您的位置: 首页 > 农业专利 > 详情页

乙炔基衍生物
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
JAESCHKE, GEORG,杰许柯 乔治,傑許柯 喬治,LINDEMANN, LOTHAR,林德曼 洛撒,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,STADLER, HEINZ,史丹勒 韩兹,史丹勒 韓茲,VIEIRA, ERIC,维拉 艾瑞克,維拉 艾瑞克,杰许柯 乔治,傑許柯 喬治,林德曼 洛撒,瑞奇 安东尼欧,瑞奇 安東尼歐,路荷 丹尼尔,路荷 丹尼爾,史丹勒 韩兹,史丹勒 韓茲,维拉 艾瑞克,維拉 艾瑞克
申请号:
TW101136749
公开号:
TWI468401B
申请日:
2012.10.04
申请国别(地区):
TW
年份:
2015
代理人:
摘要:
The present invention relates to ethynyl derivatives of formula Iwherein U is N or CH, R8is hydrogen, halogen, lower alkyl or lower alkoxy; Y is -N(R4)-, -O- or -C(R5R5’)-; wherein R4is hydrogen or lower alkyl and R5/R5’are independently hydrogen, hydroxy, lower alkyl or lower alkoxy; V is -N(R6)- or -C(R7R7’), wherein R6is hydrogen or lower alkyl and R7/R7’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; R1is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; m is 0 or 1; 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; n is 0 or 1; in case n is 1, R2/R2’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 if m is 1 and n is 0, R3and R7may form together with the carbon atoms to which they are attached a C4-6-cycloalkyl; or if m is 1 and n is 1, R2and R3or R3and R7may form together with the carbon atoms to which they are attached a C4-6-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 I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).本發明係關於式I之乙炔基衍生物其中U 係N或CH,R8係氫、鹵素、低碳烷基或低碳烷氧基;Y 係-N(R4)-、-O-或-C(R5R5')-;其中R4係氫或低碳烷基且R5/R5'獨立地係氫、羥基、低碳烷基或低碳烷氧基;V 係-N(R6)-或-C(R7R7'),其中R6係氫或低碳烷基且R7/R7'彼此獨立地係氫、低碳烷基、CH2-低碳烷氧基或可與其所附接之碳原子一起形成C3-C6-環烷基;R1係苯基或雜芳基,其視情況由鹵素、低碳烷基或低碳烷氧基取代;m 係0或1;倘若m係1,則R3/R3'彼此獨立地係氫、低碳烷基、CH2-低碳烷氧基或可與其所附接之碳原子一起形成C3-C6-環烷基;n 係0或1;倘若n係1,則
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充