1637752-28-3Relevant academic research and scientific papers
FLUOROALKYL-OXADIAZOLES AND USES THEREOF
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, (2021/06/26)
Provided herein are compounds identified as inhibitors of HDAC6 activity that can be used to treat various diseases and disorders.
Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion
Cockerill, G. Stuart,Angell, Richard M.,Bedernjak, Alexandre,Chuckowree, Irina,Fraser, Ian,Gascon-Simorte, Jose,Gilman, Morgan S. A.,Good, James A. D.,Harland, Rachel,Johnson, Sara M.,Ludes-Meyers, John H,Littler, Edward,Lumley, James,Lunn, Graham,Mathews, Neil,McLellan, Jason S.,Paradowski, Michael,Peeples, Mark E.,Scott, Claire,Tait, Dereck,Taylor, Geraldine,Thom, Michelle,Thomas, Elaine,Villalonga Barber, Carol,Ward, Simon E.,Watterson, Daniel,Williams, Gareth,Young, Paul,Powell, Kenneth
supporting information, p. 3658 - 3676 (2021/04/12)
RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a physical property directed hit profiling exercise at Reviral. This exercise encompassed collaborations with a number of contract organizations with collaborative medicinal chemistry and virology during the optimization phase in addition to those utilized as the compound proceeded through preclinical and clinical evaluation. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.
SPIRO-INDOLINES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION (RSV)
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Page/Page column 38; 39, (2016/05/02)
Benzimidazoles of formula (I): wherein: one of X and Y is an N atom or a substituted C atom, and the other is CH; L is a single bond, C1-3 alkylene, C2-3 alkenylene or C2-3 alkynylene; R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, 3- to 10-membered cycloalkyl, 5- to 10-membered heterocyclyl or 5- to 12- membered heteroaryl, each of which is unsubstituted or substituted; Z is halo, C1-6 haloalkyl, nitro, -CN, -N(R2)2, -OR2, -SR2, -S(=0)R2, or -S(=0)2R2; each R2 is independently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; and m is 0 or 1; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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, (2015/02/25)
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, W and X are as described herein, compositions including the compounds and methods of using the compounds.
NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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, (2015/02/25)
The invention provides novel compounds having the general formula:(I) wherein R1, R2, R3, R4, W and X are as described herein, compositions including the compounds and methods of using the compounds.
