Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Keshab, Sarma"'
Autor:
Mihaela M. Esanu, Edmund Leung, Nande Wright, Selcuk Calimsiz, Xiang Wang, Olivier St-Jean, Eric A. Standley, Guojun Yu, Li Wang, Dustin Bringley, Roberts Benjamin James, Jaspal Phull, Anna Chiu, Jason A. Davy, Doxsee Ian James, Jeffrey D. Ng, Wen-Tau T. Chang, Lennie Lin, Jenny Phoenix, David Allen Siler, Olga Lapina, Andrea Ambrosi, Youri Kim, Jeffrey A. O. Garber, Jinyu Shen, Bernard Kwong, Keshab Sarma, Bing Shi, Andrew Anthony Martins
Publikováno v:
Organic Process Research & Development. 25:1215-1236
This manuscript describes the chemical process development and multi-kilogram synthesis of rovafovir etalafenamide (GS-9131), a phosphonamidate prodrug nucleotide reverse transcriptase inhibitor un...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1e6d25441ec292ea6d90f7f6942f094e
https://doi.org/10.1021/acs.oprd.1c00059
https://doi.org/10.1021/acs.oprd.1c00059
Autor:
Jonah W. Curl, Olivier St-Jean, Jason A. Davy, Olga Lapina, Sangsun Park, Mary Rosario, Jeffrey A. O. Garber, Sura Ha, Bernard Kwong, David Allen Siler, Selcuk Calimsiz, Keshab Sarma, Doxsee Ian James, Jinyu Shen, Jeffrey D. Ng, Lennie Lin, Guojun Yu, Jisung Lee
Publikováno v:
Organic Process Research & Development. 25:1263-1274
Fluorinated nucleoside 1 is a key starting material in the synthesis of rovafovir etalafenamide (2), a novel nucleotide reverse transcriptase inhibitor under development at Gilead Sciences for the ...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::26f676376f843d7c8975b05c66d15f0f
https://doi.org/10.1021/acs.oprd.1c00026
https://doi.org/10.1021/acs.oprd.1c00026
Autor:
Jeffrey A. O. Garber, Edmund Leung, Olga Lapina, Selcuk Calimsiz, Keshab Sarma, Jonah W. Curl, Guojun Yu, Andrew Anthony Martins, Bing Shi, Jaspal Phull, Bernard Kwong, Jinyu Shen, Andrea Ambrosi, Sankar Mohan, Mary Rosario, Huy V. Huynh, Li Wang, Lennie Lin, Dustin Bringley, Eric A. Standley, Teague M. McGinitie, Xueqing Wang, Ben Roberts
Publikováno v:
Organic Process Research & Development. 25:1247-1262
Phosphonamidate 1 is a key fragment in the assembly of rovafovir etalafenamide, a novel nucleotide reverse transcriptase inhibitor under development at Gilead Sciences for the treatment of HIV infe...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3585ed6f2b4c9d546264e8c3574d36f6
https://doi.org/10.1021/acs.oprd.0c00428
https://doi.org/10.1021/acs.oprd.0c00428
Autor:
Nande Wright, Roberts Benjamin James, Bernard Kwong, Keshab Sarma, Smith Mark, Alan Scott Triman, Elan Shao, Jason A. Davy, Andrew Anthony Martins, Jinyu Shen, Brandon Heath Brown, Dustin Bringley, Keiko Sujino, Selcuk Calimsiz, Detian Gao
Publikováno v:
Organic Process Research & Development. 25:1237-1246
As part of the synthesis of rovafovir etalafenamide, the development and manufacturing-scale demonstration of a dioxirane-mediated oxidative elimination is described. The reaction presented multipl...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::716ab3ca237293fc9365771f045b76d4
https://doi.org/10.1021/acs.oprd.0c00439
https://doi.org/10.1021/acs.oprd.0c00439
Autor:
Judy M. Suh, Sandra Frauchiger, Michael Soth, Xiaochun Han, Ronald J. Hill, Buelent Kocer, Taygerly Joshua Paul Gergely, Jaehyeon Park, Hong Jun-Bae, Andreas Kuglstatter, Rama K. Kondru, Tobias Gabriel, Renee Litman, Yan Lou, Zachary Kevin Sweeney, Mcintosh Joel, Nolan James Dewdney, Dana Davis, David Michael Goldstein, Timothy D. Owens, Hasim Zecic, Keshab Sarma
Publikováno v:
Journal of Medicinal Chemistry. 58:512-516
Structure-based drug design was used to guide the optimization of a series of selective BTK inhibitors as potential treatments for Rheumatoid arthritis. Highlights include the introduction of a benzyl alcohol group and a fluorine substitution, each o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2706725af4b785142b07ad80c3bfd24
