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Dive into the research topics where Brian P. Stupi is active.

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Featured researches published by Brian P. Stupi.


Bioorganic & Medicinal Chemistry Letters | 2010

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.

Gary D. Probst; Simeon Bowers; Jennifer Sealy; Brian P. Stupi; Darren B. Dressen; Barbara Jagodzinska; Jose Aquino; Andrea Gailunas; Anh P. Truong; Luke Tso; Ying-Zi Xu; Roy K. Hom; Varghese John; Jay S. Tung; Michael A. Pleiss; John A. Tucker; Andrei W. Konradi; Hing L. Sham; Jacek Jagodzinski; Gergely Toth; Eric Brecht; Nanhua Yao; Hu Pan; May Lin; Dean R. Artis; Lany Ruslim; Michael P. Bova; Sukanto Sinha; Ted Yednock; Shawn Gauby

The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-gp liability compared to benzyl amine analog 1.


Bioorganic & Medicinal Chemistry Letters | 2013

Arylsulfonamide pyrimidines as VLA-4 antagonists

Ying-Zi Xu; Andrei W. Konradi; Frederique Bard; Michael S. Dappen; Lilibeth Dofiles; Mark Dreyer; Ian Gallager; Caroline Garrido; Mike Krimm; Zhenmei Liao; Elizabeth Messersmith; Linda Mutter; Michael A. Pleiss; Bhushan Samant; Christopher M. Semko; Jennifer Smith; Frank Stappenbeck; Brian P. Stupi; Chris Vandervert; Brent Welch; Brian Wipke; Ted Yednock

A series of (S)-2-(2-(diethylamino)-5-(N-alkyl-N-sulfonamido)pyrimidin-4-ylamino)-3-(4-(carbamoyloxy)phenyl)propanoic acid is discovered as orally available VLA-4 antagonists. Representative compounds 11b and 11p showed efficacy in multiple in vivo animal models. The in vitro selectivity of 11p is also described.


Archive | 2003

Heterocyclic compounds which inhibit leukocyte adhesion mediated by α4 integrins

Andrei W. Konradi; Christopher M. Semko; Ying-Zi Xu; Frank Stappenbeck; Brian P. Stupi; Jenifer L. Smith; Michael A. Pleiss; Eugene D. Thorsett


Archive | 2003

HETEROCYCLIC COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY &agr 4 INTEGRINS

Andrei W. Konradi; Christopher M. Semko; X U Ying-zi; Frank Stappenbeck; Brian P. Stupi; Jenifer L. Smith; Eugene D. Thorsett; Michael A. Pleiss


Archive | 2005

Compuestos heterociclicos que inhiben la adhesion de leucocitos mediada por integrinas alfa-4.

Andrei W. Konradi; Michael A. Pleiss; Christopher M. Semko; Jenifer L. Smith; Frank Stappenbeck; Brian P. Stupi; Eugene D. Thorsett; Ying-Zi Xu


Archive | 2003

Heterocyclische verbindungen, die die durch alpha4-integrine vermittelte leukozytenadhäsion inhibieren

Andrei W. Konradi; Christopher M. Semko; Ying-Zi Xu; Frank Stappenbeck; Brian P. Stupi; Jenifer L. Smith; Eugene D. Thorsett; Michael A. Pleiss


Archive | 2003

Heterocyclische verbindungen, die die durch alpha4-integrine vermittelte leukozytenadhäsion inhibieren Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins

Andrei W. Konradi; Christopher M. Semko; Ying-Zi Xu; Frank Stappenbeck; Brian P. Stupi; Jenifer L. Smith; Eugene D. Thorsett; Michael A. Pleiss


Archive | 2003

Heteroaryl compounds to inhibit mediated by alpha-4-integrin leukocyte adhesion

Andrei W. Konradi; Christopher M. Semko; Ying-Zi Xu; Frank Stappenbeck; Brian P. Stupi; Jenifer L. Smith; Eugene D. Thorsett; Michael A. Pleiss


Archive | 2003

Heteroaryl-verbindungen zur hemmung der durch alpha-4-integrine vermittelten leukozytenadhäsion

Andrei W. Konradi; Michael A. Pleiss; Christopher M. Semko; Jenifer L. Smith; Frank Stappenbeck; Brian P. Stupi; Eugene D. Thorsett; Ying-Zi Xu


Archive | 2003

Heteroaryl-verbindungen zur hemmung der durch alpha-4-integrine vermittelten leukozytenadhäsion Heteroaryl compounds for inhibition by alpha 4 integrins mediated leukocyte adhesion

Andrei W. Konradi; Christopher M. Semko; Ying-Zi Xu; Frank Stappenbeck; Brian P. Stupi; Jenifer L. Smith; Eugene D. Thorsett; Michael A. Pleiss

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Barbara Jagodzinska

Buck Institute for Research on Aging

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Gary D. Probst

Millennium Pharmaceuticals

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Hing L. Sham

Thermo Fisher Scientific

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