Synthesis of constrained mimics of a serine dipeptide is described. Triflated 3-hydroxypicolinic acid methyl ester was carbo-substituted using ethynylstannanes with Pd-catalysis to furnish 3-acetylenic pyridines which were hydrolysed and coupled to Ser(t-Bu)OMe before cyclization to 1-alkylidene-3-oxo-1,3-dihydropyrrolo [3,4-b]pyridine derivatives. Subsequent deprotection provided the dipeptide analogue.
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
[EN] TRIAZOLO-PYRIMIDINE ANALOGUES FOR TREATING DISEASES CONNECTED TO THE INHIBITON OF WERNER SYNDROME RECQ HELICASE (WRN)<br/>[FR] ANALOGUES DE TRIAZOLO-PYRIMIDINE POUR LE TRAITEMENT DE MALADIES LIÉES À L'INHIBITION DE L'HÉLICASE RECQ DU SYNDROME DE WERNER (WRN)
申请人:NOVARTIS AG
公开号:WO2022249060A1
公开(公告)日:2022-12-01
The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I): (I) wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.