H. Borghys

发表

Preclinical assessment of the feasibility of applying controlled release oral drug delivery to a lead series of atypical antipsychotics.

A. Megens, W. van Osdol, J. Scicinski, 2006, Journal of pharmaceutical sciences.

Dog model with implanted pump to test boosters for antiretroviral medication.

L. Baert, T. Jonckers, G. Van den Mooter, 2008, International journal of pharmaceutics.

Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus.

J. Vlach, F. Pauwels, E. Arnoult, 2016, Journal of medicinal chemistry.

A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators.

M. Mercken, F. De Ridder, L. Dillen, 2012, Journal of Alzheimer's disease : JAD.

Lipophilic nalmefene prodrugs to achieve a one-month sustained release.

J. Leysen, A. Megens, P. Herdewijn, 2016, Journal of controlled release : official journal of the Controlled Release Society.

Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators.

G. Macdonald, G. Tresadern, M. Mercken, 2012, Journal of medicinal chemistry.

Comparison of two different methods for measurement of amyloid-β peptides in cerebrospinal fluid after BACE1 inhibition in a dog model.

M. Mercken, T. Jacobs, L. Dillen, 2013, Journal of Alzheimer's disease : JAD.

JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.

D. Moechars, K. Kusakabe, L. Leclercq, 2021, Journal of medicinal chemistry.

Direct nose to brain delivery of small molecules: critical analysis of data from a standardized in vivo screening model in rats

R. Vreeken, Frederik J. R. Rombouts, A. Bottelbergs, 2020, Drug delivery.

Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.

F. Pauwels, T. Jonckers, E. Arnoult, 2017, Journal of medicinal chemistry.

1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.

Ó. Delgado, Michiel Van Gool, J. M. Alonso, 2015, Journal of medicinal chemistry.

Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators.

G. Macdonald, M. Mercken, S. Samanta, 2019, Bioorganic & medicinal chemistry letters.

Anilinotriazoles as potent gamma secretase modulators.

G. Macdonald, G. Tresadern, M. Mercken, 2014, Bioorganic & medicinal chemistry letters.

Preparation and physicochemical characterization of biodegradable nerve guides containing the nerve growth agent sabeluzole.

Joel Rosenblatt, Theo Meert, Jef Adriaensen, 2005, Biomaterials.

Pharmacokinetics and Disposition of Rilpivirine (TMC278) Nanosuspension as a Long-Acting Injectable Antiretroviral Formulation

Lieven Baert, L. Baert, M. Bouche, 2010, Antimicrobial Agents and Chemotherapy.

BACE1 Inhibition Induces a Specific Cerebrospinal Fluid β-Amyloid Pattern That Identifies Drug Effects in the Central Nervous System

K. Blennow, M. Mercken, H. Zetterberg, 2012, PloS one.

APLP1 as a cerebrospinal fluid biomarker for γ-secretase modulator treatment

K. Blennow, M. Mercken, H. Zetterberg, 2015, Alzheimer's Research & Therapy.

Young to Middle-Aged Dogs with High Amyloid-β Levels in Cerebrospinal Fluid are Impaired on Learning in Standard Cognition tests

T. Jacobs, B. Van Broeck, T. Erkens, 2016, Journal of Alzheimer's disease : JAD.

Trifluoromethyl Dihydrothiazine‐Based β‐Secretase (BACE1) Inhibitors with Robust Central β‐Amyloid Reduction and Minimal Covalent Binding Burden

K. Kusakabe, Shinji Suzuki, Y. Kido, 2019, ChemMedChem.

Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.

K. Blennow, M. Mercken, H. Zetterberg, 2010, Journal of Alzheimer's disease : JAD.

A translational assessment of preclinical versus clinical tools for the measurement of cardiac contractility: comparison of LV dP/dt(max) with echocardiography in telemetry implanted beagle dogs.

H. Geys, F. Cools, D. Gallacher, 2014, Journal of pharmacological and toxicological methods.

Correlations between Factors Determining the Pharmacokinetics and Antiviral Activity of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors of the Diaryltriazine and Diarylpyrimidine Classes of Compounds

A. D. Clark, E. Arnold, F. Daeyaert, 2004, Drugs in R&D.

Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.

Michiel Van Gool, G. Macdonald, D. Moechars, 2018, Journal of medicinal chemistry.

Use of the Actiwatch-Mini® in dog safety studies as an early indicator for drug-induced behavioural changes.

F. Cools, I. Kopljar, H. Borghys, 2020, Journal of pharmacological and toxicological methods.

Discovery of an Extremely Potent Thiazine-Based β-Secretase (BACE1) Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.

K. Kusakabe, Shinji Suzuki, N. Asada, 2019, Journal of medicinal chemistry.

APLP1 as a cerebrospinal fluid biomarker for γ-secretase modulator treatment

K. Blennow, M. Mercken, H. Zetterberg, 2015, Alzheimer's Research & Therapy.

A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators.

M. Mercken, F. De Ridder, L. Dillen, 2012, Journal of Alzheimer's disease : JAD.

Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.

Kenji Nakahara, Takahiko Yamamoto, K. Kusakabe, 2018, Journal of medicinal chemistry.

Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.

K. Kusakabe, Y. Kido, T. Fukushima, 2018, Journal of medicinal chemistry.

PRECLINICAL MULTI-SPECIES PHARMACOKINETIC/PHARMACODYNAMIC ANALYSIS OF THE ORAL BACE INHIBITOR JNJ-54861911

Y. Nakajima, G. Sakaguchi, H. Borghys, 2017, Alzheimer's & Dementia.