Patent ID: 6686385
Filing Date: 2004-02-03
Classification: A61P,C07H

Abstract:
A compound according to the formula: or a stereoisomer or pharmaceutically acceptable salt or solvate thereof, useful for inhibiting topoisomerase I and the proliferation of tumor cells, wherein:R is hydrogen, OH, OC1-7alkyl, NH2, N(C1-3alkyl)2 or C1-7alkyl, wherein said C1-7alkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, OR9 and NR9R10; Q is O, S, CH2 or NR5a; R and R5a are each independently selected from the group consisting of: hydrogen, Formula (B), Formula (C), and Formula (D): â€ƒprovided that: if Q is NR5a, then one of R5 and R5a must be hydrogen and the other must be one of Formula (B), Formula (C), and Formula (D); R1, R2 R3 and R4 are each independently selected from the group consisting of: hydrogen, C1-7alkyl, C3-7cycloalkyl, halogen, azido, NR9R10, NHC(O)NR9R10, NHC(O)OR9, C(O)OR9, SR9, and OR9, wherein said C1-7alkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, OR9 SR9 and NR9R10; or R1 and R2 together form &boxH;Nâ€”OH, &boxH;O or â€”NR9R10; or R3 and R4 together form &boxH;Nâ€”OH, &boxH;O or â€”NR9R10; W is selected from the group consisting of hydrogen, C1-7alkyl, C3-7cycloalkyl, halogen, azido, NR9R10, NHC(O)NR9R10, NHC(O)OR9, Nâ€”OH, O and OR9, wherein said C1-7alkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, OR9 and NR9R10; R7 and R8 are each independently OH or H or together form &boxH;O; R9 and R10 are each independently selected from the group consisting of: hydrogen, C1-7alkyl and C3-7cycloalkyl, wherein said C1-7alkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, OH, Oâ€”C1-7alkyl, NH2 and N(C1-3alkyl)2; or R9 and R10 together with the nitrogen atom to which they are attached form a non-aromatic 5-8 membered heterocycle containing one or two of the same or different heteroatoms selected from the group consisting of O, N and S; and X1, X1â€², X2, and X2â€² are each independently selected from the group consisting of hydrogen, halogen, cyano, OR9, â€”CF3, alkylcarbonly, C1-7alkyl, nitro, NR9R10, SR9 and C(O)OR9; wherein said C1-7alkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, OR9, SR9 and NR9R10.