Zobrazeno 1 - 10
of 75
pro vyhledávání: '"Jaume Balsells"'
Design of Prodrugs to Enhance Colonic Absorption by Increasing Lipophilicity and Blocking Ionization
Autor:
Rebecca Nofsinger, Sophie-Dorothee Clas, Rosa I. Sanchez, Abbas Walji, Kimberly Manser, Becky Nissley, Jaume Balsells, Amrithraj Nair, Qun Dang, David Jonathan Bennett, Michael Hafey, Junying Wang, John Higgins, Allen Templeton, Paul Coleman, Jay Grobler, Ronald Smith, Yunhui Wu
Publikováno v:
Pharmaceuticals, Vol 7, Iss 2, Pp 207-219 (2014)
Prodrugs are chemistry-enabled drug delivery modifications of active molecules designed to enhance their pharmacokinetic, pharmacodynamic and/or biopharmaceutical properties. Ideally, prodrugs are efficiently converted in vivo, through chemical or en
Externí odkaz:
https://doaj.org/article/f16659dde48e4fc4a5f8d5c963902bbd
Publikováno v:
Organic letters. 23(15)
A facile, scalable synthesis of previously inaccessible trifluoromethyl and perfluoroalkyl triazoles is disclosed. Mediated by copper, this catalytic protocol enables access to 4-perfluoroalkyl triazoles from commodity chemicals. A catalytic Cu(II) s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ea2c5e210bccd1e69da3e1b30e52792
https://pubmed.ncbi.nlm.nih.gov/34286985
https://pubmed.ncbi.nlm.nih.gov/34286985
Publikováno v:
European Journal of Organic Chemistry. 2020:1515-1522
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7275921a372fbcc6b0a9a3a65b89444f
https://doi.org/10.1002/ejoc.201900611
https://doi.org/10.1002/ejoc.201900611
Publikováno v:
Organic letters. 22(19)
A convergent method for the rapid preparation of substituted isocoumarins is reported. The transformation takes advantage of a spontaneous intramolecular cyclization that follows the Pd-catalyzed α-arylation of aldehydes with 2-halobenzoic esters. T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90d7febcc4bbbbcd89b021c0efc90121
https://pubmed.ncbi.nlm.nih.gov/32969657
https://pubmed.ncbi.nlm.nih.gov/32969657
Publikováno v:
Chemical Science. 9:6639-6646
The emergence of photoredox catalysis has enabled the discovery of mild and efficient conditions for the generation of a variety of radical reaction platforms. Herein is disclosed the development of a conjugate addition reaction of non-activated alky
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2dcb82933de9d955922e1dec7702ff47
https://doi.org/10.1039/c8sc02253d
https://doi.org/10.1039/c8sc02253d
Autor:
Baoqiang Wan, Scott Hoerrner, Jaume Balsells, Lu Chen, Bangping Xiang, Qinghao Chen, Lushi Tan, Carmela Molinaro, Eric M. Phillips, Zhongbo Fei, Jingjun Yin, Scott S. Ceglia, Ji Qi, Jiahui Chen, Michael Shevlin, Manuel de Lera Ruiz, Erika M. Milczek
Publikováno v:
The Journal of organic chemistry. 84(12)
A practical and efficient enantioselective synthesis of the calcitonin gene-related peptide receptor antagonist 1 has been developed. The key structural component of the active pharmaceutical ingredient is a syn-1,2-amino-fluoropiperidine 4. Two appr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b43576d65cf179b7c21a63a8f5c25048
https://pubmed.ncbi.nlm.nih.gov/31124362
https://pubmed.ncbi.nlm.nih.gov/31124362
Autor:
Patricia Miller, Yaode Wang, Joseph Della Rocca, Jeffrey L. Evelhoch, Paul J. Coleman, Kerry Riffel, Zhizhen Zeng, Elizabeth Joshi, Kun Yang, Xiaoping Zhang, Kerim Babaoglu, Eric D. Hostetler, Talakad G. Lohith, Stacey O'Malley, David Hesk, Abbas Walji, Jaume Balsells, Mona Purcell, Jing Li, Serena Xu, Brett Connolly, Stacey Melquist, Arie Struyk, Jianmin Fu, Julie A. O'Brien, Marie A. Holahan, Harold G. Selnick, Fred Hess, Aimie Ogawa, David J. Schenk, Idriss Bennacef, Cristian Salinas, Joel B. Schachter, Aileen Soriano, Liza Gantert
Publikováno v:
Journal of Medicinal Chemistry. 59:4778-4789
Neurofibrillary tangles (NFTs) made up of aggregated tau protein have been identified as the pathologic hallmark of several neurodegenerative diseases including Alzheimer's disease. In vivo detection of NFTs using PET imaging represents a unique oppo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a39b60a8ba41ad44ebe7487bf9b6714d
https://doi.org/10.1021/acs.jmedchem.6b00166
https://doi.org/10.1021/acs.jmedchem.6b00166
Autor:
Jaume Balsells, Edward J. J. Grabowski, Shane W. Krska, Nelo R. Rivera, Yongkui Sun, Joseph D. Armstrong, Bryon Simmons, Andrew M. Clausen, Felix Spindler, Yi Hsiao, Michele Kubryk, Christophe Malan, Karl B. Hansen, Nori Ikemoto, Feng Xu, Thorsten Rosner
Publikováno v:
Journal of the American Chemical Society. 142:13622-13622
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ff28a025888c0453761a46c2fa910f8b
https://doi.org/10.1021/jacs.0c06041
https://doi.org/10.1021/jacs.0c06041
Autor:
Richard G. Ball, Narayan Variankaval, Robert A. Reamer, Jaume Balsells, Gregory York, Teresa Andreani, Varsolona Richard J, Jing Li, Andrew Brunskill, Nancy N. Tsou, Jimmy O. DaSilva, Manuel de Lera Ruiz, Nobuyoshi Yasuda, Ryan D. Cohen, C. Scott Shultz
Publikováno v:
Organic Process Research & Development. 19:1882-1890
MK-8970 is an acetal carbonate prodrug of raltegravir (Isentress). This work presents the Merck team’s investigations into the polymorphism of MK-8970, the thermodynamic relationship between the discovered crystalline forms, and implementation of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a920d1d1119205fc3919acebe28359f8
https://doi.org/10.1021/acs.oprd.5b00129
https://doi.org/10.1021/acs.oprd.5b00129
Autor:
Jeremy P. Scott, Gavin W. Stewart, Carl A. Baxter, Michel Journet, Birgit Kosjek, Kevin M. Belyk, Lushi Tan, Jaume Balsells, Hongmei Li, Mahbub Alam, Christopher Wise, Cheng-yi Chen, Zhiguo Jake Song
Publikováno v:
Organic Letters. 17:1533-1536
A practical asymmetric synthesis of the complex fused bis-macrocyclic HCV protease inhibitor MK-6325 (1) is described. Through the combination of a high yielding and low catalyst loading ring-closing metathesis (RCM) to forge the 15-membered macrocyc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::19eceb81f8f069dd4828b6930195a860
https://doi.org/10.1021/acs.orglett.5b00418
https://doi.org/10.1021/acs.orglett.5b00418