Výsledky vyhledávání - "Ruth R Wexler"

Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists

Autor: Nicholas R. Wurtz, James A. Johnson, Andrew Viet, Pravin S. Shirude, Vishweshwaraiah Baligar, Sudhakara Madduri, Daniel L. Cheney, Hyunsoo Park, John A. Lupisella, Mei-Yin Hsu, Mojgan Abousleiman, Michael A. Galella, Darpandeep Aulakh, Elizabeth A. Dierks, Ricardo A. Garcia, Jacek Ostrowski, Ellen K. Kick, Ruth R. Wexler

Publikováno v: ACS Med Chem Lett

[Image: see text] Formyl peptide receptor 2 (FPR2) agonists have shown efficacy in inflammatory-driven animal disease models and have the potential to treat a range of diseases. Many reported synthetic agonists contain a phenylurea, which appears to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a365e85b2833ea7dfaf2477aac5a41a
https://doi.org/10.1021/acsmedchemlett.2c00079

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Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits

Autor: Jeffrey M. Bozarth, Pancras C. Wong, Earl J. Crain, William R. Ewing, Joseph M. Luettgen, David A. Gordon, Ruth R. Wexler, Yiming Wu, Dilger Andrew K

Publikováno v: Journal of Thrombosis and Haemostasis. 20:399-408

BACKGROUND Milvexian (BMS-986177/JNJ-70033093) is an orally bioavailable factor XIa (FXIa) inhibitor currently in phase 2 clinical trials. OBJECTIVES To evaluate in vitro properties and in vivo characteristics of milvexian. METHODS In vitro propertie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1676afb5bd0ef4a349d5e7addf749e89
https://doi.org/10.1111/jth.15588

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Identification of a Hydroxypyrimidinone Compound (21) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure

Autor: Wei Meng, Heather Finlay, Claudia Generaux, Chiuwa E. Luk, Tao Wang, Robert Paul Brigance, Joelle M. Onorato, Peter S. Gargalovic, Ruth R. Wexler, William A. Schumacher, Jeffrey S. Bostwick, Zulan Pi, Karen A. Rossi

Publikováno v: Journal of Medicinal Chemistry. 64:18102-18113

This paper describes our continued efforts in the area of small-molecule apelin receptor agonists. Recently disclosed compound 2 showed an acceptable metabolic stability but demonstrated monodemethylation of the dimethoxyphenyl group to generate atro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9f63d50e642c7389207d1baa0094a005
https://doi.org/10.1021/acs.jmedchem.1c01504

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From basic science to life-saving therapy: the rationale, and drug discovery efforts that led to the direct factor Xa inhibitor eliquis

Autor: Ruth R. Wexler, Robert M. Knabb

Publikováno v: Journal of Thrombosis and Thrombolysis. 52:403-407

Over the past few decades, drug discovery directed at the treatment and prevention of thromboembolic diseases has been challenged by the need to balance robust efficacy with improved safety relative to the standard of care. To this end, the most impa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c8cfab2e8f341f1dfe8aff979aa130b1
https://doi.org/10.1007/s11239-021-02529-w

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Design and preparation of N-linked hydroxypyridine-based APJ agonists

Autor: Jeremy M. Richter, J. Alex Bates, Peter Gargalovic, Joelle M. Onorato, Claudia Generaux, Tao Wang, David A. Gordon, Ruth R. Wexler, Heather J. Finlay

Publikováno v: Bioorganicmedicinal chemistry letters. 73

Agonism of the apelin receptor (APJ) has demonstrated beneficial effects in models of heart failure. We have previously disclosed compounds such as 4, which showed good APJ agonist activity but were metabolized to the mono-demethylated, non-interconv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::898309a657734b060ea109a87904cf66
https://pubmed.ncbi.nlm.nih.gov/35817293

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Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists

Autor: William A. Schumacher, Yan He, Peter S. Gargalovic, Tao Wang, Joelle M. Onorato, Ruth R. Wexler, James A. Johnson, Zulan Pi, Claudia Generaux, Wei Meng, Heather Finlay, David A. Gordon, Monique Phillips, Jeffrey S. Bostwick

Publikováno v: ACS Med Chem Lett

[Image: see text] The apelin receptor (APJ) is a significant regulator of cardiovascular function and is involved in heart failure and other cardiovascular diseases. (Pyr(1))apelin-13 is one of the endogenous agonists of the APJ receptor. Administrat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c497839aa78ba246784ea2c27101a0c
https://europepmc.org/articles/PMC8591725/

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