Patents by Inventor Fajun Nan

Fajun Nan has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 9216962
    Abstract: The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: December 22, 2015
    Assignee: Shanghai Puyi Chemical Co., Ltd.
    Inventors: Fajun Nan, Fei Chen, Yangming Zhang, Jia Li, Yubo Zhou, Mingbo Su, Jian Ding, Linghua Meng, Xin Xie, Shixian Wang
  • Publication number: 20140336252
    Abstract: The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.
    Type: Application
    Filed: October 23, 2012
    Publication date: November 13, 2014
    Inventors: Fajun Nan, Min Li, Zhaobing Gao, Fei Chen, Yangming Zhang, Pingzheng Zhou, Haining Hu, Haiyan Xu, Sheng Liu
  • Publication number: 20140288127
    Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajun Nan, Tao Pang, Lifang Yu, Mei Zhang
  • Patent number: 8778973
    Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: July 15, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajun Nan, Tao Pang, Lifang Yu, Mei Zhang
  • Publication number: 20140148600
    Abstract: The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase.
    Type: Application
    Filed: May 7, 2012
    Publication date: May 29, 2014
    Inventors: Fajun Nan, Fei Chen, Yangming Zhang, Jia Li, Yubo Zhou, Mingbo Su, Jian DING, Linghua Meng, Xin Xie, Shixian Wang
  • Patent number: 8653115
    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
    Inventors: Fajun Nan, Jianping Zuo, Haijun Chen, Guifeng Wang, Min Gu, Fenghua Zhu, Wei Tang
  • Patent number: 8609721
    Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: December 17, 2013
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jarda T. Wroblewski, Fajun Nan
  • Patent number: 8470763
    Abstract: Disclosed are a series of ?-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The ?-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: June 25, 2013
    Assignee: Shanghai Institute of Materia Medica Chinese Academy of Sciences
    Inventors: Fajun Nan, Jia Li, Jian Ding, Gang Liu, Chuanming Xie, Zehong Miao, Wanyi Tai
  • Patent number: 8455510
    Abstract: Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: June 4, 2013
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jian Ding, Jianping Zuo, Linqian Yu, Linghua Meng, Yangming Zhang, Na Yang, Min Gu
  • Patent number: 8426606
    Abstract: The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2?,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: April 23, 2013
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Wei Tang
  • Publication number: 20130059895
    Abstract: The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2?,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.
    Type: Application
    Filed: March 16, 2011
    Publication date: March 7, 2013
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Wei Tang
  • Publication number: 20120264793
    Abstract: The present invention discloses the pharmaceutical use of a 2?,2-bis-thiazole non-nucleoside compound of formula I as an inhibitor of hepatitis C virus (HCV). The 2?,2-bis-thiazole non-nucleoside compound can inhibit the replication of HCV, and thus has an anti-HCV activity and is useful for treating hepatitis C.
    Type: Application
    Filed: November 24, 2010
    Publication date: October 18, 2012
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Feihong Ji, Haijun Chen, Xiankun Tong
  • Patent number: 8247549
    Abstract: The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: August 21, 2012
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Min Gu, Wei Tang
  • Patent number: 8183383
    Abstract: PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or treat diseases which are related to insulin antagonism mediated by PTP1B, especially diabetes type II and obesity. The invention also provides methods for preparing these inhibitors.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: May 22, 2012
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jia Li, Yi Wei, Wei Zhang, Jingya Li, Lei Shi
  • Patent number: 8039492
    Abstract: The present invention provides a substituted cyclic compound of the following general formula I or II: its preparation process and its use as a glucagon-like peptide-1 receptor regulator for preventing or treating metabolic disorders including, but not limited to, diabetes, insulin resistance and obesity, etc.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: October 18, 2011
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Mingwei Wang, Na Li, Xin Xie, Qing Liu, Caihong Zhou, Fajun Nan, Guangxing Wang
  • Publication number: 20110201810
    Abstract: The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product.
    Type: Application
    Filed: November 6, 2008
    Publication date: August 18, 2011
    Applicant: Shanghai Institute of Materia Medica, Chinese Acad emy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Min Gu, Wei Tang
  • Publication number: 20110166172
    Abstract: Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
    Type: Application
    Filed: September 17, 2009
    Publication date: July 7, 2011
    Applicant: Shanghai institute of Materia Medica, chinese Academy of Sciences
    Inventors: Fajun Nan, Jian Ding, Jianping Zuo, Linqian Yu, Linghua Meng, Yangming Zhang, Na Yang, Min Gu
  • Publication number: 20110021624
    Abstract: Disclosed are a series of ?-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The ?-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.
    Type: Application
    Filed: December 11, 2008
    Publication date: January 27, 2011
    Inventors: Fajun Nan, Jia Li, Jian Ding, Gang Liu, Chuanming Xie, Zehong Miao, Wanyi Tai
  • Patent number: 7838682
    Abstract: The present invention provides the glucagon-like peptide-1 receptor agonists. It is indicated that the agonists have good binding capability to glucagon-like peptide-1 receptor by pharmacological tests. The present invention also provides the preparation of the agonists.
    Type: Grant
    Filed: December 25, 2003
    Date of Patent: November 23, 2010
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Mingwei Wang, Wenlong Wang, Caihong Zhou
  • Publication number: 20100197927
    Abstract: PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or treat diseases which are related to insulin antagonism mediated by PTP1B, especially diabetes type II and obesity. The invention also provides methods for preparing these inhibitors.
    Type: Application
    Filed: February 26, 2008
    Publication date: August 5, 2010
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jia Li, Yi Wei, Wei Zhang, Jingya Li, Lei Shi