Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Christopher M. Mapes"'
Autor:
Christopher M. Mapes, Shirin Shinde, Kelly J. McClure, Laurent Gomez, J. Guy Breitenbucher, Todd K. Jones, Clark A. Sehon, Neelakandha S. Mani, Marna C. W. Pippel, Xiaohu Deng, Chennagiri R. Pandit
Publikováno v:
The Journal of Organic Chemistry. 75:7950-7953
We describe a practical and scalable route to compound (Z)-1, a selective CCK1 receptor antagonist. Notable features of this concise route are (1) a regioselective construction of the pyrazole core through the reaction of an aryl hydrazine and an ela
Publikováno v:
Organic Process Research & Development. 11:482-486
We report a procedure for the concise and high-yielding syntheses of 1-piperidin-4-yl-substituted butyro- and valerolactams. Beginning with 1-benzyl-4-piperidone and γ- or δ-amino esters or acids, we have effected a tandem reductive amination−lac
Publikováno v:
The Journal of Organic Chemistry. 71:5039-5042
An efficient method for the stereoselective synthesis of (Z)-α-arylacrylates is described. Treatment of α-hydroxyesters with triflic anhydride and pyridine at 0 °C followed by warming to room temperature afforded the corresponding (Z)-α-aryl-α,
Publikováno v:
ChemInform. 38
Treatment of oxazole or 5-aryl oxazoles with i-PrMgCl smoothly generates the corresponding 2-Grignard reagents, which react with Weinreb amides to provide exclusively 2-acyl oxazole products.
Publikováno v:
The Journal of organic chemistry. 71(13)
An efficient method for the stereoselective synthesis of (Z)-alpha-arylacrylates is described. Treatment of alpha-hydroxyesters with triflic anhydride and pyridine at 0 degrees C followed by warming to room temperature afforded the corresponding (Z)-
Autor:
Mary S. Urcan, Christopher M. Mapes, Marilyn Wardlow, Kathleen M. Ogilvie, Margaret M. Faul, Carol L. Broderick, Jennifer D'Arrigo, Nancy I. Hein, Mark D. Leibowitz, Marcus F. Boehm, Anne Reifel-Miller, Mark A. Carfagna, John S. Tyhonas, Deepa Rungta, Henry Havel, Dale E. Mais, Timothy Alan Grese, Sha Liu, Robert Ardecky, Bernadette Pascual, Keith B. Marschke, Nathan Yumibe, Chahrzad Montrose-Rafizadeh, Kay Klausing, Pierre-Yves Michellys, Diane L. Crombie, Richard A. Heyman, Diane Jolley, Garrett J. Etgen
Publikováno v:
Endocrinology. 147(2)
Specific retinoid X receptor (RXR) agonists, such as LG100268 (LG268), and the thiazolidinedione (TZD) PPARgamma agonists, such as rosiglitazone, produce insulin sensitization in rodent models of insulin resistance and type 2 diabetes. In sharp contr
Autor:
Anne Reifel-Miller, Katheen M Ogilvie, Christopher M. Mapes, Mark D. Leibowitz, Donald S. Karanewsky, Marcus F. Boehm, Jyun-Hung Chen, Anthony W. Thompson, Robert Ardecky, Pierre-Yves Michellys, John S. Tyhonas, Sha Liu, Nathan Yumibe, Deepa Rungta, Timothy Alan Grese, Dale A. Mais
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(22)
New RXR-selective modulators possessing a 6-fluoro trienoic acid moiety (6Z olefin) or a fluorinated/heterocyclic-substituted benzene core ring, were synthesized in an expedient and selective way. A subset of these compounds was evaluated for their m
Autor:
Pierre-Yves Michellys, Mark D Leibowitz, Marcus F. Boehm, Jennifer D'Arrigo, Anne Reifel-Miller, Christopher M. Mapes, Robert J. Ardecky, D.A. Mais, Chahrzad Montrose-Rafizadeh, Sha Liu, Donald S. Karanewsky, John S. Tyhonas, Deepa Rungta, Timothy Alan Grese, Jyun-Hung Chen, Anthony W. Thompson, Katheen M Ogilvie
Publikováno v:
Journal of medicinal chemistry. 46(19)
Retinoid X receptor:peroxisome proliferative-activated receptor (RXR:PPAR) heterodimers play a critical role in the regulation of glucose (RXR/PPARgamma) and lipid metabolism (RXR/PPARalpha). Previously, we described a concise structure-activity rela
Autor:
John S. Tyhonas, R. Ajamie, R.A. Ardecky, Michael Gregory Bell, Christopher M. Mapes, Timothy Alan Grese, D.L. Gernert, Pierre-Yves Michellys, D.A. Mais, Nathan Yumibe, Deepa K. Rungta, Anne Reifel-Miller, Mark D. Leibowitz
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(19)
Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the positi
Autor:
Christopher M. Mapes, Anthony W. Thompson, K Klausing, Anne Reifel-Miller, Robert Ardecky, Donald S. Karanewsky, Deepa Rungta, John S. Tyhonas, Mark D. Leibowitz, Timothy Alan Grese, Sha Liu, D.A. Mais, Margaret M. Faul, Garret J. Etgen, K B Marschke, A L Faulkner, Marcus F. Boehm, Jyun-Hung Chen, Pierre-Yves Michellys, Katheen M Ogilvie, D L Crombie, Richard A. Heyman
Publikováno v:
Journal of medicinal chemistry. 46(13)
Previous data have shown that RXR-selective agonists (e.g., 3 and 4) are insulin sensitizers in rodent models of non-insulin-dependent diabetes mellitus (NIDDM). Unfortunately, they also produce dramatic increases in triglycerides and profound suppre