Methylene amine substituted arylindenopyrimidines as potent adenosine A2A/A1 antagonists
摘要:
A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally. (C) 2010 Elsevier Ltd. All rights reserved.
Methylene amine substituted arylindenopyrimidines as potent adenosine A2A/A1 antagonists
摘要:
A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally. (C) 2010 Elsevier Ltd. All rights reserved.
[EN] MACROMOLECULAR COMPOSITIONS COMPRISING INDENE-DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF<br/>[FR] COMPOSITIONS MACROMOLÉCULAIRES CONTENANT DES DÉRIVÉS D'INDÈNE , LEUR PRÉPARATION, ET LEUR UTILISATION
申请人:STICHTING TECHNISCHE WETENSCHAPPEN
公开号:WO2019110557A1
公开(公告)日:2019-06-13
The present invention relates to a method for preparing a macromolecular composition comprising indene-derivatives. The invention also relates to the macromolecular compositions per se, and to methods of using the macromolecular compositions. The macromolecular compositions are useful for undergoing subsequent reactions with small molecules.
Macromolecular compositions comprising indene-derivatives, preparation thereof, and use thereof
申请人:Stichting voor de Technische Wetenschappen
公开号:US20200368721A1
公开(公告)日:2020-11-26
The present invention relates to a method for preparing a macromolecular composition comprising indene-derivatives. The invention also relates to the macromolecular compositions per se, and to methods of using the macromolecular compositions. The macromolecular compositions are useful for undergoing subsequent reactions with small molecules.
Methylene amine substituted arylindenopyrimidines as potent adenosine A2A/A1 antagonists
作者:Brian C. Shook、Stefanie Rassnick、Daniel Hall、Kenneth C. Rupert、Geoffrey R. Heintzelman、Kristen Hansen、Devraj Chakravarty、James L. Bullington、Robert H. Scannevin、Brian Magliaro、Lori Westover、Karen Carroll、Lisa Lampron、Ronald Russell、Shawn Branum、Kenneth Wells、Sandra Damon、Scott Youells、Xun Li、Mel Osbourne、Keith Demarest、Yuting Tang、Kenneth Rhodes、Paul F. Jackson
DOI:10.1016/j.bmcl.2010.03.042
日期:2010.5
A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally. (C) 2010 Elsevier Ltd. All rights reserved.