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发明授权
CN104540827B 吡咯并苯并二氮杂卓 失效 - 权利终止 转让

吡咯并苯并二氮杂卓
摘要：
式(I)的化合物或其盐或溶剂化物，其中，点线的双键表示在C2和C3之间存在单键或双键；R2选自‑H、‑OH、＝O、＝CH2、‑CN、‑R、OR、卤基、二卤基、＝CHR、＝CHRR’、‑O‑SO2‑R、CO2R和COR；R7选自H、R、OH、OR、SH、SR、NH2、NHR、NRR’、硝基、Me3Sn和卤基；其中R和R’独立地选自可选取代的C1‑7烷基、C3‑20杂环基和C5‑20芳基；R10和R11一起形成双键，或分别选自H和QRQ，其中Q选自O、S和NH以及RQ是H或C1‑7烷基或H和SOxM，其中x是2或3，并且M是单价药用阳离子；A选自(A1)、(A2)、(A3)、(A4)或(A5)，其中X1和Y1分别选自：CH和NH；CH和NMe；N和NMe；CH和S；N和S；N和O；以及CH和O；X2和Y2分别选自：CH和NH；CH和NMe；N和NMe；CH和S；N和S；N和O；以及CH和O；Z1选自O和S；Z2选自CH和N；F选自单键和–(E‑F1)m‑；每个E独立地选自单键和–C(＝O)‑NH‑；每个F1独立地是C3‑20亚杂芳基；m是1、2或3；G选自氢、C1‑4烷基、‑C(＝O)‑O‑C1‑4烷基、‑(CH2)n‑C3‑20杂环烷基和–O‑(CH2)n‑C3‑20杂环烷基；每个n是0‑4；条件是A2不是A2’：其中A2’的X1和Y1分别选自：CH和NMe；COH和NMe；CH和S；N和NMe；N和S；以及条件是A3不是A3’：其中A3’的X2和Y2分别选自：CH和NMe；COH和NMe；CH和S；N和NMe；N和S；B是单键或(B1)，其中B1的X和Y分别选自：CH和NMe；COH和NMe；CH和S；N和NMe；N和S；以及R1是C1‑4烷基。
摘要（英）：

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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