Zobrazeno 1 - 6
of 6
pro vyhledávání: '"William Frietze"'
Autor:
Gaochao Tian, William Frietze, Michael W. Wood, Christopher R. Holmquist, Todd Andrew Brugel, William E. Palmer, Hui Xiong, Deidre E. Wilkins, Glen Ernst, William Potts, Lindsay Hinkley, Janet Marie Forst, Xia Wang, Jeffrey S. Albert, Cristobal Alhambra, Gary Steelman, Jeffrey G. Varnes, Gerald Jonak, Don Andisik, Bruce Dembofsky, Chris Allan Veale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1043-1049
A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the natur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc9dfd0d0aa8815e2e21d0c94b006632
https://doi.org/10.1016/j.bmcl.2018.02.029
https://doi.org/10.1016/j.bmcl.2018.02.029
Autor:
Jason Boer, William Frietze, Andrew P. Combs, Jack G. Shi, Frank M Nedza, Ruth Young-Sciame, Swamy Yeleswaram, Sharon Diamond, Fiona Lee, Kevin Bowman, Laurine G. Galya, Xiaoqing Yang
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 44(10)
Epacadostat (EPA, INCB024360) is a first-in-class, orally active, investigational drug targeting the enzyme indoleamine 2,3-dioxygenase 1 (IDO1). In Phase I studies, EPA has demonstrated promising clinical activity when used in combination with check
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02e17ee2a8873cce1fba23b5b5fb5871
https://pubmed.ncbi.nlm.nih.gov/27457784
https://pubmed.ncbi.nlm.nih.gov/27457784
Autor:
William Frietze, Jeffrey S. Albert, Lindsay Hinkley, William E. Palmer, Hui Xiong, Donald Andisik, Jeffrey G. Varnes, Glen Ernst, Chris Allan Veale
Publikováno v:
Tetrahedron Letters. 51:6741-6744
An efficient synthetic route based on generation and subsequent electrophilic reaction of a Boc-protected azabicyclo[2.2.1]heptane anion to prepare a potent GlyT1 uptake inhibitor (1) is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::755b63efa5db4f1809f96e8397cf4174
https://doi.org/10.1016/j.tetlet.2010.10.079
https://doi.org/10.1016/j.tetlet.2010.10.079
Autor:
William E. Palmer, Steven Wesolowski, James M. Hulsizer, Jay Liu, Megan M. King, Khanh Bui, John P. McCauley, Thomas J. Hudzik, Valerie Hoesch, Kelly Brush, Xia Wang, Donald Andisik, Cathy Dantzman, William Frietze, Glen Ernst, Kenneth Doring
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(2)
A novel series of piperazine derivatives exhibits sub-nanomolar binding and enhanced subtype selectivity as δ-opioid agonists. The synthesis and SAR are described as well as the application of computational models to improve in vitro ADME and safety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::89dd2d1268775920db400faed500817f
https://pubmed.ncbi.nlm.nih.gov/22197139
https://pubmed.ncbi.nlm.nih.gov/22197139
Autor:
William Frietze, Guyanand Singh, Randall B. Murphy, George Stoupakis, David I. Schuster, George Lem, George K. Ehrlich, Yan Ping Pan, Bing Cai
Publikováno v:
Journal of Medicinal Chemistry. 36:3923-3928
A series of N-(1-arylpropionyl)-4-aryl-1,2,3,6-tetrahydropyridines, prepared by simple Mannich condensations, have been found by radioligand binding assays to have moderate to high affinity (IC50 0.5-500 nM) for bovine cerebellar sigma receptor/bindi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76c5b2730167c178112b83263afdd43c
https://doi.org/10.1021/jm00076a021
https://doi.org/10.1021/jm00076a021
Autor:
Khojasteh, S. Cyrus1 (AUTHOR) pars@gene.com, Rietjens, Ivonne M. C. M.2 (AUTHOR), Dalvie, Deepak3 (AUTHOR), Miller, Grover4 (AUTHOR), Argikar, Upendra A. (AUTHOR), Dumouchel, Jennifer L. (AUTHOR), Dunne, Christine E. (AUTHOR), Saran, Chitra (AUTHOR), Cirello, Amanda L. (AUTHOR), Gunduz, Mithat (AUTHOR), Dekker, Stefan J. (AUTHOR), Zhang, Yongjie (AUTHOR), Chris Vos, J. (AUTHOR), Vermeulen, Nico P. E. (AUTHOR), Commandeur, Jan N. M. (AUTHOR), Scian, Michele (AUTHOR), Guttman, Miklos (AUTHOR), Bouldin, Samantha D. (AUTHOR), Outten, Caryn E. (AUTHOR), Atkins, William M. (AUTHOR)
Publikováno v:
Drug Metabolism Reviews. Aug2017, Vol. 49 Issue 3, p285-317. 33p.