BEUSKER, Patrick Henry,COUMANS, Rudy Gerardus Elisabeth,ELGERSMA, Ronald Christiaan,MENGE, Wiro Michaël Petrus Bernardus,JOOSTEN, Johannes Albertus Frederikus,SPIJKER, Henri Johannes,DE GROOT, Francis
申请号:
ES09748515
公开号:
ES2647317T3
申请日:
2009.11.03
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formulas (I) or (II): ** Formula ** or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein DB is a DNA binding moiety and is ** Formula ** R1 it is a halide (fluoride, chloride, bromide and iodide), azide, a sulfonate (for example, an optionally substituted C1-6 alkanesulfonate, such as methanesulfonate and trifluoromethanesulfonate, or an optionally substituted C7-12 alkylbenzenesulfonate, such as p-toluenesulfonate) , Succinimide N-oxide, p-nitrophenoxide, pentafluorophenoxide, tetrafluorophenoxide, a carboxylate and aminocarboxylate (carbamate) or an alkoxycarboxylate (carbonate); R2, R2 ', R3, R3', R4, R4 ', R12 and R19 are independently selected from H, OH, SH, NH2, N3, NO2, NO, CF3, CN, C (O) NH2, C (O) H, C (O) OH, halogen, Ra, SRa, S (O) Ra, S (O) 2Ra, S (O) ORa, S (O) 2ORa, OS (O) Ra, OS (O) 2Ra, OS (O) ORa, OS (O) 2ORa, ORa, NHRa, N (Ra) Rb, + N (Ra) (Rb) Rc, P (O) (ORa) (ORb), OP (O) (ORa) (ORb), SiRaRbRc, C (O) Ra, C (O) ORa, C (O) N (Ra) Rb, OC (O) Ra, OC (O) ORa, OC (O) N (Ra) Rb, N (Ra) C (O) Rb, N (Ra) C (O) ORb and N (Ra) C (O) N (Rb) Rc, in which Ra, Rb and Rc are independently selected from H and C1 alkyl -3 or optionally substituted C1-3 heteroalkyl, or R3 + R3 'and / or R4 + R4' are independently selected from>; = O,>; = S,>; = NOR18,>; = C (R18) R18 'and>; = NR18 , R18 and R18 'independently selected from H and optionally substituted C1-3 alkyl, two or more of R2, R2', R3, R3 ', R4, R4' and R12 being optionally linked by one or more bonds to form one or more optionally substituted carbocycles and / or heterocycles; X2 is selected from O, C (R14) (R14 ') and NR14', in which R14 and R14 'have the same meaning as defined for R7 and are independently selected, or R14' and R7 'are absent, giving as a result a double bond between the atoms designated to carry R7 'and R14'; R5, R5 ', R6, R6', R7 and R7 'are independently selected from H, OH, SH, NH2, N3, NO2, NO, CF3, CN, C (O) NH2, C (O) H, C ( O) OH, halog