发明公开
- 专利标题: 2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES
- 专利标题(中): 2-苯基-2-甲基咪唑并[1,2-A]吡啶衍生物
-
申请号: EP14719326.2申请日: 2014-04-25
-
公开(公告)号: EP2991983A1公开(公告)日: 2016-03-09
- 发明人: BORRONI, Edilio , GOBBI, Luca , HONER, Michael , KNUST, Henner , KOERNER, Matthias , MURI, Dieter
- 申请人: F.Hoffmann-La Roche AG
- 申请人地址: Grenzacherstrasse 124 4070 Basel CH
- 专利权人: F.Hoffmann-La Roche AG
- 当前专利权人: F.Hoffmann-La Roche AG
- 当前专利权人地址: Grenzacherstrasse 124 4070 Basel CH
- 代理机构: Poppe, Regina
- 优先权: EP13165676 20130429
- 国际公布: WO2014177458 20141106
- 主分类号: C07D471/04
- IPC分类号: C07D471/04 ; A61K31/437 ; A61P9/00
摘要:
The invention relates to compounds of formulas I and II, formula I or formula II wherein R
1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy substituted by halogen, di-lower alkyl amino, C(O)O-lower alkyl, lower alkyl substituted by hydroxy or hydroxy; R
2 is hydrogen, lower alkyl, halogen, lower alkoxy, S-lower alkyl, lower alkoxy substituted by halogen, O(CH
2 )
2 -lower alkoxy substituted by halogen, di-lower alkyl amino, alkyl amino, NH-lower alkyl substituted by halogen, N(lower alkyl)-benzyl, lower alkyl substituted by hydroxy, heterocycloalkyl optionally substituted by halogen, CH
2 -lower alkoxy, CH
2 -lower alkoxy substituted by halogen or hydroxy; or R
1 and R
2 form together with the carbon atoms to which they are attached a ring containing -OCH
2 CH
2 O-, OCH
2 O-, OCH
2 CH
2 CH
2 O- or -NHC(O)CH
2 O-; R
3 is hydrogen or lower alkoxy; R
4 is hydrogen or lower alkyl; R
5 is lower alkyl, cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or R
4 and R
5 form together with the nitrogen atom to which they are attached a ring containing -CH
2 CH
2 CHRCH
2 CH
2 -, -CH
2 CHRCH
2 CH
2 -, -CH
2 CH
2 OCH
2 CH
2 -, -CH
2 CH
2 NR'CH
2 CH
2 -, CH
2 CHR- or -CH
2 CH
2 CH
2 -; wherein R is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R' is lower alkyl substituted by halogen; R
a is hydrogen or H; R
b is hydrogen, hydroxy or
3 H; R
6 is hydrogen, halogen or lower alkyl; HetAr is selected from the group consisting of thiophenyl, furanyl, thiozolyl, benzofuranyl, pyrazolyl, benzoimidazolyl or pyridinyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The present compounds are suitable as imaging tool, which will improve diagnosis by identifying potential patients with excess of tau aggregates in the brain, which may be likely to develop Alzheimer's disease.
1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy substituted by halogen, di-lower alkyl amino, C(O)O-lower alkyl, lower alkyl substituted by hydroxy or hydroxy; R
2 is hydrogen, lower alkyl, halogen, lower alkoxy, S-lower alkyl, lower alkoxy substituted by halogen, O(CH
2 )
2 -lower alkoxy substituted by halogen, di-lower alkyl amino, alkyl amino, NH-lower alkyl substituted by halogen, N(lower alkyl)-benzyl, lower alkyl substituted by hydroxy, heterocycloalkyl optionally substituted by halogen, CH
2 -lower alkoxy, CH
2 -lower alkoxy substituted by halogen or hydroxy; or R
1 and R
2 form together with the carbon atoms to which they are attached a ring containing -OCH
2 CH
2 O-, OCH
2 O-, OCH
2 CH
2 CH
2 O- or -NHC(O)CH
2 O-; R
3 is hydrogen or lower alkoxy; R
4 is hydrogen or lower alkyl; R
5 is lower alkyl, cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or R
4 and R
5 form together with the nitrogen atom to which they are attached a ring containing -CH
2 CH
2 CHRCH
2 CH
2 -, -CH
2 CHRCH
2 CH
2 -, -CH
2 CH
2 OCH
2 CH
2 -, -CH
2 CH
2 NR'CH
2 CH
2 -, CH
2 CHR- or -CH
2 CH
2 CH
2 -; wherein R is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R' is lower alkyl substituted by halogen; R
a is hydrogen or H; R
b is hydrogen, hydroxy or
3 H; R
6 is hydrogen, halogen or lower alkyl; HetAr is selected from the group consisting of thiophenyl, furanyl, thiozolyl, benzofuranyl, pyrazolyl, benzoimidazolyl or pyridinyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The present compounds are suitable as imaging tool, which will improve diagnosis by identifying potential patients with excess of tau aggregates in the brain, which may be likely to develop Alzheimer's disease.
公开/授权文献
- EP2991983B1 2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-A]PYRIDINE DERIVATIVES 公开/授权日:2017-03-01
信息查询