Patents by Inventor Nicolas Zorn

Nicolas Zorn 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).

  • NEW CYCLOPENTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20240190889
    Abstract: The invention provides heterocyclic compounds having the general formula (1), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.
    Type: Application
    Filed: February 1, 2024
    Publication date: June 13, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Giuseppe CECERE, Luca GOBBI, Maria-Clemencia HERNANDEZ, Andreas KOBLET, Andres Miguel OLIVARES MORALES, Valerie RUNTZ-SCHMITT, Nicolas ZORN
  • SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20240002393
    Abstract: Compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: July 20, 2023
    Publication date: January 4, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Giuseppe CECERE, Luca GOBBI, Maria-Clemencia HERNANDEZ, Frédéric KNOFLACH, Andreas KOBLET, Eoin Cornelius O'CONNOR, Andres Miguel OLIVARES MORALES, Michael REUTLINGER, Valerie RUNTZ-SCHMITT, Jaclyn Ivy WAMSTEEKER CUSULIN, Nicolas ZORN
  • Substituted benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepines as GABA A GAMMA1 positive allosteric modulators
    Patent number: 11739095
    Abstract: Compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 30, 2021
    Date of Patent: August 29, 2023
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Giuseppe Cecere, Luca Gobbi, Maria-Clemencia Hernandez, Frédéric Knoflach, Andreas Koblet, Eoin Cornelius O'Connor, Andres Miguel Olivares Morales, Michael Reutlinger, Valerie Runtz-Schmitt, Jaclyn Ivy Wamsteeker Cusulin, Nicolas Zorn
  • BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
    Publication number: 20230141603
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds for treatment of CNS disorders.
    Type: Application
    Filed: October 18, 2022
    Publication date: May 11, 2023
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Giuseppe CECERE, Luca GOBBI, Maria-Clemencia HERNANDEZ, Frédéric KNOFLACH, Andreas KOBLET, Eoin Cornelius O'CONNOR, Andres Miguel OLIVARES MORALES, Valerie RUNTZ-SCHMITT, Jaclyn WAMSTEEKER CUSULIN, Nicolas ZORN
  • BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
    Publication number: 20210309664
    Abstract: Compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: March 30, 2021
    Publication date: October 7, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Giuseppe CECERE, Luca GOBBI, Maria-Clemencia HERNANDEZ, Frédéric KNOFLACH, Andreas KOBLET, Eoin Cornelius O'CONNOR, Andres Miguel OLIVARES MORALES, Michael REUTLINGER, Valerie RUNTZ-SCHMITT, Jaclyn Ivy WAMSTEEKER CUSULIN, Nicolas ZORN
  • Dimeric compounds
    Patent number: 10398702
    Abstract: The present invention provides a compound of formula I which act as inhibitors of SMAC protein binding to Inhibitor of Apoptosis Proteins (IAPs), and/or inhibitors of activated caspase protein binding to IAPs (I) their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances, alone or in combination with DR5/FAP agonist antibodies. The active compound of the present invention is useful in the amelioration, treatment or control of cancer, especially solid tumors.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: September 3, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Guido Galley, Roger Norcross, Nicolas Zorn
  • DIMERIC COMPOUNDS
    Publication number: 20190134050
    Abstract: The present invention provides a compound of formula I which act as inhibitors of SMAC protein binding to Inhibitor of Apoptosis Proteins (IAPs), and/or inhibitors of activated caspase protein binding to IAPs (I) their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances, alone or in combination with DR5/FAP agonist antibodies. The active compound of the present invention is useful in the amelioration, treatment or control of cancer, especially solid tumors.
