Abstract: 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.
Type:
Grant
Filed:
April 13, 2012
Date of Patent:
August 25, 2015
Assignees:
EAST CHINA NORMAL UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, NANJING LUYESIKE PHARMACEUTICAL CO., LTD.
Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
Type:
Grant
Filed:
May 4, 2010
Date of Patent:
February 17, 2015
Assignees:
Jiangsu Provincial Institute of Materia Medica Co., Ltd., Nanjing Luyesike Pharmaceutical Co., Ltd.
Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
Type:
Application
Filed:
May 4, 2010
Publication date:
March 1, 2012
Applicants:
Nanjing Luyesike Pharmaceutical Co., Ltd., Jiangsu Provincial Institute of Materia Medica Co. Ltd.