Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Frederick R. Nelson"'
Autor:
Marisa O. Rhiner, Thanh Blade, Eric Verdin, Scott Mills, Andrey I. Nikiforov, Frederick R. Nelson, Nancy Higley, Brianna J. Stubbs, John C. Newman, Xu Yufei, Jennifer A. Thomas
Publikováno v:
Food and Chemical Toxicology. 147:111859
A novel ketone ester, bis hexanoyl (R)-1,3-butanediol (BH-BD), has been developed as a means to elevate blood ketones, for use as an energy substrate and a signaling metabolite. The metabolism of BH-BD and its effects on blood beta-hydroxybutyrate (B
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::378e13ead06acdfbbd73e42099196dee
https://doi.org/10.1016/j.fct.2020.111859
https://doi.org/10.1016/j.fct.2020.111859
Autor:
Robin J. Kleiman, Christopher J. Schmidt, Michael L. Corman, Patrick Robert Verhoest, Christopher John Helal, Jamison B. Tuttle, Shenpinq Liu, Michelle Vanase-Frawley, Frank S. Menniti, Spiros Liras, Karen J. Coffman, Kari R. Fonseca, Michelle Marie Claffey, Caroline Proulx-Lafrance, Xinjun Hou, Frederick R. Nelson
Publikováno v:
Journal of Medicinal Chemistry. 55:9045-9054
6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943) is a novel PDE9A inhibitor identified using parallel synthetic chemistry and structure-based drug de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dc5bd4ed268fb9667a4ede29022a7fb5
https://doi.org/10.1021/jm3007799
https://doi.org/10.1021/jm3007799
Autor:
Rama Y. Chandrasekaran, Jiri Aubrecht, Frederick R. Nelson, Linda A. Chatman, Hans Rollema, Frank M. Nedza, John M. Marcek, Philip A. Iredale, Jennifer B. Munzner, Betty Pettersen, Raggon Jeffrey W, David M. Rubitski, Julie Cianfrogna, Larry C. James, Karen W. Cook, Michael J. Banker, Diane F. Wong, Anne W. Schmidt, Michael Homiski, Howard Harry R, Daniel J. Lettiere, Butler Todd W, Scot Richard Mente, Jody Freeman, Travis T. Wager, Douglas K. Spracklin
Publikováno v:
Journal of Medicinal Chemistry. 54:7602-7620
The discovery of two histamine H3 antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success in iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7c253ef2a0b55c8bf1f6522eccc0c6ed
https://doi.org/10.1021/jm200939b
https://doi.org/10.1021/jm200939b
Autor:
Carol B. Fox, Spiros Liras, Douglas S. Chapin, Frederick R. Nelson, Jayvardhan Pandit, Xinjun Hou, Christopher John Helal, John M. Humphrey, Christopher J. Schmidt, Thomas Allen Chappie, Kimberly F. Fennell, Frank S. Menniti, Zhijun Kang, Julia Cianfrogna, Judith A. Siuciak, Mary C. MacDougall, Kari R. Fonseca, Rebecca E. O’Connor, Lois K. Chenard, Eric S. Marr, Lorraine A. Lebel, Laura McDowell, Robert D. Williams
Publikováno v:
Journal of Medicinal Chemistry. 54:4536-4547
Utilizing structure-based virtual library design and scoring, a novel chimeric series of phosphodiesterase 10A (PDE10A) inhibitors was discovered by synergizing binding site interactions and ADME properties of two chemotypes. Virtual libraries were d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9470cb95f70a63260200b088b6fe12a3
https://doi.org/10.1021/jm2001508
https://doi.org/10.1021/jm2001508
Publikováno v:
Journal of Veterinary Pharmacology and Therapeutics. 33:453-460
Mealey, K.L., Waiting, D., Raunig, D.L., Schmidt, K.R., Nelson, F.R. Oral bioavailability of P-glycoprotein substrate drugs do not differ between ABCB1-1Δ and ABCB1 wild type dogs. J. vet. Pharmacol. Therap. 33, 453–460. Previous studies have indi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9b3e1b5de80da911c279fe391e7146cc
https://doi.org/10.1111/j.1365-2885.2010.01170.x
