Dale A. Rudolph
Janssen Pharmaceutica
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Publication
Featured researches published by Dale A. Rudolph.
Bioorganic & Medicinal Chemistry Letters | 2015
Dale A. Rudolph; Jesús Alcázar; Michael K. Ameriks; Ana Belen Anton; Hong Ao; Pascal Bonaventure; Nicholas I. Carruthers; Christa C. Chrovian; Meri De Angelis; Brian Lord; Jason C. Rech; Qi Wang; Anindya Bhattacharya; José Ignacio Andrés; Michael A. Letavic
The optimization efforts that led to a novel series of methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones that are potent rat and human P2X7 antagonists are described. These efforts resulted in the discovery of compounds with good drug-like properties that are capable of high P2X7 receptor occupancy in rat following oral administration, including compounds 7n (P2X7 IC50 = 7.7 nM) and 7u (P2X7 IC50 =7 .7 nM). These compounds are expected to be useful tools for characterizing the effects of P2X7 antagonism in models of depression and epilepsy, and several of the compounds prepared are candidates for effective P2X7 PET tracers.
Archive | 2004
Nicholas I. Carruthers; Wenying Chai; Xiaohu Deng; Curt A. Dvorak; Annette K. Kwok; Jimmy T. Liang; Neelakandha S. Mani; Dale A. Rudolph; Victoria D. Wong
Archive | 2010
Wenying Chai; Michael A. Letavic; Kiev S. Ly; Daniel J. Pippel; Dale A. Rudolph; Kathleen C. Sappey; Chandravadan R. Shah; Brock T. Shireman; Akinola Soyode-Johnson; Emily M. Stocking; Devin M. Swanson
Archive | 2006
Curt A. Dvorak; Dale A. Rudolph; Brock T. Shireman
Archive | 2010
Bryan James Branstetter; Michael A. Letavic; Kiev S. Ly; Dale A. Rudolph; Chandravadan R. Shah; Brock T. Shireman
Archive | 2001
Wenying Chai; Annette K. Kwok; Xiaobing Li; Dale A. Rudolph
Archive | 2006
Pascal Bonaventure; Nicholas I. Carruthers; Wenying Chai; Curt A. Dvorak; Jill A. Jablonowski; Dale A. Rudolph; Mark Seierstad; Chandravadan R. Shah; Devin M. Swanson; Victoria D. Wong
Archive | 2006
Pascal Bonaventure; Christine Dugovic; Curt A. Dvorak; Dale A. Rudolph; Jonathan Shelton
Archive | 2014
Michael A. Letavic; Dale A. Rudolph
Archive | 2001
Wenying Chai; Annette K. Kwok; Xiaobing Li; Dale A. Rudolph