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Ethinyl derivatives as allosteric modulators of mGluR5
专利权人:
F. Hoffmann-La Roche AG
发明人:
JAESCHKE, Georg,LINDEMANN, Lothar,RICCI, Antonio,RUEHER, Daniel,STADLER, Heinz,VIEIRA, Eric
申请号:
ES12767005
公开号:
ES2564884T3
申请日:
2012.10.04
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Ethynyl derivatives of the formula I ** Formula ** in which: U is N or CH, R8 is hydrogen, halogen, C1-C4 alkyl or C1-C4 alkoxy; Y is -N (R4) -, -O- or -C (R5R5 ') -; wherein R4 is hydrogen or C1-C4 alkyl and R5 / R5 'are independently hydrogen, hydroxy, C1-C4 alkyl or C1-C4 alkoxy; V is -N (R6) - or -C (R7R7 '), in which R6 is hydrogen or C1-C4 alkyl and R7 / R7' are independently hydrogen, C1-C4 alkyl, CH2-C1-C4 alkoxy or together with the carbon atom to which they are attached they can form a C3-C6 cycloalkyl; R1 is phenyl or heteroaryl, which are optionally substituted by halogen, C1-C4 alkyl or C1-C4 alkoxy; m is the number 0 or 1; in case m is 1, R3 / R3 'are independently hydrogen, C1-C4 alkyl, CH2-C1-C4 alkoxy or together with the carbon atom to which they are attached can form a C3-C6 cycloalkyl; n is the number 0 or 1; in the case where n is 1, R2 / R2 'are independently from each other hydrogen, C1-C4 alkyl, CH2-C1-C4 alkoxy or together with the carbon atom to which they are attached they can form a C3-C6 cycloalkyl; or if m is the number 1 and n is the number 0, R3 and R7 together with the carbon atoms to which they are attached can form a C4-6 cycloalkyl; or if m is the number 1 and n is the number 1, R2 and R3 or R3 and R7 together with the carbon atoms to which they are attached can form a C4-6 cycloalkyl; or a pharmaceutically acceptable acid addition salt, a racemic mixture, or the corresponding enantiomers and / or optical isomers and / or stereoisomers thereof.Derivados de etinilo de la fórmula I**Fórmula** en la que: U es N o CH, R8 es hidrógeno, halógeno, alquilo C1-C4 o alcoxi C1-C4; Y es -N(R4)-, -O- o -C(R5R5')-; en las que R4 es hidrógeno o alquilo C1-C4 y R5/R5' son con independencia hidrógeno, hidroxi, alquilo C1-C4 o alcoxi C1-C4; V es -N(R6)- o -C(R7R7'), en las que R6 es hidrógeno o alquilo C1-C4 y R7/R7' son con independencia entre sí hidrógeno, alquilo C1-C4, CH2- alcoxi C1-C4 o junto con el átomo de carbono al que están unidos pueden
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