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芳基乙炔基衍生物
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GREEN, LUKE,格林 路克,GUBA, WOLFGANG,葛巴 渥夫甘,JAESCHKE, GEORG,杰许柯 乔治,傑許柯 喬治,JOLIDON, SYNESE,裘里敦 西尼斯,LINDEMANN, LOTHAR,林德曼 洛撒,RICCI, ANTONIO,李奇 安东尼奥,李奇 安東尼奧,RUEHER, DANIEL,路荷 丹尼尔,格林 路克,葛巴 渥夫甘,杰许柯 乔治,傑許柯 喬治,裘里敦 西尼斯,林德曼 洛撒,李奇 安东尼奥,李奇 安東尼奧,路荷 丹尼尔
申请号:
TW100112500
公开号:
TWI445706B
申请日:
2011.04.11
申请国别(地区):
TW
年份:
2014
代理人:
摘要:
The present invention relates to ethynyl derivatives of formula Iwherein U is =N- or =C(R5)-; V is -CH= or -N=; W is =CH- or =N-; with the proviso that only one of U, V or W can be nitrogen. R5is hydrogen, methyl or halogen; Y is -N(R6)-, -O-, -C(R7')(R7)-, -CH2O- or -CH2S(O)2-; wherein R6is hydrogen or lower alkyl and R7/R7'are independently from each other hydrogen, hydroxy, lower alkyl or lower alkoxy; R1 is phenyl or heteroaryl, which are optionally substituted by one or two substituents, selected from halogen, lower alkyl or lower alkoxy; R2/R2'are independently from each other hydrogen, lower alkyl, hydroxy, lower alkoxy, C3-C6-cycloalkyl, CH2-lower alkoxy, or may form together with the carbon atom to which they are attached a C3-C6- cycloalkyl or a ring containing -CH2OCH2-; m is 0, 1 or 2; 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; or R3and R2may form together with the carbon atom to which they are attached a C3-6-cycloalkyl or a ring containing -(CH2)2OCH2-; n is 0 or 1; in case n is 1, R4/R4'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; R4and R2may form together with the carbon atom to which they are attached a C3-6-cycloalkyl; or if n is 0 and Y is -N(R6)-, then R6and R2may form together with the carbon atom and the nitrogen atom to which they are attached a C3-6-cycloalkyl; or if n and m are 0, then R2and R7may form together with the carbon atoms to which they are attached a C3-6-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
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