申请人:Heiser Ulrich
公开号:US20110092501A1
公开(公告)日:2011-04-21
The invention relates to novel pyrrolidine derivatives of formula (I):
wherein R
1
, R
2
and R
3
are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
本发明涉及新颖的吡咯烷衍生物,其具有如下公式(I):其中R1、R2和R3如本文所述定义,作为谷氨酰胺环化酶(QC,EC 2.3.2.5)的抑制剂。谷氨酰胺环化酶催化N末端谷氨酰胺残基形成焦谷氨酸(5-氧代脯氨酸,pGlu*)的分子内环化,并释放氨,以及催化N末端谷氨酸残基形成焦谷氨酸的分子内环化,并释放水。