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专利权人:
F. HOFFMANN-LA ROCHE AG.*
发明人:
CLAUS RIEMER,ANDREAS KOBLET,HASANE RATNI,MATTHIAS NETTEKOVEN,WALTER VIFIAN,HANNER KNUST
申请号:
MX2012006293
公开号:
MX2012006293A
申请日:
2010.12.14
申请国别(地区):
MX
年份:
2012
代理人:
摘要:
The present application relates to compounds of formula (I) wherein R1is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen n is 1, 2 or 3, if n is 2 or 3, R1can be different R2is C2-7-alkyl or C3-6-cycloalkyl R3is the group (II) wherein X is CH or N R5is hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, S(O)2-lower alkyl, -C(O)CH2O-lower alkyl, -C(O)-CH2-CN, or is - or -C(O)-cycloalkyl, cycloalkyl, or -CH2-cycloalkyl, wherein the cycloalkyl groups are optionally substituted by lower alkyl, -CH2-O-Iower alkyl, lower alkoxy, CF3, halogen or cyano, or is -C(O)-heterocycloalkyl or heterocycloalkyl, or is -C(O)-heteroaryl or is heteroaryl or is -C(O)-aryl or aryl, which heterocycloalkyl, heteroaryl or aryl groups are optionally substituted by halogen, lower alkyl, =O, lower alkoxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -C(O)-CH2-N(di-lower alkyl), C(O)NH-lower alkyl, C(O)NH2, -O-C(O)- lower alkyl, C(O)-lower alkyl, S(O)2-lower alkyl or cyano R4 is aryl, which is optionally substituted by halogen, hydroxy, lower alkyl, lower alkyl substituted by halogen, S(O)2-lower alkyl, cyano or by lower alkoxy or to a pharmaceutically active salt 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 presente solicitud se refiere a compuestos de la fórmula (I) en donde R1 es hidrógeno, halógeno, ciano, alquilo inferior o alquilo inferior sustituido por halógeno R2 es alquilo-C2-7 o cicloalquilo-C3-6 R3 es el grupo (II) en donde X es CH o N R5 es hidrógeno, -C(Q)alquilo inferior, -C(0)0-alquilo inferior, S(0)2-alquilo inferior, -C(0)CH2O-alquilo inferior, -C(0)-CH2-CN, o es - C(0)-cicloalquilo, cicloalquilo, o -CH2-cicloalquilo, en donde los grupos cicloalquilo son opcionalmente sustituidos por un alquilo inferior, -CH2-0-alquilo inferior,
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