Remynd Nv

Katholieke Universiteit Leuven

Katrien Princen

Hasane Ratni

Gerard Griffioen

Mark Rogers-Evans

Matthias Heinrich Nettekoven

Koen De Witte

Walter Vifian

Emilie Blanche

Bart De Taeye

Johan Gerard Griffioen

Giuseppe Cecere

Patrick Chaltin

Amuri Kilonda

Sara Allasia

Arnaud Didier Marie Marchand

Tom Francois L Van Dooren

Tom François L Van Dooren

Arnaud Didier Marchand

Tom Francois Van Dooren

The present provides compounds and methods for preventing and/or treating epilepsy and/or neurodegenerative disorders. More particularly, the invention provides inhibitors of PDE6δ for use in the prevention and/or treatment of neurodegenerative disorders and/or epilepsy.

Inhibitors of PDE6Delta for use in the prevention and/or treatment of epilepsy and/or neurodegenerative disorders

The present invention relates to a compound of formula (I) or a tautomer thereof, wherein R, R, R, Rand R, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of epilepsy and/or neurodegenerative diseases.

Compounds for the treatment of epilepsy, neurodegenerative disorders and other CNS disorders

The present invention relates to a compound of formula (I) or a tautomer thereof, wherein R, R, R, Rand R, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of epilepsy and/or neurodegenerative diseases. 

The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R, R, R, L, L, L, L, Land n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders. 

Oxadiazole compounds

The present invention relates to a compound of formula (IA), wherein Gis lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is &#x2014;NRR; Ris hydrogen or lower alkyl; Ris lower alkyl; tetrahydropyran-4-yl; &#x2014;CH-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or Rand Rform together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is &#x2014;CH&#x2014; or &#x2014;(CH)&#x2014;; Ar is phenyl or pyridinyl; Ris halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. 

Piperazine thiazole derivatives useful in the treatment of tauopathies such as Alzheimer's disease

The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R, R, R, L, L, L, L, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders. 

2,7-diazaspiro[3.5]nonane compounds

The present invention relates to a compound of formula (IA), wherein Gis lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is &#x2014;NRR; Ris hydrogen or lower alkyl; Ris lower alkyl; tetrahydropyran-4-yl; &#x2014;CH-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or Rand Rform together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is &#x2014;CH&#x2014;or &#x2014;(CH)&#x2014;; Ar is phenyl or pyridinyl; Ris halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. 

Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease

The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. 

Growing community of inventors

Heverlee, Belgium

Katrien Princen