发明授权
US6165980A Distamycin derivatives, process for preparing them, and their use as
antitumor and antiviral agents
失效
雷帕霉素衍生物，其制备方法及其作为抗肿瘤剂和抗病毒剂的用途
- 专利标题： Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
- 专利标题（中）： 雷帕霉素衍生物，其制备方法及其作为抗肿瘤剂和抗病毒剂的用途
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申请号： US101758申请日： 1998-07-17
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公开(公告)号： US6165980A公开(公告)日： 2000-12-26
- 发明人: Paolo Cozzi , Italo Beria , Marina Caldarelli , Maria Cristina Geroni , Enrico Pesenti
- 申请人： Paolo Cozzi , Italo Beria , Marina Caldarelli , Maria Cristina Geroni , Enrico Pesenti
- 申请人地址： ITX Milan
- 专利权人： Pharmacia & Upjohn S.p.A.
- 当前专利权人： Pharmacia & Upjohn S.p.A.
- 当前专利权人地址： ITX Milan
- 优先权： GBX9602163 19960202; GBX9613987 19960703
- 主分类号： A61K31/00
- IPC分类号： A61K31/00 ; A61K31/40 ; A61K31/415 ; A61K31/4164 ; A61K31/4178 ; A61K31/505 ; A61K31/506 ; A61P31/00 ; A61P31/12 ; A61P35/00 ; C07D207/34 ; C07D403/14 ; H04R3/00 ; H04R7/06 ; A61K38/00
摘要：
A distamycin derivative of formula (I): ##STR1## wherein: n is 2, 3 or 4;R.sub.0 is C.sub.1 -C.sub.4 alkyl or --CH.sub.2 CH.sub.2 --X.sub.2, wherein X.sub.2 is a halogen atom;R.sub.1 and R.sub.2 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, C.sub.1 -C.sub.4 alkoxy, and halogen;X.sub.1 is a halogen atom;B is selected from: ##STR2## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and m is 0, 1 or 2; with the proviso that, when R.sub.0 is --CH.sub.2 CH.sub.2 --X.sub.2, B is different from --(CH.sub.2).sub.m --NR.sub.6 R.sub.7 and at least one of R.sub.3, R.sub.4, and R.sub.5 is C.sub.1 -C.sub.4 alkyl;or a pharmaceutically acceptable salt thereof.