Template-hopping approach leads to potent, selective, and highly soluble bromo and extraterminal domain (BET) second bromodomain (BD2) inhibitors

HE Aylott, SJ Atkinson, P Bamborough… - Journal of Medicinal …, 2021 - ACS Publications
A number of reports have recently been published describing the discovery and optimization
of bromo and extraterminal inhibitors which are selective for the second bromodomain …

Improved Synthesis of a Cyclic Glutamine Analogue Used in Antiviral Agents Targeting 3C and 3CL Proteases Including SARS-CoV-2 Mpro

W Vuong, JC Vederas - The Journal of Organic Chemistry, 2021 - ACS Publications
An intermediate in the synthesis of numerous antiviral protease inhibitors is the glutamine
analogue,(3 S)-pyrrolid-2-one-3-yl-l-alanine. Preparations of compounds based on this …

1, 8-naphthyridinone compounds and uses thereof

SM Pham, J Chen, A Ansari, PS Jadhavar… - US Patent …, 2020 - Google Patents
naphthyridinone compounds as modulators of an adenosine receptor are provided. The
compounds may find use as therapeutic agents for the treatment of diseases mediated …

Heterocyclic compounds as adenosine antagonists

SM Pham, J Chen, A Ansari, PS Jadhavar… - US Patent …, 2021 - Google Patents
Aminopyrazine compounds as modulators of an adenosine receptor are provided. The
compounds may find use as therapeutic agents for the treatment of diseases mediated …

[PDF][PDF] Chemical Synthesis to Understand and Influence Biological Systems: Spin Labels, Drug Development, and Biosynthetic Investigations

W Vuong - 2022 - era.library.ualberta.ca
Spin labels are a useful tool towards the study of protein conformation and enable the
mapping of interactions between specific positions within these systems. Synthetic routes …

Substituted 1, 6-dihydropyridinones and 1, 2-dihydroisoquinolinones as bet inhibitors

SM Pham, S Chakravarty, J Kankanala, J Chen… - US Patent …, 2021 - Google Patents
US11192900B2 - Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as
bet inhibitors - Google Patents US11192900B2 - Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones …

Heterocyclic compounds as BET inhibitors

SM Pham, S Chakravarty, J Kankanala, J Chen… - US Patent …, 2023 - Google Patents
2022-05-03 Assigned to SPARCBIO LLC reassignment SPARCBIO LLC ASSIGNMENT OF
ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: CHAKRAVARTY …

2, 3-dihydrobenzohurans as bromodomain inhibitors

SJ Atkinson, EH Demont, LA Harrison… - US Patent …, 2022 - Google Patents
The genomes of eukaryotic organisms are highly organ-20 ised within the nucleus of the
cell. The long strands of The invention is directed to compounds of formula (I) duplex DNA …

Benzofuran derivatives and their use as bromodomain inhibitors

SJ Atkinson, EH Demont, LA Harrison… - US Patent …, 2022 - Google Patents
US11273146B2 - Benzofuran derivatives and their use as bromodomain inhibitors - Google
Patents US11273146B2 - Benzofuran derivatives and their use as bromodomain inhibitors …

1, 8-naphthyridinone compounds and uses thereof

SM Pham, J Kankanala, PS Jadhavar… - US Patent …, 2022 - Google Patents
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3230277 B1 9/2019 WO2003030909 A1 4/2003 2005047285 Al 5/2005 WO2005040151 A1 …