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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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. |
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