Aminomethyl substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists

Brian C. Shook; Devraj Charavarty; J. Kent Barbay; Aihua Wang; Kristi Leonard; Vernon Alford; Mark Powell; Derek A. Beauchamp; Stefanie Rassnick; Robert Scannevin; Karen Carroll; Nathaniel Wallace; Jeffrey Crooke; Mark Ault; Lisa Lampron; Lori Westover; Kenneth Rhodes; Paul F. Jackson

doi:10.1039/C1MD00082A

Aminomethyl substituted thieno[2,3-d]pyrimidines as adenosine A_2A receptor antagonists

Brian C. Shook,*^a Devraj Charavarty,^a J. Kent Barbay,^a Aihua Wang,^a Kristi Leonard,^a Vernon Alford,^a Mark Powell,^a Derek A. Beauchamp,^a Stefanie Rassnick,^b Robert Scannevin,^b Karen Carroll,^b Nathaniel Wallace,^b Jeffrey Crooke,^b Mark Ault,^b Lisa Lampron,^b Lori Westover,^b Kenneth Rhodes^b and Paul F. Jackson^a

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^a Medicinal Chemistry, Johnson & Johnson PRD, Welsh and McKean Roads, P.O. Box 776, Spring House, PA, USA
E-mail: bshook@its.jnj.com
Fax: +1 215-540-4612
Tel: +1 215-628-7047

^b CNS Biology, Johnson & Johnson PRD, Welsh and McKean Roads, P.O. Box 776, Spring House, PA, USA

Abstract

A novel series of aminomethyl substituted thieno[2,3-d]pyrimidines have been identified as adenosine A_2A receptor antagonists. Analogues show excellent in vitro activities and have excellent activity in vivo in mouse models of Parkinson's disease.

MedChemComm

Aminomethyl substituted thieno[2,3-d]pyrimidines as adenosine A_2A receptor antagonists

Abstract

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Aminomethyl substituted thieno[2,3-d]pyrimidines as adenosine A_2A receptor antagonists

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