The invention relates to prepn. of arylaminocarbonyl bicyclic sulfonamides (I) that are inhibitors of hepatitis B virus (HBV). Compds. I wherein B is a 6-membered aryl optionally contg. one or more N atoms; X is N (un)substituted with R4, or is O; Y is a single bond, a double bond, C1-4 alkanediyl, etc.; Z is C(O) or CR2R3; R1 is H, OH, etc.; R2 is H, DNH2, etc.; R3 is absent, H, D, etc.; R4 is H, OH, C1-4 alkyl; R5 is C1-3 alkyl (un)substituted with OH; R6 is C1-4 alkyl; etc., are claimed. The example compd. II was prepd. from an intermediate (also prepd.) and formaldehyde (procedure given). The compds. of the invention were evaluated for their biol. activity (data given). Compds. I are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The invention also relates to pharmaceutical compns. contg. I.
Preparation of arylaminocarbonyl bicyclic sulfonamides as inhibitors of hepatitis B virus / De Francesco, Raffaele; Donnici, Lorena; Guidotti, Luca; Iannacone, Matteo; Di Fabio, Romano; Summa, Vincenzo; Bencheva, Leda Ivanova; De Matteo, Marilenia; Ferrante, Luca; Prandi, Adolfo; Randazzo, Pietro. - (2019).
Preparation of arylaminocarbonyl bicyclic sulfonamides as inhibitors of hepatitis B virus
Summa, Vincenzo;
2019
Abstract
The invention relates to prepn. of arylaminocarbonyl bicyclic sulfonamides (I) that are inhibitors of hepatitis B virus (HBV). Compds. I wherein B is a 6-membered aryl optionally contg. one or more N atoms; X is N (un)substituted with R4, or is O; Y is a single bond, a double bond, C1-4 alkanediyl, etc.; Z is C(O) or CR2R3; R1 is H, OH, etc.; R2 is H, DNH2, etc.; R3 is absent, H, D, etc.; R4 is H, OH, C1-4 alkyl; R5 is C1-3 alkyl (un)substituted with OH; R6 is C1-4 alkyl; etc., are claimed. The example compd. II was prepd. from an intermediate (also prepd.) and formaldehyde (procedure given). The compds. of the invention were evaluated for their biol. activity (data given). Compds. I are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The invention also relates to pharmaceutical compns. contg. I.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.