Patents Assigned to Neurogen Corporation
  • Patent number: 8759361
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: June 24, 2014
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Patent number: 8334382
    Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: December 18, 2012
    Assignee: Neurogen Corporation
    Inventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
  • Publication number: 20120208829
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: August 22, 2011
    Publication date: August 16, 2012
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Patent number: 8003656
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 22, 2007
    Date of Patent: August 23, 2011
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Publication number: 20110160187
    Abstract: The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
    Type: Application
    Filed: May 6, 2005
    Publication date: June 30, 2011
    Applicant: Neurogen Corporation
    Inventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
  • Patent number: 7935702
    Abstract: Substituted biaryl quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: October 12, 2005
    Date of Patent: May 3, 2011
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Kevin J. Hodgetts, Scott Michael Capitosti
  • Publication number: 20110002855
    Abstract: Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Application
    Filed: June 25, 2008
    Publication date: January 6, 2011
    Applicant: NEUROGEN CORPORATION
    Inventors: Timothy M. Caldwell, Yang Gao, Linghong Xie, Yuelian Xu
  • Patent number: 7851474
    Abstract: Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: December 14, 2010
    Assignee: Neurogen Corporation
    Inventors: Linghong Xie, Joseph W. Ochterski, Yang Gao, Bingsong Han, Timothy M. Caldwell, Yuelian Xu, John M. Peterson, Ping Ge, Robert Ohliger
  • Patent number: 7795262
    Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: March 8, 2007
    Date of Patent: September 14, 2010
    Assignee: Neurogen Corporation
    Inventors: Yang Gao, Bingsong Han, Linghong Xie
  • Publication number: 20100217012
    Abstract: Processes and intermediates are provided for the preparation of substituted aminomethyl 2,3,8,9-tetrahydiO-7H-1,4-dioxino[2.3-e]indo]-8-ones of the Formula (A) wherein the variables n, R and R3 are as described herein. Such compounds are useful, for example, as dopamine receptor agonists.
    Type: Application
    Filed: March 26, 2008
    Publication date: August 26, 2010
    Applicant: NEUROGEN CORPORATION
    Inventors: Zhe-qing Wang, Andrew J. Staab, Christopher K. Seekamp, George P. Luke
  • Patent number: 7728009
    Abstract: Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: June 1, 2010
    Assignee: Neurogen Corporation
    Inventors: Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
  • Patent number: 7662830
    Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptors activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 13, 2005
    Date of Patent: February 16, 2010
    Assignee: Neurogen Corporation
    Inventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
  • Publication number: 20100008866
    Abstract: Cis-cyclohexyl substituted pyrimidinone derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: May 6, 2009
    Publication date: January 14, 2010
    Applicant: Neurogen Corporation
    Inventors: Charles A. Blum, Manuka Ghosh, Isamir Martinez, Xuechun Zhang, Xiaozhang Zheng
  • Patent number: 7642267
    Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
    Type: Grant
    Filed: November 19, 2007
    Date of Patent: January 5, 2010
    Assignee: Neurogen Corporation
    Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
  • Publication number: 20090286767
    Abstract: Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: February 9, 2009
    Publication date: November 19, 2009
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Stéphane De Lombaert, Kevin J. Hodgetts
  • Patent number: 7566712
    Abstract: Biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: July 28, 2009
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Charles A. Blum, Stéphane De Lombaert, Taeyoung Yoon, Xiaozhang Zheng
  • Publication number: 20090069347
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: August 22, 2007
    Publication date: March 12, 2009
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Patent number: 7488740
    Abstract: Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: July 14, 2004
    Date of Patent: February 10, 2009
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Stéphane De Lombaert, Kevin J. Hodgetts
  • Patent number: 7482350
    Abstract: 4,5-disubstituted-2-arylpyrimidines of Formula I and Formula II are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: January 27, 2009
    Assignee: Neurogen Corporation
    Inventors: George D. Maynard, Manuka Ghosh, Jun Yuan, Kevin S. Currie, Scott Mitchell, Qin Guo, He Zhao
  • Publication number: 20090023737
    Abstract: Compounds of the Formula: are provided, as are methods for their preparation. The variables Z1, Z2, R3, Z4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
    Type: Application
    Filed: February 9, 2005
    Publication date: January 22, 2009
    Applicant: NEUROGEN CORPORATION
    Inventors: Yuelian Xu, Bingsong Han, Linghong Xie, George D. Maynard