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Thomas Daniel Aicher
Researcher at Novartis
Publications - 62
Citations - 1540
Thomas Daniel Aicher is an academic researcher from Novartis. The author has contributed to research in topics: Glucokinase & Pyruvate dehydrogenase kinase. The author has an hindex of 21, co-authored 62 publications receiving 1466 citations. Previous affiliations of Thomas Daniel Aicher include Marquette University & Harvard University.
Papers
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Journal ArticleDOI
Total synthesis of halichondrin B and norhalichondrin B
Thomas Daniel Aicher,Keith R. Buszek,Francis G. Fang,Craig J. Forsyth,Sun Ho Jung,Yoshito Kishi,Michael C. Matelich,Paul Michael Scola,Denice M. Spero,Suk Kyoon Yoon +9 more
Journal ArticleDOI
Synthetic studies towards halichondrins
TL;DR: An efficient, stereocontrolled route to construct the polycyclic ring system found at the C.1 −C.15 moiety of halichondrins is reported in this article.
Journal ArticleDOI
Secondary Amides of (R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionic Acid as Inhibitors of Pyruvate Dehydrogenase Kinase
Thomas Daniel Aicher,Robert C. Anderson,Jiaping Gao,Suraj S. Shetty,Gary M. Coppola,James L. Stanton,Douglas C. Knorr,Donald Mark Sperbeck,Leonard J. Brand,Christine C. Vinluan,Emma L. Kaplan,Carol J. Dragland,Tomaselli Hc,A. Islam,R. J. Lozito,Xilin Liu,Wieslawa Maniara,William S. Fillers,Dominick DelGrande,R. E. Walter,William R. Mann +20 more
TL;DR: Methyl substitution of the piperazine at the 2- and 5-positions markedly increased the potency of the lead compound (>1,000-fold) and oral bioavailability of the compounds in this series is good and is optimal when the 4-position of thepiperazine is substituted with an electron-poor benzoyl moiety.
Patent
Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
Thomas Daniel Aicher,Mark Joseph Chicarelli,Ronald Jay Hinklin,Hongqi Tian,Owen Brendan Wallace +4 more
TL;DR: In this article, the authors provided compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1 (HBDE) and a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient.
Journal ArticleDOI
Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.
Gregory Raymond Bebernitz,Thomas Daniel Aicher,James L. Stanton,Jiaping Gao,Suraj S. Shetty,Douglas C. Knorr,Robert J. Strohschein,Jennifer Tan,Leonard J. Brand,Charles Liu,Wei H. Wang,Christine C. Vinluan,Emma L. Kaplan,Carol J. Dragland,Dominick DelGrande,Amin Islam,Robert J. Lozito,Xilin Liu,Wieslawa Maniara,William R. Mann +19 more
TL;DR: Small electron-withdrawing groups on the ortho position of the anilide increased potency 20-40-fold and could be of utility to ameliorate conditions of inappropriate blood lactate elevation.