Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Darren B. Dressen"'
Autor:
Anna Liao, Gary Probst, Pamela S. Keim, Kang Hu, Roy K. Hom, David A. Quincy, Michael S. Dappen, Grace T. Kwong, Jenifer Smith, Martin L. Neitzel, Ying-zi Xu, Elizabeth F. Brigham, Kevin P. Quinn, Frédérique Bard, Minghua Sun, Jing Wu, John-Michael Sauer, Dora Kholodenko, Hongbin Zhang, William Wallace, Matthew N. Mattson, Patricia Sacayon, Jacek Jagodzinski, Hing L. Sham, Brian T. Peterson, Simeon Bowers, Jennifer Marugg, Guriqbal S. Basi, Lee H. Latimer, Susanna S. Hemphill, Darren B. Dressen, Karina Wong, Kevin Tanaka, Michael P. Bova, Pamela Santiago, Daniel K. Ness, Anh P. Truong, Wes Zmolek, Lany Ruslim, Christopher Willits, Michael K. Lee, Andrei W. Konradi, Xiaocong M. Ye, Lam Nguyen, Chris M. Semko, Ted A. Yednock, Ruth N. Motter, Albert W. Garofalo, Erich Goldbach, Pearl Tanaka, Danielle L. Aubele
Publikováno v:
Journal of Medicinal Chemistry. 56:5261-5274
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c5b61686f688dd0abd9c5edac66d7201
https://doi.org/10.1021/jm301741t
https://doi.org/10.1021/jm301741t
Autor:
Chris M. Semko, Danielle L. Aubele, Guriqbal S. Basi, Wes Zmolek, Gary Probst, Matthew N. Mattson, Elizabeth F. Brigham, Erich Goldbach, Karina Wong, William A Wallace, John-Michael Sauer, Hing L. Sham, Lan K. Nguyen, Michael P. Bova, Andrei W. Konradi, Albert W. Garofalo, Susanna S. Hemphill, Darren B. Dressen, Kevin P. Quinn, Minghua Sun, Anh P. Truong, Simeon Bowers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5791-5794
The structure–activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate β-amyloid peptide synthesis via γ-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c797a2f9e3d425d83f37dc2fbd3a6ac
https://doi.org/10.1016/j.bmcl.2011.08.008
https://doi.org/10.1016/j.bmcl.2011.08.008
Autor:
Darren B. Dressen, Ying-Zi Xu, Jenifer L. Smith, Xiaocong M. Ye, Elizabeth F. Brigham, Erich Goldbach, Anh P. Truong, Hing L. Sham, Michael P. Bova, Jennifer Marugg, Guriqbal S. Basi, Jacek Jagodzinski, Hongbin Zhang, Michael A. Pleiss, Andrei W. Konradi, Albert W. Garofalo, John-Michael Sauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2195-2199
Discovery of a series of pyrazolopiperidine sulfonamide based gamma-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold wer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0387338b2339269ae539bce793e3d886
https://doi.org/10.1016/j.bmcl.2010.02.039
https://doi.org/10.1016/j.bmcl.2010.02.039
Autor:
Jay S. Tung, Balazs G. Szoke, David W. G. Wone, Michael A. Pleiss, Albert W. Garofalo, Jon E. Hawkinson, Dennis S. Hom, Heather Zhang, Jennifer L. Marugg, Martin L. Neitzel, Jing Wu, Darren B. Dressen, Jacek Jagodzinski
Publikováno v:
Journal of Medicinal Chemistry. 50:5161-5167
The B1 receptor is an attractive target for the treatment of pain and inflammation. A series of 3-carboxamido-5-phenacylamino pyrazole B1 receptor antagonists are described that exhibit good potency against B1 and high selectivity over B2. Initially,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e4a3be695c64bc74dc9e0ae3d18382e
https://doi.org/10.1021/jm051292n
https://doi.org/10.1021/jm051292n
Autor:
William Gallaway, Robert W. Ley, Francine S. Grant, Cesar Tio, Susan Petusky, Michael A. Pleiss, Darren B. Dressen, Mary M. Sherman, Lu Zhang, Dimitri Sarantakis, Semko Christopher M, Reinhardt Bernhard Baudy, Andrei W. Konradi, Susan Ashwell, Donna M. Huryn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1651-1654
A pro-drug strategy to identify orally efficacious VLA-4 antagonists is described. Potential pro-drugs were evaluated for their physical chemical characteristics and in vitro properties, including solubility, stability, permeability and plasma stabil
