Patents Assigned to Institute of Pharmacology and Toxicology Academy of Military Medical Sciences, P.L.A. China
  • Publication number: 20160318896
    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
  • Publication number: 20160311767
    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
  • Patent number: 9457008
    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
  • Patent number: 9428496
    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
    Inventors: Song Li, Hongliang Wang, Junhai Xiao, Xian Zhang, Lili Wang, Zhibing Zheng, Wu Zhong, Yunde Xie, Xingzhou Li, Xinbo Zhou, Guoming Zhao, Xiaokui Wang
  • Patent number: 9421188
    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
  • Patent number: 9359314
    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
  • Publication number: 20160137619
    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
    Inventors: Song LI, Wu ZHONG, Shuang CAO, Lili WANG, Zhibing ZHENG, Junhai XIAO, Xinbo ZHOU
  • Patent number: 9340492
    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
  • Publication number: 20160115160
    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
    Inventors: Song LI, Junhai XIAO, Xian ZHANG, Wu ZHONG, Zhibing ZHENG, Lili WANG, Yunde XIE, Xingzhou LI, Xinbo ZHOU, Xiaokui WANG
  • Patent number: 9272992
    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
    Inventors: Song Li, Wu Zhong, Zhibing Zheng, Xinbo Zhou, Junhai Xiao, Yunde Xie, Lili Wang, Xingzhou Li, Guoming Zhao, Xiaokui Wang, Hongying Liu
  • Patent number: 9260534
    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
  • Publication number: 20160002184
    Abstract: The invention relates to a compound of formula I, and a preparation method and use thereof. The compound has a bacterial quorum-sensing regulatory effect, and can be used for prevention and/or treatment of a disease caused by a bacterial infection.
    Type: Application
    Filed: December 10, 2013
    Publication date: January 7, 2016
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A, China
    Inventors: Song LI, Junhai XIAO, Mingming ZHAO, Wu ZHONG, Lili WANG, Zhibing ZHENG, Yunde XIE, Xingzhou LI, Guoming ZHAO, Xinbo ZHOU, Xiaokui WANG, Wei CHEN
  • Patent number: 9187507
    Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R1 is H or methyl; each R2 is independently —R3 or —OR3, each R3 is independently C1-C8 alkyl, C3-C8 cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: November 17, 2015
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Bohua Zhong, Xinhua He, Yongguang Wang, He Liu
  • Patent number: 9149467
    Abstract: The present invention relates to a sustained-release composition containing 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof as an active ingredient, preparation thereof and the compound. The composition is suitable for oral administration by one time per day, and achieves the peak plasma concentration at 1.0 to 3 hours after oral administration. The composition is suitable for manufacturing a medicament for treatment of cognitive dysfunction syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, or senile dementia.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: October 6, 2015
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Science P.L.A. China
    Inventors: Song Li, Wu Zhong, Zhibing Zheng, Junhai Xiao, Bing Li, Yunde Xie, Xinbo Zhou
  • Patent number: 9139543
    Abstract: The present invention relates to a compound of Formula (I), or an isomer, pharmaceutically acceptable salt and solvate thereof; the present invention further relates to a pharmaceutical composition, which comprises the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents; the present invention further relates to the use of the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, for anti-apoptosis, prophylaxis or treatment of a disease or symptom associated with apoptosis, especially for protecting myocardial cells, and prophylaxis or treatment of a disease or symptom associated with cardiomyocyte apoptosis.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: September 22, 2015
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Wu Zhong, Juan Liu, Kunlun He, Junhai Xiao, Xinbo Zhou
  • Publication number: 20150203460
    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: Application
    Filed: August 24, 2012
    Publication date: July 23, 2015
    Applicant: 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
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Patent number: 9034382
    Abstract: The present invention relates to an oseltamivir phosphate granule and preparation method thereof. The said granule comprises 1.97-19.8 wt. % oseltamivir phosphate, 75.0-97.5 wt. % diluent, 0.1-5.0 wt. % binder, optionally 1.0-5.0 wt. % edible flavoring essence, sweetener and/or edible pigment. It is prepared by using 30-55 v/v % aqueous ethanol solution as moistening agent. The granules prepared by the formulation and method according to the present invention have good uniformity and stability and are water-soluble. The administration dosage of the granules can be conveniently selected based on the age and body weight of patients. The oseltamivir phosphate granule is suitable for administering to old people, children and flu gravis patients and those patients that swallow inconveniently or difficulty. The preparation of the granule is simple and low in production cost.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: May 19, 2015
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Wu Zhong, Junhai Xiao, Yunde Xie, Xingzhou Li, Hao Cui, Zhibing Zheng
  • Publication number: 20150133556
    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: Application
    Filed: October 10, 2014
    Publication date: May 14, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
    Inventors: Song LI, Wu ZHONG, Zhibing ZHENG, Xinbo ZHOU, Junhai XIAO, Yunde XIE, Lili WANG, Xingzhou LI, Guoming ZHAO, Xiaokui WANG, Hongying LIU
  • Publication number: 20150119430
    Abstract: The present invention relates to a compound of Formula (I), or an isomer, pharmaceutically acceptable salt and solvate thereof; the present invention further relates to a pharmaceutical composition, which comprises the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents; the present invention further relates to the use of the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, for anti-apoptosis, prophylaxis or treatment of a disease or symptom associated with apoptosis, especially for protecting myocardial cells, and prophylaxis or treatment of a disease or symptom associated with cardiomyocyte apoptosis.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 30, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Wu Zhong, Juan Liu, Kunlun He, Junhai Xiao, Xinbo Zhou