Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
摘要:
We have discovered that polar 7-substituents of pyridopyrimidine derivatives affect not only whole cell AK inhibitory potency. but also selectivity in causing locomotor side effects in vivo animal models. We have identified compound, 1o, which has potent whole cell AK inhibitory potency, analgesic activity and minimal reduction of locomotor activity. (C) 2003 Elsevier Ltd. All rights reserved.
1,6-DIHYDRO-1,3,5,6-TETRAAZA-AS-INDACENE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
申请人:Pitts William J.
公开号:US20100210629A1
公开(公告)日:2010-08-19
The present invention provides for tricyclic compounds having the formula (I),
wherein R
1
, R
2
, R
5
, R
6
, R
7
, and R
8
are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
作者:Guo Zhu Zheng、Yue Mao、Chih-Hung Lee、John K. Pratt、John R. Koenig、Richard J. Perner、Marlon D. Cowart、Gregory A. Gfesser、Steve McGaraughty、Katharine L. Chu、Chang Zhu、Haixia Yu、Kathy Kohlhaas、Karen M. Alexander、Carol T. Wismer、Joseph Mikusa、Michael F. Jarvis、Elizabeth A. Kowaluk、Andrew O. Stewart
DOI:10.1016/s0960-894x(03)00642-5
日期:2003.9
We have discovered that polar 7-substituents of pyridopyrimidine derivatives affect not only whole cell AK inhibitory potency. but also selectivity in causing locomotor side effects in vivo animal models. We have identified compound, 1o, which has potent whole cell AK inhibitory potency, analgesic activity and minimal reduction of locomotor activity. (C) 2003 Elsevier Ltd. All rights reserved.