公开(公告)号：US20140128421A1

公开(公告)日：2014-05-08

申请号：US14112583

申请日：2012-04-13

申请人： Wei Lv ,  Shanbao Yu ,  Yu Luo ,  Yi Chen ,  Jian Ding

发明人： Wei Lv ,  Shanbao Yu ,  Yu Luo ,  Yi Chen ,  Jian Ding

IPC分类号： C07D491/22

CPC分类号： C07D491/22

摘要： Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.

摘要翻译： 提供了如通式I所示的含有7-元内酯环的喜树碱化合物及其药学上可接受的盐以及其制备方法和用途。 在通式Ⅰ中，R 1是H，C 1 -C 3烷基，乙酰基或丙酰基; R2是H，C1〜C6烷基，C3〜C6环烷基，哌啶基; 或被氨基取代的C 1-6烷基; R3是H，C1〜C3烷基或被氨基取代的C1〜C6烷基; R4是H，羟基或C1〜C6烷氧基; R5是H或C1〜C6烷氧基; 或R 4和R 5彼此连接形成-OCH 2 O-或-OCH 2 CH 2 O-。 该化合物具有良好的抗肿瘤活性，可以通过口服给药，静脉内注射和肌内注射等临床使用。

公开(公告)号：US09115150B2

公开(公告)日：2015-08-25

申请号：US14112583

申请日：2012-04-13

申请人： Wei Lv ,  Shanbao Yu ,  Yu Luo ,  Yi Chen ,  Jian Ding

发明人： Wei Lv ,  Shanbao Yu ,  Yu Luo ,  Yi Chen ,  Jian Ding

IPC分类号： C07D491/22

CPC分类号： C07D491/22

摘要： Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.

摘要翻译： 提供了如通式I所示的含有7-元内酯环的喜树碱化合物及其药学上可接受的盐以及其制备方法和用途。 在通式I中，R 1是H，C 1 -C 3烷基，乙酰基或丙酰基; R2是H，C1〜C6烷基，C3〜C6环烷基，哌啶基; 或被氨基取代的C 1-6烷基; R3是H，C1〜C3烷基或被氨基取代的C1〜C6烷基; R4是H，羟基或C1〜C6烷氧基; R5是H或C1〜C6烷氧基; 或R 4和R 5彼此连接形成-OCH 2 O-或-OCH 2 CH 2 O-。 该化合物具有良好的抗肿瘤活性，可以通过口服给药，静脉内注射和肌内注射等临床使用。