Indole derivatives for the prevention and/or treatment of diabetes and associated metabolic disorders
AssigneesConsejo Superior De Investigaciones Cientificas (Csic), Centro De InvestigacióN BioméDica En Red (Ciber)
InventorsAna Castro Morera, Pascual Sanz Bigorra, Marta Vela Ruiz, Maria Adelaida Garcia Gimeno
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Abstract
The invention relates to substituted heterocyclic indole derivatives of Formula (I), which act as activators of the AMP-activated protein kinase (AMPK) and to the use of them for the treatment and prevention of diseases or disorders regulated by AMPK. As a result, these compounds can be used for the treatment of inflammatory, autoimmune, cardiovascular, neurological diseases and cancer.
Claims17
A method for the treatment and/or prevention of a disease, disorder, or prophylaxis mediated by the AMPK enzyme comprising administering to a person in need thereof a compound of formula (I),
- its pharmaceutically acceptable salts, solvates., and hydrates where,
- A is selected from between 5- or 6-membered phenyl or heteroaryl containing a heteroatom selected from between nitrogen and oxygen,
- R1 is selected from among hydrogen, benzyl and 2-(3-hydroxypyridyl)methyl;
- R2, R3 and R4 are independently selected from among hydrogen, C1-C18 alkyl, C3-C10 cycloalkyl, C2-C10 heterocycloalkyl, C2-C18 alkenyl, hydroxyl, C1-C6-O-alkyl, optionally substituted C7-C12-O-aralkyl, —NRaRb, —NCORa, —CO2Ra, —CONRaRb, halogen, —CN, —NO2, —CORa, C6-C18 aryl and optionally substituted C4-C18 heteroaryl,
- with the condition that at least one of R2, R3 or R4 is different from hydrogen when A is phenyl;
- and
- Ra and Rb are independently selected from among hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C2-C7 heterocycloalkyl, C2-C18 alkenyl, C5-C18 aryl and optionally substituted C4-C18 heteroaryl, Ra and Rb can form a C3-C7 carbocycle.
A compound of formula (II),
- its pharmaceutically acceptable salts, hydrates and solvates where,
- R1 is selected from among hydrogen, benzyl and 2-(3-hydroxypyridyl)methyl;
- R5, R6 and R7 are independently selected from among hydrogen, C3-C10 cycloalkyl, C2-C10 heterocyclolkyl, hydroxyl, optionally substituted C7-C12-O-aralkyl, —NRaRb, —NCORa, —CO2Ra, —CONRaRb, —CN, —NO2, C5-C18 aryl and optionally substituted C4-C18 heteroaryl,
- with the condition that at least one of R5, R6 or R7 is different from hydrogen;
- Ra and Rb are independently selected from among hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C2-C7 heterocycloalkyl, C2-C18 alkenyl, C5-C18 aryl and optionally substituted C4-C18 heteroaryl;
- and
- Ra and Rb can form a C3-C7 carbocycle.
(canceled)
Dependencies are inferred from the claim text.