EMMANUEL PINARD,ALEXANDER FLOHR,HERVE SCHAFFHAUSER,THERESA MARIA BALLARD,KATRIN GROEBKE ZBINDEN,THOMAS RYCKMANS
申请号：
MX2015017343
公开号：
MX2015017343A
申请日:
2014.08.27
申请国别(地区):
MX
年份:
2016
代理人:
摘要：
The present invention relates to compounds of formula I wherein R1 halogen, lower alkyl, lower alkoxy, cyano, phenyl, C(O)NHCH3, C(O)NH2, lower alkyl substituted by halogen or is a five-membered heteroaryl group, optionally substituted by lower alkyl Y1 is N or CH Y2 is CH and if Y1 is CH, Y1 and Y2 may form together with the C-atoms to which they are attached a ring, containing −CH=N-N(CH3)-, -CH=N-N(H)- X is CH or N R is (CH2)m-cycloalkyl, optionally substituted by hydroxy, lower alkoxy or lower alkyl, or is tetrahydropyran, optionally substituted by hydroxy, or is lower alkoxy, substituted by hydroxy, or is lower alkyl substituted by one or two hydroxy, or is (CH2)m-pyridinyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, or is L-phenyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, and L is a bond, -CH(CH2OH)- or −CH2CH(OH)- n is 0, 1 or 2 m is 0 or 1 or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds of the present invention are muscarinic M1 receptor positive allosteric modulators (PAM) and hence are useful in the treatment of diseases, mediated by the muscarinic M1 receptor, such as Alzheimers disease, cognitive impairment, schizophrenia, pain or sleep disorders.La presente invención se refiere a compuestos de la fórmula I en la que R1 es un halógeno, un alquilo inferior, un alcoxi inferior, ciano, fenilo, C(O)NHCH3, C(O)NH2, un alquilo inferior sustituido con un halógeno o es un grupo heteroarilo de cinco miembros, opcionalmente sustituido con un alquilo inferior Y1es N o CH Y2es CH y si Y1 es CH, Y1 e Y2 pueden formar un anillo junto con los átomos de C a los que están unidos, e incluyen -CH=N-N(CH3)-, -CH=N-N(H)- X es CH o N R es (CH2)m-cicloalquilo, opcionalmente sustituido con un hidroxi, un alcoxi inferior o un alquilo inferior, o es tetrahidropirano, opcionalmente
