Abstract: The present invention relates to (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates compounds, preparing methods thereof, pharmaceutical compositions containing said compounds and preparing methods thereof, and the clinical uses of said compounds as neuramidinase inhibitors for anti-influenza.
Type:
Grant
Filed:
October 10, 2014
Date of Patent:
December 13, 2016
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
Abstract: The invention relates to a tizoxanide carbamate compound of Formula I and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, and their pharmaceutical use.
Type:
Application
Filed:
July 4, 2014
Publication date:
November 24, 2016
Applicant:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Abstract: The present invention relates to a compound of formula (I), a stereomeride, pharmaceutically acceptable salt, a solvate or an N-oxide thereof, a medicine composition comprising the compound, a method for preparing the compound, and a usage of the compound in treating diseases related to Hsp70. The diseases are preferably selected from tumors, neurodegenerative diseases, and allogeneic transplantation rejection and infection.
Type:
Application
Filed:
December 19, 2014
Publication date:
November 17, 2016
Applicant:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Wu ZHONG, Song LI, Yanqun ZENG, Junhai XIAO, Xinbo ZHOU, Zhibing ZHENG, Xingzhou LI, Xiaokui WANG, Lili WANG
Abstract: Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.
Type:
Grant
Filed:
January 15, 2013
Date of Patent:
November 15, 2016
Assignees:
The Institute of Pharmacology and Toxicology Academy of Military Medical Science P.L.A. CHINA, PEKING UNIVERSITY
Abstract: The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.
Type:
Application
Filed:
December 19, 2014
Publication date:
November 3, 2016
Applicant:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Wu ZHONG, Song LI, Yanqun ZENG, Junhai XIAO, Xinbo ZHOU, Zhibing ZHENG, Xingzhou LI, Xiaokui WANG
Abstract: The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic.
Type:
Application
Filed:
December 18, 2014
Publication date:
October 27, 2016
Applicant:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Wu ZHONG, Song LI, Yanqun ZENG, junhai XIAO, Xinbo ZHOU, Zhibing ZHENG, Xingzhou LI, Xiaokui WANG
Abstract: The present invention relates to site-specific PEGylated linear salmon calcitonin analogs, or pharmaceutically acceptable salts thereof, process for their preparation, pharmaceutical compositions comprising them, and their use for the preparation of a medicament for the treatment or prevention of diseases associated with bone metabolism, e.g., osteoporosis.
Type:
Grant
Filed:
June 4, 2008
Date of Patent:
October 11, 2016
Assignee:
INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A.
Abstract: The present invention provides a joint product comprising synephrine and topiramate, in which the synephrine or salt thereof is administered in form of rapid-release preparation, preferably rapid-release pellet, having daily dose of 2 mg to 25 mg, preferably 5 mg to 20 mg; the topiramate is administered in form of sustained-release or controlled-release preparation, preferably sustained-release pellet, having daily dose of 20 mg to 100 mg, preferably 23 mg to 92 mg. The composition is used for treatment of obesity or other diseases associated with obesity.
Type:
Grant
Filed:
March 22, 2013
Date of Patent:
October 4, 2016
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Song Li, Chunsheng Gao, Wu Zhong, Yuli Wang, Meiyan Yang, Li Shan, Xinbo Zhou, Zhibing Zheng, Xiaokui Wang
Abstract: A pegylated artesunate derivative, a pharmaceutical composition and uses thereof, the pegylated artesunate derivative is represented by the general formula (I): The pegylated artesunate derivative has activity comparable to that of artesunate, increased water solubility and stability, and an extended half-life in vivo.
Type:
Application
Filed:
April 12, 2013
Publication date:
September 1, 2016
Applicants:
Beijing Kaizheng Biotech Development Co. LTD, Institute of Pharmacology and Toxicology Academy of Military Medical Sciences PLA China, Institute of Pharmacology and Toxicology Academy of Military Medical Sciences PLA China
Abstract: Disclosed is as a substituted thiazolamine derivative represented by Formula I or a pharmaceutically acceptable salt thereof or a hydrate thereof (the definitions of each group in the formula are as presented in the description), and the application thereof in the prevention and/or treatment of viral diseases induced by picornavirus. Also disclosed is a pharmaceutical composition containing the compound.
