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专利权人:
F. HOFFMANN-LA ROCHE AG.*
发明人:
HEINZ STADLER,HASANE RATNI,MATTHIAS NETTEKOVEN,PHILIPPE JABLONSKI,ANGELIQUE PATINY-ADAM
申请号:
MX2012008147
公开号:
MX2012008147A
申请日:
2011.04.15
申请国别(地区):
MX
年份:
2012
代理人:
摘要:
The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, -C(0)-lower alkyl, -C(0)-CH2-lower alkoxy, -C(0)-C3-6-cycloalkyl, -(CH2)°-C(0)-NR,R, -(CH2)°S(0)2- lower alkyl or -S(0)2-NR,R o is 0 or 1 R,R are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a 5 or 6 membered heterocycloalkyl ring R2 is hydrogen or lower alkyl R3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen and may be the same or different in case n is 2 n is 1 or 2 Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen or to a pharmaceutically active acid addition salt. It has surprisingly been found that the compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.La presente invención, se relaciona con un compuesto de la Fórmula (I) en donde R1 es hidrógeno, alquilo inferior, alquilo inferior substituido por halógeno, bencilo, -C(O)-alquilo inferior, -C(O)-CH2-alcoxi inferior, C-(O)cicloalquil-C3-6 -(CH2)o-C(O)-NR,R´, -(CH2)0S(O)2-alquilo inferior o -S(O)2-NR,R´ o es 0 o 1 R, R´ son independientemente uno de otro hidrógeno o alquilo inferior, o pueden formar junto con el átomo N al cual están unidos 5 o 6 miembros del anillo heterocicloalquilo R2 es hidrógeno o alquilo inferior R3 es halógeno, alcoxi inferior, alquilo inferior substituido por halógeno o alcoxi inferior substituido por halógeno y pueden ser iguales o diferentes en caso de que n sea 2 n
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