https://doi.org/10.1111/j.1365-2885.2010.01170.x
Autor:
Christopher J. Schmidt, Frank S. Menniti, Kari R. Fonseca, Spiros Liras, Robert D. Williams, Michelle Vanase-Frawley, Frederick R. Nelson, Christopher John Helal, Eric S. Marr, Patrick Robert Verhoest, Xinjun Hou, Shenping Liu, Lois K. Chenard, Michael L. Corman, Anne W. Schmidt, Caroline Proulx-Lafrance, Robin J. Kleiman
Publikováno v:
Journal of Medicinal Chemistry. 52:7946-7949
By use of chemical enablement and prospective design, a novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of producing in vivo elevations of brain cGMP.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36f96537fb0d514fc2467932c7482e6c
https://doi.org/10.1021/jm9015334
https://doi.org/10.1021/jm9015334
Autor:
John F. Harms, Christopher J. Schmidt, Anne W. Schmidt, Caroline Proulx-Lafrance, Eric S. Marr, Michael L. Corman, Kari R. Fonseca, Frank S. Menniti, Douglas S. Chapin, Rebecca E. O’Connor, Jayvardhan Pandit, Xinjun Hou, Judith A. Suiciak, Spiros Liras, Frederick R. Nelson, Patrick Robert Verhoest
Publikováno v:
Journal of Medicinal Chemistry. 52:5188-5196
By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique "selectivity pocket" for PDE10A inhibitors, and interaction
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a341156c8abee650cd13eb030ec9826b
https://doi.org/10.1021/jm900521k
https://doi.org/10.1021/jm900521k
Publikováno v:
Drug Metabolism and Disposition. 37:946-955
The role of breast cancer resistance protein (Bcrp) and the combined activities of Bcrp and P-glycoprotein (P-gp, Mdr1a/1b) in limiting the brain penetration of drugs at the blood-brain barrier (BBB) were investigated using wild-type FVB, Mdr1a/1b(-/
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8630730ade3fbc27cedd4f50adc7eb3
https://doi.org/10.1124/dmd.108.024489
https://doi.org/10.1124/dmd.108.024489
Autor:
Zhijun Kang, Christopher J. Schmidt, Mark W. Bundesmann, Stanley Jung, Patrick Robert Verhoest, Frank S. Menniti, Xinjun Hou, Michelle Vanase-Frawley, Kristina S. Fors, Mary MacDougall-Murphy, Frederick R. Nelson, Kari R. Fonseca, Laura McDowell, Shenping Lui, Jiaying Zhong, Michelle Marie Claffey, Spiros Liras, Rebecca E. O’Connor, Mihály Hajós, William E. Hoffman, Stacey L. Becker, Anne W. Schmidt, Robin J. Kleiman, Christopher John Helal
Publikováno v:
Journal of medicinal chemistry. 55(21)
Phosphodiesterase 9A inhibitors have shown activity in preclinical models of cognition with potential application as novel therapies for treating Alzheimer's disease. Our clinical candidate, PF-04447943 (2), demonstrated acceptable CNS permeability i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed10b9b6a81fdbb8d4255c6f8a9d1925
https://pubmed.ncbi.nlm.nih.gov/23025719
https://pubmed.ncbi.nlm.nih.gov/23025719
Autor:
Travis T, Wager, Betty A, Pettersen, Anne W, Schmidt, Douglas K, Spracklin, Scot, Mente, Todd W, Butler, Harry, Howard, Daniel J, Lettiere, David M, Rubitski, Diane F, Wong, Frank M, Nedza, Frederick R, Nelson, Hans, Rollema, Jeffrey W, Raggon, Jiri, Aubrecht, Jody K, Freeman, John M, Marcek, Julie, Cianfrogna, Karen W, Cook, Larry C, James, Linda A, Chatman, Philip A, Iredale, Michael J, Banker, Michael L, Homiski, Jennifer B, Munzner, Rama Y, Chandrasekaran
Publikováno v:
Journal of medicinal chemistry. 54(21)
The discovery of two histamine H(3) antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success in id
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::2437f9ba9156d813302f64ee16a8582b
https://pubmed.ncbi.nlm.nih.gov/21928839
https://pubmed.ncbi.nlm.nih.gov/21928839