Patents Assigned to Neurogen Corporation
  • 5-Substituted-2-arylpyrazines
    Publication number: 20070043056
    Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Application
    Filed: October 23, 2006
    Publication date: February 22, 2007
    Applicant: Neurogen Corporation
    Inventors: Taeyoung Yoon, Ping Ge, Stephane De Lombaert, Raymond Horvath, Dario Doller, Kevin Hodgetts, Lu Yan Zhang, Bernd Kaiser, Xuechun Zhang, Cunyu Zhang, Jim Darrow, Yasuchika Yamaguchi
  • 5-substituted-2-arylpyrazines
    Patent number: 7179807
    Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: August 20, 2003
    Date of Patent: February 20, 2007
    Assignee: Neurogen Corporation
    Inventors: Taeyoung Yoon, Ping Ge, Stéphane De Lombaert, Raymond F. Horvath, Dario Doller, Kevin J. Hodgetts, Lu Yan Zhang, Bernd Kaiser, Xuechun Zhang, Yasuchika Yamaguchi, Cunyu Zhang, Jim Darrow
  • Amino methyl imidazoles as C5a receptor modulators
    Patent number: 7169775
    Abstract: Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: January 30, 2007
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, He Zhao, Suoming Zhang, Yang Gao
  • 5-substituted 2-aryl-4-pyrimidinones
    Patent number: 7169790
    Abstract: Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: June 7, 2005
    Date of Patent: January 30, 2007
    Assignee: Neurogen Corporation
    Inventors: Kevin J. Hodgetts, Dario Doller
  • Melanin concentrating hormone receptor ligands: substituted 2-(4-benzyl-piperazin-1-ylmethyl)- and 2-(4-benzyl-diazepan-1-ylmethyl)-1H-benzoimidazole analogues
    Patent number: 7160879
    Abstract: Melanin concentrating hormone receptor ligands (especially substituted 2-(4-benzyl-piperazin-1-ylmethyl)-1H-benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: January 9, 2003
    Date of Patent: January 9, 2007
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, John M. Peterson, Cheryl Steenstra, Yiping Shen, Linda M. Gustavson, Christopher Mach, Alan Hutchison
  • Substituted biaryl amides as C5A receptor modulators
    Patent number: 7148225
    Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.
    Type: Grant
    Filed: November 19, 2004
    Date of Patent: December 12, 2006
    Assignee: Neurogen Corporation
    Inventors: Yang Gao, Alan J. Hutchinson, Wallace C. Pringle, Taeyoung Yoon, He Zhao
  • Monkey and canine melanin concentrating hormone receptors
    Patent number: 7141391
    Abstract: Isolated polynucleotides encoding monkey and canine Melanin Concentrating Hormone (MCH) Type 2 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH receptor polypeptides, and isolated MCH receptor polypeptides are also provided. MCH receptor polynucleotides and polypeptides may be used, for example, to identify agents that specifically interact with MCH receptor. Such agents find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: November 28, 2006
    Assignee: Neurogen Corporation
    Inventors: Michele Bennet Kinrade, Robbin M. Brodbeck, Stephen M. Waters, James E. Krause
  • Imidazol-1-ylmethyl pyridazine derivatives
    Patent number: 7122546
    Abstract: The invention provides imidazol-1-ylmethyl pyridazine derivatives of the formula: that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar 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: Grant
    Filed: October 7, 2003
    Date of Patent: October 17, 2006
    Assignee: Neurogen Corporation
    Inventors: Linghong Xie, Bingsong Han, Yuelian Xu, George D. Maynard
  • Substituted pyrirmidin-4-ylamine analogues as vanilloid receptor ligands
    Publication number: 20060229308
    Abstract: Substituted pyrimidyl-4-ylamine analogues are provided, of the Formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate Vanilloid 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: July 15, 2004
    Publication date: October 12, 2006
    Applicant: Neurogen Corporation
    Inventors: Charles Blum, Harry Brielmann, Kevin Hodgetts
  • Bicyclic and tricyclic heteroaromatic compounds
    Publication number: 20060217384
    Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
    Type: Application
    Filed: May 30, 2006
    Publication date: September 28, 2006
    Applicant: Neurogen Corporation, A Corporation of the state of Delaware
    Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
  • Fused pyrrolecarboxamides; GABA brain receptor ligands
    Patent number: 7109351
    Abstract: Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
