Prolinamide-tetrazole derivatives as nk3 receptor antagonists
AssigneeHoffmann-La Roche Inc.
InventorsBo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Abstract
The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).
Claims7
A compound of formula I
- wherein
- R1 is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms;
- R2 is hydrogen or halogen;
- R3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen;
- and
- n is 0, 1 or 2;
- or a pharmaceutically acceptable acid addition salt thereof.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R1 is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms;
- R2 is hydrogen or halogen;
- R3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen;
- and
- n is 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
A process for preparation of a compound of formula I,
- wherein
- R1 is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms;
- R2 is hydrogen or halogen;
- R3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen;
- and
- n is 0, 1 or 2;
- which process comprises
- reacting a compound of formula
- with R1C(O)H, acetic acid and NaBH(OAc)3
- to give a compound of formula
Dependencies are inferred from the claim text.