[EN] NOVEL IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS LRRK2 INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS IMIDAZO[4,5-C]QUINOLÉINE UTILISÉS EN TANT QU'INHIBITEURS DE LRRK2
申请人:PFIZER
公开号:WO2018163066A1
公开(公告)日:2018-09-13
The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
Novel Imidazo[4,5-c]Quinoline And Imidazo[4,5-c][1,5]Naphthyridine Derivatives As LRRK2 Inhibitors
申请人:Pfizer Inc.
公开号:US20170073343A1
公开(公告)日:2017-03-16
The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof
wherein R
1
, R
1a
, R
1b
, R
2
, R
4
, R
5
, R
6
, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
The present invention provides novel cyclic substituted imidazo[4,5- c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof, wherein R1, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
Utilizing on- and off-line monitoring tools to follow a kinetic resolution step during flow synthesis
作者:Kathleen A. Farley、Usa Reilly、Dennis P. Anderson、Brian P. Boscoe、Mark W. Bundesmann、David A. Foley、Manjinder S. Lall、Chao Li、Matthew R. Reese、Jiangli Yan
DOI:10.1002/mrc.4494
日期:2017.4
In situ reactionmonitoring tools offer the ability to track the progress of a synthetic reaction in real time to facilitate reaction optimization and provide kinetic/mechanistic insight. Herein, we report the utilization of flowNMR, flow IR, and other off‐line spectroscopy tools to monitor the progress of a flow chemistry reaction. The on‐line and off‐line tools were selected to facilitate the stereoselective