Search Results - "Breitenbucher, JGuy"

Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase by Keith, John M., Apodaca, Richard, Xiao, Wei, Seierstad, Mark, Pattabiraman, Kanaka, Wu, Jiejun, Webb, Michael, Karbarz, Mark J., Brown, Sean, Wilson, Sandy, Scott, Brian, Tham, Chui-Se, Luo, Lin, Palmer, James, Wennerholm, Michelle, Chaplan, Sandra, Breitenbucher, J. Guy

“…A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by…”
Get full text

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)p y rimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists by Rech, Jason C, Bhattacharya, Anindya, Branstetter, Bryan J, Love, Christopher J, Leenaerts, Joseph E, Cooymans, Ludwig P, Eckert, William A, Ao, Hong, Wang, Qi, Chaplan, Sandra R, Wickenden, Alan D, Lebsack, Alec D, Breitenbucher, JGuy

“…The synthesis, SAR and preclinical characterization of a series of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)p y…”
Get full text

The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors by Keith, John M., Tichenor, Mark S., Apodaca, Richard L., Xiao, Wei, Jones, William M., Seierstad, Mark, Pierce, Joan M., Palmer, James A., Webb, Michael, Karbarz, Mark J., Scott, Brian P., Wilson, Sandy J., Wennerholm, Michelle L., Rizzolio, Michele, Rynberg, Raymond, Chaplan, Sandra R., Breitenbucher, J. Guy

“…The SAR of brain penetration for a series of heteroaryl piperazinyl- and piperadinyl-urea fatty acid amide hydrolase (FAAH) inhibitors is described…”
Get full text

Activation of TRPA1 by farnesyl thiosalicylic acid by Maher, Michael, Ao, Hong, Banke, Tue, Nasser, Nadia, Wu, Nyan-Tsz, Breitenbucher, J Guy, Chaplan, Sandra R, Wickenden, Alan D

“…The nonselective cation channel TRPA1 (ANKTM1, p120) is a potential mediator of pain, and selective pharmacological modulation of this channel may be…”
Get more information

Discovery of a novel series of selective HCN1 blockers by McClure, Kelly J., Maher, Michael, Wu, Nancy, Chaplan, Sandra R., Eckert, William A., Lee, Dong H., Wickenden, Alan D., Hermann, Michelle, Allison, Brett, Hawryluk, Natalie, Breitenbucher, J. Guy, Grice, Cheryl A.

“…Identification of some selective and potent HCN1 blockers is described. The discovery of a series of novel, potent, and selective blockers of the cyclic…”
Get full text

Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH) by Timmons, Amy, Seierstad, Mark, Apodaca, Rich, Epperson, Matt, Pippel, Dan, Brown, Sean, Chang, Leon, Scott, Brian, Webb, Michael, Chaplan, Sandra R., Breitenbucher, J. Guy

“…Efforts to improve the properties of the well studied ketooxazole FAAH inhibitor OL-135 resulted in the discovery of a novel propylpiperidine series of FAAH…”
Get full text

2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2 by Neff, Danielle K., Lee-Dutra, Alice, Blevitt, Jonathan M., Axe, Frank U., Hack, Michael D., Buma, Johnathan C., Rynberg, Raymond, Brunmark, Anders, Karlsson, Lars, Breitenbucher, J. Guy

“…A series of benzimidazole compounds containing pendant alcohol and amine moieties was found to be active against checkpoint kinase Chk2. These compounds were…”
Get full text

Heteroaryl urea inhibitors of fatty acid amide hydrolase: Structureamutagenicity relationships for arylamine metabolites by Tichenor, Mark S, Keith, John M, Jones, William M, Pierce, Joan M, Merit, Jeff, Hawryluk, Natalie, Seierstad, Mark, Palmer, James A, Webb, Michael, Karbarz, Mark J, Wilson, Sandy J, Wennerholm, Michelle L, Woestenborghs, Filip, Beerens, Dominiek, Luo, Lin, Brown, Sean M, Boeck, Marlies De, Chaplan, Sandra R, Breitenbucher, JGuy

“…The structure-activity relationships for a series of heteroaryl urea inhibitors of fatty acid amide hydrolase (FAAH) are described. Members of this class of…”
Get full text

Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists by HAWRYLUK, Natalie A, MERIT, Jeffrey E, FREEDMAN, Jamie M, SCOTT, Brian P, WICKENDEN, Alan D, CHAPLAN, Sandra R, BREITENBUCHER, J. Guy, LEBSACK, Alec D, BRANSTETTER, Bryan J, HACK, Michael D, SWANSON, Nadia, HONG AO, MAHER, Michael P, BHATTACHARYA, Anindya, QI WANG

“…Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent…”
Get full text

Identification and synthesis of 2,7-diamino-thiazolo[5,4- d]pyrimidine derivatives as TRPV1 antagonists by Lebsack, Alec D., Branstetter, Bryan J., Hack, Michael D., Xiao, Wei, Peterson, Matthew L., Nasser, Nadia, Maher, Michael P., Ao, Hong, Bhattacharya, Anindya, Kansagara, Mena, Scott, Brian P., Luo, Lin, Rynberg, Raymond, Rizzolio, Michele, Chaplan, Sandra R., Wickenden, Alan D., Guy Breitenbucher, J.

“…The identification and synthesis of 2,7-diamino-thiazolo[5,4- d]pyrimidines as TRPV1 antagonists is described. An exploration of the structure–activity…”
Get full text

1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties by LEBSACK, Alec D, RECH, Jason C, HONG AO, MAHER, Michael P, HERRMANN, Michelle, FREEDMAN, Jamie, SCOTT, Brian P, LIN LUO, BHATTACHARYA, Anindya, QI WANG, CHAPLAN, Sandra R, WICKENDEN, Alan D, BRANSTETTER, Bryan J, BREITENBUCHER, J. Guy, HAWRYLUK, Natalie A, MERIT, Jeffrey E, ALLISON, Brett, RYNBERG, Raymond, BUMA, Johnathan, RIZZOLIO, Michele, SWANSON, Nadia

“…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…”
Get full text

Novel non-benzimidazole chk2 kinase inhibitors by McClure, Kelly J., Huang, Liming, Arienti, Kristen L., Axe, Frank U., Brunmark, Anders, Blevitt, Jon, Guy Breitenbucher, J.

“…A number of benzimidazole replacements were synthesized and examined to gain a greater understanding of the SAR around this novel series of chk2 kinase…”
Get full text

SAR studies of 1,5-diarylpyrazole-based CCK sub(1) receptor antagonists by Gomez, Laurent, Hack, Michael D, McClure, Kelly, Sehon, Clark, Huang, Liming, Morton, Magda, Li, Lina, Barrett, Terrance D, Shankley, Nigel, Breitenbucher, JGuy

“…A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK sub(1) receptor. Here, we report the syntheses and SAR studies…”
Get full text

Identification of 2-arylbenzimidazoles as potent human histamine H sub(4) receptor ligands by Lee-Dutra, Alice, Arienti, Kristen L, Buzard, Daniel J, Hack, Michael D, Khatuya, Haripada, Desai, Pragnya J, Nguyen, Steven, Thurmond, Robin L, Karlsson, Lars, Edwards, James P, Breitenbucher, JGuy

“…A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H sub(4) receptor. Structure-activity…”
Get full text