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Substituted triazole derivatives and their use as neurokinin 3 receptor antagonists
专利权人:
F. Hoffmann-La Roche AG
发明人:
Riemer, Claus,Spooren, Will,Hoener, Marius,Gobbi, Luca Claudio
申请号:
AU2012203624
公开号:
AU2012203624A1
申请日:
2012.06.21
申请国别(地区):
AU
年份:
2012
代理人:
摘要:
#$%^&*AU2012203624A120120712.pdf#####SUBSTITUTED TRIAZOLE DERIVATIVES AND THEIR USE AS NEUROKININ 3 RECEPTOR ANTAGONISTS Abstract The present invention relates to compounds of formula (I) 5 ORR R N N N NN R3 H N-N wherein R' is -(CRR')n-aryl-(CRR'),-heteroaryl, -(CRR'),-O-aryl or -(CRR'),-Oheteroaryl, wherein the aryl or heteroaryl groups are unsubstituted or substituted by one 10 or two substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or unsubstituted or substituted phenyl, wherein the substitution on the phenyl group may be lower alkyl or halogen, or is (CRR')n-2-benzo[1.3]dioxolyl; R/R' are independently from each other hydrogen, lower alkyl or are together with the carbon atom to which they are attached a cycloalkyl group; is R2/R3 are independently from each other hydrogen, lower alkyl, phenyl or cycloalkyl or may form together with the N- atom to which they are attached a five or six membered saturated heterocycle; n is 0 or 1; and to pharmaceutically suitable acid addition salts thereof. The invention includes all stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and 20 non-racemic mixtures thereof. It has been found that the present compounds are selective allosteric positive modulators of the human NK-3 receptor for the treatment of anxiety, depression, bipolar disorders, Parkinson's disease, schizophrenia and pain.
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