Universiteit Antwerpen

Universiteit Gent

Vib Vzw

Other

Fox Chase Cancer Center

Universitair Ziekenhuis Antwerpen

Shakturana Cv

Heeres, Jan

Koen Augustyns

Pieter Van Der Veken

Jurgen Joossens

Peter Vandenabeele

Paul Cos

Benedicte Yvonne De Winter

Hannah Ceuleers

Hanne Van Spaendonk

Tom Vanden Berghe

Sam Hofmans

Cedric Joossen

Jan Heeres

Paulus Joannes Lewi

Viktor Magdolen

Christel Vangestel

Sigrid Stroobants

Wim Martinet

Anne-Marie Lambeir

Jeroen Van Soom

Lars Devisscher

Venkatraj Muthusamy

Kevin Karel Florentina Arien

Guido Louis Emile Vanham

Koen Jansen

Matthias Cleenewerck

Ingrid De Meester

Leen Heirbaut

Achiel Haemers

Guido R Y De Meyer

Jonathan D Cheng

Anne-Marie Virginie Renée Lambeir

Ammar Kurdi

Simon Scharpé

Guido RY De Meyer

Kevin Karel Florentina ARIËN

The present invention relates to compounds for use in the prevention and/or treatment of PAR-related diseases, such as for example: pain and ocular disorders. More in particular, the present invention provides bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of pancreatitis-related pain, IBS (irritable bowel syndrome), IBD (inflammatory bowel disease), dry eye disease and conjunctivitis sicca. These inhibitors were found to have a different inhibitory profile compared to diphenyl guanidinophenylethylphosphonates leading to a more pronounced effect on these conditions.

Bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of PAR-related diseases

The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.

3-(benzylamino)-4-(cyclohexylamino)-n-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 analogues as cell death inhibitors for treating e.g. stroke

The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer. Halogenated benzotropolones described here are of formula 

Halogenated benzotropolones as ATG4B inhibitors

The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.

KLK4 inhibitors

This disclosure relates to a novel class of compounds having the structure of formula I as defined herein and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. This disclosure also comprises methods of treating a subject by administering a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof to the subject. These compounds are useful for the conditions disclosed herein. This disclosure further comprises methods for making the compounds of formula I and corresponding intermediates.

3,4-diaminobenzenesulfonamide derivatives for inhibiting cell death

The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.

Triazines with suitable spacers for treatment and/or prevention of HIV infections

The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders. 

FAP inhibitors

The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis.

Urokinase inhibitors

Growing community of inventors

Hoogstraten, Belgium

Koen Augustyns