogen or lower alkoxy;
- or is phenyl substituted by cyano or halogen;
- and
- R2 is lower alkyl, halogen, pyrazolyl, 3-methyl-[1,2,4]oxazolyl, 5-methyl-[1,2,4]oxadiazol-3-yl, pyridyl substituted by cyano, or is phenyl substituted by halogen, or is cyano, lower alkoxy, or is piperidin-2-one;
- or pharmaceutically active salt, stereoisomer or a racemic or non-racemic mixture thereof.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- A is selected from the groups (a), (b) or (c):
- or is cycloalkyl, optionally substituted by lower alkyl (c);
- Ar1 is phenyl or a six membered heteroaryl;
- X1 is N or CH;
- X2 is N—R1 or O;
- R1 is S(O)2-lower alkyl, C(O)-cycloalkyl substituted by lower alkyl, or is C(O)-lower alkyl, lower alkyl, cyano, cycloalkyl or is a six membered heteroaryl substituted by lower alkyl, cyano, C(O)-lower alkyl, halogen, lower alkyl substituted by halogen or lower alkoxy;
- or is phenyl substituted by cyano or halogen;
- and
- R2 is lower alkyl, halogen, pyrazolyl, 3-methyl-[1,2,4]oxazolyl, 5-methyl-[1,2,4]oxadiazol-3-yl, pyridyl substituted by cyano, or is phenyl substituted by halogen, or is cyano, lower alkoxy, or is piperidin-2-one;
- or pharmaceutically active salt, stereoisomer or a racemic or non-racemic mixture thereof and a therapeutically acceptable carrier.
Dependencies are inferred from the claim text.