Patents by Inventor Robert Mazzola

Robert Mazzola 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).

  • 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
  • Compounds for the treatment of inflammatory disorders
    Patent number: 7598242
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: October 6, 2009
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • 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
  • Selective D/Dreceptor antagonists for the treatment of obesity and CNS disorders
    Patent number: 7504391
    Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: March 17, 2009
    Assignee: Schering Corporation
    Inventors: Duane A. Burnett, William J. Greenlee, Brian McKittrick, Jing Su, Zhaoning Zhu, Thavalakulamgara K. Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
  • 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
  • Preparation and use of compounds as protease inhibitors
    Publication number: 20080176868
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocylcyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
    Type: Application
    Filed: June 12, 2006
    Publication date: July 24, 2008
    Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X.H. Le, Gang Qian, 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
  • Compounds for the treatment of inflammatory disorders
    Publication number: 20070191332
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, wherein n, M, V, T, W, X, U, R1 and R2 are as disclosed in the present specification, and which compounds are useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Application
    Filed: August 10, 2006
    Publication date: August 16, 2007
    Inventors: Zhaoning Zhu, Robert Mazzola, Wensheng Yu, Joseph Kozlowski
  • 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
  • Compounds for the treatment of inflammatory disorders
    Publication number: 20060252778
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Application
    Filed: June 1, 2005
    Publication date: November 9, 2006
    Inventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert Mazzola, Tin-Yau Chan, Henry Vaccaro, Brian McKittrick, Joseph Kozlowski, Brian Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline Ting, Kristin Rosner, Gerald Shipps, M. Siddiqui, David Belanger, Chaoyang Dai, Dansu Li, Vinay Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
  • 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
  • Compounds for the treatment of inflammatory disorders
    Patent number: 7034057
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: April 25, 2006
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Compounds for the treatment of inflammatory disorders
    Publication number: 20060063843
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Application
    Filed: October 20, 2005
    Publication date: March 23, 2006
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Selective D1/D5 receptor antagonists for the treatment of obesity and CNS disorders
    Publication number: 20050075325
    Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Application
    Filed: May 20, 2004
    Publication date: April 7, 2005
    Inventors: Duane Burnett, William Greenlee, Brian McKirtrick, Jing Su, Zhaoning Zhu, Thavalakulamgara Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
  • Compounds for the treatment of inflammatory disorders
    Patent number: 6838466
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: January 4, 2005
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Compounds for the treatment of inflammatory disorders
    Publication number: 20040102418
    Abstract: This invention relates to compounds of the Formula (I): 1
    Type: Application
    Filed: November 19, 2003
    Publication date: May 27, 2004
    Inventors: Zhoaning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Compounds for the treatment of inflammatory disorders
    Publication number: 20040038941
    Abstract: This invention relates to compounds of the Formula (I): 1
    Type: Application
    Filed: December 19, 2002
    Publication date: February 26, 2004
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih