Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Robert J. Cherney"'
Autor:
Anne Rose, Qihong Zhao, Kumaravel Selvakumar, Percy H. Carter, Prakash Anjanappa, Jing Chen, Sandhya Mandlekar, Mary Ellen Cvijic, Andrew J. Tebben, Songmei Xu, Gregory D. Brown, Venkatram Reddy Paidi, Arvind Mathur, Douglas G. Batt, Jian Pang, Joel C. Barrish, Robert J. Cherney, Melissa Yarde, Ragini Vuppugalla
Publikováno v:
ACS Med Chem Lett
[Image: see text] BMS-813160 (compound 3) was identified as a potent and selective CCR2/5 dual antagonist. Compound 3 displayed good permeability at pH = 7.4 in PAMPA experiments and demonstrated excellent human liver microsome stability. Pharmacokin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8d0c6d25f05a8ec4cbd4e45bae9db09
https://doi.org/10.1021/acsmedchemlett.1c00373
https://doi.org/10.1021/acsmedchemlett.1c00373
Autor:
Andrew J. Tebben, Sandhya Mandlekar, Michael A. Gallela, Songmei Xu, Robert J. Cherney, Mary Ellen Cvijic, Anne Rose, John V. Duncia, Mary F. Malley, Yang Michael G, Arvind Mathur, Percy H. Carter, Amy A. Sarjeant, Jian Pang, Bei Wang, Zili Xiao, Ragini Vuppugalla, Purnima Khandelwal, Qihong Zhao, Gardner Daniel S, Joseph B. Santella, Douglas G. Batt, Gregory D. Brown, Rulin Zhao
Publikováno v:
ACS Med Chem Lett
[Image: see text] To improve the metabolic stability profile of BMS-741672 (1a), we undertook a structure–activity relationship study in our trisubstituted cyclohexylamine series. This ultimately led to the identification of 2d (BMS-753426) as a po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f70e15f407bd4570156fbac55e9e1f1
https://doi.org/10.1021/acsmedchemlett.1c00082
https://doi.org/10.1021/acsmedchemlett.1c00082
Autor:
Dauh-Rurng Wu, Joseph Pawluczyk, Robert J. Cherney, Joseph A. Tino, Shiuhang Yip, T. G. Murali Dhar, James Kempson, Jianqing Li, Darpandeep Aulakh, Amy A. Sarjeant, Daniel Smith, Arvind Mathur, Cornelius Lyndon A M, Subramaniam Krishnananthan
Publikováno v:
The Journal of Organic Chemistry. 85:10988-10993
We describe an efficient synthetic route to differentially protected diester, 1-(tert-butyl) 4-methyl (1R,2S,4R)-2-methylcyclohexane-1,4-dicarboxylate (+)-1, via palladium-catalyzed methoxycarbonylation of an enol triflate derived from a Hagemann's e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8fba5ca413d795699a30093fecc6e060
https://doi.org/10.1021/acs.joc.0c01169
https://doi.org/10.1021/acs.joc.0c01169
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:
Mary Ellen Cvijic, Andrew J. Tebben, Jian Pang, Mary F. Malley, Ruowei Mo, Joseph B. Santella, Songmei Xu, Qihong Zhao, Douglas G. Batt, Jing Chen, Anne Rose, Bei Wang, Hong Shi, Marta Dabros, Anurag S. Srivastava, Percy H. Carter, Purnima Khandelwal, Yang Michael G, Gardner Daniel S, Gregory D. Brown, Sandhya Mandlekar, Michael Galella, Rulin Zhao, Zili Xiao, John V. Duncia, Sarah C. Traeger, Joel C. Barrish, Robert J. Cherney, Soo S. Ko
Publikováno v:
ACS Medicinal Chemistry Letters. 10:300-305
[Image: see text] We encountered a dilemma in the course of studying a series of antagonists of the G-protein coupled receptor CC chemokine receptor-2 (CCR2): compounds with polar C3 side chains exhibited good ion channel selectivity but poor oral bi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df5aa828abdf2f0d6f0a23ce2ce17d65
