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乙炔基衍生物
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
BIEMANS, BARBARA,比曼斯 芭芭拉,GUBA, WOLFGANG,葛巴 渥夫甘,JAESCHKE, GEORG,杰许柯 乔治,傑許柯 喬治,RICCI, ANTONIO,瑞奇 安东尼欧,瑞奇 安東尼歐,RUEHER, DANIEL,路荷 丹尼尔,路荷 丹尼爾,VIEIRA, ERIC,维拉 艾瑞克,維拉 艾瑞克,比曼斯 芭芭拉,葛巴 渥夫甘,杰许柯 乔治,傑許柯 喬治,瑞奇 安东尼欧,瑞奇 安東尼歐,路荷 丹尼尔,路荷 丹尼爾,维拉 艾瑞克,維拉 艾瑞克
申请号:
TW103132854
公开号:
TW201524963A
申请日:
2014.09.23
申请国别(地区):
TW
年份:
2015
代理人:
摘要:
The present invention relates to compounds of formula I wherein Y is N or C-R1’; G is a 5 or 6-membered aromatic or heteroaromatic ring containing 0, 1, 2 or 3 heteroatoms, selected from the group consisting of phenyl, pyridinyl with different N-positions, imidazolyl, pyrazinyl, pyrimidinyl, thiophenyl, thiazolyl, pyrazolyl or thiadiazolyl, which are optionally substituted by l, 2 or 3 substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or NRR’; R and R’ are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a five or six membered saturated heterocyclic group which may contain an additional oxygen, NH, or N-lower alkyl group; R1 is hydrogen, halogen or lower alkyl substituted by halogen; R1’ is hydrogen, halogen or lower alkyl substituted by halogen; R2 is hydrogen, lower alkyl, lower alkoxyalkyl, cycloalkyl or heterocycloalkyl; or R2 may form together with the closest carbon atom in group G a group for A being -CH2-, -CH2CH2, or -C(CH3)2-, R3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; 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 been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson’s disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.本發明係關於式I之化合物其中Y 為N或C-R1';G 為含有0、1、2或3個雜原子之5員或6員芳族或雜芳族環,其係選自由苯基、具有不同N-位置之吡啶基、咪唑基、吡嗪基、嘧啶基、苯硫基、噻唑基、吡唑基或噻二唑基組成之群,該等基團視情況經1、2或3個選自由鹵素、低碳烷基、低碳烷氧基、經鹵素取代之低碳烷氧基或NRR'組成之群的取代基取代;R及R'彼此獨立地為氫或低碳烷基,或可連同其所連接之N原子形成可含有額外的氧、NH或N-低碳烷基之五員或六員飽和雜環基;R1 為氫、鹵素或經鹵素取代之低碳烷基;R1' 為氫、鹵素或經鹵素取代之低碳烷基;R2 為氫、低碳烷基、低碳烷氧烷基、環烷基
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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