4-FLUORO-(4-(4-BENZYL)PIPERIDIN-1-YL)(2-(PYRIMIDIN-4-YL)PYRIDIN-3-YL)METHANONE DERIVATIVES AND SIMILAR COMPOUNDS AS CYP46A1 INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS

The present invention refers to 4-Fluoro-(4-(4-Benzyl)piperidin-l-yl) (2-(pyrimidin-4-yl)pyridin-3-yl)methanone derivatives and similar compounds of formula (I) as CYP46A1 inhibitors for the treatment of neurodegenerative disorders, epilepsy, developmental and epileptic encephalopathies, psychiatric...

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Hauptverfasser: HOPPER, ALLEN TAYLOR, LA, DANIEL, BLANCO-PILLADO, MARIA-JESUS, MISCHKE, STEVEN
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LA, DANIEL
BLANCO-PILLADO, MARIA-JESUS
MISCHKE, STEVEN
description The present invention refers to 4-Fluoro-(4-(4-Benzyl)piperidin-l-yl) (2-(pyrimidin-4-yl)pyridin-3-yl)methanone derivatives and similar compounds of formula (I) as CYP46A1 inhibitors for the treatment of neurodegenerative disorders, epilepsy, developmental and epileptic encephalopathies, psychiatric disorders, and spasms; Neurodegenerative disorders such as e.g. Alzheimer's disease, mild cognitive impairment, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, cerebral infarction, glaucoma, and multiple sclerosis; Psychiatric disorders such as e.g. schizophrenia, autism spectrum disorder, delusional disorder, schizoaffective disorder, and depression. An exemplary compound is e.g. (4-fluoro-4-(4-fluorobenzyl) piperidin-l-yl)(2-(py rim idin-4-yl)py rid in-3-y I) methanone (example 3, compound 1). La présente invention concerne des dérivés de 4-fluoro-(4-(4-benzyl)pipéridin-1-yl)(2- (pyrimidin-4-yl)pyridin-3-yl)méthanone et des composés similaires de formule (I) utilisés en tant qu'inhibiteurs de CYP46A1 pour le traitement d'affections neurodégénératives, de l'épilepsie, des encéphalopathies du développement et épileptiques, des troubles psychiatriques et des spasmes; d'affections neurodégénératives telles que la maladie d'Alzheimer, le déficit cognitif léger, la chorée de Huntington, la maladie de Parkinson, la sclérose latérale amyotrophique, les lésions cérébrales traumatiques, l'infarctus cérébral, le glaucome et la sclérose en plaques; de troubles psychiatriques tels que la schizophrénie, les troubles du spectre autistique, les troubles délirants, les troubles schizo-affectifs et la dépression. Un composé donné à titre d'exemple est, par exemple, la (4-fluoro-4-(4-fluorobenzyl)pipéridin-1-yl)(2-(pyrimidin-4-yl)pyridin-3-yI)méthanone (exemple 3, composé 1).
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An exemplary compound is e.g. (4-fluoro-4-(4-fluorobenzyl) piperidin-l-yl)(2-(py rim idin-4-yl)py rid in-3-y I) methanone (example 3, compound 1). La présente invention concerne des dérivés de 4-fluoro-(4-(4-benzyl)pipéridin-1-yl)(2- (pyrimidin-4-yl)pyridin-3-yl)méthanone et des composés similaires de formule (I) utilisés en tant qu'inhibiteurs de CYP46A1 pour le traitement d'affections neurodégénératives, de l'épilepsie, des encéphalopathies du développement et épileptiques, des troubles psychiatriques et des spasmes; d'affections neurodégénératives telles que la maladie d'Alzheimer, le déficit cognitif léger, la chorée de Huntington, la maladie de Parkinson, la sclérose latérale amyotrophique, les lésions cérébrales traumatiques, l'infarctus cérébral, le glaucome et la sclérose en plaques; de troubles psychiatriques tels que la schizophrénie, les troubles du spectre autistique, les troubles délirants, les troubles schizo-affectifs et la dépression. 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An exemplary compound is e.g. (4-fluoro-4-(4-fluorobenzyl) piperidin-l-yl)(2-(py rim idin-4-yl)py rid in-3-y I) methanone (example 3, compound 1). La présente invention concerne des dérivés de 4-fluoro-(4-(4-benzyl)pipéridin-1-yl)(2- (pyrimidin-4-yl)pyridin-3-yl)méthanone et des composés similaires de formule (I) utilisés en tant qu'inhibiteurs de CYP46A1 pour le traitement d'affections neurodégénératives, de l'épilepsie, des encéphalopathies du développement et épileptiques, des troubles psychiatriques et des spasmes; d'affections neurodégénératives telles que la maladie d'Alzheimer, le déficit cognitif léger, la chorée de Huntington, la maladie de Parkinson, la sclérose latérale amyotrophique, les lésions cérébrales traumatiques, l'infarctus cérébral, le glaucome et la sclérose en plaques; de troubles psychiatriques tels que la schizophrénie, les troubles du spectre autistique, les troubles délirants, les troubles schizo-affectifs et la dépression. 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An exemplary compound is e.g. (4-fluoro-4-(4-fluorobenzyl) piperidin-l-yl)(2-(py rim idin-4-yl)py rid in-3-y I) methanone (example 3, compound 1). La présente invention concerne des dérivés de 4-fluoro-(4-(4-benzyl)pipéridin-1-yl)(2- (pyrimidin-4-yl)pyridin-3-yl)méthanone et des composés similaires de formule (I) utilisés en tant qu'inhibiteurs de CYP46A1 pour le traitement d'affections neurodégénératives, de l'épilepsie, des encéphalopathies du développement et épileptiques, des troubles psychiatriques et des spasmes; d'affections neurodégénératives telles que la maladie d'Alzheimer, le déficit cognitif léger, la chorée de Huntington, la maladie de Parkinson, la sclérose latérale amyotrophique, les lésions cérébrales traumatiques, l'infarctus cérébral, le glaucome et la sclérose en plaques; de troubles psychiatriques tels que la schizophrénie, les troubles du spectre autistique, les troubles délirants, les troubles schizo-affectifs et la dépression. Un composé donné à titre d'exemple est, par exemple, la (4-fluoro-4-(4-fluorobenzyl)pipéridin-1-yl)(2-(pyrimidin-4-yl)pyridin-3-yI)méthanone (exemple 3, composé 1).</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 4-FLUORO-(4-(4-BENZYL)PIPERIDIN-1-YL)(2-(PYRIMIDIN-4-YL)PYRIDIN-3-YL)METHANONE DERIVATIVES AND SIMILAR COMPOUNDS AS CYP46A1 INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS
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