FLYGARE JOHN A.,GUNZNER-TOSTE JANET L.,PILLOW THOMAS,HOWARD PHILIP WILSON,MASTERSON LUKE
申请号：
NZ62320912
公开号：
NZ623209A
申请日:
2012.10.12
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
A conjugate of formula (A): the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3； R2 is independently selected from H, OH, =0, =CH2, CN, R, OR, =CH-RD, =C(RD)2, 0-S02-R, C02R and COR, and optionally further selected from halo or dihalo； where RD is independently selected from R, C02R, COR, CHO, C02H, and halo； R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR&rsquo；, NO2, Me3Sn and halo； R7is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR&rsquo；, N02, Me3Sn and halo； Y is selected from a single bond, and a group of formulae A1 or A2: where N shows where the group binds to the N10 of the PBD moiety； RL1 and RL2 are independently se!ected from H and methyl, or together with the carbon atom to which they are bound form a cyclopropylene group； CBA represents a cell binding agent； Q is independently selected from O, S and NH； R11 is either H, or R or, where Q is O, S03M, where M is a metal cation； R and R&rsquo； are each independently selected from optionally substituted C1-12alkyl, C3-20 heterocyclyl and C5-20aryl groups, and optionally in relation to the group NRR&rsquo；, R and R&rsquo； together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-； 6- or Z-metfibered heteracyciie ring； wherein R12 R16, R19 and R17 are as defined for R2, R6, R9 and R7 respectively: wherein R&rdquo； is a Calky!ene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H} ； NMe and/or aromatic rings, e.g. benzene or pyridine, which rings are optional y substituted； X and X&rsquo； are independently selected from O, S and N(H).
