Timothy Heffron

发表

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2012, Journal of medicinal chemistry.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Steve Price, E. Bradley, BinQing Wei, 2013, Journal of medicinal chemistry.

Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels.

Timothy Heffron, 2018, Neuro-oncology.

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

C. Eigenbrot, Ivana Yen, S. Sideris, 2016, ACS medicinal chemistry letters.

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2014, Journal of medicinal chemistry.

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

D. Sutherlin, S. Sideris, L. Friedman, 2010, Journal of medicinal chemistry.

Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947

J. Lubach, Xingrong Liu, C. Hop, 2020, Drug Metabolism and Disposition.

Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947

J. Lubach, Xingrong Liu, C. Hop, 2020, Drug Metabolism and Disposition.

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

M. Belvin, E. Bradley, M. Ultsch, 2013 .

Synthesis of skipped enynes via phosphine-promoted couplings of propargylcopper reagents

T. Jamison, Timothy Heffron, J. D. Trenkle, 2003 .

Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.

E. Bradley, BinQing Wei, J. Lesnick, 2013, Bioorganic & medicinal chemistry letters.

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

D. Sutherlin, S. Sideris, Leslie B. Lee, 2011, Bioorganic & medicinal chemistry letters.

Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

BinQing Wei, D. Sutherlin, J. Lesnick, 2011, Journal of medicinal chemistry.

Application of Reactive Enols in Synthesis: A Versatile, Efficient, and Stereoselective Construction of the Welwitindolinone Carbon Skeleton

M. Shamji, B. Stoltz, J. L. Wood, 1999 .

Ladder polyether synthesis via epoxide-opening cascades directed by a disappearing trimethylsilyl group.

T. Jamison, E. Merino, Graham Simpson, 2010, The Journal of organic chemistry.

Ladder polyether synthesis via epoxide-opening cascades using a disappearing directing group.

T. Jamison, E. Merino, Graham Simpson, 2006, Journal of the American Chemical Society.

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.

C. Eigenbrot, Ivana Yen, S. Sideris, 2016, Bioorganic & medicinal chemistry letters.

SiMe3-based homologation-epoxidation-cyclization strategy for ladder THP synthesis.

T. Jamison, Timothy Heffron, 2003, Organic letters.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

D. Sutherlin, L. Friedman, Leslie B. Lee, 2010, Bioorganic & medicinal chemistry letters.

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

L. Rangell, H. Phillips, H. Koeppen, 2016, Drug Metabolism and Disposition.

Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer.

Timothy Heffron, 2016, Journal of medicinal chemistry.

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

S. Sideris, Leslie B. Lee, K. Edgar, 2016, ACS medicinal chemistry letters.

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.

Karl A. Merrick, T. O'Brien, A. Jakalian, 2019, Bioorganic & medicinal chemistry letters.

CNS Anticancer Drug Discovery and Development Conference White Paper.

Patrick J. Paddison, D. Berry, J. Sarkaria, 2015, Neuro-oncology.

The Discovery and Process Chemistry Development of GDC-0084, a Brain Penetrating Inhibitor of PI3K and mTOR

A. McClory, Timothy Heffron, Andreas Stumpf, 2016 .

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

W. Forrest, Kyung Song, L. Friedman, 2021, bioRxiv.

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.

Siew K. Yeap, C. Eigenbrot, Ivana Yen, 2016, Journal of medicinal chemistry.

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

Belen Dominguez-Fernandez, C. Eigenbrot, Ivana Yen, 2015, Journal of medicinal chemistry.

Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation

Siew K. Yeap, C. Eigenbrot, Ivana Yen, 2014, Journal of medicinal chemistry.

Noncovalent wild-type-sparing inhibitors of EGFR T790M.

J. Settleman, K. Politi, S. Sideris, 2013, Cancer discovery.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

S. Steinbacher, Steve Price, E. Gancia, 2016, Journal of medicinal chemistry.

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

D. Sutherlin, S. Sideris, Irina S. Chuckowree, 2010, Bioorganic & medicinal chemistry letters.

CNS Anticancer Drug Discovery and Development: 2016 conference insights.

P. Tonge, V. Levin, W. Weiss, 2017, CNS oncology.

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

S. Sideris, Leslie B. Lee, K. Edgar, 2012, Journal of medicinal chemistry.

Prevalence of acid-reducing agents (ARA) in cancer populations and ARA drug-drug interaction potential for molecular targeted agents in clinical development.

Leslie Z Benet, Brian Dean, L. Benet, 2013, Molecular pharmaceutics.

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.

Steve Price, M. Belvin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer.

BinQing Wei, Y. Franke, E. Day, 2019, Structure.

Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

Hoai An Le Thi, E. Gancia, BinQing Wei, 2021, ACS medicinal chemistry letters.

Targeting the PI3K Pathway in the Brain—Efficacy of a PI3K Inhibitor Optimized to Cross the Blood–Brain Barrier

J. Sarkaria, H. Phillips, S. Kharbanda, 2012, Clinical Cancer Research.

A probabilistic method to report predictions from a human liver microsomes stability QSAR model: a practical tool for drug discovery

Man-Ling Lee, Ignacio Aliagas, Timothy Heffron, 2015, Journal of Computer-Aided Molecular Design.

From Discovery to Market Readiness: The Research and Development of the β-Sparing Phosphatidylinositol 3-Kinase Inhibitor Taselisib

A. Schuster, S. Staben, R. Angelaud, 2019, ACS Symposium Series.

DEGAS: Sharing and Tracking Target Compound Ideas with External Collaborators

Man-Ling Lee, Ignacio Aliagas, Jennafer Dotson, 2012, J. Chem. Inf. Model..

Characterization of Anti-Neovascularization Activity and Ocular Pharmacokinetics of PI3K/mTOR Inhibitor GNE-947

C. Hop, S. Shahidi-Latham, J. Nonomiya, 2020 .

Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

Hoai An Le Thi, E. Gancia, Weiru Wang, 2021, ACS medicinal chemistry letters.