Type:
Grant
Filed:
December 6, 2011
Date of Patent:
August 30, 2016
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Abstract: The present invention provides a combination product, which comprises immediate release pellet of phentermine and sustained-release pellet of topiramate, wherein the pellet of topiramate includes: a) a blank pellet core; b) an active drug layer that contains topiramate and is free of binding agent, the layer being located on surface of the blank pellet core; c) a sustained-release coating layer containing ethyl cellulose and PVP K30, the sustained-release coating layer being located on external of the active drug layer. The present invention further discloses a method for preparing the combination product.
Type:
Grant
Filed:
March 20, 2013
Date of Patent:
August 23, 2016
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Song Li, Chunsheng Gao, Wu Zhong, Yuli Wang, Meiyan Yang, Li Shan, Xinbo Zhou, Zhibing Zheng, Xiaokui Wang
Abstract: The present invention relates to a thiazine amide derivative and a pharmaceutical use thereof, and particularly to a compound of formula I (in the formula, variables are as described in the specification), a pharmaceutically acceptable salt, solvate or hydrate thereof. The present invention further relates to a method for preparing the compound, a pharmaceutical composition containing the compound, and a method or use thereof for prevention or treatment of neurodegenerative diseases.
Type:
Grant
Filed:
August 24, 2012
Date of Patent:
June 7, 2016
Assignee:
Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China
Inventors:
Song Li, Junhai Xiao, Dan Han, Wu Zhong, Lili Wang, Zhibing Zheng, Yunde Xie, Xinbo Zhou, Xingzhou Li, Xiaokui Wang, Dan Jiang, Wei Chen, Hongying Liu
Abstract: Disclosed in the present disclosure are substances having tyrosine kinase inhibitory activity and a preparation method and use thereof, wherein the substances are the compounds having the structure of general formula (I) or the geometric isomers or pharmaceutical salts thereof. Through evaluation on tyrosine kinase inhibitory activity and related experiments, the present disclosure demonstrates that these compounds have a good tyrosine kinase inhibitory activity, and may inhibit a variety of tumor cells, and thus may be developed into drugs for preventing and treating tumor diseases, especially liver cancer, lung cancer and neuroblastoma.
Type:
Application
Filed:
June 20, 2013
Publication date:
June 2, 2016
Applicant:
INSTITUTE OF RADIATION MEDICINE, CHINA ACADEMY OF MILITARY MEDICAL SCIENCES PLA
Inventors:
Xiaoming Yang, Lin Wang, Changyan Li, Yiqun Zhan, Jing Liu, Teng Luo, Haiyan Yan, Shouguo Zhang, Wei Li, Xiaoxue Wen, Tao Peng, Lu Li
Abstract: The present invention pertains to field of pharmaceutical chemicals, and relates to thiazole inner salt compounds, preparation methods and uses thereof. Specifically, the present invention relates to a compound of Formula I, hydrates or pharmaceutically acceptable salts thereof. The compound of Formula I of the present invention is a potent cross-linking protein cleavage agent, has a stable structure, good physical and chemical properties, and good pharmacological activities, and is suitable for large scale production to obtain samples with stable, controllable and reliable quality, thereby being suitable for pharmaceutical development.
Type:
Application
Filed:
July 9, 2014
Publication date:
May 19, 2016
Applicant:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Abstract: Meta-diarylaniline or meta-diarylpyridinamine compounds, methods for preparing the same and uses thereof in manufacture of a medicament. The compounds according to the present application have strong inhibitory activity (at nM level) against wild-type and various drug-resistant HIV viral strains, exhibit good druggability, and can be easily synthesized.
Type:
Grant
Filed:
July 15, 2013
Date of Patent:
May 17, 2016
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Lan Xie, Chin-Ho Chen, Lianqi Sun, Na Liu
Abstract: Provided are a compound of formula I which can be used as a drug against small RNA virus infections, and optical isomers, pharmaceutically acceptable salts, solvates or hydrates thereof. Also provided are the preparation method of the compound, the method for using the compound for treating bacterial infections and the use of the compound in the preparation of a drug for preventing and/or treating viral diseases caused by small RNA viruses.
