Remynd Nv

Katholieke Universiteit Leuven, Ku Leuven R&d

Remynd

Nv Remynd

K. U. Leuven R&d Remynd

Katholieke Universiteit Levun

Katholieke Universiteit Leuven

Gerard Griffioen

Hasane Ratni

Katrien Princen

Tom Van Dooren

Mark Rogers-Evans

Arnaud Marchand

Patrick Chaltin

Amuri Kilonda

Matthias Heinrich Nettekoven

Sara Allasia

Veronica Rojas De La Parra

Walter Vifian

Koen De Witte

Emilie Blanche

Bart De Taeye

Giuseppe Cecere

Stefaan Wera

Hein Roger Duhamel

Ellen Gommé

Nele Van Damme

Verónica Rojas De La Parra

Sara Alassia

Annick Lauwers

Kristel Marie Edith Coupet

Ingrid Van Der Auwera

Marleen Lox

Tine Decruy

Ellen Gomme

Kristel Marie Coupet

Matthias Nettekoven

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

This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic &#x3b1;-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

Indole amide derivatives and related compounds for use in the treatment of neurodegenerative diseases

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

This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic &#x3b1;-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R, R, R, R, R, E, n, Y, Y, Y, Y, Y, B, R, and m are as defined in the claims. 

Compounds for the treatment of neurodegenerative diseases

This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic &#x3b1;-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R, R, R, R, E, n, Y, Y, Y, Y, Y, L, B, R, and m are as defined in the claims. 

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. 

1, 2, 4-thiadiazol-5-ylpiperazine derivatives useful in the treatment of neurodegenerative diseases

This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an &#x3b1;-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients.

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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic &#x3b1;-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. 

This invention provides specifically substituted 1,2,4-thiadiazole derivatives for use in the treatment of an &#x3b1;-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides various methods for producing such substituted 1,2,4-thiadiazole derivatives.

Thiadiazole derivatives for the treatment of neurodegenerative diseases

The invention provides novel 1,2,4-thiadiazole derivatives useful for preventing or treating an &#x3b1;-synucleopathy such as Parkinson's disease, as well as pharmaceutical compositions including them as biologically active ingredients, and methods for manufacturing them. 

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Linden, Belgium

Gerard Griffioen