ANTONIO RICCI,GEORG JAESCHKE,LOTHAR LINDEMANN,HEINZ STADLER,ERIC VIEIRA,DANIEL RUEHER
申请号：
MX2014004144
公开号：
MX2014004144A
申请日:
2012.10.04
申请国别(地区):
MX
年份:
2014
代理人:
摘要：
The present invention relates to ethynyl derivatives of formula (I) wherein U is N or CH, R8 is hydrogen, halogen, lower alkyl or lower alkoxyY is –N(R4)-, -O- or –C(R5R5)- wherein R4 is hydrogen or lower alkyl and R5/R5 are independently hydrogen, hydroxy, lower alkyl or lower alkoxy V is –N(R6)- or –C(R7R7), wherein R6 is hydrogen or lower alkyl and R7/R7 are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloalkyl R1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy m is 0 or 1 in case m is 1, R3/R3 are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloalkyl n is 0 or 1 in case n is 1, R2/R2 are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloalkyl or if m is 1 and n is 0, R3 and R7 may form together with the carbon atoms to which they are attached a C4-6-cycloalkyl or if m is 1 and n is 1, R2 and R3 or R3 and R7 may form together with the carbon atoms to which they are attached a C4-6-cycloalkyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula (I) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).La presente invención se refiere a derivados de etinilo de la fórmula I (ver Fórmula) en la que: U es N o CH, R8 es hidrógeno, halógeno, alquilo inferior o alcoxi inferior Y es -N(R4)-, -O- o -C(R5R5)- en las que R4 es hidrógeno o alquilo inferior y R5/R5 son con independencia hidrógeno, hidroxi, alquilo inferior o alcoxi inferior V es -N(R6)- o -C(R7R7), en las que R6 es hidrógeno o alquilo inferior y R7/R7 son
