Phosphonic acid naphthylureas and their antiantiogenic and...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/22 (2006.01) C07F 9/38 (2006.01) C07F 9/44 (2006.01)

Patent

CA 2297900

Novel phosphonic acid agents are synthesized and characterized and their pharmaceutical compositions provided. Their method of use for the inhibition of angiogenesis and metalloproteinase and the treatment of tumors is also shown. Embodiments of the phosphonic acid agents include: (P-Yn1)m1-Q1-K-(Q2- (Yn2-P)m2)j wherein P is a phosphonic group or a phosphonic salt, Y is -OCO-, - NR1CO- or CON(R1)R2-; R1 is H, CH2CO2H, or substituted or unsubstituted alkyl; R2 is substituted alkyl, aryl or arylalkyl; Q1 and Q2 are substituted or unsubstituted aryl groups; K is H, -NH-CO-NH-, -NH-CS-NH-, -NHCO-R3-CONH- or - NHCS-R3-CSNH-; provided when K is H, R3 is a substituted or unsubstituted aryl group; j is 0; j is 0,1,2; n1 and n2 are independently 0,1 or 2; and m1 and m2 are independently an integer from 1-4.

La présente invention concerne de nouveaux agents substitués à l'acide phosphonique et leurs compositions pharmaceutiques. Ces nouveaux agents sont définis par la formule suivante: (P-Yn1)m1-Q-K-(Q2-(Yn2-P)m2)j dans laquelle Y représente -OCO-, NR1CO- ou CON(R1)R2-; Q1 et Q2 représentent des groupes aryle substitués ou non substitués; K représente H, -NHCONH-, NHCS-NH, -NHCO-R3- ou -NHCSR3-CSNH-; à condition que K représente H, j représente 0; j représente 0,1,2; n1 et n2 représentent indépendamment 0,1 ou 2; et m1 et m2 représentent indépendamment un entier compris entre 1 et 4.

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