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cfdecbaca32d6714e423ac8aa609ba6e
https://doi.org/10.1016/j.bmcl.2004.01.062
https://doi.org/10.1016/j.bmcl.2004.01.062
Autor:
Jay S. Tung, Michael A. Pleiss, Albert W. Garofalo, Erich Goldbach, Cheryl A. Bales, David W. G. Wone, James E. Audia, Stephen Sohn, Darren B. Dressen, Thomas Edward Mabry, Angela Phuc, Nissen Jeffrey S, Thorsett Eugene D, Folmer Beverly K, Jing Wu, Harry F. Dovey, Ashley C. Guinn, Lee H. Latimer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:3051-3053
Potent, small molecule A beta inhibitors have been prepared that incorporate an alanine core bracketed by an N-terminal arylacetyl group and various C-terminal amino alcohols. The compounds exhibit stereospecific inhibition as demonstrated in an in v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e54cab507103921c3382fac6a78953b0
https://doi.org/10.1016/s0960-894x(02)00684-4
https://doi.org/10.1016/s0960-894x(02)00684-4
Autor:
Judevin Lugar, Kevin P. Quinn, Anna Liao, Darren B. Dressen, Linda Chen, Thomas N. Thompson, Elizabeth J. Holsztynska, Francine S. Farouz, Whitney Dunn, Christopher Vandevert, Ying-Zi Xu, Michael Jefferies, Thorsett Eugene D, Mark Dreyer, Michael A. Pleiss, Ted Yednock, Andrei W. Konradi, Stephen B. Freedman, Linda Mutter, Semko Christopher M
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
A series of N-(pyrimidin-4-yl)-phenylalanine VLA-4 antagonists is described. Optimization of substituents at the 2 and 5 positions of the pyrimidine ring gave 14, a very potent VLA-4 inhibitor which is orally active in a sheep asthma model.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::982509e7bd4eb62add7249a723781903
https://pubmed.ncbi.nlm.nih.gov/21316228
https://pubmed.ncbi.nlm.nih.gov/21316228
Autor:
Jay S. Tung, Nanhua Yao, Shawn Gauby, Kevin P. Quinn, May Lin, Lany Ruslim, Jennifer Sealy, Michael A. Pleiss, Luke Tso, John A. Tucker, Hu Pan, Gergely Toth, Sukanto Sinha, Andrei W. Konradi, Varghese John, Ying-Zi Xu, Anh P. Truong, Darren B. Dressen, Wes Zmolek, Gary Probst, Hing L. Sham, Eric Brecht, Jagodzinska Barbara, Jacek Jagodzinski, Michael P. Bova, Simeon Bowers, Roy K. Hom, John-Michael Sauer, Dean R. Artis, Brian P. Stupi, Ted Yednock, Andrea Gailunas, Jose Aquino
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(20)
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17be19225486b99a904b3317b2c59a1f
https://pubmed.ncbi.nlm.nih.gov/20822903
https://pubmed.ncbi.nlm.nih.gov/20822903
Autor:
Ted Yednock, Chris M. Semko, Hing L. Sham, Darren B. Dressen, Gary Probst, John-Michael Sauer, Albert W. Garofalo, Kevin P. Quinn, Michael P. Bova, Jing Wu, Michael S. Dappen, Simeon Bowers, Martin L. Neitzel, Pamela S. Keim, Karina Wong, Guriqbal S. Basi, Roy K. Hom, Erich Goldbach, Anh P. Truong, Andrei W. Konradi, Susanna S. Hemphill, William A Wallace, Lan K. Nguyen, Elizabeth F. Brigham, Danielle L. Aubele, Frederique Bard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7553
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::49d496068a972d5629e4dba9b9fa5644
https://doi.org/10.1016/j.bmcl.2010.10.090
https://doi.org/10.1016/j.bmcl.2010.10.090
Autor:
Mary M. Sherman, Lu Zhang, Reinhardt Bernhard Baudy, William Gallaway, Francine S. Grant, Andrei W. Konradi, Dimitri Sarantakis, Semko Christopher M, Cesar Tio, Michael A. Pleiss, Susan Ashwell, Robert W. Ley, Donna M. Huryn, Darren B. Dressen, Susan Petusky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5449
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6e0ec897667a80c7a3531d629f4328b5
https://doi.org/10.1016/j.bmcl.2004.07.006
https://doi.org/10.1016/j.bmcl.2004.07.006