Patents by Inventor Mark J. Macielag

Mark J. Macielag 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).

  • BENZIMIDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
    Publication number: 20170057929
    Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.
    Type: Application
    Filed: August 23, 2016
    Publication date: March 2, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark J. Macielag, Rui Zhang, Yue-Mei Zhang, Bin Zhu, Michael H. Parker, Donald W. Ludovici, Daniel J. Parks, Bart L. DeCorte, Michael N. Greco
  • CHEMICALLY MODIFIED QUINOLINE AND QUINOLONE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
    Publication number: 20170057922
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the CB1 receptor. Such compounds are represented by Formula (I) wherein R1, R2, R3, L1, n, v, r, w, and g are defined herein. and further represented by Formula (II) wherein the group “X?Y”, ring A, R10, R11, R30, W, and t are defined herein.
    Type: Application
    Filed: August 17, 2016
    Publication date: March 2, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark J. Macielag, Yue-Mei Zhang, Michael N. Greco, Barry A. Springer, William V. Murray
  • INDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
    Publication number: 20170057925
    Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.
    Type: Application
    Filed: August 17, 2016
    Publication date: March 2, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark J. Macielag, Rui Zhang, Michael H. Parker, Bart L. DeCorte, Michael N. Greco
  • Sulfonamides as TRPM8 modulators
    Patent number: 9434711
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: September 6, 2016
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Shawn T Branum, Raymond W Colburn, Scott L Dax, Christopher M Flores, Michele C Jetter, Yi Liu, Donald Ludovici, Mark J Macielag, Jay M Matthews, James J McNally, Laura M Andraka, Ronald K Russell, Ning Qin, Christopher Teleha, Kenneth M Wells, Scott C Youells, Mark A Youngman
  • Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
    Patent number: 9375430
    Abstract: Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: June 28, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Margery Connelly, Christopher M. Flores, Mark J. Macielag
  • Imidazo[1,2-?]pyridine sulfonamides as TRPM8 modulators
    Patent number: 9067935
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, and are defined herein.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: June 30, 2015
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J Macielag, Mingde Xia, James J McNally, Jay M Matthews
  • BENZIMIDAZOLE DERIVATIVES USEFUL TRPM8 CHANNEL MODULATORS
    Publication number: 20150150882
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.
    Type: Application
    Filed: February 10, 2015
    Publication date: June 4, 2015
    Inventors: Mark J. Macielag, Mingde Xia, Xiaoqing Xu
  • Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
    Patent number: 8987247
    Abstract: Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Margery Connelly, Christopher M. Flores, Mark J. Macielag
  • Benzimidazole derivatives useful as TRPM8 channel modulators
    Patent number: 8981113
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: March 17, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark J Macielag, Mingde Xia, Xiaoqing Xu
  • SULFONAMIDES AS TRPM8 MODULATORS
    Publication number: 20140315899
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Andraka, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • 4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators
    Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors
    Patent number: 8815839
    Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Kristen Chevalier, Jose Clemente, Scott L Dax, Chris Flores, Li Liu, Mark J Macielag, Mark McDonnell, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang, Bin Zhu
  • Sulfonamides as TRPM8 modulators
    Patent number: 8809327
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: August 19, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Di-azetidinyl diamide as monoacylglcerol lipase inhibitors
    Patent number: 8759533
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
    Patent number: 8759333
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors
    Patent number: 8748417
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 10, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Yue-Mei Zhang, Peter J. Connolly, Shu-Chen Lin, Mark J. Macielag
  • Azetidinyl diamides as monoacylglycerol lipase inhibitors
    Patent number: 8697683
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: April 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen M. Chevalier, Jose Clemente, Peter J. Connolly, Christopher M. Flores, Shu-Chen Lin, Li Liu, John R. Mabus, Mark J. Macielag, Mark E. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Pyrimidine compounds as delta opioid receptor modulators
    Patent number: 8685990
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, and L, A, and Ra are defined herein.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: April 1, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Peter J. Connolly, Gilles Bignan, Chaozhong Cai, Scott L. Dax, Bart L. DeCorte, Shu-Chen Lin, Li Liu, Mark J. Macielag, Philip M. Pitis, Yue-Mei Zhang, Bin Zhu, Wei He
  • IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES AS TRPM8 MODULATORS
    Publication number: 20140088098
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, and are defined herein.
    Type: Application
    Filed: November 25, 2013
    Publication date: March 27, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, Mingde Xia, James J. McNally, Jay M. Matthews
  • Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors
    Patent number: 8637498
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Mark E. McDonnell, Bin Zhu