https://doi.org/10.1021/jm500305p
https://doi.org/10.1021/jm500305p
Autor:
Bill Bingenheimer, Hong Jun-Bae, Qingwu Jin, Michael Welch, Michael Allen Matchett, Erin M. O'brien, James Edward Paul Davidson, Keshab Sarma, Gary R. Lee
Publikováno v:
Organic Process Research & Development. 18:228-238
A scalable and convergent synthesis of a BTK (Bruton’s tyrosine kinase) inhibitor has been developed. Synthetic routes to key intermediates were explored for the scale-up campaign, especially the process for 6-dimethylaminodihydroisoquinolinone, wh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2b1027a98be9ddbbb804a8972b8541c1
https://doi.org/10.1021/op4001077
https://doi.org/10.1021/op4001077
Autor:
Jaehyeon Park, Harlan F Reese, Yun-Chou Tan, Hasim Zecic, Martin Stahl, Keshab Sarma, Renee Litman, Alejandra Trejo, William Bingenheimer, Michael Soth, David Michael Goldstein, Mary Welch, Eric Brian Sjogren, Man-Ling Sung, Sandra Frauchiger, Nolan James Dewdney, Bong San Pablo, Eva Papp, Daniel McWeeney, Ronald J. Hill, Paul Weller, Manjiri Ghate, JoAnn La Fargue, Brian Wong, Stacie A. Dalrymple, James Patrick Dunn, David Mark Rotstein, Richard T. Roberts, Bradford Graves, Rebecca T Suttman, Mcintosh Joel, Farrell Robert P, Andreas Kuglstatter, Chen Jian Jeffrey, Fujun Li, Humberto Bartolome Arzeno, Brad Loe, Tobias Gabriel
Publikováno v:
Journal of Medicinal Chemistry. 54:2255-2265
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5bdfa3e0a0a96eaca0eea2feab67e249
https://doi.org/10.1021/jm101423y
https://doi.org/10.1021/jm101423y
Autor:
Yanzhou Liu, Keshab Sarma, Tom Alfredson, Fujun Li, Justin Chow, Fangling Lin, Kate Comstock, Michael Brandl
Publikováno v:
Journal of Pharmaceutical and Biomedical Analysis. 53:710-716
RG7128 is a di-ester prodrug of a cytidine analog for the treatment of hepatitis C virus (HCV) infection. The structures of nine low level impurities (0.05-0.10%) in RG7128 drug substance were elucidated. The majority of the impurities were formed du
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c309d9b1f4283560a0c1c3a0fac4625d
https://doi.org/10.1016/j.jpba.2010.04.003
https://doi.org/10.1016/j.jpba.2010.04.003
Autor:
Cooper Gary F, Dan Fishlock, Sunil Sukhtankar, Gary M. Lee, Keshab Sarma, James Edward Paul Davidson, Michael Welch, Michael Martin
Publikováno v:
Organic Process Research & Development. 14:477-480
Robust and scalable syntheses of some synthetically useful 3,5-disubstituted phenols are presented. The process involves the selective displacement of a halogen by nucleophilic aromatic substitution using a preformed mixture of potassium tert-butoxid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9cc3db81c0d7c453fd799b369029b91a
https://doi.org/10.1021/op900322u
https://doi.org/10.1021/op900322u
Autor:
Qingwu Jin, Yu Li, Jennifer Fretland, Julie Q. Hang, Dimitrio Stefanidis, Gabrielle Heilek, Hassan Javanbakht, Jeffrey Wu, Weiling Liang, Fang‐Jie Zhang, Jesper A. Jernelius, Nidhi Arora, Judy M. Suh, Petra Inbar, Michael Welch, Seth F. Harris, Klaus Klumpp, Guoping Su, Donald Roy Hirschfeld, Ralf Roetz, Armando G. Villaseñor, Keshab Sarma, Zachary Kevin Sweeney, J. Roland Billedeau, Joshua Kennedy-Smith, Mark D. Smith, James Edward Paul Davidson
Publikováno v:
ChemMedChem. 4:88-99
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are part of the preferred treatment regimens for individuals infected with HIV. These NNRTI-based regimens are efficacious, but the most popular NNRTIs have a low genetic barrier to resistance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::454bae71e060e01fe27efb0014a6b6df
https://doi.org/10.1002/cmdc.200800262
https://doi.org/10.1002/cmdc.200800262