84892-13-7Relevant academic research and scientific papers
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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, (2020/02/16)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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, (2019/11/04)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as an A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as an A2A receptor antagonist.
Enantioselective Hydrogen Atom Transfer: Discovery of Catalytic Promiscuity in Flavin-Dependent 'Ene'-Reductases
Sandoval, Braddock A.,Meichan, Andrew J.,Hyster, Todd K.
, p. 11313 - 11316 (2017/08/30)
Flavin has long been known to function as a single electron reductant in biological settings, but this reactivity has rarely been observed with flavoproteins used in organic synthesis. Here we describe the discovery of an enantioselective radical dehalogenation pathway for α-bromoesters using flavin-dependent 'ene'-reductases. Mechanistic experiments support the role of flavin hydroquinone as a single electron reductant, flavin semiquinone as the hydrogen atom source, and the enzyme as the source of chirality.
SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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, (2015/06/25)
A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (" cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceuticall acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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, (2011/12/14)
A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I , or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof
The discovery of AZD9164, a novel muscarinic M3 antagonist
Mete, Antonio,Bowers, Keith,Chevalier, Eric,Donald, David K.,Edwards, Helen,Escott, Katherine J.,Ford, Rhonan,Grime, Ken,Millichip, Ian,Teobald, Barry,Russell, Vince
scheme or table, p. 7440 - 7446 (2012/02/04)
The optimization of a new series of muscarinic M3 antagonists is described, leading to the identification of AZD9164 which was progressed into the clinic for evaluation of its potential as a treatment for COPD.
A NOVEL 4-METHYLBENZENESULPHONATE SALT AND A PROCESS FOR PREPARING A PHARMACEUTICAL COMPOSITION COMPRISING THE SALT
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Page/Page column 20-21, (2010/12/29)
The invention provides a 4-methylbenzenesulphonate salt of the muscarinic antagonist (R)- 1-(4-fluorophenethyl)-3-((S)-2-phenyl-2-(piperidin-1 -yl)propanoyloxy)-1- azoniabicyclo[2.2.2]octane and its use in therapy,as well as a process for preparing a pharmaceutical composition comprising the salt and its use in therapy.
Single enantiomer free-radical chemistry - Lewis acid-mediated reductions of racemic halides using chiral non-racemic stannanes
Dakternieks, Dainis,Perchyonok, V. Tamara,Schiesser, Carl H.
, p. 3057 - 3068 (2007/10/03)
Additions of one to two equivalents of Lewis acids that include magnesium salts to free-radical reduction reactions involving ester functionalized radicals and (1R,2S,5R)-menthyldiphenyltin hydride 4, bis((1R,2S,5R)-menthyl) phenyltin hydride 5, tris((1R,
Enantioselectivity of the transfer of hydrogen atoms to acyclic prochiral carbon-centred radicals using chiral tin hydrides
Schwarzkopf, Kay,Blumenstein, Michael,Hayen, Ahlke,Metzger, Jürgen O.
, p. 177 - 181 (2007/10/03)
Racemic α-bromo esters 2 have been reduced via prochiral radicals 5 with low to moderate enantioselectivities using chiral tin hydrides 1 with a stereogenic tin atom containing chiral 2-[(1-dimethylaminoalkyl)phenyl] ligands. The tin hydrides 1 were mixtures of diastereomers. It could be shown that the minor diastereomer of tin hydrides 1a and 1b reacts with good enantioselectivity whereas the major diastereomer reacts almost unselectively. The observed enantioselectivities are also strongly influenced by steric effects of the substituents attached to the radical centre.
Acide 2-fluoro-2-phenyl propanoique: preparation et utilisation comme agent chiral de derivation
Hamman, S.
, p. 225 - 232 (2007/10/02)
The enantiomers of 2-fluoro-2-phenyl propanoic acid have been separated and their absolute configurations determined: the specific rotation of the acid with an R configuration is 20D= -28.5 deg (c=1.5, ethanol).This acid has been
