The title compounds I [A = alkyl, cyanoalkyl, aryl, etc.; B = absent, O, S, SO, SO2, NH, N(H)​CO; R = (un)​substituted aryl, heteroaryl, heterocycle] and pharmaceutically acceptable salts thereof, able to activate efficaciously the AMPK enzymic complex, and therefore useful in the prophylaxis and therapeutic treatment of diseases and disorders in particular metabolic disorders, such as diabetes and obesity, immune-​mediated inflammatory pathologies and cancer, were prepared and​/or claimed. E.g., a 2-​step synthesis of (2-​(cyanomethyl)​-​1,​3-​dioxoisoindolin-​5-​yl)​benzamide, starting from 5-​aminoisoindoline-​1,​3-​dione and benzoyl chloride, was described. Exemplified compounds I were tested for AMPK activation in the C2C12 cell line (data given)​. Pharmaceutical composition comprising compound I was disclosed.

Preparation of isoindoline derivatives for use as AMPK activators

Antonioli, Luca;Fornai, Matteo;Blandizzi, Corrado;La Motta, Concettina
2018-01-01

Abstract

The title compounds I [A = alkyl, cyanoalkyl, aryl, etc.; B = absent, O, S, SO, SO2, NH, N(H)​CO; R = (un)​substituted aryl, heteroaryl, heterocycle] and pharmaceutically acceptable salts thereof, able to activate efficaciously the AMPK enzymic complex, and therefore useful in the prophylaxis and therapeutic treatment of diseases and disorders in particular metabolic disorders, such as diabetes and obesity, immune-​mediated inflammatory pathologies and cancer, were prepared and​/or claimed. E.g., a 2-​step synthesis of (2-​(cyanomethyl)​-​1,​3-​dioxoisoindolin-​5-​yl)​benzamide, starting from 5-​aminoisoindoline-​1,​3-​dione and benzoyl chloride, was described. Exemplified compounds I were tested for AMPK activation in the C2C12 cell line (data given)​. Pharmaceutical composition comprising compound I was disclosed.
2018
File in questo prodotto:
File Dimensione Formato  
Patent_AMPK_Isoindoline.pdf

accesso aperto

Descrizione: Brevetto depositato
Tipologia: Documento in Post-print
Licenza: Tutti i diritti riservati (All rights reserved)
Dimensione 165.67 kB
Formato Adobe PDF
165.67 kB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/958131
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact