Design, Optimization, and Biological Evaluation of Novel Keto-Benzimidazoles as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A)
Hu, Essa, Kunz, Roxanne K, Chen, Ning, Rumfelt, Shannon, Siegmund, Aaron, Andrews, Kristin, Chmait, Samer, Zhao, Sharon, Davis, Carl, Chen, Hang, Lester-Zeiner, Dianna, Ma, Ji, Biorn, Christopher, Shi, Jianxia, Porter, Amy, Treanor, James, Allen, Jennifer R
Published in Journal of medicinal chemistry (14.11.2013)
Published in Journal of medicinal chemistry (14.11.2013)
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Discovery of Clinical Candidate 1‑(4-(3-(4-(1H‑Benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), A Potent, Selective, and Efficacious Inhibitor of Phosphodiesterase 10A (PDE10A)
Hu, Essa, Chen, Ning, Bourbeau, Matthew P, Harrington, Paul E, Biswas, Kaustav, Kunz, Roxanne K, Andrews, Kristin L, Chmait, Samer, Zhao, Xiaoning, Davis, Carl, Ma, Ji, Shi, Jianxia, Lester-Zeiner, Dianna, Danao, Jean, Able, Jessica, Cueva, Madelyn, Talreja, Santosh, Kornecook, Thomas, Chen, Hang, Porter, Amy, Hungate, Randall, Treanor, James, Allen, Jennifer R
Published in Journal of medicinal chemistry (14.08.2014)
Published in Journal of medicinal chemistry (14.08.2014)
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Journal Article
Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors
Hu, Essa, Kunz, Roxanne K., Rumfelt, Shannon, Chen, Ning, Bürli, Roland, Li, Chun, Andrews, Kristin L., Zhang, Jiandong, Chmait, Samer, Kogan, Jeffrey, Lindstrom, Michelle, Hitchcock, Stephen A., Treanor, James
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
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Journal Article
Rapid Identification of a Novel Small Molecule Phosphodiesterase 10A (PDE10A) Tracer
Hu, Essa, Ma, Ji, Biorn, Christopher, Lester-Zeiner, Dianna, Cho, Robert, Rumfelt, Shannon, Kunz, Roxanne K, Nixey, Thomas, Michelsen, Klaus, Miller, Silke, Shi, Jianxia, Wong, Jamie, Hill Della Puppa, Geraldine, Able, Jessica, Talreja, Santosh, Hwang, Dah-Ren, Hitchcock, Stephen A, Porter, Amy, Immke, David, Allen, Jennifer R, Treanor, James, Chen, Hang
Published in Journal of medicinal chemistry (24.05.2012)
Published in Journal of medicinal chemistry (24.05.2012)
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Journal Article
Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit
Hu, Essa, Tasker, Andrew, White, Ryan D, Kunz, Roxanne K, Human, Jason, Chen, Ning, Bürli, Roland, Hungate, Randall, Novak, Perry, Itano, Andrea, Zhang, Xuxia, Yu, Violeta, Nguyen, Yen, Tudor, Yanyan, Plant, Matthew, Flynn, Shaun, Xu, Yang, Meagher, Kristin L, Whittington, Douglas A, Ng, Gordon Y
Published in Journal of medicinal chemistry (12.06.2008)
Published in Journal of medicinal chemistry (12.06.2008)
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Journal Article
Use of Thallium(I) Ethoxide in Suzuki Cross Coupling Reactions
Frank, Scott A, Chen, Hou, Kunz, Roxanne K, Schnaderbeck, Matthew J, Roush, William R
Published in Organic letters (24.08.2000)
Published in Organic letters (24.08.2000)
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Journal Article
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the N‑Arylsulfonamido‑N′‑arylpiperazine Series
Nishimura, Nobuko, Norman, Mark H, Liu, Longbin, Yang, Kevin C, Ashton, Kate S, Bartberger, Michael D, Chmait, Samer, Chen, Jie, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steven R, Kunz, Roxanne K, Pennington, Lewis D, Poon, Steve F, Siegmund, Aaron, Sivits, Glenn, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (10.04.2014)
Published in Journal of medicinal chemistry (10.04.2014)
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Journal Article
AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer
Chen, Hang, Lester-Zeiner, Dianna, Shi, Jianxia, Miller, Silke, Glaus, Charlie, Hu, Essa, Chen, Ning, Able, Jessica, Biorn, Christopher, Wong, Jamie, Ma, Ji, Michelsen, Klaus, Hill Della Puppa, Geraldine, Kazules, Tim, Dou, Hui Hannah, Talreja, Santosh, Zhao, Xiaoning, Chen, Ada, Rumfelt, Shannon, Kunz, Roxanne K, Ye, Hu, Thiel, Oliver R, Williamson, Toni, Davis, Carl, Porter, Amy, Immke, David, Allen, Jennifer R, Treanor, James
Published in The Journal of pharmacology and experimental therapeutics (01.02.2015)
Published in The Journal of pharmacology and experimental therapeutics (01.02.2015)
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Journal Article
