Guanidino-substituted compounds

Details Guanidino-substituted compounds Guanidino-substituted compounds

C - Chemistry, Metallurgy

07

H

C07H 15/04 (2006.01) A61K 31/155 (2006.01) A61K 31/35 (2006.01) A61K 31/38 (2006.01) A61K 31/445 (2006.01) A61K 31/70 (2006.01) C07C 279/04 (2006.01) C07C 279/16 (2006.01) C07D 211/06 (2006.01) C07D 211/36 (2006.01) C07D 309/08 (2006.01) C07D 335/02 (2006.01) C07H 15/08 (2006.01)

Patent

CA 2188452

Novel guanidino-substituted compounds are described having general formula (I) or a salt, hydrate or solvate thereof, in which X is selected from C, O, N and S; R1 and R3 are independently -(W)a-(R6)b-Z, wherein a and b are independently 0 or 1; W is NH, O or S; R6 is C1-8alkylene in which one or two non-adjacent, intervening carbon atoms thereof is optionally replaced with nitrogen or oxygen; and Z is H, OH or -NH-C(NH)-NH2; provided that when b is 0 then Z is H; R2 is selected from H and OH; and R4 and R5 are independently C1- 8alkylene in which one of the carbon atoms thereof is optionally replaced with nitrogen or oxygen. Compounds in accordance with formula (I) have been found to inhibit HIV replication.

Nouveaux composés substitués par guanidino correspondant à la formule générale (I), ou leur sel, hydrate ou solvate. Dans cette formule, X est choisi entre C, O, N et S; R¿1? et R¿3? représentent indépendamment -(W)¿a?-(R¿6?)¿b?-Z, où a et b valent séparément 0 ou 1; W représente NH, O ou S; R¿6? représente alkylène C¿1-8? dont un ou deux atomes de carbone intermédiaires et non adjacents sont éventuellement remplacés par azote ou oxygène; et Z représente H, OH ou -NH-C(NH)-NH¿2?, à condition que Z représente H quand b vaut 0; R¿2? est choisi entre H et OH; et R¿4? et R¿5? représentent indépendamment alkylène C¿1-8? dont un des atomes de carbone est éventuellement remplacé par azote ou oxygène. Des composés conformes à la formule (I) inhibent la réplication du VIH.

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