发明授权
US08592576B2 Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases
有权
用于治疗增殖性疾病的不对称吡咯并苯并二氮杂二聚体
- 专利标题: Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases
- 专利标题(中): 用于治疗增殖性疾病的不对称吡咯并苯并二氮杂二聚体
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申请号: US13123327申请日: 2009-10-16
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公开(公告)号: US08592576B2公开(公告)日: 2013-11-26
- 发明人: Philip Wilson Howard , Stephen John Gregson , Luke Masterson
- 申请人: Philip Wilson Howard , Stephen John Gregson , Luke Masterson
- 申请人地址: CH St-Legier-la Chiesaz
- 专利权人: Spirogen Sarl
- 当前专利权人: Spirogen Sarl
- 当前专利权人地址: CH St-Legier-la Chiesaz
- 代理机构: Michael Best & Friedrich LLP
- 优先权: GB0819095.1 20081017
- 国际申请: PCT/GB2009/002498 WO 20091016
- 国际公布: WO2010/043880 WO 20100422
- 主分类号: C07D487/04
- IPC分类号: C07D487/04
摘要:
Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N═C═O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH═CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.
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