Invention Grant
- Patent Title: Pyrrolobenzodiazepines
- Patent Title (中): 吡咯并苯并二氮杂卓
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Application No.: US13124232Application Date: 2009-10-16
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Publication No.: US08487092B2Publication Date: 2013-07-16
- Inventor: Philip Wilson Howard , Stephen John Gregson , ZhiZhi Chen , Arnaud Charles Tiberghien , Luke Masterson
- Applicant: Philip Wilson Howard , Stephen John Gregson , ZhiZhi Chen , Arnaud Charles Tiberghien , Luke Masterson
- Applicant Address: CH St-Legier-La Chiesaz
- Assignee: Spirogen Developments SARL
- Current Assignee: Spirogen Developments SARL
- Current Assignee Address: CH St-Legier-La Chiesaz
- Agency: Michael Best & Friedrich LLP
- Priority: GB0819097.7 20081017
- International Application: PCT/GB2009/002495 WO 20091016
- International Announcement: WO2010/043877 WO 20100422
- Main IPC: C07D519/00
- IPC: C07D519/00

Abstract:
The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, 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; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R″—X— linking the monomers; wherein R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g. benzene or pyridine; and each X is independently selected from O, S, or N(H); or any pair of adjacent groups from R6 to R9 together form a group —O—(CH2)p—O—, where p is 1 or 2, and salts and solvates thereof, and their use as intermediates for the preparation of other PBD compounds.
Public/Granted literature
- US20110201803A1 PYRROLOBENZODIAZEPINES Public/Granted day:2011-08-18
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