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).

  • Pyridine N-oxide derivatives useful as factor XIa inhibitors
    Patent number: 11814364
    Abstract: The present invention is directed to pyridine N-oxide derivatives, stereoisomers, isotopologues, isotopomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Grant
    Filed: March 17, 2022
    Date of Patent: November 14, 2023
    Assignee: Janssen Pharmaceutica NV
    Inventors: Guozhang Xu, Boying Guo, Zhijie Liu, Jing Zhang, Micheal D. Gaul, Eugene B. Grant, Mark J. Macielag, Tianbao Lu, Tho V. Thieu
  • COMPOUNDS USEFUL AS FACTOR XIA INHIBITORS
    Publication number: 20230312560
    Abstract: The present invention is directed to Factor XIa inhibitors, tautomers, stereoisomers, isotopologues, and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders, and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Application
    Filed: July 21, 2021
    Publication date: October 5, 2023
    Inventors: Guozhang XU, Mark J. MACIELAG, Zhijie LIU, Tho V. THIEU, Ravi NARGUND
  • 3-(1H-IMIDAZOL-2-YL)-2,3,8,8A-TETRAHYDROINDOLIZIN-5(1H)-ONE DERIVATIVES USEFUL AS FACTOR XIA INHIBITORS
    Publication number: 20230295157
    Abstract: The present invention is directed to 3-(1H-imidazol-2-yl)-2,3,8,8a-tetrahydroindolizin-5(1H)-one derivatives, stereoisomers, isotopologues, and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Application
    Filed: July 22, 2021
    Publication date: September 21, 2023
    Inventors: Guozhang XU, Micheal D. GAUL, Tho V. THIEU, Jing ZHANG, Mark WALL, Ling Hua GAO, Bin ZHU, Tianbao LU, Boying GUO, Zhijie LIU, Ravi NARGUND, Mark J. MACIELAG
  • Bicyclic Pyridin-2-one and pyrimidin-4-one Derivatives Useful As a Factor XIa Inhibitors
    Publication number: 20230183233
    Abstract: The present invention is directed to bicyclic pyridinon-2-one and pyrimidin-4-one derivatives, stereoisomers, isotopologues, and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Application
    Filed: July 21, 2022
    Publication date: June 15, 2023
    Inventors: Guozhang Xu, Mark J. Macielag, Micheal D. Gaul, Zhijie Liu
  • Bicyclic Pyridin-2-one and pyrimidin-4-one Derivatives Useful As a Factor XIa Inhibitors
    Publication number: 20230097157
    Abstract: The present invention is directed to bicyclic pyridinon-2-one and pyrimidin-4-one derivatives, stereoisomers, isotopologues, and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Application
    Filed: July 21, 2022
    Publication date: March 30, 2023
    Inventors: Guozhang Xu, Mark J. Macielag, Micheal D. Gaul, Tho V. Thieu, Zhijie Liu
  • PYRIDINE N-OXIDE DERIVATIVES USEFUL AS FACTOR XIA INHIBITORS
    Publication number: 20230091768
    Abstract: The present invention is directed to pyridine N-oxide derivatives, stereoisomers, isotopologues, isotopomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Application
    Filed: March 17, 2022
    Publication date: March 23, 2023
    Inventors: Guozhang Xu, Boying Guo, Zhijie Liu, Jing Zhang, Micheal D. Gaul, Eugene B. Grant, Mark J. Macielag, Tianbao Lu, Tho V. Thieu
  • 5-oxo-1,2,3,5,8,8a-hexahydroindolizine-3-carboxamide Derivatives Useful As a Factor XIa Inhibitors
    Publication number: 20230064443
    Abstract: The present invention is directed to 5-oxo-1,2,3,5,8,8a-hexahydroindolizine-3-carboxamide derivatives, stereoisomers, isotopologues, and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
    Type: Application
    Filed: July 21, 2022
    Publication date: March 2, 2023
    Inventors: Guozhang Xu, Mark J. Macielag
  • Cylcoalkenyl derivatives useful as agonists of the GPR120 and/or GPR40 receptors
    Patent number: 11230526
    Abstract: The present invention is directed to cycloalkenyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the GPR120 and/or GPR40 receptors. More particularly, the compounds of the present invention are agonists of GPR120 and/or GPR40, useful in the treatment of, for example, obesity, Type II Diabetes Mellitus, dyslipidemia, etc.
    Type: Grant
    Filed: March 5, 2019
    Date of Patent: January 25, 2022
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Mark J. Macielag, Mark Wall, Michael P. Winters, Yue-Mei Zhang, Zhihua Sui
  • ACYLSUFONAMIDE COMPOUNDS USEFUL AS EP3 RECEPTOR ANTAGONISTS
    Publication number: 20210253562
    Abstract: The present invention is directed to acylsulfonamide derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Application
    Filed: June 28, 2019
    Publication date: August 19, 2021
    Inventors: Bin Zhu, Mark J. Macielag
  • Pyridin-2-one derivatives of formula (I) useful as EP3 receptor antagonists
    Patent number: 10590083
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: March 17, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xuqing Zhang, Mark J. Macielag
  • Pyridin-2-one derivatives of formula (III) useful as EP3 receptor antagonists
    Patent number: 10399944
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: September 3, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xuqing Zhang, Mark J. Macielag
  • Pyridin-2-one derivatives of formula (II) useful as EP3 receptor antagonists
    Patent number: 10336701
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: July 2, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xuqing Zhang, Mark J. Macielag
  • PYRIDIN-2-ONE DERIVATIVES OF FORMULA (I) USEFUL AS EP3 RECEPTOR ANTAGONISTS
    Publication number: 20190047959
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Application
    Filed: August 9, 2018
    Publication date: February 14, 2019
    Inventors: Xuqing Zhang, Mark J. Macielag
  • PYRIDIN-2-ONE DERIVATIVES OF FORMULA (III) USEFUL AS EP3 RECEPTOR ANTAGONISTS
    Publication number: 20190047961
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Application
    Filed: August 9, 2018
    Publication date: February 14, 2019
    Inventors: Xuqing Zhang, Mark J. Macielag
  • PYRIDIN-2-ONE DERIVATIVES OF FORMULA (II) USEFUL AS EP3 RECEPTOR ANTAGONISTS
    Publication number: 20190047960
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Application
    Filed: August 9, 2018
    Publication date: February 14, 2019
    Inventors: Xuqing Zhang, Mark J. Macielag
  • BENZIMIDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
    Publication number: 20190031618
    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: October 3, 2018
    Publication date: January 31, 2019
    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
  • Benzimidazole derivatives useful as CB-1 inverse agonists
    Patent number: 10118900
    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: Grant
    Filed: August 23, 2016
    Date of Patent: November 6, 2018
    Assignee: 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
    Patent number: 9815790
    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: Grant
    Filed: August 17, 2016
    Date of Patent: November 14, 2017
    Assignee: 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
    Patent number: 9682940
    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: Grant
    Filed: August 17, 2016
    Date of Patent: June 20, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark J. Macielag, Rui Zhang, Michael H. Parker, Bart L. DeCorte, Michael N. Greco
  • Benzimidazole derivatives useful TRPM8 channel modulators
    Patent number: 9636345
    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: February 10, 2015
    Date of Patent: May 2, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Mark J. Macielag, Mingde Xia, Xiaoqing Xu