1-oxa-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the production thereof

摘要

Disclosed is a process for production of and a compound of formula I wherein: X is a hetero atom of NRa where Ra is H or a protecting group, Y and Z are one or more substitutents linked to any available carbon atom independently selected from the list consisting of H, halogen, alkyl, alkenyl, alkynyl, halo-alkyl, hyroxy, alkoxy, trifluoromethyl, triflouromethoxy, alkanoyl, amino, amino-alkyl, N-amino, N,N-di(alkyl)amino, thiol, alkylthio, sulfonyl, alkylsulfonyl, sulfinyl, alkylsulfinyl, carboxy, alkoxycarmonyl, cyano and nitro, and R1 is selected from the list consisting of H, alkyl, CHO, (CH2)2COOH, (CH2)2CO2Et, (CH2)mL and a substituent of formula II as defined, wherin m is 1 or 3 and L is OH or Br. Compounds of formula I are disclosed use in a medicament for the treatment of inflammation. In particular the compounds are disclosed for their inhibition of tumour necrosis factor-alpha(TNF-alpha) and interleukin-1 (IL-1) production.