Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
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Paragraph 0373
(2017/11/06)
HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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(2016/05/19)
Convenient synthesis of 2-substituted 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones
A new synthetic route was elaborated at our laboratory providing a convenient access to 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones (diazaoxindoles), a compound family of biological relevance. Treatment of the easily available ethyl 2-(4-chloropyrimidin-5-yl)acetate derivatives with ammonia afforded the corresponding 2-(4-aminopyrimidin-5-yl)acetamides, which were finally cyclized to the target compounds.
Kókai, Eszter,Nagy, József,Tóth, Tünde,Kupai, József,Huszthy, Péter,Simig, Gyula,Volk, Balázs
p. 767 - 773
(2016/03/23)
5,7-DIHYDRO-6H-PYRROLO[2,3-D]PYRIMIDIN-6-ONE DERIVATIVES FOR MARK INHIBITION
Compounds of formula I: are potent and selective inhibitors of microtubule affinity regulating kinase (MARK), and hence find use in treatment of Alzheimer's disease and other conditions associated with hyperphosphorylation of tau.
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(2010/01/07)
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