DZIERBA, Carolyn Diane,DASGUPTA, Bireshwar,MACOR, John E.,BRONSON, Joanne J.,RAJAMANI, Ramkumar,KARAGEORGE, George N.
申请号：
ES14792665
公开号：
ES2678877T3
申请日:
2014.10.08
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A compound of formula (I) ** (See formula) ** or a pharmaceutically acceptable salt thereof, in which: n is 0, 1 or 2； R1 is selected from -CH2NRaRb, -C (O) NRaRb, -CH2OR6 and -CO2R6； R2 is selected from hydrogen and -CO2R6； R3 is selected from hydrogen and Br； when n is 1, R4 is selected from halo, haloalkyl, hydroxy C1-C3 alkyl, -OR6； or, when n is 2, the two R4 groups are in adjacent carbon atoms and, together with the atoms to which they are attached, form a five-membered ring selected from ** (See formula) ** in which " indicates the point of attachment to the six-member aromatic ring； R5 is selected from C2 alkenyl, -NHC (O) R7, -C (O) NHR7, ** (See formula) ** each R6 is independently hydrogen or C1-C6 alkyl； R7 is selected from C1-C6 alkyl and C1-C6 aminoalkyl； R8 is selected from C1-C6 aminoalkyl, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl and phenyl； and Ra and Rb are independently selected from hydrogen, C1-C3 alkoxy C1-C3 alkyl, C1-C3 alkyl, C2-C6 aminoalkyl, C1-C3 cyanoalkyl, C3-C6 cycloalkyl C1-C3 alkyl, ** (See formula) ** Ra and Rb, together with the nitrogen atom to which they are attached, form a ring selected from azetidinyl, morpholinyl, piperazinyl, piperidinyl, pyrrolidinyl, ** (See formula) ** where the ring is optionally substituted with one or two independently selected substituents among C1-C3 acylamino, C1-C3 alkyl, amino, C1-C3 aminoalkyl, hydroxy and methylamino for use in the treatment or management of a disease or disorder mediated by AAK1 activity selected from Alzheimer's disease, bipolar disorder, pain , Parkinson's disease and schizophrenia.Un compuesto de fórmula (I) **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en la que: n es 0, 1 o 2； R1 se selecciona entre -CH2NRaRb, -C(O)NRaRb, -CH2OR6 y -CO2R6； R2 se selecciona entre hidrógeno y -CO2R6； R3 se selecciona entre hidrógeno y Br； cuando n es 1, R4 se selecciona entre halo, haloalquilo, hidroxialquilo C1-C3, -OR6； o, cuando n es 2, los
