- PEPTIDYLARGININE DEIMINASES (PAD) INHIBITORS
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The present invention relates to compounds of the formula (I): as inhibitors of peptidylarginine deiminases (PADs). It also concerns their use in therapy, particularly in the prophylaxis or treatment of neural injury, and other conditions including cancer, multiple sclerosis, glaucoma, arthritis, rheumatoid arthritis lupus, Alzheimer's disease, and ulcerative colitis.
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Page/Page column 84-85
(2014/12/12)
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- Discovery of phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H- pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance
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Structure-based evolution of the original fragment leads resulted in the identification of 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2- methylmorpholin-4-yl]-1H-pyrimidin-2-one, (S)-21, a potent, selective phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor with favourable in vivo antiplatelet effect. Despite its antiplatelet action, (S)-21 did not significantly increase bleeding time in dogs. Additionally, due to its enhanced selectivity over p110α, (S)-21 did not induce any insulin resistance in rats.
- Giordanetto, Fabrizio,Wallberg, Andreas,Ghosal, Saswati,Iliefski, Tommy,Cassel, Johan,Yuan, Zhong-Qing,Von Wachenfeldt, Henrik,Andersen, Soren M.,Inghardt, Tord,Tunek, Anders,Nylander, Sven
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supporting information
p. 6671 - 6676,6
(2012/12/12)
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- Pteridines. Part XLI. Synthesis and Properties of 6,7,8-Trimethyl-4-thiolumazine
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The first representative of the 8-substituted 4-thiolumazine series has been synthesized.In a sequence of reactions, 4,6-dichloropyrimidin-2-(1H)-one (1) is first converted into 4-chloro-6-(methylamino)pyrimidin-2(1H)-one (6), then the Cl-atom displaced b
- Huebsch, Walter,Pfleiderer, Wolfgang
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p. 738 - 743
(2007/10/02)
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