Pharmaceutical compounds

Details Pharmaceutical compounds Pharmaceutical compounds

2006-11-07

2006-11-07

Habte, Kahsay (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S116000, C544S295000, C544S343000, C514S250000

Reexamination Certificate

active

07132419

ABSTRACT:
A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I)wherein each of R1to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2NR10(CH2)nCN, NR10COR11, OCOR11or COR10;each of R5to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6alkoxy, C1–C6alkyl, SR10and N(R12)2;Q is C1–C6alkylene which is unsubstituted or substituted by (i) C1–C6alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12);R8and R9, which are the same or different, are each hydrogen or C1–C6alkyl, or R8and R9together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8and R9is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above;R10is hydrogen, C1–C6alkyl, C3–C6cycloalkyl, benzyl or phenyl;R11is C1–C6alkyl, C3–C6cycloalkyl, benzyl or phenyl;each R12, which are the same or different, is hydrogen, C1–C6alkyl cycloalkyl, benzyl or phenyl, or the two R12groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; andn is 1, 2 or 3;or a pharmaceutically acceptable salt thereof;with the proviso that at least one of R1to R4is other than hydrogen.These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

REFERENCES:
patent: 172 744 (1986-02-01), None
patent: 195198 (1987-03-01), None
patent: 93/24096 (1993-12-01), None
patent: 98/12181 (1998-03-01), None
patent: WO 98/1281 (1998-03-01), None
patent: 98/45272 (1998-10-01), None
patent: WO 98/45272 (1998-10-01), None
Cecil Textbook of Medicine , 20thEdition, vol. 2., pp. 1739-1747.
Rewcastle et al. {Journal of Medicinal Chemistry, vol. 30, No. 5, 1987, pp. 843-851}.
Rewcastle et al; “Potential Antitumor Agents . 51. Synthesis and Anititumor Acitivity of Substituted Phenazine-1-Carboxamides”; Journal of Medicinal Chemistry, US, American, Chemical Society. Washington, vol. 30 No. 5, 1987, pp. 843-851, XP002051604.

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