Fredericamycin derivatives as medicaments for treating tumours

A compound according to the general formula Ia or Ib:

• wherein in each,
• R1 is H, C1-C6 alkyl, cycloalkyl, or C1-C4 alkylcycloalkyl;
• R2 is C1-C14 alkyl, C2-C14 alkenyl, C1-C4 alkylaryl, heteroaryl, C1-C4 alkyl heteroaryl, cycloalkyl, C1-C4 alkyl-cycloalkyl, heterocycloalkyl, C1-C4 alkylheterocycloalkyl, CmH2m+o−pYp CH2NHCOR21, CH2NHCSR21, CH2S(O)nR21, with n=0, 1, 2, CH2SCOR21, CH2OSO2—R21, CHO, CH═NOH, CH(OH)R21, —CH═NOR21, —CH═NOCOR21, —CH═NOCH2CONR21R22, —CH═NOCH(CH3)CONR21R22, —CH═NOC(CH3)2CONR21 R22, —CH═N—NHCO—R23, —CH═N—NHCO—CH2NHCOR21, —CH═N—O—CH2NHCOR21, —CH═N—NHCS—R23, —CH═CR24R25 (trans or cis), COOH, COOR21, CONR21R22, —CH═NR21, —CH═N—NR21R22,
• —CH═N—NHSO2 aryl, or —CH═N—NHSO2 heteroaryl;
• wherein, m is 1 to 6, o is 1, p is 1 to 2m+o;
• m is 2 to 6, o is −1, p is 1 to 2m+o;
• or
• m is 4 to 6, o is −2, p is 1 to 2m+o;
• and
• Y independently from each other is selected from the group consisting of halogen, OH, OR21, NH2, NHR21, NR21R22, SH and SR21;
• and
• wherein X′ is NR215, O, or S;
• and R211, R212, R213, R214, and R215 are independently from each other H or C1-C6 alkyl;
• R21, R22 are independently from each other C1-C14 alkyl, C1-C14 alkanoyl, C1-C6 alkylhydroxy, C1-C6 alkylamino, C1-C6 alkylamino-C1-C6 alkyl, C1-C6 alkylamino-di-C1-C6 alkyl, cycloalkyl, C1-C4 alkylcycloalkyl, heterocycloalkyl, C1-C4 alkylheterocycloalkyl, aryl, aryloyl, C1-C4 alkylaryl, heteroaryl, heteroaryloyl, C1-C4 alkylheteroaryl, cycloalkanoyl, C1-C4 alkanoylcycloalkyl, heterocycloalkanoyl, C1-C4 alkanoylheterocycloalkyl, C1-C4 alkanoylaryl, C1-C4 alkanoylheteroaryl, or mono- and di-sugar linked through a C atom which would carry an OH group in the sugar, wherein the sugars are independently from each other selected from the group consisting of glucuronic acid and its stereo isomers at all optical C-atoms, aldopentoses, and aldohexoses, including their desoxy compounds;
• R23 independently of R21, is R21, CH2-pyridinium salts, or CH2-tri-C1-C6 alkylammonium salts;
• R24 independently of R21, is R21, H, CN, COCH3, COOH, COOR21, CONR21R22, NH2, or NHCOR21;
• R25 independently of R21, is R21, H, CN, COCH3, COOH, COOR21, CONR21R22, NH2, or NHCOR21;
• or
• R24, R25 together are C4-C8 cycloalkyl;
• R3 is H, F, Cl, Br, I, OH, OR31, NO2, NH2, NHR31, NR31R32, NHCHO, NHCOR31, NHCOCF3, CH3−mhalm or OCOR31, wherein hal is Cl or F and m is 1, 2 or 3;
• R31, 32 independently from each other are C1-C6 alkyl;
• R5, R6 Independently from each other are H, C1-C14 alkyl, C2-C14 alkenyl, aryl, C1-C4 alkylaryl, heteroaryl, C1-C4 alkylheteroaryl, cycloalkyl, C1-C4 alkylcycloalkyl, heterocycloalkyl, C4 alkylheterocycloalkyl, CmH2m+o−pYp, or R5 and R6, together with X1—C—C—X2, form a ring with 5, 6, or 7 members,
• wherein, m is 1 to 6, o is 1, p is 1 to 2m+o;
• m is 2 to 6, o is −1, p is 1 to 2m+o;
• or
• m is 4 to 6, o is −2, p is 1 to 2m+o;
• and
• Y independently from each other is selected from the group consisting of halogen, OH, OR21, NH2, NHR21, NR21R22, SH and SR21;
• R4, R7, R8 independently from each other are H, C1-C6 alkyl, CO—R41;
• R41 independently from R21 is R21;
• X1 is O, S, NH, N—C1-C8 alkyl, or N-cycloalkyl;
• X2 is O, S, NH, N—C1-C8 alkyl, or N-cycloalkyl;
• Y1 is O, or N—R9, wherein R9, independently from R5, is R5;
• Y2 is O, or N—R10, wherein R10, independently from R5, is R5;
• and, if Y1 or Y2 are N—R9 or N—R10, X2—R6 may be H;
• Y3 is O, S, or NH;
• or a stereoisomer, tautomer or physiologically tolerable salt thereof.