Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Benjamin Adam Fish"'
Autor:
Chakrapani Subramanyam, Gregory W. Kauffman, Patrick B. Mullins, Longfei Xie, Stefanus J. Steyn, John M. Humphrey, Eddie Yang, Patrick Robert Verhoest, Beth C. Vetelino, Tuan P. Tran, Butler Todd W, Benjamin Adam Fish, Martin Pettersson, Kelly R. Bales, Antonia F. Stepan, Christopher J. O’Donnell, Cory Michael Stiff, Kathleen M. Wood, Michael Eric Green, Douglas S. Johnson, Leslie R. Pustilnik, Christopher W. am Ende
Publikováno v:
ACS Medicinal Chemistry Letters. 6:596-601
Herein we describe the design and synthesis of a series of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) for Alzheimer's disease (AD) that achieve good alignment of potency, metabolic stability, and low MDR efflux ratios, while also maintai
Autor:
Benjamin Adam Fish, Patrick B. Mullins, Christopher W. am Ende, Thayalan Navaratnam, Tuan P. Tran, Michael Eric Green, Chakrapani Subramanyam, Martin Pettersson, Christopher J. O’Donnell, Kathleen M. Wood, Longfei Xie, Liming Zhang, Douglas S. Johnson, Leslie R. Pustilnik, Kelly R. Bales, Subas M. Sakya, Gregory W. Kauffman, Cory Michael Stiff, Beth C. Vetelino, Ricardo Lira
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2906-2911
We report the discovery and optimization of a novel series of dihydrobenzofuran amides as γ-secretase modulators (GSMs). Strategies for aligning in vitro potency with drug-like physicochemical properties and good microsomal stability while avoiding
Autor:
Christina J. Crump, Suita V. Castro, De-Ming Chau, Kelly R. Bales, Kwangwook Ahn, Yue-Ming Li, Cory Michael Stiff, Natalya Gertsik, Benjamin Adam Fish, Nikolay Pozdnyakov, Douglas S. Johnson
Publikováno v:
ACS Chemical Neuroscience. 2:705-710
Aβ42 is believed to play a causative role in Alzheimer's disease (AD) pathogenesis. γ-Secretase modulators (GSMs) are actively being pursued as potential AD therapeutics because they selectively alter the cleavage site of the amyloid precursor prot
Autor:
Chakrapani Subramanyam, Kelly R. Bales, Thayalan Navaratnam, Gregory W. Kauffman, Cory Michael Stiff, Patrick Robert Verhoest, Benjamin Adam Fish, Beth C. Vetelino, Michael Eric Green, Tuan P. Tran, Longfei Xie, Douglas S. Johnson, Leslie R. Pustilnik, Nikolay Pozdnyakov, Christopher W. am Ende, Kathleen M. Wood, Martin Pettersson, Patrick B. Mullins, Christopher J. O’Donnell, Liming Zhang, Subas M. Sakya
Publikováno v:
Journal of medicinal chemistry. 57(3)
Herein we describe the design and synthesis of a novel series of γ-secretase modulators (GSMs) that incorporates a pyridopiperazine-1,6-dione ring system. To align improved potency with favorable ADME and in vitro safety, we applied prospective phys