基本信息:
- 专利标题： OXADIAZOLES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
- 申请号：PCT/US2003/024912 申请日：2003-08-08
- 公开(公告)号：WO2004014370A3 公开(公告)日：2004-02-19
- 发明人： WENSBO, David , XIN, Tao , STEFANAC, Tomislav , ARORA, Jalaj , MCLEOD, Donald, A. , KERS, Annika , MALMBERG, Johan , OSCARSSON, Karin , EDWARDS, Louise , ISAAC, Methvin , SLASSI, Abdelmalik , STORMANN, Thomas, M.
- 申请人： ASTRAZENECA AB , NPS PHARMACEUTICALS, INC. , WENSBO, David , XIN, Tao , STEFANAC, Tomislav , ARORA, Jalaj , MCLEOD, Donald, A. , KERS, Annika , MALMBERG, Johan , OSCARSSON, Karin , EDWARDS, Louise , ISAAC, Methvin , SLASSI, Abdelmalik , STORMANN, Thomas, M.
- 申请人地址： R & D Headquarters, Global Intellectual Property, S-151 85 Sodertalje SE
- 专利权人： ASTRAZENECA AB,NPS PHARMACEUTICALS, INC.,WENSBO, David,XIN, Tao,STEFANAC, Tomislav,ARORA, Jalaj,MCLEOD, Donald, A.,KERS, Annika,MALMBERG, Johan,OSCARSSON, Karin,EDWARDS, Louise,ISAAC, Methvin,SLASSI, Abdelmalik,STORMANN, Thomas, M.
- 当前专利权人： ASTRAZENECA AB,NPS PHARMACEUTICALS, INC.,WENSBO, David,XIN, Tao,STEFANAC, Tomislav,ARORA, Jalaj,MCLEOD, Donald, A.,KERS, Annika,MALMBERG, Johan,OSCARSSON, Karin,EDWARDS, Louise,ISAAC, Methvin,SLASSI, Abdelmalik,STORMANN, Thomas, M.
- 当前专利权人地址： R & D Headquarters, Global Intellectual Property, S-151 85 Sodertalje SE
- 代理机构： BENT, Stephen, A.
- 优先权： US60/402,039 20020809
- 主分类号： A61K31/4245
- IPC分类号： A61K31/4245
摘要：
The present invention relates to new compounds of formula (I), wherein P, Q, X 1 , X 2 , X 3 , X 4 , R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , m, n, o, p and q are defined as in any one of claims 1 to 12, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy. It has been found that the compounds according to the present invention, or salts therof, exhibit a high degree of potency and selectivity for individual metabotropic glutamate receptor (mGluR) subtypes. In particular there are compounds according to the present invention that are potent and selective for the mGluR Group I receptor and more particularly for mGluR5. Thus, it is expected that the compounds of the invention are well suited for the prevention and/or treatment of mGluR5 receptor-mediated disorders such as acute and chronic neurological and psychiatric disorders and chronic and acute pain disorders.
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K31/00 | 含有机有效成分的医药配制品 |
| --------A61K31/33 | .杂环化合物 |
| ----------A61K31/335 | ..仅有氧作为环杂原子的，例如制霉色基素 |
| ------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的，例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
| --------------A61K31/4245 | ....口恶二唑 |