Purine and guanine derivatives as pnp inhibitors

Details Purine and guanine derivatives as pnp inhibitors Purine and guanine derivatives as pnp inhibitors

C - Chemistry, Metallurgy

07

D

C07D 473/18 (2006.01) A61K 31/52 (2006.01) C07D 473/00 (2006.01) C07D 473/30 (2006.01)

Patent

CA 2226958

Compounds of formula (I) wherein n = 1 or 2; R1 is H, NH2 or halogen; R2 is H or NH2; R3 represents the group CR6R7R8 where R6, R7 and R8 are the same or different and are each H, C1-6 alkyl or C1-6 haloalkyl; R4 and R5 are the same or different and are each H, CO2H, CO2C1-6 alkyl, NHSO2CF3, tetrazole or (CR9R10)p(Y)q(CR9R10)tZ where (CR9R10)p or (CR9R10)t is straight or branched chain bearing the substituents R9 and R10 when p or t > 1; R9 and R10 are the same or different and are each C0-6 alkyl-Z; P = 1-3; q = 0 or 1; t = 0-4, provided that t > 0 when q = 1; Y = O, NH or S(O)m where m = 0-2; and Z is H, CN, CO2H, CO2C1-6 alkyl, NHSO2CF3 tetrazole, triazole, CONH2, CON(C1-6 alkyl)2, CONH(C1-6 alkyl), SO2 N H (C1-6 alkyl) or SO2N(C1-6 alkyl)2; or a salt; solvate or hydrate thereof.

L'invention concerne des composés de la formule (I), leur sel, solvate ou hydrate. Dans cette formule, n est égal à 1 ou 2, R?1¿ est H, NH¿2? ou un halogène; R?2¿ est H ou NH¿2?; R?3¿ représente le groupe CR?6¿R?7¿R?8¿ où R?6¿, R?7¿ et R?8¿ sont identiques ou différents et représentent chacun H, alkyleC¿1-6? ou haloalkyleC¿1-6?; R?4¿ et R?5¿ sont identiques ou différents et représentent chacun H, CO¿2?H, CO¿2?alkyleC¿1-6?, NHSO¿2?CF¿3?, tétrazole ou (CR?9¿R?10¿)¿p?(Y)¿q?(CR?9¿R?10¿)¿t?Z où (CR?9¿R?10¿)¿p? ou (CR?9¿R?10¿)¿t? est une chaîne droite ou ramifiée, portant les substituant R?9¿ et R?10¿ quand p et t > 1; R?9¿ et R?10¿ sont identiques ou différents et représentent chacun alkylC¿0-6?-Z; p est égal à 1-3; q est égal à 0 ou 1; t est égal à 0-4, à condition que t > 0 quand q est égal à 1; Y représente O, NH ou S(O)¿m? où m est égal à 0-2; Z est H, CN, CO¿2?H, CO¿2?alkyleC¿1-6?, NHSO¿2?CF¿3?, tétrazole, triazole, CONH¿2?, CON(alkyleC¿1-6?), CONH(alkyleC¿1-6?)SO¿2?NH(alkyleC¿1-6?) ou SO¿2?N(alkyleC¿1-6?).

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