- 专利标题: N-(5-(BIPHEN-4-YLMETHYLOXY)PENTYL)-SUBSTITUTED IMINOSUGARS AS INHIBITORS OF GLUCOSYLCERAMIDE SYNTHASE
-
申请号: EP18191316.1申请日: 2015-03-23
-
公开(公告)号: EP3461812A1公开(公告)日: 2019-04-03
- 发明人: OVERKLEEFT, Herman Steven , VAN BOECKEL, Stan , AERTS, Johannes Maria Franciscus Gerardus , GHISAIDOOBE, Amar , VAN DEN BERG, Richard
- 申请人: Academisch Medisch Centrum , Universiteit Leiden
- 申请人地址: Meibergdreef 9 1105 AZ Amsterdam NL
- 专利权人: Academisch Medisch Centrum,Universiteit Leiden
- 当前专利权人: Academisch Medisch Centrum,Universiteit Leiden
- 当前专利权人地址: Meibergdreef 9 1105 AZ Amsterdam NL
- 代理机构: Boult Wade Tennant LLP
- 优先权: EP14162104 20140327
- 主分类号: C07D211/46
- IPC分类号: C07D211/46 ; A61K31/445 ; A61P3/00 ; A61P25/16 ; A61P9/10
摘要:
The present invention concerns D-deoxygalactonojirimycin derivatives shown below. These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same D -galacto configuration. Therefore, compounds of the present invention are effective in the treatment of diseases which are associated with an irregular level of cytosolic or lysosomal glucosylceramide and/or higher glycosphingolipids, such as a lysosomal storage disorder, such as Gaucher disease, Fabry disease, Tay-Sachs disease, Sandhoff disease, GM1 gangliosidosis, Sialidosis, Niemann Pick disease type C and AMRF, or a symptom of one of the diseases collectively classed as metabolic syndrome, such as obesity, insulin resistance, hyperlipidemia, hypercholesterolemia, polycystic kidney disease, type II diabetes and chronic inflammation, or a neurodenegerative disorder, such as Parkinson disease or Lewy-body dementia.
公开/授权文献
信息查询