申请人:UNIV DUBLIN
公开号:WO2015107122A1
公开(公告)日:2015-07-23
Compounds of the formula A-X-Y-B and compositions are described which are useful especially for treatment of angiogenesis-related diseases or disorders such as neovascularisation of the eye, age- related macular degeneration, diabetic retinopathy or cancer, wherein A is a six membered heteroaryl ring containing 2 nitrogen atoms which is optionally substituted with R1; R1 is H, CI-6 alkyl, CN, CONR2R3; R2 and R3 which may be the same or different and selected from H, CI-6 alkyl or R2 and R3 form a ring; the group X-Y is an alkyne or alkene, in the case wherein X-Y is an alkene the double bond may be cis or trans and optionally substituted with R1 B is an aryl; or five or six membered heteroaryl ring containing 1 to 3 heteroatoms, both of which may optionally substituted with one or more R4; R4 is R1 or OR5; R5 is H, COR6 or R6; and R6 is CI-6 alkyl and salts thereof.
描述了化合物A-X-Y-B的结构式和组成物,这些化合物特别适用于治疗与血管生成相关的疾病或疾病,如眼部新血管生成、年龄相关性黄斑变性、糖尿病性视网膜病变或癌症,其中A是一个含有2个氮原子的六元杂环芳基环,可选择地取代为R1;R1为H、CI-6烷基、CN、CONR2R3;R2和R3可以相同也可以不同,选择自H、CI-6烷基或R2和R3形成环;X-Y是炔烃或烯烃,如果X-Y是烯烃,则双键可以为顺式或反式,并可选择地取代为R1;B是芳基;或含有1至3个杂原子的五元或六元杂环芳基环,两者均可选择地取代为一个或多个R4;R4为R1或OR5;R5为H、COR6或R6;R6为CI-6烷基及其盐。