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Etinilo derivatives as modulators of metabotropic glutamate receptor
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
BIEMANS, Barbara,GUBA, Wolfgang,JAESCHKE, Georg,LINDEMANN, Lothar,OHARA, Fionn,RICCI, Antonio,RUEHER, Daniel,VIEIRA, Eric
申请号:
PE0023372017
公开号:
PE03562018A1
申请日:
2016.07.11
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
Etinilo refers to compounds of formula (i) wherein R1 is lower alkyl R2 is phenyl or pyridinyl n is 0 to 2 V and u are each or CH2 l is a heteroaryl Group of five or sixS Elements such as pyridine, pyrimidine, pyrazole, among others.Preferred compounds are: (8S) - 3 - difluoro - 2.6 - [4 - (2 - feniletinil) phenyl] - 2 - methyl - spiro [6,7 dihydro - 5H - isoquinolin - 8.6 - hexahidropirimidin] - 2 , 4 - dione (6S) - 3 - [26 - difluoro - 4 - [2 - (3-pyridyl) Ethinyl] phenyl] - 1 - methyl - spiro [hexahidropirimidin - 6.1 - Tetralin] - 2.4 - dione among others. It also relates to a Pharmaceutical composition.These compounds are positive allosteric modulators (MAP) metabotropic glutamate receptor 4 (mglur4) is useful for the treatment of Parkinsons disease, anxiety, emesis,AutismSE REFIERE A COMPUESTOS DERIVADOS DE ETINILO DE FORMULA (I) DONDE R1 ES ALQUILO INFERIOR R2 ES FENILO O PIRIDINILO n ES DE 0 A 2 V Y U SON CADA UNO O U CH2 L ES UN GRUPO HETEROARILO DE CINCO O SEIS ELEMENTOS TAL COMO PIRIDINA, PIRIMIDINA, PIRAZOL, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (8S)-3-[2,6-DIFLUORO-4-(2-FENILETINIL)FENIL]-1-METIL-SPIRO[6,7-DIHIDRO-5H-ISOQUINOLIN-8,6-HEXAHIDROPIRIMIDIN]-2,4-DIONA (6S)-3-[2,6-DIFLUORO-4-[2-(3-PIRIDIL)ETINIL]FENIL]-1-METIL-SPIRO[HEXAHIDROPIRIMIDIN-6,1-TETRALIN]-2,4-DIONA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS (MAP) DEL RECEPTOR METABOTROPICO DEL GLUTAMATO 4 (mGluR4) SIENDO UTILES PARA EL TRATAMIENTO DE LA ENFERMEDAD DEL PARKINSON, ANSIEDAD, EMESIS, AUTISMO
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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