Publications by authors named "Randall Hungate"

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Discovery of Phosphodiesterase 10A (PDE10A) PET Tracer AMG 580 to Support Clinical Studies.
Essa Hu, Ning Chen, Roxanne K Kunz, Dah-Ren Hwang, Klaus Michelsen, Randall Hungate

ACS Med Chem Lett· July 2016

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Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Lewis D Pennington, Michael D Bartberger, Michael D Croghan, Kristin L Andrews, Kate S Ashton, Randall W Hungate

J Med Chem· December 2015

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Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Timothy D Cushing, Xiaolin Hao, Youngsook Shin, Kristin Andrews, Matthew Brown, Randall Hungate

J Med Chem· January 2015

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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).
Essa Hu, Ning Chen, Matthew P Bourbeau, Paul E Harrington, Kaustav Biswas, Randall Hungate

J Med Chem· August 2014

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Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency.
Wenyuan Qian, Jian Jeffrey Chen, Jason Human, Toshihiro Aya, Jiawang Zhu, Randall W Hungate

Bioorg Med Chem Lett· January 2012

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Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.
Kate S Ashton, David J St Jean, Steve F Poon, Matthew R Lee, John G Allen, Randall Hungate

Bioorg Med Chem Lett· September 2011

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Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Matthew L Brown, Wade Aaron, Richard J Austin, Angela Chong, Tom Huang, Randall Hungate

Bioorg Med Chem Lett· September 2011

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3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
Jian Jeffrey Chen, Thomas Nguyen, Derin C D'Amico, Wenyuan Qian, Jason Human, Randall W Hungate

Bioorg Med Chem Lett· June 2011

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Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
Daqing Sun, Zhulun Wang, Seb Caille, Michael DeGraffenreid, Felix Gonzalez-Lopez de Turiso, Randall Hungate

Bioorg Med Chem Lett· January 2011

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Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity.
Justin K Murray, Chenera Balan, Alan M Allgeier, Annie Kasparian, Vellarkad Viswanadhan, Randall W Hungate

J Comb Chem· September 2010

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Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists.
Qingyian Liu, Wenyuan Qian, Aiwen Li, Kaustav Biswas, Jian Jeffrey Chen, Randall W Hungate

Bioorg Med Chem Lett· August 2010

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Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Jacob A Kaizerman, Wade Aaron, Songzhu An, Richard Austin, Matt Brown, Randall Hungate

Bioorg Med Chem Lett· August 2010

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Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Murielle M Véniant, Clarence Hale, Randall W Hungate, Kyung Gahm, Maurice G Emery

J Med Chem· June 2010

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Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Brian S Lucas, Wade Aaron, Songzhu An, Richard J Austin, Matthew Brown, Randall Hungate

Bioorg Med Chem Lett· June 2010

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2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.
Qingping Zeng, Matthew P Bourbeau, G Erich Wohlhieter, Guomin Yao, Holger Monenschein, Randall Hungate

Bioorg Med Chem Lett· March 2010

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Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Qingping Zeng, John G Allen, Matthew P Bourbeau, Xianghong Wang, Guomin Yao, Randall Hungate

Bioorg Med Chem Lett· March 2010

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Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
John G Allen, Matthew P Bourbeau, G Erich Wohlhieter, Michael D Bartberger, Klaus Michelsen, Randall Hungate

J Med Chem· November 2009

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Stereoselective synthesis of anti-N-protected 3-amino-1,2-epoxides by nucleophilic addition to N-tert-butanesulfinyl imine of a glyceraldehyde synthon.
Scott S Harried, Michael D Croghan, Matthew R Kaller, Patricia Lopez, Wenge Zhong, Randall Hungate

J Org Chem· August 2009

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Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
Dustin L McMinn, Yosup Rew, Athena Sudom, Seb Caille, Michael Degraffenreid, Randall Hungate

Bioorg Med Chem Lett· March 2009

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Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.
Yosup Rew, Dustin L McMinn, Zhulun Wang, Xiao He, Randall W Hungate

Bioorg Med Chem Lett· March 2009

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Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Christopher Fotsch, Michael D Bartberger, Eric A Bercot, Michelle Chen, Rod Cupples, Randall W Hungate

J Med Chem· December 2008

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Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.
Kaustav Biswas, Toshihiro Aya, Wenyuan Qian, Tanya A N Peterkin, Jian Jeffrey Chen, Randall W Hungate

Bioorg Med Chem Lett· September 2008

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Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.
Roxanne K Kunz, Shannon Rumfelt, Ning Chen, Dawei Zhang, Andrew S Tasker, Randall Hungate

Bioorg Med Chem Lett· September 2008

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Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
Mike Frohn, Vellarkad Viswanadhan, Alexander J Pickrell, Jennifer E Golden, Kristine M Muller, Randall Hungate

Bioorg Med Chem Lett· September 2008

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Design, synthesis, and biological evaluation of potent c-Met inhibitors.
Noel D D'Angelo, Steven F Bellon, Shon K Booker, Yuan Cheng, Angela Coxon, Randall Hungate

J Med Chem· September 2008

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