Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Freeman, Jennifer C."'
Autor:
Gilbert Diaz, Lee C. Preusser, Ann Mikhail, Christopher A. Ogiela, Lynch John K, Philip R. Kym, Lisa M. Hernández, Dariusz Wodka, Gang Zhao, Doug H. Falls, Eugene N. Bush, James S. Polakowski, Andrew S. Judd, Robin Shapiro, Hing L. Sham, James J. Napier, Christine A. Collins, Kennan C. Marsh, Victoria Knourek-Segel, Glenn A. Reinhart, Thomas J Campbell, Sevan Brodjian, Michael E. Brune, Brian A. Droz, Mathew M. Mulhern, Kathryn Houseman, Regina M. Reilly, Brian D. Dayton, Ryan M. Fryer, James T. Limberis, Rajesh R. Iyengar, Freeman Jennifer C
Publikováno v:
Journal of Medicinal Chemistry. 49:6569-6584
Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to the identification of a chromone-2-carboxamide series as having excellent safety against t
Autor:
Hing L. Sham, Regina M. Reilly, Freeman Jennifer C, Lee C. Preusser, Mathew M. Mulhern, Dariusz Wodka, Kennan C. Marsh, Andrew S. Judd, Jason A. Segreti, Ryan M. Fryer, Rajesh R. Iyengar, Gang Zhao, Lynch John K, Brian D. Dayton, Sevan Brodjian, Anil Vasudevan, Lisa M. Hernández, James J. Napier, Christine A. Collins, Seble Wagaw, Glenn A. Reinhart, Thomas J Campbell, Andrew J. Souers, Ju Gao, James S. Polakowski, Philip R. Kym
Publikováno v:
Journal of Medicinal Chemistry. 49:2339-2352
An inactin-anesthetized rat cardiovascular (CV) assay was employed in a screening mode to triage multiple classes of melanin-concentrating hormone receptor 1 (MCHr1) antagonists. Lead identification was based on a compound profile producing high drug
Autor:
Christine A. Collins, Victoria Knourek-Segel, Philip R. Kym, Dariusz Wodka, Hing L. Sham, Brad J. Geddes, Rajesh R. Iyengar, Anil Vasudevan, Ju Gao, Su Jen Lai, Elizabeth K. Govek, Thomas A. Fey, Freeman Jennifer C, Gang Zhao, Dennis G Fry, Michael E. Brune, Jennifer Lee Che, Brian D. Dayton, Doug H. Falls, Kennan C. Marsh, Andrew J. Souers, James Brown, Jon Roses, Michael A. Patane, Matthew J. LaMarche, Cathleen Mcdowell, Lee C. Preusser, Lisa E. Hernandez, Mathew M. Mulhern, Courtney Cullis, Tom Marsilje, Sevan Brodjian, Lynch John K, Eugene N. Bush, Sells Todd B, Robin Shapiro, Christopher Blackburn, Andrew S. Judd, Glenn A. Reinhart
Publikováno v:
Journal of Medicinal Chemistry. 48:5888-5891
4-(1-Benzo[1,3]dioxol-5-ylmethylpiperidine-4-ylmethyl)-6-chlorochromen-2-one (7) is a potent, orally bioavailable melanin concentrating hormone receptor 1 (MCHr1) antagonist that causes dose-dependent weight loss in diet-induced obese mice. Further e
Autor:
Ruth L. Martin, Andrew S. Judd, Sevan Brodjian, Dariusz Wodka, Gilbert Diaz, Lynch John K, Philip R. Kym, Sandra Leitza, Hing L. Sham, Freeman Jennifer C, Mathew M. Mulhern, Gang Zhao, Andrew J. Souers, Christine A. Collins, Sue Swanson, Brian D. Dayton, Rajesh R. Iyengar, Kathryn Houseman, Regina M. Reilly, H. Doug Falls, Ju Gao, Zhi Su
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(4)
The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety led to the discovery of 19, a compound that showed excellent MCHr1 binding and functional
Autor:
Ann Mikhail, Sandra Leitza, Gilbert Diaz, Brian D. Dayton, Lynch John K, Robin Shapiro, Kathryn Houseman, Freeman Jennifer C, Philip R. Kym, Dariusz Wodka, Sevan Brodjian, Eugene N. Bush, Ju Gao, Regina M. Reilly, Gary Gintant, Kennan C. Marsh, Mathew M. Mulhern, Andrew S. Judd, Christine A. Collins, Victoria Knourek-Segel, Andrew J. Souers, Lisa E. Hernandez, H. Douglas Falls, James T. Limberis, Rajesh R. Iyengar, Gang Zhao, Hing L. Sham
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(8)
A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated
Autor:
Dariusz Wodka, David W A Beno, Rajesh R. Iyengar, Kennan C. Marsh, Freeman Jennifer C, Michael E. Brune, Lynch John K, James J. Napier, Brian D. Dayton, Andrew S. Judd, Regina M. Reilly, Gilbert Diaz, Mathew M. Mulhern, H. Doug Falls, Chong J. Chen, Andrew J. Souers, Gang Zhao, Brian A. Droz, Philip R. Kym, Christine A. Collins, Lisa E. Hernandez, Ju Gao, Eugene N. Bush, Hing L. Sham, Victoria Knourek-Segel, Sevan Brodjian, Robin Shapiro
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(4)
The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the identification of a series of chiral racemic compounds that displayed good to excellent functional pote
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
Autor:
Mathew M. Mulhern, Seble Wagaw, Brian D. Dayton, Philip R. Kym, Freeman Jennifer C, Sevan Brodjian, Kenneth M. Engstrom, Kennan C. Marsh, Anil Vasudevan, Andrew J. Souers, Robin Shapiro, Derek Wodka, Eugene N. Bush, Mary K. Verzal, Michael E. Brune, Lisa E. Hernandez, Lynch John K, Christine A. Collins, Ju Gao, Doug H. Falls
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(23)
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100nM. Compounds 19 and 28, two of the more potent com
Autor:
Judd, Andrew S., Souers, Andrew J., Wodka, Dariusz, Zhao, Gang, Mulhern, Mathew M., Iyengar, Rajesh R., Gao, Ju, Lynch, John K., Freeman, Jennifer C., Falls, H. Douglas, Brodjian, Sevan, Dayton, Brian D., Reilly, Regina M., Gintant, Gary, Limberis, James T., Mikhail, Ann, Leitza, Sandra T., Houseman, Kathryn A., Diaz, Gilbert, Bush, Eugene N., Shapiro, Robin, Knourek-Segel, Victoria, Hernandez, Lisa E., Marsh, Kennan C., Sham, Hing L., Collins, Christine A., Kym, Philip R.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2007 17(8):2365-2371
Autor:
Iyengar, Rajesh R., Lynch, John K., Mulhern, Mathew M., Judd, Andrew S., Freeman, Jennifer C., Gao, Ju, Souers, Andrew J., Zhao, Gang, Wodka, Dariusz, Doug Falls, H., Brodjian, Sevan, Dayton, Brian D., Reilly, Regina M., Swanson, Sue, Su, Zhi, Martin, Ruth L., Leitza, Sandra T., Houseman, Kathryn A., Diaz, Gilbert, Collins, Christine A., Sham, Hing L., Kym, Philip R.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2007 17(4):874-878
Autor:
Souers, Andrew J., Iyengar, Rajesh R., Judd, Andrew S., Beno, David W.A., Gao, Ju, Zhao, Gang, Brune, Michael E., Napier, James J., Mulhern, Mathew M., Lynch, John K., Freeman, Jennifer C., Wodka, Dariusz, Chen, Chong J., Falls, H. Doug, Brodjian, Sevan, Dayton, Brian D., Diaz, Gilbert J., Bush, Eugene N., Shapiro, Robin, Droz, Brian A., Knourek-Segel, Victoria, Hernandez, Lisa E., Marsh, Kennan C., Reilly, Regina M., Sham, Hing L., Collins, Christine A., Kym, Philip R.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2007 17(4):884-889