    Type: Application
    Filed: May 5, 2017
    Publication date: May 9, 2019
    Inventors: Alexander FLOHR, Guido GALLEY, Roger NORCROSS, Nicolas ZORN
  • Heterobicyclo-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A anatagonist properties
    Patent number: 10011615
    Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Xianhai Huang, Timothy J. Henderson, Jae-Hun Kim, Christopher Boyce, Pauline Ting, Junying Zheng, Edward Metzger, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Qiaolin Deng
  • Piperazine derivatives as HIV protease inhibitors
    Patent number: 9840478
    Abstract: The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter D. Williams, John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Kartik M. Keertikar, H. Marie Loughran, Jessie J. Manikowski, Gregori J. Morriello, Dong-Ming Shen, Edward C. Sherer, Jurgen Schultz, Sherman T. Waddell, Catherine M. Wiscount, Nicolas Zorn, Xin-Jie Chu, Satyanarayana Tummanapalli, Vijayasaradhi Sivalenka, Bin Hu, Tao Ji, Bin Zhong
  • HETEROBICYCLO-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
    Publication number: 20170197991
    Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Application
    Filed: February 2, 2017
    Publication date: July 13, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Xianhai Huang, Timothy J. Henderson, Jae-Hun Kim, Christopher Boyce, Pauline Ting, Junying Zheng, Edward Metzger, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Qiaolin Deng
  • Piperazine-substituted [1,2,4]triazolo[1,5-C]quinazolin-5-amine compounds with Aantagonist properties
    Patent number: 9676780
    Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: June 13, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Michael Berlin, Pauline Ting, Gang Zhou, Tao Yu, Christopher Boyce, Joseph Michael Kelly, Jayaram R. Tagat, Junying Zheng, Xianhai Huang, Wei Zhou, Jae-Hun Kim, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Rajan Anand, Qiaolin Deng
  • Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
    Patent number: 9549917
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: January 24, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Casey C. McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
  • Heterocyclic compounds and methods of use thereof for the treatment of hepatitis C
    Patent number: 9549921
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: January 24, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Zhong Lai, Xing Dai, Dong Xiao, Clare London, Nicolas Zorn, Ravi Nargund, Anandan Palani, Casey C. McComas, Peng Li, Xuanjia Peng, Richard Soll
  • Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
    Patent number: 9493461
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Zhong Lai, Ravi Nargund, Karen Marcantonio, Dong Xiao, Linda L. Brockunier, Nicolas Zorn, Qun Dang, Xuanjia Peng, Peng Li
  • PIPERAZINE-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
    Publication number: 20160194330
    Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 7, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Michael Berlin, Pauline Ting, Gang Zhou, Tao Yu, Christopher Boyce, Joseph Michael Kelly, Jayaram R. Tagat, Junying Zheng, Xianhai Huang, Wei Zhou, Jae-Hun Kim, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Rajan Anand, Qiaolin Deng
  • Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 9364482
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Ravi Nargund, Dong Xiao, Nicolas Zorn, Qun Dang, Casey C. McComas, Xuanjia Peng, Peng Li, Richard Soll
  • PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS
    Publication number: 20160159752
    Abstract: The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Application
    Filed: July 29, 2014
    Publication date: June 9, 2016
    Applicants: Merck Sharp & Dohme Corp., MSD R&D (CHINA) CO., LTD.
    Inventors: Peter D. Williams, John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Kartik M. Keertikar, H. Marie Loughran, Jessie J. Manikowski, Gregori J. Morriello, Dong-Ming Shen, Edward C. Sherer, Jurgen Schultz, Sherman T. Waddell, Catherine M. Wiscount, Nicolas Zorn, Xin-Jie Chu, Satyanarayana Tummanapalli, Vijayasaradhi Sivalenka, Bin Hu, Tao Ji, Bin Zhong
  • HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C
    Publication number: 20160143895
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: June 19, 2014
    Publication date: May 26, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Zhong Lai, Xing Dai, Dong Xiao, Clare London, Nicolas Zorn, Ravi Nargund, Anandan Palani, Casey C. McComas, Peng Li, Xuanjia Peng, Richard Soll
  • SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20160136172
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: June 19, 2014
    Publication date: May 19, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xing DAI, Hong LIU, Anandan PALANI, Shuwin HE, Ravi NARGUND, Dong XIAO, Nicolas ZORN, Qun DANG, Casey C. MCCOMAS, Xuanjia PENG, Peng LI, Richard SOLL
  • Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 9265773
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: August 20, 2012
    Date of Patent: February 23, 2016
    Assignees: Merck Sharp & Dohme Corp., MSD Italia S.R.L.
    Inventors: Casey C. McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund