JAESCHKE, GEORG,STADLER, HEINZ,VIEIRA, ERIC,LINDEMANN, LOTHAR,RICCI, ANTONIO,RUEHER, DANIEL
申请号：
ECSP14013296
公开号：
ECSP14013296A
申请日:
2014.04.07
申请国别(地区):
EC
年份:
2014
代理人:
摘要：
The present Invention relates to Derivatives of the formula in the etinilo: u is n or CH, R8 is Hydrogen, halogen, alkyl or alkoxy is lower and Lower； n - (R4) -, - or - or - C (r5r5 ')； in the R4 is Hydrogen or lower alkyl and R5 / R5' are independently Hydrogen, alkyl, Hydroxy, Lower or lower alkoxy； V - N (r6) - or - C (r7r7 '),Where is Hydrogen or lower alkyl R6 and R7 / R7 is independently between Hydrogen, Lower alkyl, alkoxy or CH2 - Lower along with the carbon Atom to which they are United Can form a cycloalkyl C3 C6； r1 is phenyl or heteroaryl, which are optionally substituted by has L u00f3geno, Lower alkoxy alkyl or lower Number； M is 0 OR 1； in the case that m is 1,R3 / R3 are independently between Hydrogen, Lower alkyl, alkoxy or CH2 - Lower along with the carbon Atom to which they are United Can form a cycloalkyl C3 C6； n is 0 OR 1； in the case that n is 1 / R2, R2 'are Independence each other with Hydrogen Lower alkyl,CH2 or lower alkoxy - along with the carbon Atom to which they are United Can form a cycloalkyl or C3 C6； IF m is the Number 1, and N is the Number 0, R3 and R7 along with the carbon Atoms to which they are United Can form a cycloalkyl C4 - 6； or if M is the n is the Number 1 and Number 1,R2 and R3 and R7 R3 or together with carbon Atoms to which they are United Can form a cycloalkyl C4 - 6； or a pharmaceutically acceptable acid Addition Salt, a racemic mixture, and / or the corresponding enantiomers or optical isomers and / or stereoisomers of the same.It has now been found that the compounds of the 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 Ien 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
