Novel phosphonic acid based prodrugs of pmea and its analogues

Details Novel phosphonic acid based prodrugs of pmea and its analogues Novel phosphonic acid based prodrugs of pmea and its analogues

C - Chemistry, Metallurgy

07

F

C07F 9/6574 (2006.01) A61K 31/52 (2006.01) A61K 31/665 (2006.01) A61K 31/675 (2006.01) A61K 31/70 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2485702

Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: Formula 1wherein:M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2- phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9- (2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9- (2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2- phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2- phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine;V is selected from a group consisting of phenyl, 2- pyridyl , 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3- thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6;R6 is selected from the group consisting of C1-C3 alkyl, and CF3;and pharmaceutically acceptable salts thereof.

La présente invention concerne des pro-médicaments de formule I, leur utilisations, leurs intermédiaires et un procédé pour les produire. Dans la formule I: M et V sont en position cis l'un par rapport à l'autre et MPO¿3?H¿2? est un acide phosphonique choisi dans le groupe qui comprend 9-(2-phosphonylméthoxyéthyl)adénine, (R)-9-(2-phosphonylméthoxy propyl)adénine, 9-(2-phosphonylméthoxyéthyl)guanine, 9-(2-phosphonylméthoxy éthyloxy)adénine, 9-(2-phosphonylméthoxyéthyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylméthoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylméthoxypropyl)adénine, 9-(3-hydroxy-2-phosphonylméthoxypropyl)guanine, et (S)-9-(3-fluoro-2-phosphonyl méthoxypropyl)adénine; V est choisi dans le groupe qui comprend phényle, 2-pyridyle, 3-pyridyle, 4-pyridyle, 2-furanyle, 3-furanyle, 2-thiényle, et 3-thiényle, tous éventuellement substitués par 1 à 3 substituants choisis dans le groupe qui comprend F, Cl, Br, alkyle en C1-C3, CF¿3? et OR?6¿; R?6¿ est choisi dans le groupe qui comprend alkyle en C1-C3, et CF¿3?; et des sels correspondants, acceptables d'un point de vue pharmaceutique.

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