M. Letavic

发表

Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

P. Bonaventure, Kiev S. Ly, T. Lovenberg, 2010, Bioorganic & medicinal chemistry letters.

Indole- and benzothiophene-based histamine H3 antagonists.

Cheryl A. Grice, T. Lovenberg, N. Carruthers, 2010, Bioorganic & medicinal chemistry letters.

2-Aryloxymethylmorpholine histamine H(3) antagonists.

P. Bonaventure, Kiev S. Ly, N. Carruthers, 2008, Bioorganic & medicinal chemistry letters.

Histamine H3 receptor antagonists: from target identification to drug leads.

P. Bonaventure, F. Kamme, T. Lovenberg, 2007, Biochemical pharmacology.

Transient P 2 X 7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy

Michael A. Farrell, N. Delanty, R. Conroy, 2019 .

Blockade of the brain histamine H3 receptor by JNJ-39220675: preclinical PET studies with [11C]GSK189254 in anesthetized baboon

N. Carruthers, J. Fowler, J. Logan, 2012, Psychopharmacology.

Orexin Receptor Antagonists

M. Letavic, B. Shireman, 2017 .

In vitro microbiological characterization of a novel azalide, two triamilides and an azalide ketal against bovine and porcine respiratory pathogens.

B. Yang, M. Letavic, N. A. Evans, 2004, The Journal of antibiotics.

Preclinical pharmacokinetics and metabolism of 6‐(4‐(2,5‐difluorophenyl)oxazol‐5‐yl)‐3‐isopropyl‐[1,2,4]‐triazolo[4,3‐a]pyridine, a novel and selective p38α inhibitor: identification of an active metabolite in preclinical species and human liver microsomes

A. Kalgutkar, E. Choo, K. McClure, 2006, Biopharmaceutics & drug disposition.

Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

T. Lovenberg, N. Carruthers, Hong Ao, 2016, Journal of medicinal chemistry.

Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.

P. Bonaventure, J. A. Jablonowski, Kiev S. Ly, 2007, Bioorganic & medicinal chemistry letters.

Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.

Kiev S. Ly, Sandy J. Wilson, T. Lovenberg, 2007, Bioorganic & medicinal chemistry letters.

Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.

P. Bonaventure, Kiev S. Ly, T. Lovenberg, 2015, Journal of medicinal chemistry.

Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia

P. Bonaventure, T. Lovenberg, N. Carruthers, 2015, The Journal of Pharmacology and Experimental Therapeutics.

P2X7 antagonists as potential therapeutic agents for the treatment of CNS disorders.

A. Bhattacharya, J. Rech, M. Letavic, 2014, Progress in medicinal chemistry.

Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists.

P. Bonaventure, C. Dvorak, T. Lovenberg, 2011, European journal of pharmacology.

PET Imaging of the P2X7 Ion Channel with a Novel Tracer [18F]JNJ-64413739 in a Rat Model of Neuroinflammation

Tamara Berdyyeva, H. Kolb, Wei Zhang, 2019, Molecular Imaging and Biology.

Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.

P. Bonaventure, N. Carruthers, Hong Ao, 2015, Bioorganic & medicinal chemistry letters.

Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists.

N. Carruthers, Hong Ao, A. Bhattacharya, 2015, ACS medicinal chemistry letters.

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

F. Lombardo, A. Kalgutkar, E. Laird, 2006, Bioorganic & medicinal chemistry letters.

Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.

J. A. Jablonowski, Kiev S. Ly, Sandy J. Wilson, 2007, Bioorganic & medicinal chemistry letters.

Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy

Donncha F. O’Brien, Michael A. Farrell, N. Delanty, 2016, The Journal of Neuroscience.

The evolution of P2X7 antagonists with a focus on CNS indications.

A. Bhattacharya, B. Savall, J. Rech, 2016, Bioorganic & medicinal chemistry letters.

Preclinical Evaluation of a P2X7 Receptor–Selective Radiotracer: PET Studies in a Rat Model with Local Overexpression of the Human P2X7 Receptor and in Nonhuman Primates

W. Vanduffel, G. Bormans, X. Langlois, 2016, The Journal of Nuclear Medicine.

P2X7 receptor antagonists for the treatment of systemic inflammatory disorders.

A. Bhattacharya, Christine F Gelin, M. Letavic, 2020, Progress in medicinal chemistry.

Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia

M. Papp, T. Lovenberg, N. Carruthers, 2018, Neuropsychopharmacology.

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

P. Bonaventure, C. Dvorak, T. Lovenberg, 2017, Journal of medicinal chemistry.

Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.

N. Carruthers, Hong Ao, A. Bhattacharya, 2016, Bioorganic & medicinal chemistry letters.

A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334.

P. Bonaventure, T. Lovenberg, N. Carruthers, 2015, European journal of pharmacology.

Neuropharmacology and analgesia A novel radioligand for the ATP-gated ion channel P 2 X 7 : [ 3 H ] JNJ-54232334

P. Bonaventure, T. Lovenberg, N. Carruthers, 2015 .

Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

P. Bonaventure, N. Carruthers, Hong Ao, 2013, ACS medicinal chemistry letters.

Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists.

P. Bonaventure, T. Lovenberg, N. Carruthers, 2016, ACS chemical neuroscience.

Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models

D. Henshall, T. Engel, W. Fischer, 2016, PloS one.

JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats

E. Levin, P. Bonaventure, T. Lovenberg, 2011, Psychopharmacology.

Pharmacological characterization of JNJ-28583867, a histamine H(3) receptor antagonist and serotonin reuptake inhibitor.