https://doi.org/10.1021/acsmedchemlett.8b00439
https://doi.org/10.1021/acsmedchemlett.8b00439
Autor:
Lyndon A M, Cornelius, Jianqing, Li, Daniel, Smith, Subramaniam, Krishnananthan, Shiuhang, Yip, Dauh-Rurng, Wu, Joseph, Pawluczyk, Darpandeep, Aulakh, Amy A, Sarjeant, James, Kempson, Joseph A, Tino, Arvind, Mathur, T G, Murali Dhar, Robert J, Cherney
Publikováno v:
The Journal of organic chemistry. 85(16)
We describe an efficient synthetic route to differentially protected diester, 1-(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::df07183df8f1f4be77277c2b6f15bcdc
https://pubmed.ncbi.nlm.nih.gov/32687358
https://pubmed.ncbi.nlm.nih.gov/32687358
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:
Carolyn A. Weigelt, Xiaomei Gu, Stacey Skala, Paul Davies, Jenny Xie, John S. Sack, T. G. Murali Dhar, Melissa Yarde-Chinn, James Neels, Michael A. Poss, Stefan Ruepp, Robert J. Cherney, Christine Goldstein, Joseph A. Tino, Luisa Salter-Cid, Kevin Stefanski, Vojkan Susulic, Rajeev S. Bhide, Xiaoxia Yang, Anurag S. Srivastava, Zheming Ruan, Lan-Ying Qin, Cornelius Lyndon A M, Ruth Bosnius
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:855-861
As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a62fd58c8612f99a2829596d8b0690e5
https://doi.org/10.1016/j.bmcl.2017.01.016
https://doi.org/10.1016/j.bmcl.2017.01.016
Autor:
Tian Qin, Julien C. Vantourout, Michael R. Collins, Phil S. Baran, Shouliang Yang, Pavlo S. Lebed, Pavel K. Mykhailiuk, Cian Kingston, Jacob T. Edwards, Jason S. Chen, Robert J. Cherney, Rohan R. Merchant, Natalia M. Padial, Daniel C. Schmitt, Brittany Sanchez, Gary M. Gallego, Matthew A. Perry, Monika M. Kruszyk, James J. Mousseau, Shengyang Ni
Publikováno v:
Digibug. Repositorio Institucional de la Universidad de Granada
instname
Journal of the American Chemical Society
instname
Journal of the American Chemical Society
We would like to thank Enamine Ltd for providing samples of several acids. We are grateful to Dr. Dee- Hua Huang and Dr. Laura Pasternack (Scripps Research) for assistance with nuclear magnetic resonance (NMR) spectroscopy and Mr. Andrew Badwal (Pfiz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ddbb19e7bf9b728018562965565794c
http://hdl.handle.net/10481/59869
http://hdl.handle.net/10481/59869
Autor:
Georgia Cornelius, Carolyn A. Weigelt, Sha Li, Dauh-Rurng Wu, David Marcoux, Luisa Salter-Cid, Aberra Fura, Melissa Yarde, Shiuhang Yip, Peng Li, John Hynes, Tara Sherry, Max Ruzanov, Rex Denton, Robert J. Cherney, Yue-Zhong Shu, Jinhong Wang, Mary Ellen Cvijic, Zili Xiao, David J. Shuster, Jenny Xie, Purnima Khandelwal, Kevin Stefanski, T. G. Murali Dhar, Qing Shi, Yang Michael G, Mary T. Obermeier, Silvi A. Chacko, Javed Khan, John S. Sack, Joseph A. Tino, Qihong Zhao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127521
In order to rapidly develop C6 and C8 SAR of our reported tricyclic sulfone series of RORγt inverse agonists, a late-stage bromination was employed. Although not regioselective, the bromination protocol allowed us to explore new substitution pattern
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bea96801b270e44f686650249c45be29
https://doi.org/10.1016/j.bmcl.2020.127521
https://doi.org/10.1016/j.bmcl.2020.127521