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- | MK 8876 / Merck (MSD), islatravir (MK-8591) / Merck (MSD)
Journal: Cocrystal Synthesis through Crystal Structure Prediction. (Pubmed Central) - Jun 6, 2023
Computational finite-temperature corrections enabled determination of relative crystallization propensities of the triol-DABCO cocrystals with different stoichiometries and prediction of the triol-l-proline polymorphs in the free-energy landscape. The triol-l-proline cocrystal was obtained during subsequent targeted cocrystallization experiments and was found to exhibit an improved melting point and deliquescence behavior over the triol-free acid, which could be considered as an alternative solid form in the synthesis of islatravir.
- | MK 8876 / Merck (MSD)
Journal: Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B. (Pubmed Central) - Apr 1, 2021
This strategic approach demonstrated that, even within limited reaction scope, multi-step parallel libraries could provide access to more complex chemical space. This expedient access facilitates diverse, purpose-driven optimization of SAR and physicochemical properties.
- | MK 8876 / Merck (MSD)
Journal: Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase. (Pubmed Central) - Aug 2, 2020
Similar to clinical developmental compound MK-8876, N-linked (compounds 1 and 2) and C-linked (compounds 3 and 4) tetracyclic structures maintained broad spectrum anti-replicon potency profiles and demonstrated moderate to excellent oral bioavailability and pharmacokinetic parameters across the three preclinical animal species. To better understand the importance of tetracyclic structures related to pan genotypic potency profiles especially against clinically relevant GT1a variants, the teracycles with different ring size were prepared and in vitro evaluations suggested compounds with six number ring have better overall potency profiles.
- MK 8876 / Merck (MSD)
Enrollment change: Safety, Pharmacokinetics, and Pharmacodynamics of MK-8876 in Participants With Hepatitis C Infection (MK-8876-003) (clinicaltrials.gov) - May 26, 2014
P1, N=9, Completed, Sponsor: Merck Sharp & Dohme Corp.
To better understand the importance of tetracyclic structures related to pan genotypic potency profiles especially against clinically relevant GT1a variants, the teracycles with different ring size were prepared and in vitro evaluations suggested compounds with six number ring have better overall potency profiles. N=50 --> 9
- MK 8876 / Merck (MSD)
Trial completion: Safety, Pharmacokinetics, and Pharmacodynamics of MK-8876 in Participants With Hepatitis C Infection (MK-8876-003) (clinicaltrials.gov) - May 26, 2014
P1, N=9, Completed, Sponsor: Merck Sharp & Dohme Corp.
N=50 --> 9 Active, not recruiting --> Completed
- MK 8876 / Merck (MSD)
Enrollment closed: Safety, Pharmacokinetics, and Pharmacodynamics of MK-8876 in Participants With Hepatitis C Infection (MK-8876-003) (clinicaltrials.gov) - Apr 21, 2014
P1, N=50, Active, not recruiting, Sponsor: Merck Sharp & Dohme Corp.
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- | MK 8876 / Merck (MSD)
New P1 trial: Safety, Pharmacokinetics, and Pharmacodynamics of MK-8876 in Participants With Hepatitis C Infection (MK-8876-003) (clinicaltrials.gov) - Aug 26, 2013
P1, N=50, Active, not recruiting, Sponsor: Merck Sharp & Dohme Corp.