发明名称 PYRROLOBENZODIAZEPINES AND ANTIBODY DISULFIDE CONJUGATES THEREOF
摘要 A compound of formula I:;;wherein 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.
申请公布号 US2016074527(A1) 申请公布日期 2016.03.17
申请号 US201514856914 申请日期 2015.09.17
申请人 Genentech, Inc. 发明人 Flygare John A.;Pillow Thomas H.
分类号 A61K47/48;C07K16/30;C07K16/32;C07K16/28;A61K45/06;C07D519/00 主分类号 A61K47/48
代理机构 代理人
主权项 1. A compound of formula I: wherein 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, ═O, ═CH2, CN, R, OR, ═CH—RD, ═C(RD)2, O—SO2—R, CO2R and COR, and optionally further selected from halo or dihalo; where RD is independently selected from R, CO2R, COR, CHO, CO2H, and halo; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, 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 selected from H and methyl, or together with the carbon atom to which they are bound form a cyclopropylene group; Q is independently selected from O, S and NH; R11 is either H, or R or, where Q is O, SO3M, where M is a metal cation; R and R′ are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR′, R and R′ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring; wherein R12, R16, R19 and R17 are as defined for R2, R6, R9 and R7 respectively; wherein R″ is a C3-12 alkylene 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 optionally substituted; andX and X′ are independently selected from O, S and N(H).
地址 South San Francisco CA US
您可能感兴趣的专利