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US 2006/0217393 A1Published application
NK-1 receptor antagonists
AssigneeHoffmann-La Roche Inc.
InventorsChristoph Funk, Torsten Hoffmann, Andreas Koblet
Life of this patent
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Abstract
The present invention relates to compounds of formula I wherein R is methyl; and R1 is 4-methyl-4-oxy-piperazin-1-yl; or R is CH2OH and R1 is 4-methyl-piperazin-1-yl or is 4-methyl-4-oxy-piperazin-1-yl; and to pharmaceutically acceptable acid addition salts thereof for the treatment of NK-1 receptor related diseases, for example depression, Parkinson's disease, Alzheimer's disease, anxiety, emesis, and pain.
Claims13
A compound of formula I
- wherein
- R is methyl;
- and
- R1 is 4-methyl-4-oxy-piperazin-1-yl;
- or
- R is CH2OH and
- R1 is 4-methyl-piperazin-1-yl or is 4-methyl-4-oxy-piperazin-1-yl;
- or a pharmaceutically acceptable acid addition salt thereof.
5 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
- wherein
- R is methyl;
- and
- R1 is 4-methyl-4-oxy-piperazin-1-yl;
- or
- R is CH2OH and
- R1 is 4-methyl-piperazin-1-yl or is 4-methyl-4-oxy-piperazin-1-yl;
- or a pharmaceutically acceptable salt thereof
- and a pharmaceutically acceptable carrier.
6 more elements
A process for preparing a compound of formula I
- wherein
- R is methyl;
- and
- R1 is 4-methyl-4-oxy-piperazin-1-yl;
- or
- R is CH2OH and
- R1 is 4-methyl-piperazin-1-yl or is 4-methyl-4-oxy-piperazin-1-yl;
- or a pharmaceutically acceptable acid addition salt thereof,
- which process is selected from the group consisting of
- a) reacting a compound of formula
- with potassium peroxymonosulfate (2 KHSO5.KHSO4.K2SO4)
- to obtain a compound of formula
- and
- b) reacting a compound of formula
- with NaBH4
- to obtain a compound of formula
13 more elements
Dependencies are inferred from the claim text.