B. Heckmann

发表

Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.

T. Christophe, C. Menet, B. Allart, 2021, Journal of medicinal chemistry.

BMP-7 inhibits TGF-β-induced invasion of breast cancer cells through inhibition of integrin β3 expression

E. Danen, H. van Dam, T. van Laar, 2011, Cellular Oncology.

Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.

J. Steyaert, N. Triballeau, K. Conrath, 2017, Journal of medicinal chemistry.

Targeting of α(v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer.

J. Feyen, G. van der Pluijm, J. Buijs, 2011, Neoplasia.

Autotaxin facilitates selective LPA receptor signaling

A. Perrakis, W. Moolenaar, Fernando Salgado-Polo, 2022, bioRxiv.

Pharmacological profile and efficacy of GLPG1690, a novel ATX inhibitor for COPD treatment

S. Dupont, N. Desroy, R. Blanqué, 2015 .

Inhibition of Autotaxin with GLPG1690 Increases the Efficacy of Radiotherapy and Chemotherapy in a Mouse Model of Breast Cancer

M. Wuest, F. Wuest, Jennifer Dufour, 2019, Molecular Cancer Therapeutics.

Safety, Pharmacokinetics, and Pharmacodynamics of the Autotaxin Inhibitor GLPG1690 in Healthy Subjects: Phase 1 Randomized Trials

S. Dupont, E. M. van der Aar, J. Desrivot, 2019, Journal of clinical pharmacology.

Sulfonylureas and sulfonylcarbamates as new non-tetrazole angiotensin II receptor antagonists. Discovery of a highly potent orally active (imidazolylbiphenylyl)sulfonylurea (HR 720).

H. Heitsch, M. Fortin, G. Hamon, 1995, Journal of medicinal chemistry.

Oxidative decarboxylation of mandelate ethers and α-substituted phenylacetates via dioxetanone generation

S. Chandrasekhar, J. Falck, C. Mioskowski, 1992 .

Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fib

N. Triballeau, M. Lamers, B. Hrvačić, 2017, Journal of medicinal chemistry.

CHIRAL ACETALS : STEREOCONTROLLED SYNTHESES OF 16-,17-, AND 18-HYDROXYEICOSATETRAENOIC ACIDS, CYTOCHROME P-450 ARACHIDONATE METABOLITES

J. Falck, J. Capdevila, C. Mioskowski, 1996 .

Chiral Acetals: Stereocontrolled Syntheses of 16‐, 17‐, and 18‐ Hydroxyeicosatetraenoic Acids, Cytochrome P‐450 Arachidonate Metabolites.

J. Falck, J. Capdevila, C. Mioskowski, 2010 .

Nucleophilic substitution at the acetalic center of mandelate 1,3-dioxolan-4-ones using magnesio-copper reagents: Application to the synthesis of chiral secondary alcohols.

J. Falck, C. Mioskowski, B. Heckmann, 1992 .

Targeting of Alpha-V Integrins Reduces Malignancy of Bladder Carcinoma

G. van der Pluijm, R. Pelger, G. van der Horst, 2014, PloS one.

BMP-7 inhibits TGF-β-induced invasion of breast cancer cells through inhibition of integrin β3 expression

E. Danen, H. van Dam, T. van Laar, 2011, Cellular Oncology.

Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.

N. Triballeau, Denis Bucher, T. Christophe, 2021, Journal of medicinal chemistry.

Enantiospecific synthesis of 17- and 18-hydroxyeicosatetraenoic acids, cytochrome P450 arachidonate metabolites

J. Falck, J. Capdevila, C. Mioskowski, 1992 .

Favorable human safety, pharmacokinetics and pharmacodynamics of the autotaxin inhibitor GLPG1690, a potential new treatment in COPD

S. Dupont, J. Desrivot, Liesbeth Fagard, 2015 .

Strong reversal of the lung fibrosis disease signature by autotaxin inhibitor GLPG1690 in a mouse model for IPF

S. Dupont, M. Ongenaert, R. Blanqué, 2016 .

Grignard additions to α,β-unsaturated dioxolanones: preparation of chiral allylic alcohols and protected α-hydroxy aldehydes

J. Falck, C. Mioskowski, B. Heckmann, 1996 .

Balanced AT1 and AT2 angiotensin II antagonists. I. New orally active 5-carboxyl imidazolyl biphenyl sulfonylureas

M. Fortin, P. Deprez, A. Corbier, 1995 .

Balanced AT1 and AT2 Angiotensin II Antagonists. Part 1. New Orally Active 5-Carboxyl Imidazolyl Biphenyl Sulfonylureas

M. Fortin, P. Deprez, A. Corbier, 1996 .

Balanced AT1 and AT2 angiotensin II antagonists. II. Potent 5 α-hydroxyacid imidazolyl biphenyl sulfonylureas

M. Fortin, P. Deprez, A. Corbier, 1995 .

Balanced AT1 and AT2 angiotensin II antagonists. III. potent and orally active 5-β-ketosulfoxide imidazolyl biphenyl sulfonylureas

M. Fortin, P. Deprez, A. Corbier, 1995 .