发明授权
US06753316B1 Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
失效
类似于霉素的丙烯酰基衍生物，其制备方法及其作为抗肿瘤剂的用途
- 专利标题： Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
- 专利标题（中）： 类似于霉素的丙烯酰基衍生物，其制备方法及其作为抗肿瘤剂的用途
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申请号： US09623506申请日： 2000-09-19
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公开(公告)号： US06753316B1公开(公告)日： 2004-06-22
- 发明人: Paolo Cozzi , Pier Giovanni Baraldi , Italo Beria , Marina Caldarelli , Laura Capolongo , Romeo Romagnoli
- 申请人： Paolo Cozzi , Pier Giovanni Baraldi , Italo Beria , Marina Caldarelli , Laura Capolongo , Romeo Romagnoli
- 优先权： GB9806689 19980327
- 主分类号： A61K31415
- IPC分类号： A61K31415
摘要：
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1 and R2, which are the same or different, are selected from hydrogen, halogen, and C1-C4 alkyl; R3 is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and —C≡N; wherein R4, R5, R6, R7, R8, R10, R11, and R12 are, independently from each other, hydrogen or C1-C4 alkyl; and R9 is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R4, R5 and R6 is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.
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