532934-95-5Relevant articles and documents
UREA DERIVATIVES AS PYRUVATE KINASE ACTIVATORS
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Paragraph 483-485, (2022/02/15)
The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia.
Prodrug Approach toward the Development of a PET Radioligand for Imaging the GluN2A Subunits of the NMDA Receptor
Gruber, Stefan,Waser, Valérie,Thiel, Zacharias,Ametamey, Simon M.
supporting information, p. 4584 - 4587 (2021/06/28)
A straightforward synthesis of a fluorine-18-labeled prodrug of AFA233 is reported. The key step in the preparation of [18F]AFA233-prodrug is the selective deprotection of the tert-butyl protection groups of the quinoxalinedione moiety without cleavage of the tert-butyl-S-acyl-2-thioethyl protection groups on the phosphate esters. In addition, the preparation of the nonradioactive prodrug reference compound of AFA233 is reported.
TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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Page/Page column 58, (2013/11/05)
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as m PGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
FUSED PYRAZINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 70-71, (2010/06/11)
A series of quinoxaline derivatives, and analogues thereof, which are functionalised further by a substituted phenyl or pyridinyl moiety, being selective inhibitors of PO kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
Substituted Heterocyclic Ethers and Their Use in CNS Disorders
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Page/Page column 49, (2009/01/24)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
The nitration of 8-methylquinoxalines in mixed acid
Marterer, Wolfgang,Prikoszovich, Walter,Wiss, Jacques,Prashad, Mahavir
, p. 318 - 323 (2013/09/06)
8-Methylquinoxalines are nitrated surprisingly efficiently at C-5 following a simple nitration protocol with mixed acid at 40-50°C. The implications of halogen functionalisation at C-6 and modification of the mixed acid conditions on the relative rates of conversion and process safety are discussed. Competing side reactions for 6-halo-8-methylquinoxalines involve hydrolysis at C-6 and halogenation at C-7 or C-5.