Patents by Inventor Zhong-Yue Sun

Zhong-Yue Sun 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).

  • Aspartyl protease inhibitors
    Patent number: 8168641
    Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: June 7, 2007
    Date of Patent: May 1, 2012
    Assignee: Schering Corporation
    Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
  • GAMMA SECRETASE MODULATORS
    Publication number: 20110306593
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
    Type: Application
    Filed: November 11, 2009
    Publication date: December 15, 2011
    Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
  • GAMMA SECRETASE MODULATORS
    Publication number: 20110294756
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 12, 2009
    Publication date: December 1, 2011
    Inventors: Zhaoning Zhu, William J., Xianhai Huang, Jun Qin, XIaoxiang Liu, Hongmei Li, Wei Zhou, Anandan Palani, Xiaohong Zhu, Monica L. Vicarel, Mihirbaran Mandal, Zhong-Yue Sun, Chad E. Bennett, Troy Michael McCracken, Gioconda V. Gallo
  • GAMMA SECRETASE MODULATORS
    Publication number: 20110257156
    Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 5, 2009
    Publication date: October 20, 2011
    Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
  • HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    Publication number: 20110218194
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: May 16, 2011
    Publication date: September 8, 2011
    Applicant: Schering Corporation & Pharmacopeia Drug Discovery Inc.
    Inventors: Zhaoning Zhu, Brian A. Mckittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachel C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Heterocyclic aspartyl protease inhibitors
    Patent number: 7973067
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: July 5, 2011
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachel C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    Publication number: 20100292203
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: January 26, 2010
    Publication date: November 18, 2010
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan
  • GAMMA SECRETASE MODULATORS
    Publication number: 20100255005
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: May 28, 2008
    Publication date: October 7, 2010
    Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
  • GAMMA SECRETASE MODULATORS
    Publication number: 20100247514
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: May 5, 2008
    Publication date: September 30, 2010
    Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Theodros Asberom, Xianhai Huang, Xiaohong Zhu, Mark D. McBriar, Dmitri A. Pissarnitski, Zhiqiang Zhao, Ruo Xu, Hongmei Li, Anandan Palani, Johannes H. Voigt, Robert D. Mazzola, JR., John Clader, Hubert Josien, Jun Qin
  • Heterocyclic aspartyl protease inhibitors
    Patent number: 7763609
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: July 27, 2010
    Assignees: Schering Corporation, Pharmacopeia, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Heterocyclic aspartyl protease inhibitors
    Patent number: 7700603
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: June 9, 2005
    Date of Patent: April 20, 2010
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Brian A McKittrick, Zhong-Yue Sun, Yuanzan C Ye, Johannes H Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Gang Qian, Dawit Tadesse
  • HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    Publication number: 20090306047
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 10, 2009
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    Publication number: 20090258868
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 15, 2009
    Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Heterocyclic aspartyl protease inhibitors
    Patent number: 7592348
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: December 13, 2004
    Date of Patent: September 22, 2009
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Neuropeptide receptor modulators
    Patent number: 7459450
    Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: April 28, 2005
    Date of Patent: December 2, 2008
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Zhong-Yue Sun, Yuanzan C. Ye, Deborra E. Mullins, Brian McKittrick, Andrew Stamford, William J. Greenlee
  • Heterocyclic aspartyl protease inhibitors
    Publication number: 20080200445
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula 1.
    Type: Application
    Filed: February 23, 2007
    Publication date: August 21, 2008
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan Ye, Johannes Voigt, Corey Strickland, Elizabeth Smith, Andrew Stamford, William Greenlee, Robert Mazzola, John Caldwell, Jared Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy Le, Kurt Saionz, Suresh Babu, Rachael Hunter, Michelle Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • ASPARTYL PROTEASE INHIBITORS
    Publication number: 20070287692
    Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Application
    Filed: June 7, 2007
    Publication date: December 13, 2007
    Inventors: Yusheng Wu, Ulrich Iserloh, Jared Cumming, Xiaoxiang Liu, Robert Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
  • Heterocyclic aspartyl protease inhibitors
    Publication number: 20070072852
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 13, 2004
    Publication date: March 29, 2007
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan Ye, Johannes Voigt, Corey Strickland, Elizabeth Smith, Andrew Stamford, William Greenlee, Robert Mazzola, John Caldwell, Jared Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy Le, Kurt Saionz, Suresh Babu, Rachael Hunter
  • Heterocyclic aspartyl protease inhibitors
    Publication number: 20060111370
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: June 9, 2005
    Publication date: May 25, 2006
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan Ye, Johannes Voigt, Corey Strickland, Elizabeth Smith, Andrew Stamford, William Greenlee, Robert Mazzola, John Caldwell, Jared Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy Le, Kurt Saionz, Suresh Babu, Rachael Hunter, Michelle Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Neuropeptide receptor modulators
    Publication number: 20060089351
    Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Application
    Filed: April 28, 2005
    Publication date: April 27, 2006
    Inventors: Zhaoning Zhu, Zhong-Yue Sun, Yuanzan Ye, Deborra Mullins, Brian McKitrtick, Andrew Stamford, William Greenlee