P. Bonaventure, Sandy J. Wilson, T. Lovenberg, 2007, European journal of pharmacology.

Correlation of the structure of chiral o,o′-bisphenol-Ti(IV) complexes with ligand electronic effects. A relationship between Lewis acidity and angle strain

E. Corey, S. Sarshar, M. C. Noe, 1994 .

Microwave assisted, palladium catalyzed aminocarbonylations of heteroaromatic bromides using solid Mo(CO)6 as the carbon monoxide source

Kiev S. Ly, M. Letavic, 2007 .

ENANTIOSELECTIVE TOTAL SYNTHESIS OF GRACILINS B AND C USING CATALYTIC ASYMMETRIC DIELS-ALDER METHODOLOGY

E. Corey, M. Letavic, 1995 .

Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase.

Dennis E Danley, P. Lemotte, M. Mansour, 2005, Journal of medicinal chemistry.

Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.

P. Bonaventure, Kiev S. Ly, Sandy J. Wilson, 2008, Bioorganic & medicinal chemistry letters.

Recent medicinal chemistry of the histamine H3 receptor.

C. Dvorak, N. Carruthers, Michael A Letavic, 2006, Progress in medicinal chemistry.

Asymmetric induction in reactions of styrenes with 1,4-benzoquinones utilizing chiral titanium(IV) complexes

T. Engler, M. Letavic, J. Reddy, 1991 .

Assymetric quinone-based Deils-Alder reactions

T. Engler, F. Takusagawa, M. Letavic, 1992 .

Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors.

Dennis E Danley, D. Danley, G. Schulte, 2002, Bioorganic & medicinal chemistry letters.

Competitive binding assays for high-affinity binders in the presence of endogenous ligands: application to biotin-binding proteins.

M. Letavic, H. B. White, T. McGahan, 1991, Analytical biochemistry.

Stereoselective syntheses of three different classes of neolignans from the same starting materials

T. Engler, M. Letavic, D. Wei, 1993 .

microRNA targeting of the P2X7 purinoceptor opposes a contralateral epileptogenic focus in the hippocampus

E. Jimenez-Mateos, C. Mooney, D. Henshall, 2015, Scientific Reports.

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

C. Dvorak, N. Carruthers, A. Bhattacharya, 2018, Journal of medicinal chemistry.

Asymmetric Reactions of 2-Methoxy-1,4-benzoquinones with Styrenyl Systems: Enantioselective Syntheses of 8-Aryl-3-methoxybicyclo[4.2.0]oct-3-en-2,5-diones, 7-Aryl-3-hydroxybicyclo[3.2.1]oct-3-en-2,8-diones, 2-Aryl-6-methoxy-2,3-dihydrobenzofuran-5-ols, and Pterocarpans

T. Engler, R. Iyengar, M. Letavic, 1999 .

Synthesis and activity of a novel class of tribasic macrocyclic antibiotics: the triamilides.

Jeffrey M. Casavant, Hengmiao Cheng, M. Letavic, 2002, Bioorganic & medicinal chemistry letters.

Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ‐47965567

P. Bonaventure, T. Lovenberg, Hong Ao, 2013, British journal of pharmacology.

Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.

T. Lovenberg, N. Carruthers, S. Bembenek, 2008, Bioorganic & medicinal chemistry.

Benzimidazolone p38 inhibitors.

C. Gabel, T. Carty, John T Barberia, 2004, Bioorganic & medicinal chemistry letters.

Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition.

L. Xing, S. Selness, H. Shieh, 2010, Bioorganic & medicinal chemistry letters.

Molecular mechanism and structural basis of small-molecule modulation of the gating of acid-sensing ion channel 1

R. DesJarlais, D. Lin, Robyn Miller, 2021, Communications Biology.

Blockade of the brain histamine H3 receptor by JNJ-39220675: preclinical PET studies with [11C]GSK189254 in anesthetized baboon

N. Carruthers, J. Fowler, J. Logan, 2012, Psychopharmacology.

Pharmacology of a Novel Central Nervous System–Penetrant P2X7 Antagonist JNJ-42253432

P. Bonaventure, T. Lovenberg, N. Carruthers, 2014, The Journal of Pharmacology and Experimental Therapeutics.

Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice

P. Bonaventure, T. Lovenberg, C. Dugovic, 2017, Frontiers in Behavioral Neuroscience.

In-vitro and in-vivo characterization of JNJ-7925476, a novel triple monoamine uptake inhibitor.

Brian Lord, Leah Aluisio, Pascal Bonaventure, 2008, European journal of pharmacology.

Preclinical Evaluation and Nonhuman Primate Receptor Occupancy Study of 18F-JNJ-64413739, a PET Radioligand for P2X7 Receptors

H. Kolb, Wei Zhang, A. Bhattacharya, 2019, The Journal of Nuclear Medicine.

Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.

P. Bonaventure, Kiev S. Ly, T. Lovenberg, 2015, ACS Medicinal Chemistry Letters.

Histamine H3 antagonists as wake-promoting and pro-cognitive agents.

M. Letavic, E. Stocking, 2008, Current topics in medicinal chemistry.

Design, Synthesis and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.

T. Koudriakova, K. Coe, Xiaohui Jiang, 2020, Journal of medicinal chemistry.

Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors.

Chul Yu, Mark C. Noe, Lisa M. Reeves, 2003, Bioorganic & medicinal chemistry letters.

1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.

N. Carruthers, T. Koudriakova, K. Coe, 2019, ACS medicinal chemistry letters.

Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.

C. Dvorak, N. Carruthers, J. Alcázar, 2023, Journal of medicinal chemistry.

PET Imaging of the P2X7 Ion Channel with a Novel Tracer [18F]JNJ-64413739 in a Rat Model of Neuroinflammation

Tamara Berdyyeva, H. Kolb, Wei Zhang, 2019, Molecular Imaging and Biology.