Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease
摘要:
In the course of a programme aimed at identifying Nurr1/NOT agonists for potential treatment of Parkinson's disease, a few hits from high throughput screening were identified and characterized. A combined optimization pointed to a very narrow and stringent structure activity relationship. A comprehensive program of optimization led to a potent and safe candidate drug displaying neuroprotective and anti-inflammatory activity in several in vitro and in vivo models.
6-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
申请人:PEYRONEL Jean-Francois
公开号:US20100317675A1
公开(公告)日:2010-12-16
Compounds of formula (I):
in which:
X, R
1
, R
2
, R
3
and R
4
are as defined in the disclosure, or an acid addition salt thereof; and therapeutic use thereof.
式(I)的化合物:其中:X、R1、R2、R3和R4如本公开中所定义,或其酸盐;以及其治疗用途。
6-heterocyclic-imidazo[1,2-α]pyridine-2-carboxamide derivatives, preparation and therapeutic use thereof
申请人:Sanofi
公开号:US08314109B2
公开(公告)日:2012-11-20
Compounds of formula (I):
in which:
X, R1, R2, R3 and R4 are as defined in the disclosure, or an acid addition salt thereof; and therapeutic use thereof.
6-HETEROCYCLIC IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
申请人:PEYRONEL Jean-Francois
公开号:US20130041152A1
公开(公告)日:2013-02-14
Compounds of formula (I):
in which:
X, R
1
, R
2
, R
3
and R
4
are as defined in the disclosure, or an acid addition salt thereof; and therapeutic use thereof.