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QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
专利权人:
发明人:
BUNGARD, CHRISTOPHER JAMES,邦贾德 克里斯多夫 詹姆士,邦賈德 克里斯多夫 詹姆士,CONVERSO, ANTONELLA,康瓦索 安东尼拉,康瓦索 安東尼拉,DE LEON, PABLO,帝 里昂 帕布罗,帝 里昂 帕布羅,HANNEY, BARBARA,汉尼 芭芭拉,漢尼 芭芭拉,HARTINGH, TIMOTHY JOHN,哈汀 提摩西 约翰,哈汀 提摩西 約翰,M
申请号:
TW101140837
公开号:
TWI605040B
申请日:
2012.11.02
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimers disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.本發明提供式(I)喹啉甲醯胺及喹啉甲腈化合物其中環A、RQ、-L-、R1、n、R2及R3係如本文所定義。本發明化合物適用作非競爭性mGluR2拮抗劑或mGluR2負向異位性調節劑(NAM),且用於藉由向患者投與治療有效量之本發明化合物或其醫藥學上可接受之鹽來治療患者(較佳人類)之涉及mGluR2-NAM受體之疾病或病症(可能包括阿茲海默氏病、認知障礙、精神分裂症及其他情緒障礙、疼痛障礙及睡眠障礙)的方法。本發明亦係有關包含本發明化合物或其醫藥學上可接受之鹽(視情況與一或多種另外的活性成分組合)及醫藥學上可接受之載劑的醫藥組合物及本發明化合物及醫藥組合物在治療該等疾病中之用途。
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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