Zobrazeno 1 - 10
of 63
pro vyhledávání: '"David Marcoux"'
Autor:
John Hynes, Antonio Ramirez, John R. Coombs, Jade McDaniel, David Marcoux, Francisco González-Bobes, T. G. Murali Dhar, Amy A. Sarjeant, Arthur Han, Qing Shi, Christopher A. Farley, William P. Gallagher, Bhupinder Sandhu
Publikováno v:
Organic Letters. 23:60-65
The use of the unprecedented annulating reagents methyl N-(tert-butylsulfinyl)-4-chlorobutanimidate and methyl N-(tert-butylsulfinyl)-5-bromopentanimidate enables the diastereoselective preparation of 5- and 6-membered carbocycles bearing three conti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74155f755af11fec471be78e17587fdd
https://doi.org/10.1021/acs.orglett.0c03695
https://doi.org/10.1021/acs.orglett.0c03695
Autor:
John L. Gilmore, Kim W. McIntyre, Lois D. Lehman-McKeeman, David Marcoux, Hai-Yun Xiao, Georgia Cornelius, Alaric J. Dyckman, Mary Ellen Cvijic, Jenny Xie, Yang Michael G, T. G. Murali Dhar, Zili Xiao, Tracy L. Taylor, Anthony M. Marino, Ding Ren Shen, Percy H. Carter, Paul Levesque, Arvind Mathur, Huadong Sun, Hong Shi
Publikováno v:
ACS Med Chem Lett
[Image: see text] Efforts aimed at increasing the in vivo potency and reducing the elimination half-life of 1 and 2 led to the identification of aryl ether and thioether-derived bicyclic S1P(1) differentiated modulators 3–6. The effects of analogs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::415fc075f357363f95afa2908797c5ae
https://doi.org/10.1021/acsmedchemlett.0c00333
https://doi.org/10.1021/acsmedchemlett.0c00333
Autor:
Carolyn A. Weigelt, Sha Li, David Marcoux, Georgia Cornelius, Qihong Zhao, Mary Ellen Cvijic, John E. Macor, Jingwu Duan, Melissa Yarde, Muthalagu Vetrichelvan, David J. Shuster, Qingjie Liu, Richard Rampulla, Kim W. McIntyre, Mary T. Obermeier, Shiuhang Yip, Purnima Khandelwal, Sureshbabu Vishwakrishnan, Anuradha Gupta, Virna Borowski, Peng Li, Kevin Stefanski, Sridharan Ramlingam, Myra Beaudoin-Bertrand, Nageswara Maddala, Sridhar Vanteru, Percy H. Carter, Arvind Mathur, Aberra Fura, Max Ruzanov, John Hynes, Dauh-Rurng Wu, Jinhong Wang, Luisa Salter-Cid, John S. Sack, Cornelius Lyndon A M, Anurag S. Srivastava, Robert J. Cherney, Kumaravel Selvakumar, Mushkin Basha, Arun Kumar Gupta, Douglas G. Batt, Rex Denton, Sukhen Karmakar, Qing Shi, Ananta Karmakar, Naveen Manjunath, Javed Khan, Jenny Xie, Joseph A. Tino, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 62:9931-9946
RORγt is an important nuclear receptor that regulates the production of several pro-inflammatory cytokines such as IL-17 and IL-22. As a result, RORγt has been identified as a potential target for the treatment of various immunological disorders su
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eeada291586349dd371c5b816894adb
https://doi.org/10.1021/acs.jmedchem.9b01369
https://doi.org/10.1021/acs.jmedchem.9b01369
Autor:
John Hynes, Joseph A. Tino, Qihong Zhao, Hyunsoo Park, David Marcoux, Jinhong Wang, Sha Li, Melissa Yarde, Michael Galella, Dauh-Rurng Wu, Shiuhang Yip, T. G. Murali Dhar, Myra Beaudoin Bertrand, Mary Ellen Cvijic, Carolyn A. Weigelt
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(19)
RORγt is the master regulator of the IL-23/IL-17 axis, a pathway that is clinically validated for the treatment of various immunological disorders. Over the last few years, our group has reported different chemotypes that potently act as inverse ago
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::307e35ae3f143d2795ef84311d15d921
https://pubmed.ncbi.nlm.nih.gov/32763309
https://pubmed.ncbi.nlm.nih.gov/32763309
Autor:
Alaric Dyckman, Jenny Xie, Lois D Lehman-McKeeman, Marn Ellen Cvijic, Ding Ren Shen, Dauh-Rurng Wu, Arvind Mathur, Georgia Cornelius, Anthony Marino, Paul Levesque, Hong Shi, Andres Hernandez, David Marcoux, Michael Yang, T. G. Murali Dhar, Hai-Yun Xiao, John Lodge Gilmore
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07f19bf75ab5a1d51b52f15362ce3665
https://doi.org/10.1021/scimeetings.0c02440
https://doi.org/10.1021/scimeetings.0c02440
Autor:
