Výsledky vyhledávání - "Mimi L. Quan"

Akademický článek

Improved efficacy/safety profile of factor XIa inhibitor BMS‐724296 versus factor Xa inhibitor apixaban and thrombin inhibitor dabigatran in cynomolgus monkeys

Autor: Pancras C. Wong, Mimi L. Quan

Publikováno v: Research and Practice in Thrombosis and Haemostasis, Vol 5, Iss 4, Pp n/a-n/a (2021)

Abstract Background Inhibition of activated factor XI (FXIa) is a promising antithrombotic drug target. BMS‐724296 is a selective, reversible, small‐molecule inhibitor of human FXIa (Ki 0.3 nM). Objectives This study assessed effects of BMS‐724

Externí odkaz: https://doaj.org/article/e78756cbf8ac470c9d57790955d6d9aa

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Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies

Publikováno v: Bioorganicmedicinal chemistry letters. 30(21)

Structure-activity relationship optimization on a series of phenylpyrazole amides led to the identification of a dual ROCK1 and ROCK2 inhibitor (25) which demonstrated good potency, kinome selectivity and favorable pharmacokinetic profiles. Compound

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::995bf0c5f6f2e8dbdc6c12fb55d1327a
https://pubmed.ncbi.nlm.nih.gov/32798651

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Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors

Autor: Jodi K. Muckelbauer, Mimi L. Quan, Zilun Hu, Cailan Wang, Nathan L. Cheadle, Ruth R. Wexler, Songmei Xu, Doree F. Sitkoff, Leonard P. Adam

Publikováno v: Bioorganicmedicinal chemistry letters. 30(21)

A novel series of 5H-chromeno[3,4-c]pyridine, 6H-isochromeno[3,4-c]pyridine and 6H-isochromeno[4,3-d]pyrimidine derivatives as dual ROCK1 and ROCK2 inhibitors is described. Optimization led to compounds with sub-nanomolar inhibitory affinity for both

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a771617c75ca86b6686207a9e2540a42
https://pubmed.ncbi.nlm.nih.gov/32805407

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Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 27:3833-3839

Optimization of macrocyclic inhibitors of FXIa is described which focused on modifications to both the macrocyclic linker and the P1 group. Increases in potency were discovered through interactions with a key hydrophobic region near the S1 prime pock

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3f2d0a4ceae94a72657bf9a2edc652c
https://doi.org/10.1016/j.bmcl.2017.06.058

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Factor XIa Inhibitors as New Anticoagulants

Autor: Ruth R. Wexler, Donald J. P. Pinto, Mimi L. Quan, Joseph M. Luettgen, William R. Ewing, Joanne M. Smallheer, Dietmar A. Seiffert, Karen A. Rossi

Publikováno v: Journal of medicinal chemistry. 61(17)

With the introduction of thrombin and factor Xa inhibitors to the oral anticoagulant market, significant improvements in both efficacy and safety have been achieved. Early clinical and preclinical data suggest that inhibitors of factor XIa can provid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24c4691d084872e14b97277c8e4f4d0a
https://pubmed.ncbi.nlm.nih.gov/29775297

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Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors

Autor: Wei Han, Ruth R. Wexler, Yiming Wu, Cailan Wang, Joseph M. Luettgen, Zilun Hu, Karen A. Rossi, Jeffrey M. Bozarth, Steven Sheriff, Joseph E. Myers, Dietmar A. Seiffert, Mimi L. Quan

Publikováno v: Bioorganicmedicinal chemistry letters. 28(6)

Pyridazine and pyridazinone derivatives were designed and synthesized as coagulation factor XIa inhibitors. Potent and selective inhibitors with single digit nanomolar affinity for factor XIa were discovered. Selected inhibitors demonstrated moderate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::634978adce71914a42a7f5d8e2dbc094
https://pubmed.ncbi.nlm.nih.gov/29501396

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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25(7):1635-1642

Compound 2 was previously identified as a potent inhibitor of factor XIa lacking oral bioavailability. A structure-based approach was used to design analogs of 2 with novel P1 moieties with good selectivity profiles and oral bioavailability. Further

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d3270445178be90c7e69e6738db98ec

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Pyridine and pyridinone-based factor XIa inhibitors

Autor: Todd J. Friends, Frank A. Barbera, Vidhyashankar Ramamurthy, Dietmar A. Seiffert, Alan R. Rendina, Tianan Fang, Karen A. Rossi, James R. Corte, Jeffrey M. Bozarth, Mimi L. Quan, Paul E. Morin, Jon J. Hangeland, Joseph M. Luettgen, Anzhi Wei, Ruth R. Wexler

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:925-930

The structure-activity relationships (SAR) of six-membered ring replacements for the imidazole ring scaffold is described. This work led to the discovery of the potent and selective pyridine (S)-23 and pyridinone (±)-24 factor XIa inhibitors. SAR an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9087a62525e5bf9f489209c37ee40dc6
https://doi.org/10.1016/j.bmcl.2014.12.050

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