Modified prodrug forms of AP/AMP
AssigneeVion Pharmaceuticals, Inc.
InventorsTerrence W. Doyle, Srinivasa Karra, Zujin Li, Xu Lin, John Mao, Qi Qiao, Yang Xu
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds according to the structure: 1 Where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, Cl, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group; R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.
Claims59
A compound according to the structure:
- 6
- Where R is H or CH3;
- R2 is phosphate which can be free acid or salt;
- R3 is H, F, Cl, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group;
- R4is H, F, Cl, Br, I, OCH3, OCF3 or CF3;
- and
- R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3,
- with the proviso that at least one of R3, R4, R5 or R6 are other than H and when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H.
A pharmaceutical composition comprising an effective amount of a compound for treating neoplasia according to the structure:
- 7
- Where R is H or CH3;
- R2 is free acid phosphate or phosphate salt;
- R3 is H, F, Cl, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group;
- R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3;
- and
- R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3,
- with the proviso that at least one of R3, R4, R5 or R6 is other than H and when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H, optionally, in combination with a pharmaceutically acceptable additive, carrier or excipient.
A method of treating neoplasia in a patient in need of therapy comprising administering to said patient an effective amount of a compound according to the structure:
- 8
- Where R is H or CH3;
- R2 is phosphate which can be free acid or phosphate salt;
- R3 is H, F, Cl, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group;
- R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3;
- and
- R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3,
- with the proviso that at least one of R3, R4, R5 or R6 is other than H and when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H, optionally, in combination with a pharmaceutically acceptable additive, carrier or excipient.
A method of treating neoplasia in a patient in need of therapy comprising administering to said patient in combination an effective amount of a compound according to the structure:
- 9
- Where R is H or CH3;
- R2 is phosphate which can be free acid or salt;
- R3 is H, F, Cl, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group;
- R4is H, F, Cl, Br, I, OCH3, OCF3 or CF3;
- and
- R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3,
- with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H, optionally, in combination with a pharmaceutically acceptable additive, carrier or excipient and an effective amount of at least one anti-cancer agent which acts to damage DNA.
Dependencies are inferred from the claim text.