Qingjie Liu, Mary T. Obermeier, John S. Sack, Carolyn A. Weigelt, Georgia Cornelius, Percy H. Carter, David J. Shuster, Luisa Salter-Cid, Aberra Fura, Virna Borowski, Jingwu Duan, Purnima Khandelwal, Qing Shi, Robert J. Cherney, Cornelius Lyndon A M, Jinhong Wang, Jenny Xie, Max Ruzanov, Kevin Stefanski, Rex Denton, T. G. Murali Dhar, David Marcoux, Shiuhang Yip, Melissa Yarde, Douglas G. Batt, Javed Khan, Joseph A. Tino, Qihong Zhao, Anurag S. Srivastava, Arvind Mathur, Mary Ellen Cvijic, John E. Macor, Sha Li, Dauh-Rurng Wu
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel tricyclic analogues were designed, synthesized, and evaluated as RORγt inverse agonists. Several of these compounds were potent in an IL-17 human whole blood assay and exhibited excellent oral bioavailability in mouse pharmac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12c0984e9b1636552c6620f1a6235555
https://pubmed.ncbi.nlm.nih.gov/32551004
https://pubmed.ncbi.nlm.nih.gov/32551004
Autor:
Purnima Khandelwal, John Hynes, Hyunsoo Park, David Marcoux, Michael Galella, T. G. Murali Dhar, Qing Shi, Mariah C. Meehan
Publikováno v:
Organic Letters. 20:337-340
The purpose of this letter is to document the use of protected chloroethyl and chloropropyl amines as conformationally unrestricted ambiphilic reagents that undergo annulation reactions with Michael acceptors. This reaction is wide in scope and utili
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b45d4112dd032272d7214f8907154e08
https://doi.org/10.1021/acs.orglett.7b03548
https://doi.org/10.1021/acs.orglett.7b03548
Autor:
Marta Dabros, Paul Levesque, Elizabeth M. Heimrich, Arvind Mathur, Percy H. Carter, Richard Rampulla, Anuradha Gupta, Lois D. Lehman-McKeeman, Huadong Sun, David Marcoux, Ding Ren Shen, Xiaoxia Yang, Xia D. Zhou, Hai-Yun Xiao, Dauh-Rurng Wu, Louis J. Lombardo, Hong Shi, Zheng Yang, Mary Ellen Cvijic, Alaric J. Dyckman, Kim W. McIntyre, Luisa Salter-Cid, Celia D’Arienzo, Anthony M. Marino, Bala Pragalathan, Georgia Cornelius, Jenny Xie, T. G. Murali Dhar, Tracy L. Taylor, Rochelle Thomas
Publikováno v:
MedChemComm. 8:725-729
Recently, our research group reported the identification of prodrug amino-alcohol 2 as a potent and efficacious S1P1 receptor modulator. This molecule is differentiated preclinically over the marketed drug fingolimod (Gilenya 1), whose active phospha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d2e68634039d58468401fb206f57908e
https://doi.org/10.1039/c6md00539j
https://doi.org/10.1039/c6md00539j
Autor:
Ding Ren Shen, Mary Ellen Cvijic, Hai-Yun Xiao, Alaric J. Dyckman, Yu-Wen Li, Bala Pragalathan, Joel C. Barrish, Georgia Cornelius, Peng Li, Tracy L. Taylor, Zili Xiao, Lois D. Lehman-McKeeman, Jianlin Feng, Dauh-Rurng Wu, John L. Gilmore, Percy H. Carter, David Marcoux, Zheng Yang, Arvind Mathur, Elizabeth M. Heimrich, Kim W. McIntyre, Bethanne M. Warrack, Anuradha Gupta, Yang Michael G, Luisa Salter-Cid, Praveen Balimane, Virna Borowski, Jenny Xie, T. G. Murali Dhar, Alda Fernandes, Anthony M. Marino
Publikováno v:
Journal of Medicinal Chemistry. 59:11138-11147
We describe a highly efficient route for the synthesis of 4a (BMS-986104). A key step in the synthesis is the asymmetric hydroboration of trisubstituted alkene 6. Particularly given the known difficulties involved in this type of transformation (6
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec587a5bf6e33d17913adf16699fae01
https://doi.org/10.1021/acs.jmedchem.6b01433
https://doi.org/10.1021/acs.jmedchem.6b01433
Autor:
Mariah C. Meehan, John Hynes, Hyunsoo Park, Qing Shi, John R. Coombs, Purnima Khandelwal, Nathaniel S. Greenwood, Michael Galella, T. G. Murali Dhar, David Marcoux, William P. Gallagher, Carlos A. Guerrero, Bhupinder Sandhu, Francisco Gonzalez Bobes
Publikováno v:
Organic letters. 21(22)
This communication highlights the use of chiral sulfinamides as nitrogen nucleophiles in intermolecular aza-Michael reactions. When chiral sulfinamides are coupled to a chloroethyl group, the corresponding novel annulating reagents can be used to str
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::890cccb906b6d95ea4e06c65d6474292
https://pubmed.ncbi.nlm.nih.gov/31647672
https://pubmed.ncbi.nlm.nih.gov/31647672