Patent ID: 6268375
Filing Date: 2001-07-31
Classification: A61P,C07D

Abstract:
A camptothecin compounds having the structure: ##STR7##whereX and Y are each independently NO.sub.2, NH.sub.2, H, F, Cl, Br, I, COOH, OH, O--C.sub.1-6 alkyl, SH, S--C.sub.1-6 alkyl, CN, NH--C.sub.1-6 alkyl, N(C.sub.1-6 alkyl).sub.2, CHO, C.sub.1-8 alkyl, N.sub.3,--Z--(CH.sub.2).sub.a --N--((CH.sub.2).sub.b OH).sub.2, wherein Z is selected from the group consisting of O, NH and S, and a and b are each independently an integer of 2 or 3,--Z--(CH.sub.2).sub.a --N--(C.sub.1-6 alkyl).sub.2 wherein Z is selected from the group consisting of O, NH and S, and a is an integer of 2 or 3,--CH.sub.2 --L, where L is halogen (F, Cl, Br, I), .sup.+N.sub.2, .sup.+ (OR.sup.1).sub.2, .sup.+ S(R.sup.1).sub.2, .sup.+ N(R.sup.1).sub.3, OC(O)R.sup.1, OSO.sub.2 R.sup.1, OSO.sub.2 CF.sub.3, OSO.sub.2 C.sub.4 F.sub.9, C.sub.1-6 alkyl-C(.dbd.O)--, C.sub.4-18 aryl--C(.dbd.O)--, C.sub.1-6 alkyl-SO.sub.2 --, perfluoro C.sub.1-6 alkyl-SO.sub.2 -- and C.sub.4-18 aryl-SO.sub.2 --, (where each R.sup.1 independently is C.sub.1-6 alkyl, C.sub.4-18 aryl or C.sub.4-18 ArC.sub.1-6 alkyl); or--CH.sub.2 NR.sup.2 R.sup.3, where (a) R.sup.2 and R.sup.3 are, independently, hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-6 alkyl, C.sub.2-6 alkenyl, hydroxy-C.sub.1-6 alkyl, C.sub.1-6 alkoxy-C.sub.1-6 COR.sup.4 where R.sup.4 is hydrogen, C.sub.1-6 alkyl, perhalo-C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-6 alkyl, C.sub.2-6 alkenyl, hydroxy-C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-C.sub.1-6 alkyl, or (b) R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached form a saturated 3-7 membered heterocyclic ring which may contain a O, S or NR.sup.5 group, where R.sup.5 is hydrogen, C.sub.1-6 alkyl, perhalo-C.sub.1-6 alkyl, aryl, aryl substituted with one or more groups selected from the group consisting of C.sub.1-6 alkyl, halogen, nitro, amino, C.sub.1-6 alkylamino, perhalo-C.sub.1-6 alkyl, hydroxy-C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-C.sub.1-6 alkyl and --COR.sup.6 where R.sup.6 is hydrogen, C.sub.1-6 alkyl perhalo-C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl, and aryl substituted with one or more C.sub.1-6 alkyl, perhalo-C.sub.1-6 alkyl, hydroxy-C.sub.1-6 alkyl, or C.sub.1-6 alkoxy-C.sub.1-6 alkyl groups;R.sup.7 is H, or C(O)--(CH.sub.2).sub.m --NR.sup.8 R.sup.9, where m is an integer of 1-6 or --C(O)CHR.sup.10 NR.sup.8 R.sup.9, where R.sup.10 is the side chain of one of the naturally occurring .alpha.amino acids, R.sup.8 and R.sup.9 are, independently, hydrogen, C.sub.1-8 alkyl or --C(O)CHR.sup.11 NR.sup.12 R.sup.13, where R.sup.11 is the side chain of one of the naturally occurring .alpha.-amino acids and R.sup.12 and R.sup.13 are each independently hydrogen or C.sub.1-8 alkyl; andn is an integer of 1 or 2.