Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Bryan James Branstetter"'
Autor:
Alec D. Lebsack, Alan D. Wickenden, Sandra R. Chaplan, Qi Wang, Jason C. Rech, Love Christopher John, William A. Eckert, J. Guy Breitenbucher, Ludwig Paul Cooymans, Leenaerts Joseph Elisabeth, Anindya Bhattacharya, Bryan James Branstetter, Hong Ao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4781-4784
The synthesis, SAR and preclinical characterization of a series of 6-chloro- N -(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists is described herein. The lead compounds are pote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::388b93925ee3e02bc3395487919b3389
https://doi.org/10.1016/j.bmcl.2016.08.029
https://doi.org/10.1016/j.bmcl.2016.08.029
Autor:
Michael P. Maher, Sandra R. Chaplan, Jing Liu, Jason C. Rech, Brian Scott, William A. Eckert, Bryan James Branstetter, Hong Ao, Anne E. Fitzgerald, Yi Liu, Nyantsz Wu, Michele C. Rizzolio, Anindya Bhattacharya, Jamie M. Freedman, Alec D. Lebsack, Nadia Swanson, J. Guy Breitenbucher, Dong H. Li, Alan D. Wickenden, Kia Sepassi, Mena Kansagara
Publikováno v:
European Journal of Pharmacology. 663:40-50
As an integrator of multiple nociceptive and/or inflammatory stimuli, TRPV1 is an attractive therapeutic target for the treatment of various painful disorders. Several TRPV1 antagonists have been advanced into clinical trials and the initial observat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3ec72a42cddf9b6c3b6d41084678c9d
https://doi.org/10.1016/j.ejphar.2011.05.001
https://doi.org/10.1016/j.ejphar.2011.05.001
Autor:
Michelle Herrmann, Brett D. Allison, Alec D. Lebsack, Nadia Swanson, Hong Ao, Johnathan C. Buma, Brian Scott, J. Guy Breitenbucher, Jason C. Rech, Bryan James Branstetter, Alan D. Wickenden, Raymond Rynberg, Michael P. Maher, Sandra R. Chaplan, Anindya Bhattacharya, Lin Luo, Qi Wang, Michele C. Rizzolio, Natalie A. Hawryluk, Jamie M. Freedman, Jeffrey E. Merit
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7142-7146
Based upon a previously reported lead compound 1, a series of 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines were synthesized and evaluated for improved physiochemical and pharmacokinetic properties while maintaining TRP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0182b4a94e494ac8544ddd208e9dfff8
https://doi.org/10.1016/j.bmcl.2010.09.006
https://doi.org/10.1016/j.bmcl.2010.09.006
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists
Autor:
Qi Wang, J. Guy Breitenbucher, Hong Ao, Michael D. Hack, Bryan James Branstetter, Alan D. Wickenden, Jamie M. Freedman, Alec D. Lebsack, Nadia Swanson, Michael P. Maher, Sandra R. Chaplan, Natalie A. Hawryluk, Jeffrey E. Merit, Brian Scott, Anindya Bhattacharya
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7137-7141
Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::577da627a65a624579ac5616942548f2
https://doi.org/10.1016/j.bmcl.2010.09.023
https://doi.org/10.1016/j.bmcl.2010.09.023
Autor:
Matthew L. Peterson, Bryan James Branstetter, Lin Luo, Alec D. Lebsack, Michael P. Maher, Sandra R. Chaplan, Michele C. Rizzolio, Anindya Bhattacharya, J. Guy Breitenbucher, Nadia Nasser, Hong Ao, Wei Xiao, Michael D. Hack, Mena Kansagara, Brian Scott, Alan D. Wickenden, Raymond Rynberg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:40-46
We have identified and synthesized a series of 2,7-diamino-thiazolo[5,4-d]pyrimidines as TRPV1 antagonists. An exploration of the structure-activity relationships at the 2-, 5-, and 7-positions of the thiazolo[5,4-d]pyrimidine led to the identificati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fadee51d99950e2ecde1addb8a648049
https://doi.org/10.1016/j.bmcl.2008.11.024
https://doi.org/10.1016/j.bmcl.2008.11.024