85620-84-4Relevant academic research and scientific papers
CHOLINE METABOLISM INHIBITORS
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Page/Page column 50; 52-54; 105-107, (2020/07/05)
The present disclosure relates to compounds, compositions and methods for inhibiting choline metabolism, e.g., conversion of choline to trimethylamine. Disclosed herein are compounds, compositions, and methods for inhibiting choline metabolism, e.g., conversion of choline to TMA. Also disclosed herein are compounds, methods and compositions for inhibiting choline metabolism by gut microbiota resulting in reduction in the formation of trimethylamine (TMA) and trimethylamine N-oxide (TMAO).
COMPOUNDS AND COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO NTRK
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Page/Page column 64; 65, (2017/03/14)
This invention relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants.
Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors
Volgraf, Matthew,Chan, Lina,Huestis, Malcolm P.,Purkey, Hans E.,Burkard, Michael,Geck Do, Mary,Harris, Julie,Hunt, Kevin W.,Liu, Xingrong,Lyssikatos, Joseph P.,Rana, Sumeet,Thomas, Allen A.,Vigers, Guy P.A.,Siu, Michael
, p. 2477 - 2480 (2014/05/20)
The development of 1,3,4,4a,5,10a-hexahydropyrano[3,4-b]chromene analogs as BACE1 inhibitors is described. Introduction of the spirocyclic pyranochromene scaffold yielded several advantages over previous generation cores, including increased potency, reduced efflux, and reduced CYP2D6 inhibition. Compound 13 (BACE1 IC50 = 110 nM) demonstrated a reduction in CSF Aβ in wild type rats after a single dose.
Novel olefin-phosphorus hybrid and diene ligands derived from carbohydrates
Grugel, Holger,Minuth, Tobias,Boysen, Mike M. K.
experimental part, p. 3248 - 3258 (2010/11/18)
Starting from readily available monosaccharides d-glucose and d-arabinose, a family of novel chiral diene and olefin-phosphinite hybrid ligands has been designed. These ligands were prepared by attaching phosphinite or allylic donor sites onto unsaturated carbohydrate scaffolds. In rhodium(I)-catalysed conjugate addition of boronic acids to enones, the olefin-phosphinite hybrids gave products in up to 99% ee and above, whereas the dienes only led to modest enantioselectivity. However, by shifting the allylic donor sites from position 4 of the pyranose to the anomeric centre, an unexpected reversal of the stereoinduction process was observed. Georg Thieme Verlag Stuttgart New York.
ENANTIOSPECIFIC TOTAL SYNTHESIS OF PSEUDOMONIC ACIDS FROM ARABINOSE
Fleet, G. W. J.,Gough, M. J.,Shing, T. K. M.
, p. 3661 - 3664 (2007/10/02)
The enantiospecific synthesis of pseudomonic acids from arabinose is described.
ENANTIOSPECIFIC SYNTHESES OF INTERMEDIATES IN THE TOTAL SYNTHESIS OF PSEUDOMONIC ACIDS
Fleet, G. W. J.,Gough, M. J.
, p. 4509 - 4512 (2007/10/02)
Enantiospecific syntheses of 1S,6S-3,7-dioxabicyclonon-4-en-8-one (1) and of the enantiomer (2) from D- and L-arabinose respectively have been achieved by two different routes.The conversion of (1) to 6S-(3R-acetanilido)-3,6-dihydro-2H-pyranyl-N,N-dimethylacetamide (3), a key intermediate in the synthesis of pseudomonic acids, is described.