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 2. Leveraging Structure-Based Drug Design to Identify Analogues with Improved Pharmacokinetic Profiles
St. Jean, David J., Ashton, Kate S., Bartberger, Michael D., Chen, Jie, Chmait, Samer, Cupples, Rod, Galbreath, Elizabeth, Helmering, Joan, Hong, Fang-Tsao, Jordan, Steven R., Liu, Longbin, Kunz, Roxanne K., Michelsen, Klaus, Nishimura, Nobuko, Pennington, Lewis D., Poon, Steve F., Reid, Darren, Sivits, Glenn, Stec, Markian M., Tadesse, Seifu, Tamayo, Nuria, Van, Gwyneth, Yang, Kevin C., Zhang, Jiandong, Norman, Mark H., Fotsch, Christopher, Lloyd, David J., Hale, Clarence
Published in Journal of medicinal chemistry (23.01.2014)
Published in Journal of medicinal chemistry (23.01.2014)
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Journal Article
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility
Rzasa, Robert M., Frohn, Michael J., Andrews, Kristin L., Chmait, Samer, Chen, Ning, Clarine, Jeffrey G., Davis, Carl, Eastwood, Heather A., Horne, Daniel B., Hu, Essa, Jones, Adrie D., Kaller, Matthew R., Kunz, Roxanne K., Miller, Silke, Monenschein, Holger, Nguyen, Thomas, Pickrell, Alexander J., Porter, Amy, Reichelt, Andreas, Zhao, Xiaoning, Treanor, James J.S., Allen, Jennifer R.
Published in Bioorganic & medicinal chemistry (01.12.2014)
Published in Bioorganic & medicinal chemistry (01.12.2014)
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Journal Article
Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3)
Hu, Essa, Kunz, Roxanne K., Rumfelt, Shannon, Andrews, Kristin L., Li, Chun, Hitchcock, Stephen A., Lindstrom, Michelle, Treanor, James
Published in Bioorganic & medicinal chemistry letters (15.11.2012)
Published in Bioorganic & medicinal chemistry letters (15.11.2012)
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Journal Article
Diastereoselective synthesis of the endo- and exo-spirotetronate subunits of the quartromicins. The first enantioselective Diels-Alder reaction of an acyclic (Z)-1,3-diene
Roush, William R, Limberakis, Chris, Kunz, Roxanne K, Barda, David A
Published in Organic letters (02.05.2002)
Published in Organic letters (02.05.2002)
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Journal Article
Discovery of Phosphodiesterase 10A (PDE10A) PET Tracer AMG 580 to Support Clinical Studies
Hu, Essa, Chen, Ning, Kunz, Roxanne K, Hwang, Dah-Ren, Michelsen, Klaus, Davis, Carl, Ma, Ji, Shi, Jianxia, Lester-Zeiner, Dianna, Hungate, Randall, Treanor, James, Chen, Hang, Allen, Jennifer R
Published in ACS medicinal chemistry letters (14.07.2016)
Published in ACS medicinal chemistry letters (14.07.2016)
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Journal Article
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors
Kunz, Roxanne K., Rumfelt, Shannon, Chen, Ning, Zhang, Dawei, Tasker, Andrew S., Bürli, Roland, Hungate, Randall, Yu, Violeta, Nguyen, Yen, Whittington, Douglas A., Meagher, Kristin L., Plant, Matthew, Tudor, Yanyan, Schrag, Michael, Xu, Yang, Ng, Gordon Y., Hu, Essa
Published in Bioorganic & medicinal chemistry (15.09.2008)
Published in Bioorganic & medicinal chemistry (15.09.2008)
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Journal Article
Studies on the synthesis of the quartromicins: partial stereochemical assignment of quartromicins A3 and D3 and diastereoselective synthesis of the endo- and exo-spirotetronate subunits
Roush, William R, Barda, David A, Limberakis, Chris, Kunz, Roxanne K
Published in Tetrahedron (05.08.2002)
Published in Tetrahedron (05.08.2002)
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Journal Article
Diastereoselective Synthesis of the e ndo- and e xo-Spirotetronate Subunits of the Quartromicins. The First Enantioselective Diels−Alder Reaction of an Acyclic (Z)-1,3-Diene
Roush, William R, Limberakis, Chris, Kunz, Roxanne K, Barda, David A
Published in Organic letters (02.05.2002)
Published in Organic letters (02.05.2002)
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Journal Article
Studies on the synthesis of the quartromicins: partial stereochemical assignment of quartromicins A 3 and D 3 and diastereoselective synthesis of the endo- and exo-spirotetronate subunits
Roush, William R, Barda, David A, Limberakis, Chris, Kunz, Roxanne K
Published in Tetrahedron (2002)
Published in Tetrahedron (2002)
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Journal Article