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专利权人:
F. HOFFMANN-LA ROCHE AG.*
发明人:
HASANE RATNI,MATTHIAS NETTEKOVEN,WALTER VIFIAN
申请号:
MX2012015268
公开号:
MX2012015268A
申请日:
2011.07.04
申请国别(地区):
MX
年份:
2013
代理人:
摘要:
The invention relates to a compound of general formula : (I) wherein A is selected from the groups (a), (b) or (c): formula (II) or formula (III) (b) or is cycloalkyl, (c) optionally substituted by lower alkyl (c)Ar1 is phenyl or a six membered heteroarylX1 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 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 to pharmaceutically active salts, sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof..It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinsons disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).La invención se refiere a un compuesto de la fórmula general I en donde A se selecciona de los grupos (a), (b) o (c): la fórmula (II) o la fórmula (III) (b) o es cicloalquilo, (c) opcionalmente sustituido con alquilo inferior (c) Ar1 es fenilo o un heteroarilo de seis miembros X1 es N o CH X2 es N-R1 u O R1 es S(O)2 alquilo inferior C(O)-cicloalquilo sustituido con alquilo inferior, o es C(O)-alquilo inferior, alquilo inferior, ciano, cicloalquilo o es un heteroarilo de E miembros sustituido con alquilo inferior, ciano, C(O)(alquilo inferior), halógeno, alquilo inferior sustituido con halógeno o alcoxi inferior o es fenilo sustituido con ciano o halógeno R2 es alquilo infe
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