ANTONIO RICCI,DANIEL RUEHER,ERIC VIEIRA,GEORG JAESCHKE,HEINZ STADLER,LOTHAR LINDEMANN
申请号：
BR112014007898
公开号：
BR112014007898A2
申请日:
2012.10.04
申请国别(地区):
BR
年份:
2017
代理人:
摘要：
Patent Summary: "Ethinyl derivatives as allosteric modulators of mglur5". the present invention relates to ethinyl derivatives of formula (i) wherein u is n or ch, r 8 is hydrogen, halogen, lower alkyl or lower alkoxy； y is -n (r4) -, -or 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 '), where r6 is hydrogen or lower alkyl and r7 / r7' are independently hydrogen, lower alkyl, ch2-lower alkoxy, or may form, together with the carbon atom to which they are attached, a C 3 -C 6 cycloalkyl； R1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy； m is 0 or 1； in the case m is 1, r3 / r3 'are independently 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 the case n is 1, r 2 / r 2 'are independently of each other hydrogen, lower alkyl, ch 2-lower alkoxy or may form, together with the carbon atom to which they are attached, a C 3 -C 6 -cycloalkyl； or if m is 1 and n is 0, r 3 and r 7 may form, together with the carbon atoms to which they are attached, a C 4-6 cycloalkyl； or if m is 1 and n is 1, r 2 and r 3 or r 3 and r 7 may form, together with the carbon atoms to which they are attached, a C 4-6 cycloalkyl； or a pharmaceutically acceptable acid addition salt, a racemic mixture, or its enantiomer and / or optical isomer and / or stereoisomer thereof. The compounds of formula I have been found to be allosteric modulators of the metabotropic glutamate 5 subtype 5 receptor (mglur5).resumo patente de invenção: "derivados de etinila como moduladores alostéricos de mglur5". a presente invenção refere-se aos derivados de etinila de fórmula (i) em que u é n ou ch, r8 é hidrogênio, halogênio, alquila inferior ou alcóxi inferior； y é -n(r4)-, -o- ou -c(r5r5')-； em que r4 é hidrogênio ou alquila inferior e r5/r5' são independen
