The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
A novel one‐pot [4+2]‐benzannulation approach to substituted carbazoles is accomplished by acid‐catalyzed C3‐propargylation of 2‐alkenyl/aryl indoles with 1‐aryl propargylicalcohols, followed by cycloisomerization. A variety of 2‐alkenylated indoles and 2‐aryl/heteroaryl indoles successfully participated in this tandem reaction with 1‐aryl/heteroaryl propargylicalcohols to provide diversely substituted
catalyst prepared from easily available chiral amino acids was evaluated in a model reaction betweenoxindole and methyl vinyl ketone, and the catalyst derived from isoleucine was found to be the best. Michaeladditions of 3‐monosubstituted oxindoles to methyl vinyl ketone, acrolein or propargyl aldehyde proceeded smoothly to afford 3,3‐disubstitutedoxindoles in good to excellent yields with moderate
[EN] SUBSTITUTED SULFONAMIDE DERIVATIVES<br/>[FR] DÉRIVÉS SUBSTITUÉS DE SULFONAMIDE
申请人:GRUENENTHAL GMBH
公开号:WO2009124746A1
公开(公告)日:2009-10-15
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers or pharmaceutically acceptable salts thereof.