C. Dehnhardt

发表

NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats

Angela Hussainkhel, S. Decker, Matthew Waldbrook, 2021, bioRxiv.

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.

David R. Anderson, S. Wright, V. Rao, 2017, Journal of medicinal chemistry.

Application of Quantitative NMR in Pharmacological Evaluation of Biologically Generated Metabolites: Implications in Drug Discovery

R. Talaat, A. Mutlib, J. Scatina, 2011, Drug Metabolism and Disposition.

Inhibitors of voltage-gated sodium channel Nav1.7: patent applications since 2010.

C. Cohen, Shaoyi Sun, C. Dehnhardt, 2014, Pharmaceutical patent analyst.

3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.

J. Bidlack, M. Wentland, W. Duan, 2001, Bioorganic & medicinal chemistry letters.

Abstract 723: Beyond temsirolimus: Discovery of PKI-587 a highly efficacious dual PI3K/mTOR inhibitor

R. Abraham, N. Brooijmans, L. Feldberg, 2010 .

Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.

N. Brooijmans, L. Feldberg, R. Mallon, 2010, Journal of medicinal chemistry.

Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.

N. Brooijmans, Steven C. Kim, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Practical One‐Pot Procedure for the Synthesis of 1,2,3,4‐Tetrahydroquinolines by the Imino‐Diels‐Alder Reaction

C. Dehnhardt, Y. Espinal, A. M. Venkatesan, 2008 .

Highly Stereoselective Synthesis of a Chiral Methyl Group by a Facially Controlled Sigmatropic [1,5]-Hydrogen Shift

J. Mulzer, M. McDonald, H. Floss, 1999 .

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Journal of medicinal chemistry.

Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.

Yogesh Sabnis, J. Chrencik, G. Whitlock, 2017, Journal of medicinal chemistry.

Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor

L. Feldberg, R. Mallon, J. Lucas, 2011, Clinical Cancer Research.

Cancer Therapy : Preclinical Antitumor Efficacy of PKI-587 , a Highly Potent Dual PI 3 K / mTOR Kinase Inhibitor

L. Feldberg, R. Mallon, J. Lucas, 2011 .

PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.

L. Feldberg, R. Mallon, J. Lucas, 2010, Bioorganic & medicinal chemistry letters.

Antitumor Efficacy Profile of PKI-402, a Dual Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor

L. Feldberg, R. Mallon, J. Gibbons, 2010, Molecular Cancer Therapeutics.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

N. Brooijmans, L. Feldberg, R. Mallon, 2011, Bioorganic & medicinal chemistry letters.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.

Judy Lucas, Irwin Hollander, Robert Mallon, 2010, Journal of medicinal chemistry.

Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition.

M. Follettie, N. Brooijmans, J. Lucas, 2010, Journal of medicinal chemistry.

2,4-Diamino-quinazolines as inhibitors of beta-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer.

J. Lucas, T. Mansour, K. Arndt, 2009, Bioorganic & medicinal chemistry letters.

Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain.

D. Sutherlin, D. Hackos, S. Decker, 2018, Cell reports.

Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.

D. Sutherlin, D. Hackos, A. D. White, 2018, Journal of medicinal chemistry.

Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

Jun Li, Christine Tam, Daniel F. Ortwine, 2015, Science.

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.

D. Sutherlin, Jun Chen, D. Hackos, 2019, Journal of medicinal chemistry.

Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity.

Benjamin D. Sellers, D. Sutherlin, D. Hackos, 2018, Journal of medicinal chemistry.

Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy.

R. DeVita, S. Decker, Matthew Waldbrook, 2019, Journal of medicinal chemistry.

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.

Shifeng Liu, R. Oballa, D. Sutherlin, 2016, ACS medicinal chemistry letters.

Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.

Xufeng Sun, J. Bidlack, M. Wentland, 2003, Journal of medicinal chemistry.

Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310.

D. Sutherlin, Jun Chen, D. Hackos, 2021, Journal of medicinal chemistry.

Identification of aryl sulfonamides as novel and potent inhibitors of NaV1.5.

Angela Hussainkhel, J. Empfield, Jr., 2021, Bioorganic & medicinal chemistry letters.

Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free‐Energy Perturbation (FEP)

Atli Thorarensen, Joseph McDonald, A. Moretto, 2016, ChemMedChem.

Stereoselective synthesis of an active metabolite of the potent PI3 kinase inhibitor PKI-179.

T. Mansour, S. Ayral-Kaloustian, L. McDonald, 2010, The Journal of organic chemistry.

The Discovery of the Nav1.7 Inhibitor GDC-0276 and Development of an Efficient Large-Scale Synthesis

D. Sutherlin, R. Angelaud, Andreas Stumpf, 2019, ACS Symposium Series.

NaV1.6 inhibition drives the efficacy of voltage-gated sodium channel inhibitors to prevent electrically induced seizures in both wild type and Scn8aN1768D/+ gain-of-function mice

Wei Zhang, Angela Hussainkhel, Matthew Waldbrook, 2023, bioRxiv.

Application of Quantitative NMR in Pharmacological Evaluation of Biologically Generated Metabolites: Implications in Drug Discovery

R. Talaat, A. Mutlib, J. Scatina, 2011, Drug Metabolism and Disposition.

Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free‐Energy Perturbation (FEP)

A. Moretto, L. Fitz, A. Thorarensen, 2016, ChemMedChem.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Journal of medicinal chemistry.

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Journal of medicinal chemistry.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Bioorganic & medicinal chemistry letters.