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: Disclosed are new thienyl [3,2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
Type:
Grant
Filed:
October 23, 2012
Date of Patent:
June 2, 2015
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Cisen Pharmaceutical Co., Ltd.
Inventors:
Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
Type:
Application
Filed:
April 23, 2013
Publication date:
May 21, 2015
Applicants:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
Inventors:
Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen
Abstract: A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises a rigid membrane, a push layer, a drug layer, an isolation layer and an aesthetic coating, wherein the rigid membrane contains a semi-permeable polymer, a porogen and/or a plasticizer and has one or more drug release orifices on one end, the push layer comprises an expanding material, an osmotic agent, a binder, a colorant and a lubricant, the drug layer contains a pharmaceutically active ingredient, a hydrophilic polymer, an osmotic agent, a colorant, a lubricant and an antistatic agent, the isolation layer is located between the inner surface of the rigid membrane and the push layer, and contains a hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows an increasing drug release rate at early stage and keeps a constant drug release rate at later stage.
Type:
Grant
Filed:
November 22, 2010
Date of Patent:
December 30, 2014
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, QILU Pharamceutical Co., Ltd.
Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.
Type:
Grant
Filed:
December 10, 2009
Date of Patent:
October 28, 2014
Assignees:
Topharman Shanghai Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Topharman Shandong Co., Ltd.
Abstract: The present invention disclosed a medical use of cucurbitane triterpenoids represented by the following formula and isolated from Momordica charantia L. of Cucurbitaceae family in the preparation of medications for prevention and treatment of diabetes and obesity. The above cucurbitane triterpenoids may be acted as a glucose uptake stimulator, an agonist for the translocation of glucose transporter 4 (GLUT4) to the cell membrane, and an activator of adenosine monophosphate-activated protein kinase (AMPK). They may have potential for the prevention and treatment of diabetes and obesity.
Type:
Grant
Filed:
January 14, 2009
Date of Patent:
May 13, 2014
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, The Garvan Institute of Medical Research, Australia
Inventors:
Yang Ye, Minjia Tan, Changqiang Ke, Tong Chen, Xiqiang Li, Edward Kraegen, Jiming Ye, David James, Gregory Cooney
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:
Application
Filed:
April 13, 2012
Publication date:
May 8, 2014
Applicants:
EAST CHINA NORMAL UNIVERSITY, NANJING LUYESKIE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
Type:
Grant
Filed:
January 17, 2007
Date of Patent:
April 1, 2014
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.
Type:
Application
Filed:
November 27, 2013
Publication date:
March 27, 2014
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to the use of 3,8,12,14,17,20-oxo-substituted pregnene glycosides having the following formula I in the preparation of healthcare products, food additives and drugs for losing body weight, controlling body weight and inhibiting appetite of human beings or animals, wherein, R1 is a saccharide group, and R2 is an acyl group.
Type:
Application
Filed:
November 7, 2011
Publication date:
February 27, 2014
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Weimin Zhao, Shuangzhu Liu, Zhenhua Chen, Luoyi Wang
Abstract: The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.
Type:
Grant
Filed:
June 13, 2007
Date of Patent:
February 18, 2014
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof.
Type:
Application
Filed:
January 20, 2012
Publication date:
January 30, 2014
Applicants:
TOPHARMAN SHANGHAI CO., LTD., TOPHARMAN SHANDONG CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to a structurally novel [1,2,4]triazolo[4,3-b][1,2,4]triazine compounds represented by formula (I) or formula (II), pharmaceutically acceptable salts thereof, prodrugs thereof, hydrates or solvates thereof, and also relates to a preparation method of the compounds, a pharmaceutical composition including a therapeutically effective amount of the compounds, as well as the use thereof as protein tyrosine kinase inhibitors, particularly as c-Met inhibitors, in the preparation of medicaments for the prevention and/or treatment of diseases associated with c-Met abnormality.
Type:
Application
Filed:
December 8, 2011
Publication date:
December 5, 2013
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The invention demonstrates the application of an artemisinin derivative and its pharmaceutical salt. The artemisinin derivatives diarteether amine and its pharmaceutical salt inhibit the proliferation of leukemic cells, block the cell cycle of leukemic cells and induce the apoptosis of leukemic cells. Artemisinin derivatives of the present invention and its pharmaceutical salt can be used for the preparation of anti-leukemia medicines, especially for treatment of acute leukemia and, what's more, for the treatment of acute myeloid leukemia.
Type:
Application
Filed:
January 16, 2012
Publication date:
November 28, 2013
Applicant:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Inventors:
Jianqing Mi, Ying Li, Yu Peng, Yu Zhang, Ruimin Nie, Jingjing Liu, Jin Wang, Yueying Wang, Xun Cai, Yang Li, Saijuan Chen, Zhenyi Wang
Abstract: A method for preparing induced pluripotent stem (iPS) cells, which comprises steps as follows: step 1, introducing one or more stem cell pluripotency factors into somatic cells; step 2, culturing the somatic cells, into which the stem cell pluripotency factor has been introduced in the Step 1, by using medium supplemented with lithium salt; and step 3, identifying and characterizing the induced pluripotent stem cells. Furthermore, there provided a medium for preparing induced pluripotent stem cells, which comprising lithium salt. The medium supplemented with lithium salt is used for efficiently inducing pluripotent stem cells. Lithium salt is able to increase the production efficiency of mouse iPS cells by 5-60 times. The present method for inducing iPS cells is in favor of improving the safety of iPS technique and application of iPS cells in regenerative medicine.
Type:
Application
Filed:
November 7, 2011
Publication date:
November 7, 2013
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
Type:
Application
Filed:
December 2, 2011
Publication date:
October 3, 2013
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Jianping Zuo, Youhong Hu, Wei Tang, Bo Chao, Xiankun Tong, Dewen Li, Feihong Ji, Peilan He
Abstract: Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following general formula (I), preparation methods and uses thereof in preparing medicament for treating infectious diseases, especially infectious diseases caused by multi-drug resistant bacteria, are disclosed.
Type:
Grant
Filed:
May 12, 2011
Date of Patent:
August 13, 2013
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Nanjing Changao Pharmaceutical Science & Technology Co., Limited
Inventors:
Yushe Yang, Qisheng Xin, Houxing Fan, Bin Guo, Xin Liu, Huili He, Wei Li, Zhan Li
Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.
Type:
Grant
Filed:
March 18, 2009
Date of Patent:
August 6, 2013
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia.
Type:
Grant
Filed:
July 7, 2006
Date of Patent:
August 6, 2013
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Topharman Shanghai Co., Ltd.
Abstract: The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity.
Type:
Grant
Filed:
October 23, 2009
Date of Patent:
July 9, 2013
Assignees:
Topharman Shanghai Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Inventors:
Yongjun Mao, Jianfeng Li, Jin Zheng, Zheng Liu, Kai Xie, Haihong Li, Jing Shi, Ye Li, Jingshan Shen