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Piperazine and [1,4] diazepan derivatives as NK antagonists
专利权人:
F. Hoffmann-La Roche AG
发明人:
Nettekoven, Matthias,Ratni, Hasane,Wu, Xihan,Knust, Henner
申请号:
AU2008263982
公开号:
AU2008263982B2
申请日:
2008.06.04
申请国别(地区):
AU
年份:
2012
代理人:
摘要:
The present invention relates to a compound of Formula (I) wherein Ris hydrogen or lower alkyl; is hydrogen, fluoro, hydroxy or lower alkyl; Ris hydrogen or lower alkyl; R is -CHR-A R ishydrogen, lower alkyl, fluoro, CF, CHOH or cycloalkyl;A is aryl or heteroaryl, which rings are unsubstituted or substituted by (R)o;R may be the same or not when o is more than one, and is heteroaryl, loweralkyl, lower alkoxy, cyano, halogen, lower alkyl substituted by halogen, loweralkoxy substituted by halogen or NRR; o is 1, 2 or 3; R,R are independently hydrogen or lower alkyl; R is loweralkyl; R is lower alkyl, lower alkoxy or halogen; n is 1 or 2; m is 1 or2; or to a pharmaceutically suitable acid addition salt thereof. The inventionincludes all sterioisomeric forms, including individual diastereoisomersand enantiomers of the compound of Formula (I) as well as racemic and non-racemicmixtures thereof. It has been found that the present compounds are high potentialNK-3 receptor antagonists for the treatment of depression, pain, psychosis,Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivitydisorder (ADHD).
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