1439900-56-7Relevant articles and documents
A Chemoenzymatic Synthesis of the (RP)-Isomer of the Antiviral Prodrug Remdesivir
Bigley, Andrew N.,Narindoshvili, Tamari,Raushel, Frank M.
, p. 3038 - 3043 (2020)
The COVID-19 pandemic threatens to overwhelm healthcare systems around the world. The only current FDA-approved treatment, which directly targets the virus, is the ProTide prodrug remdesivir. In its activated form, remdesivir prevents viral replication by inhibiting the essential RNA-dependent RNA polymerase. Like other ProTide prodrugs, remdesivir contains a chiral phosphorus center. The initial selection of the (SP)-diastereomer for remdesivir was reportedly due to the difficulty in producing the pure (RP)-diastereomer of the required precursor. However, the two currently known enzymes responsible for the initial activation step of remdesivir are each stereoselective and show differential tissue distribution. Given the ability of the COVID-19 virus to infect a wide array of tissue types, inclusion of the (RP)-diastereomer may be of clinical significance. To help overcome the challenge of obtaining the pure (RP)-diastereomer of remdesivir, we have developed a novel chemoenzymatic strategy that utilizes a stereoselective variant of the phosphotriesterase from Pseudomonas diminuta to enable the facile isolation of the pure (RP)-diastereomer of the chiral precursor for the chemical synthesis of the (RP)-diastereomer of remdesivir.
Substituted N4-hydroxycytidine derivatives and prodrug thereof for anti-novel coronavirus therapy
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Paragraph 0237-0240, (2020/08/26)
The invention relates to a substituted N4-hydroxycytidine derivative with a structure as shown in a formula I, a prodrug and a pharmaceutical composition thereof, and a method of using the compositionfor the treatment of viral infections. The structure of
PYRROLO[1,2-f][1,2,4]TRIAZINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS
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Paragraph 0451-0455, (2015/05/26)
Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.