265108-36-9Relevant articles and documents
Structure-Guided Design of Potent Inhibitors of SARS-CoV-2 3CL Protease: Structural, Biochemical, and Cell-Based Studies
Dampalla, Chamandi S.,Rathnayake, Athri D.,Perera, Krishani Dinali,Jesri, Abdul-Rahman M.,Nguyen, Harry Nhat,Miller, Matthew J.,Thurman, Hayden A.,Zheng, Jian,Kashipathy, Maithri M.,Battaile, Kevin P.,Lovell, Scott,Perlman, Stanley,Kim, Yunjeong,Groutas, William C.,Chang, Kyeong-Ok
, p. 17846 - 17865 (2021/12/13)
The COVID-19 pandemic is having a major impact on public health worldwide, and there is an urgent need for the creation of an armamentarium of effective therapeutics, including vaccines, biologics, and small-molecule therapeutics, to combat SARS-CoV-2 and emerging variants. Inspection of the virus life cycle reveals multiple viral- and host-based choke points that can be exploited to combat the virus. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention, and the design of inhibitors of the protease may lead to the emergence of effective SARS-CoV-2-specific antivirals. We describe herein the results of our studies related to the application of X-ray crystallography, the Thorpe–Ingold effect, deuteration, and stereochemistry in the design of highly potent and nontoxic inhibitors of SARS-CoV-2 3CLpro.
COMPOUNDS AND METHODS FOR TREATING OXALATE-RELATED DISEASES
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Paragraph 0795, (2021/02/26)
Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject are also provided.
CRYSTAL OF TRICYCLIC COMPOUND
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, (2020/08/25)
The present application relates to a crystal of a tricyclic compound, in particular to a crystal of (S)-8-(4,4-difluorocyclohexyl)-8H-thieno[3,4]pyrrolo[1,5-a]imidazole, a preparation method therefor, a crystal composition and a pharmaceutical composition thereof and the use thereof. The X-ray powder diffraction spectrum of the crystal of the compound of formula I in the present application, represented by a 2θ value, has a diffraction peak at about 11.49°, 15.05°, 20.14°, 21.53° or 21.79°. The crystal of the compound of formula I in the present application has excellent physical properties, high safety and metabolic stability, and has a good inhibitory effect on IDO and a high medicinal value.