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ETHYNYL DERIVATIVES
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GREEN,LUKE,GUBA, WOLFGANG,JAESCHKE,GEORG,JOLIDON,SYNESE,LINDEMANN,LOTHAR,STADLER,HEINZ,VIEIRA,ERIC
申请号:
MYPI 2012002710
公开号:
MY162998A
申请日:
2010.12.14
申请国别(地区):
MY
年份:
2017
代理人:
摘要:
THE PRESENT INVENTION RELATES TO ETHYNYL DERIVATIVES OF FORMULA (I) WHEREIN X IS N OR C-R¹; Y IS N OR C-R²; Z IS CH OR N; R⁴ IS A 6-MEMBERED AROMATIC SUBSTITUENT CONTAINING 0, 1 OR 2 NITROGEN ATOMS, OPTIONALLY SUBSTITUTED BY 1 TO 3 GROUPS, SELECTED FROM HALOGEN, LOWER ALKYL, LOWER ALKOXY OR NRR’; R¹ IS HYDROGEN, LOWER ALKYL, LOWER ALKOXY, HYDROXY, LOWER HYDROXYALKYL, LOWER CYCLOALKYL OR IS HETEROCYCLOALKYL OPTIONALLY SUBSTITUTED WITH HYDROXY OR ALKOXY; R² IS HYDROGEN, CN, LOWER ALKYL OR HETEROCYCLOALKYL; R AND R’ ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN OR LOWER ALKYL; OR TO A PHARMACEUTICALLY ACCEPTABLE SALT OR ACID ADDITION SALT, TO A RACEMIC MIXTURE, OR TO ITS CORRESPONDING ENANTIOMER AND/OR OPTICAL ISOMER AND/OR STEREOISOMER THEREOF. IT HAS NOW SURPRISINGLY BEEN FOUND THAT THE COMPOUNDS OF GENERAL FORMULA (I) ARE POSITIVE ALLOSTERIC MODULATORS (PAM) OF THE METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE 5 (mGluR5) AND THEY ARE THEREFORE USEFUL FOR THE TREATMENT OF DISEASES RELATED TO THIS RECEPTOR.
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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