公开(公告)号：EP1586319B1

公开(公告)日：2009-10-21

申请号：EP05075779.8

申请日：2005-04-04

申请人： Noscira, S.A.

发明人： Martinez, Gil ,  Dorronsoro Diaz, Isabel ,  Alonso Cascon, Mercedes ,  Panizodel Pliego, Gema ,  Fuertes Huerta, Ana ,  Perez Puerto, Maria José ,  Medina Padilla, Miguel

IPC分类号： A61K31/433 ,  C07D285/08 ,  C07D417/04 ,  A61P25/28 ,  A61P3/10

CPC分类号： C07D285/08 ,  C07D417/04

公开(公告)号：EP1646622B1

公开(公告)日：2010-11-03

申请号：EP04743319.8

申请日：2004-07-09

申请人： NOSCIRA, S.A.

发明人： Martinez Gil, Ana ,  Dorronsoro Diaz, Isabel ,  Rubio Arrieta, Laura ,  Alonso Gordillo, Diana ,  Fuertes Huerta, Ana ,  Morales-Alcelay, Susana ,  Del Monte Millan, Maria ,  Garcia Palomero, Esther ,  Usan Egea, Paola ,  De Austria, Celia ,  Medina Padilla, Miguel ,  Munoz Ruiz, Pilar

IPC分类号： C07D401/12 ,  A61K31/473 ,  A61P25/28

CPC分类号： C07D401/12

摘要： The invention provides compounds of formula: (I) which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the β-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer’s disease.