发明名称 |
PRODRUG FORMS OF KINASE INHIBITORS AND THEIR USE IN THERAPY |
摘要 |
The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocyde or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3, and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer. |
申请公布号 |
EP2406262(B1) |
申请公布日期 |
2016.02.17 |
申请号 |
EP20100751067 |
申请日期 |
2010.03.11 |
申请人 |
AUCKLAND UNISERVICES LIMITED |
发明人 |
SMAILL, JEFFREY, BRUCE;PATTERSON, ADAM VORN;DENNY, WILLIAM, ALEXANDER;WILSON, WILLIAM ROBERT;LU, GUO-LIANG;ANDERSON, ROBERT, FORBES;LEE, HO HUAT;ASHOORZADEH, AMIR;HAY, MICHAEL PATRICK |
分类号 |
C07D471/04;A61K31/4178;A61K31/4709;A61K31/517;A61K31/519;A61P35/00;C07D239/94;C07D403/12;C07D403/14;C07D405/14 |
主分类号 |
C07D471/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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