Type:
Application
Filed:
May 28, 2014
Publication date:
April 28, 2016
Applicant:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Abstract: The present invention discloses a class of mercaptonicotinic acid compound and preparation method and use thereof; the general structural formula of the compound is as shown in Formula I. Experiment demonstrates that the mercaptonicotinic acid compound could inhibit activity of botulinum toxin endopeptidase and tetanus toxin endopeptidase in vitro, which has a significant protective effect on botulinum toxin poisoning in mice, and can be used for preparing medicine intended to prevent and/or treat botulism, as well as to prevent botulinum toxin exposure and tetanus.
Type:
Application
Filed:
May 19, 2014
Publication date:
March 24, 2016
Applicants:
INSTITUTE OF MICROBIOLOGY AND EPIDEMIOLOGY, ACADEMY OF MILITARY MEDICAL SCIENCES, PR CHINA, THE SECOND MILITARY MEDICAL UNIVERSITY
Inventors:
Hui WANG, Wannian ZHNG, Zhenyuan MIAO, Tao LI, Xiong LIU, Yuelin WU, Sen LUO, Chunquan SHENG, Xiaoxue LU, Jianzhong YAO
Abstract: The application of flagellin derivative CZLC31 from Salmonella in preparation of medicines for preventing and treating inflammatory bowel disease (IBD) is introduced in this invention. The CZLC331 protein has a good preventive and therapeutic effect for IBD, such as ulcerative colitis (UC) and Crohn's disease (CD) in this invention. Therefore, this protein can be prepared into the drug for prevention and treatment of IBD. It has been found that the bad efficacy, slow onset, long course of treatment, side effects can be significantly avoided for existing clinical IBD drugs, it can reduce the patient's pain during the treatment in this invention. The rehabilitation and quality of life of the patients have been largely improved. The drug will play an important role in the prevention and treatment of IBD in this invention, and has broad application prospects.
Type:
Application
Filed:
November 13, 2015
Publication date:
March 3, 2016
Applicants:
SUZHOU SCISCAPE BIOMEDICINE SCIENCE & TECHNOLOGY CO. LTD., INSTITUTE OF RADIATION MEDICINE, ACADEMY OF MILITARY MEDICAL SCIENCES, PEOPLE'S LIB
Inventors:
Chenggang ZHANG, Junhuai LI, Yang XU, Yonghong WU, Weiguang LI, Yanchun ZHANG, Yan GAO, Zhihui LI
Abstract: The present invention relates to (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates compounds, preparing methods thereof, pharmaceutical compositions containing said compounds and preparing methods thereof, and the clinical uses of said compounds as neuramidinase inhibitors for anti-influenza.
Type:
Grant
Filed:
August 16, 2013
Date of Patent:
March 1, 2016
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
Abstract: Disclosed are PEG-modified Exendin-4 analogs and uses thereof. In particular, disclosed are PEG-modified Exendin-4 analogs as shown in formula (I), i.e., PEG-M-X-(Ex-4), or pharmaceutically acceptable salts thereof, as well as Exendin-4 analogs as shown in formula (II), i.e., [Aap]Exendin-4, wherein the symbols are as defined in the specification. Further disclosed are methods for preparing PEG-modified Exendin-4 analogs, uses of PEG-modified Exendin-4 analogs, compositions comprising the same, as well as use of the Exendin-4 analogs in the preparation of the PEG-modified Exendin-4 analogs. In the PEG-modified Exendin-4 analogs, modification by polyethylene glycol occurs in a site-directed manner in the peptide chains of the Exendin-4 analogs. The PEG-modified Exendin-4 analogs can be used to prevent and/or treat diseases and/or symptoms related to decreased activity of GLP-1 receptors, such as type II diabetes.
Type:
Grant
Filed:
August 11, 2011
Date of Patent:
February 16, 2016
Assignees:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China, Chengdu Yiping Medical Science & Technology Co., Ltd.
Inventors:
Keliang Liu, Yuanjun Liang, Xiaoyu Xu, Sicheng Li