Patents by Inventor Jianxin Gu

Jianxin Gu 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).

  • Analogs of 17-hydroxywortmannin as PI3K inhibitors
    Patent number: 7666901
    Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3, and R8 are defined herein.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: February 23, 2010
    Assignee: Wyeth
    Inventors: Arie Zask, Ping Cai, Jianxin Gu, Joshua Kaplan, Ker Yu, Tianmin Zhu
  • Processes for the convergent synthesis of calicheamicin derivatives
    Publication number: 20090312530
    Abstract: This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.
    Type: Application
    Filed: August 17, 2009
    Publication date: December 17, 2009
    Applicant: Wyeth
    Inventors: Justin Keith Moran, Jianxin Gu
  • Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies
    Patent number: 7625726
    Abstract: Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with dicarboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: December 1, 2009
    Assignee: Wyeth
    Inventors: Jianxin Gu, Ping Cai, Mark E. Ruppen
  • Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
    Patent number: 7605257
    Abstract: Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.
    Type: Grant
    Filed: March 5, 2007
    Date of Patent: October 20, 2009
    Assignee: Wyeth
    Inventors: Jianxin Gu, Mark Ruppen, Tianmin Zhu, Mahdi Fawzi
  • PURIFIED PYRROLOQUINOLINE QUINONE FORTIFIED FOOD
    Publication number: 20090191320
    Abstract: Food products fortified by purified PQQ and methods of application and production are disclosed. A method of preserving a food product comprising admixing an effective amount of purified PQQ or a compound containing purified PQQ derivatives with a foodstuff to provide an inhibiting means to microorganism growth in the food product.
    Type: Application
    Filed: February 25, 2008
    Publication date: July 30, 2009
    Inventors: JIANXIN GU, Xiaojing Yun, Xiaoning Chen, Si Zhang, Junwu Yang, Yihong Wu
  • 41-Methoxy isotope labeled rapamycin 42-ester
    Patent number: 7538119
    Abstract: 41-methoxy-labeled rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) compounds are provided, along with methods for the synthesis and use thereof.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: May 26, 2009
    Assignee: Wyeth
    Inventors: Jianxin Gu, Mark Ruppen
  • PROCESS FOR PREPARING RAPAMYCIN 42-ESTERS AND FK-506 32-ESTERS WITH DICARBOXYLIC ACID, PRECURSORS FOR RAPAMYCIN CONJUGATES AND ANTIBODIES
    Publication number: 20090029426
    Abstract: Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with dicarboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.
    Type: Application
    Filed: September 29, 2008
    Publication date: January 29, 2009
    Applicant: Wyeth
    Inventors: Jianxin Gu, Ping Cai, Mark E. Ruppen
  • Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies
    Patent number: 7445916
    Abstract: Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with dicarboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: November 4, 2008
    Assignee: Wyeth
    Inventors: Jianxin Gu, Ping Cai, Mark E. Ruppen
  • WORTMANNIN-RAPAMYCIN CONJUGATE AND USES THEREOF
    Publication number: 20080249123
    Abstract: A rapamycin—wortmannin conjugate is described, in which the conjugate is formed by linking the rapamycin and wortmannin together in such a manner that the rapamycin and the wortmannin are separated following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 9, 2008
    Applicant: Wyeth
    Inventors: JIANXIN GU, Ker Yu, Judy Lucas, Mark Ruppen, Arie Zask, Semiramis Ayral-Kaloustian
  • WORTMANNIN-RAPALOG CONJUGATE AND USES THEREOF
    Publication number: 20080249124
    Abstract: An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 9, 2008
    Applicant: Wyeth
    Inventors: Jianxin GU, Ker Yu, Judy Lucas, Mark Ruppen, Arie Zask, Semiramis Ayral-Kaloustian
  • Type of oligosaccharides and their sulfate derivatives
    Patent number: 7365191
    Abstract: This invention involves a type of oligosacoharides and its their sulfate derivatives. The backbone of the oligosaccharides consists of 4 to 14 glucose residues, while the side chains contain 0 to 4 glucose residues. There are at least one 1->3? linkage and ?-(1->3)-Iinkage or ?-(1->4) linkage in the backbone. These oligosaccharides, and their sulfates have immune enhancing, antitumor, and antiviral activities. They can be used in immune enhancing, antitumor, and antiviral medicine compounds that would be used as therapeutic treatments.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: April 29, 2008
    Assignee: Shanghaimed Co., Ltd
    Inventors: Fanzuo Kong, Jun Ning, Jianxin Gu
  • Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
    Publication number: 20070212371
    Abstract: Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.
    Type: Application
    Filed: March 5, 2007
    Publication date: September 13, 2007
    Applicant: Wyeth
    Inventors: Jianxin Gu, Mark Ruppen, Tianmin Zhu, Mahdi Fawzi
  • Regiospecific synthesis of rapamycin 42-ester derivatives
    Patent number: 7268144
    Abstract: A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acetylation of 42-hydroxy of rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic solvent.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: September 11, 2007
    Assignee: Wyeth
    Inventors: Jianxin Gu, Ping Cai, Mark E. Ruppen
  • Processes for the convergent synthesis of calicheamicin derivatives
    Publication number: 20070197455
    Abstract: This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.
    Type: Application
    Filed: February 20, 2007
    Publication date: August 23, 2007
    Applicant: Wyeth
    Inventors: Justin Keith Moran, Jianxin Gu
  • 41-Methoxy isotope labeled rapamycin 42-ester
    Publication number: 20070105888
    Abstract: 41-methoxy-labeled rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) compounds are provided, along with methods for the synthesis and use thereof.
    Type: Application
    Filed: November 3, 2006
    Publication date: May 10, 2007
    Applicant: Wyeth
    Inventors: Jianxin Gu, Mark Ruppen
  • Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779
    Patent number: 7202256
    Abstract: Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: April 10, 2007
    Assignee: Wyeth
    Inventors: Jianxin Gu, Mark E. Ruppen, Panolil Raveendranath, Warren Chew, Chia-Cheng Shaw
  • Analogs of 17-hydroxywortmannin as P13K inhibitors
    Publication number: 20060128793
    Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3, and R8 are defined herein.
    Type: Application
    Filed: October 13, 2005
    Publication date: June 15, 2006
    Applicant: Wyeth
    Inventors: Arie Zask, Ping Cai, Jianxin Gu, Joshua Kaplan, Ker Yu, Tianmin Zhu
  • Processing for preparing monoprotected diols from symmetric diols
    Patent number: 6995001
    Abstract: This invention provides a two-step enzymatic process for the synthesis of monoprotected diols from symmetric diols.
    Type: Grant
    Filed: September 26, 2003
    Date of Patent: February 7, 2006
    Assignee: Wyeth Holdings Corporation
    Inventors: Jianxin Gu, Mark Edward Ruppen
  • Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779
    Publication number: 20050234086
    Abstract: Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
    Type: Application
    Filed: April 12, 2005
    Publication date: October 20, 2005
    Applicant: Wyeth
    Inventors: Jianxin Gu, Mark Ruppen, Panolil Raveendranath, Warren Chew, Chia-Cheng Shaw
  • Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies
    Publication number: 20050234087
    Abstract: Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with dicarboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.
    Type: Application
    Filed: April 12, 2005
    Publication date: October 20, 2005
    Applicant: Wyeth
    Inventors: Jianxin Gu, Ping Cai, Mark Ruppen