BENZODIAZEPINE DERIVATIVES AND USES THEREOF IN MEDICAL FIELD

摘要

The invention concerns benzodiazepine derivatives of formula wherein Y it is SOSUB2 /SUBor NR, wherein R is H or CSUB1/SUB-CSUB6 /SUBalkyl; X is H, CSUB1/SUB-CSUB12 /SUBalkyl, -CO, -SO, -SOSUB2/SUB, or -CO-RSUB2/SUB, SO-RSUB2/SUB, SOSUB2/SUB-RSUB2/SUB, wherein RSUB2 /SUBis selected from H, CSUB1/SUB-CSUB12 /SUBalkyl, (CSUB3-C/SUBSUB8 /SUBcycloalkyl) CSUB0/SUB-CSUB6 /SUBalkyl, CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl, CSUB2/SUB-CSUB6 /SUBalkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, -CN, -NHSUB2/SUB, -OH, -NOSUB2/SUB, COORSUB3/SUB, wherein RSUB3 /SUBis selected from H, CSUB1/SUB-CSUB12 /SUBalkyl, (CSUB3/SUB-CSUB8 /SUBcycloalkyl) CSUB0/SUB-CSUB6 /SUBalkyl, CSUB1/SUB-CSUB6 /SUBalkoxy, CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl, or CSUB2/SUB-CSUB6 /SUBalkoxy carbonyl; phenyl, benzyl, naphtyl, biphenyl, or heterocycle n is 0-6; RSUB4 /SUBis selected from H, OH, COOH, CN, CSUB1/SUB-CSUB6 /SUBalkyl, CSUB1/SUB-CSUB6 /SUBalkoxy, CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl, CSUB2/SUB-CSUB6 /SUBalkoxycarbonyl, -CO, -SO, -SOSUB2/SUB, or -CO-RSUB5/SUB, SO-RSUB5/SUB, SOSUB2/SUB-RSUB2/SUB, -OCO-RSUB5/SUB, OSO-RSUB5/SUB, SOSUB2/SUB-RSUB5/SUB, COORSUB5/SUB, SOORSUB5/SUB, SOSUB2/SUBORSUB5/SUB, NHRSUB5/SUB, NHCORSUB5/SUB, NHSOSUB2/SUBRSUB5/SUB, SRSUB5/SUB, SCORSUB5/SUB, wherein RSUB5 /SUBis selected from H, CSUB1/SUB-CSUB6 /SUBalkyl, CSUB1/SUB-CSUB6 /SUBalkoxy, CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl, or CSUB2/SUB-CSUB6 /SUBalkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, -CN, -NHSUB2/SUB, SUBOH, -NO/SUBSUB2/SUB, COORSUB5'/SUB, wherein RSUB5 /SUBis selected from H, CSUB1/SUB-CSUB12 /SUBalkyl, (CSUB3/SUB-CSUB8 /SUBcycloalkyl) CSUB0/SUB-CSUB6 /SUBalkyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, CSUB1/SUB-CSUB6 /SUBalkyl, CSUB1/SUB-CSUB6 /SUBalkoxy, CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl, or CSUB2/SUB-CSUB6 /SUBalkoxy carbonyl; RSUB6 /SUBand RSUB7 /SUBindependently of each other are selected from the group consisting of H, OH, halogen, CN, NHSUB2/SUB, NOSUB2/SUB, COORSUB3/SUB, CSUB1/SUB-CSUB6 /SUBalkyl, CSUB1/SUB-CSUB6 /SUBalkoxy, CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl, and CSUB2/SUB-CSUB6 /SUBalkoxy carbonyl; RSUB3 /SUBis H, CSUB1/SUB-CSUB6 /SUBalkyl CSUB2/SUB-CSUB6 /SUBalkenyl, CSUB2/SUB-CSUB6 /SUBalkynyl or physiologically acceptable salts and uses thereof in medical field, particularly as anti-tumoral agents.