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1. 发明申请

US20150126495A1 PYRROLOBENZODIAZEPINES 有权
公开(公告)号：US20150126495A1
公开(公告)日：2015-05-07
申请号：US14397843
申请日：2013-04-30
申请人： UCL BUSINESS PLC , SPIROGEN SÀRL
发明人： Philip Wilson Howard , David Edwin Thurston , Khondaker Mirazur Rahman , Peter William Taylor
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound of formula (I) or a salt or solvate thereof, wherein the dotted double bond indicates the presence of a single or double bond between C2 and C3; R2 is selected from —H, —OH, ═O, ═CH2, —CN, —R, OR, halo, dihalo, ═CHR, ═CHRR′, —O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, nitro, Me3Sn and halo; where R and R′ are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and QRQ respectively, where Q is selected from O, S and NH and RQ is H or C1-7 alkyl or H and SOxM, where x is 2 or 3, and M is a monovalent pharmaceutically acceptable cation; A is selected from (A1), (A2), (A3), (A4) or (A5) where X1 and Y1 are selected from: CH and NH; CH and NMe; N and NMe; CH and S; N and S; N and O; and CH and O, respectively; X2 and Y2 are selected from: CH and NH; CH and NMe; N and NMe; CH and S; N and S; N and O; and CH and O, respectively; Z1 is selected from O and S; Z2 is selected from CH and N; F is selected from a single bond and -(E-F1)m-; each E is independently selected from a single bond, and —C(═O)—NH—; each F1 is independently a C3-20 heteroarylene group; m is 1, 2 or 3; G is selected from hydrogen, C1-4alkyl, —C(═O)—O—C1-4alkyl, —(CH2)n—C3-20 heterocycloalkyl, and —O—(CH2)n—C3-20 heterocycloalkyl group; each n is 0-4; provided that A2 is not A2′, where X1 and Y1 of A2′ are selected from: CH and NMe; COH and NMe; CH and S; N and NMe; N and S, respectively; and provided that A3 is not A3′, where X2 and Y2 of A3′ are selected from: CH and NMe; COH and NMe; CH and S; N and NMe; N and S, respectively; B is either a single bond or (B1), where X and Y of B1 are selected from: CH and NMe; COH and NMe; CH and S; N and NMe; N and S, respectively; and R1 is C1-4 alkyl.

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