3-PHENYL-1-BENZOTHIOPHENE-2-CARBOXYLIC ACID DERIVATIVES AS BRANCHED-CHAIN ALPHA KETO ACID DEHYDROGENASE KINASE INHIBITORS FOR THE TREATMENT OF DIABETES, KIDNEY DISEASES, NASH AND HEART FAILURE

The present invention refers to compounds of Formula (I) as branched-chain alpha keto acid dehydrogenase kinase inhibitors and/or degraders for the treatment of e.g. diabetes, kidney diseases, NASH and heart failure. Preferred compounds are e.g. 3-phenyl-1-benzothiophene-2- carboxylic acid derivativ...

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Hauptverfasser: O'' Keefe CAMERON Kimberly, GRIFFITH David Andrew, REESE Matthew Richard, FILIPSKI Kevin James, BUZON Leanne Marie, KORMOS Bethany Lyn, DEBOYACE Kevin Francis, MARTINEZ ALSINA Luis Angel, LIU Shenping, ZHANG Yuan, ROTH FLACH Rachel Jane
Format: Patent
Sprache:eng ; spa
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Zusammenfassung:The present invention refers to compounds of Formula (I) as branched-chain alpha keto acid dehydrogenase kinase inhibitors and/or degraders for the treatment of e.g. diabetes, kidney diseases, NASH and heart failure. Preferred compounds are e.g. 3-phenyl-1-benzothiophene-2- carboxylic acid derivatives. An exemplary compound is e.g. 3-(5,7-difluoro-3,4-dihydro-2H-1- benzopyran-6-yl)-6-fluoro-1-benzothiophene-2-carboxylic acid (example 1) The present application discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof. La presente invención se refiere a compuestos de la Fórmula (I) (ver Fórmula) Fórmula I como inhibidores y/o degradadores de alfa cetoácido deshidrogenasa quinasa de cadena ramificada, para el tratamiento de, por ejemplo diabetes, enfermedad renal, NASH e insuficiencia cardíaca; son compuestos preferidos, por ejemplo, derivados de ácido 3-fenil-1-benzotiofeno-2-carboxílico; un compuesto ilustrativo es, por ejemplo, ácido 3-(5,7-difluoro-3,4-d ihidro-2H-1-benzopiran-6-il)-6-fluoro-1-benzotiofeno-2-carboxílic o (ejemplo 1); (ver Fórmula) la presente solicitud divulga la síntesis y caracterización de compuestos ilustrativos, así como sus datos farmacológicos.