    Type: Grant
    Filed: August 30, 2000
    Date of Patent: September 19, 2006
    Assignee: Neurogen Corporation
    Inventors: Pamela Albaugh, Kenneth Shaw, Alan Hutchison
  • Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands
    Publication number: 20060199823
    Abstract: Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Application
    Filed: March 24, 2006
    Publication date: September 7, 2006
    Applicant: Neurogen Corporation
    Inventors: Ping Ge, Raymond Horvath, Lu Zhang, Yasuchika Yamaguchi, Bernd Kaiser, Xuechun Zhang, Suoming Zhang, He Zhao
  • 1-phenyl-4-benzylpiperazines dopamine receptor subtype specific ligands
    Patent number: 7101887
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1–C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1–C4 alkyl, C1–C4 alkoxy, alkylthio, hydroxy, amino, mono(C1–C4)alkylamino, di(C1–C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: September 5, 2006
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Xi Chen
  • Capsaicin receptor agonists
    Publication number: 20060194805
    Abstract: Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VR1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin 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: April 26, 2006
    Publication date: August 31, 2006
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Charles Blum, Harry Brielmann, Timothy Caldwell, Daniel Cortright, Kevin Hodgetts, John Peterson, Xiaozhang Zheng
  • Substituted quinazolin-4-ylamine analogues
    Publication number: 20060173003
    Abstract: Substituted quinazolin-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 1, 2006
    Publication date: August 3, 2006
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Charles Blum, Harry Brielmann, Timothy Caldwell, Stephane De Lombaert, Kevin Hodgetts, Xiaozhang Zheng, James Krause, Uri Herzberg
  • Heteroaryl fused aminoalkyl imidazole derivates: selective modulators of GABAA receptors
    Publication number: 20060160842
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
    Type: Application
    Filed: December 6, 2005
    Publication date: July 20, 2006
    Applicant: Neurogen Corporation
    Inventors: Robert DeSimone, Alan Hutchison, Kenneth Shaw, Daniel Rosewater
  • Melanin concentrating hormone receptors
    Patent number: 7078187
    Abstract: Isolated polynucleotides encoding monkey Melanin Concentrating Hormone (MCH) Type 1 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH1R polypeptides, and isolated MCH1R polypeptides are also provided. MCH1R polynucleotides and polypeptides may be used, for example, to identify compounds that specifically interact with MCH receptor. Such compounds find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: July 18, 2006
    Assignee: Neurogen Corporation
    Inventors: Michele Bennett Kinrade, Robbin M. Brodbeck, James E. Krause
  • Melanin concentrating hormone receptors
    Patent number: 7078484
    Abstract: Isolated polynucleotides encoding monkey Melanin Concentrating Hormone (MCH) Type 1 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH1R polypeptides, and isolated MCH1R polypeptides are also provided. MCH1R polynucleotides and polypeptides may be used, for example, to identify compounds that specifically interact with MCH receptor. Such compounds find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: July 18, 2006
    Assignee: Neurogen Corporation
    Inventors: Michele Bennet Kinrade, Robbin M. Brodbeck, Stephen M. Waters, James E. Krause
  • Substituted (heterocycloalkyl)methyl azole derivatives as c5a receptor modulators
    Publication number: 20060154917
    Abstract: (Heterocycloalkyl)methyl azole derivatives of Formula (I) are provided: Formula I wherein A is oxygen, sulfur, or NR; J and K and each L are independently oxygen, sulfur, NH, or CH2; and the remaining variables are defined herein. Such compounds are modulators of C5a receptors, and preferably bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. Also provided herein are pharmaceutical compositions comprising such compounds, as well as methods for using such compounds in treating a variety of inflammatory and immune system disorders.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 13, 2006
    Applicant: Neurogen Corporation
    Inventors: Suoming Zhang, He Zhao, Yang Gao, Andrew Thurkauf, George Maynard, Bertrand Chenard, Robert Ohliger, John Peterson
  • Substituted quinazolin-4-ylamine analogues
    Patent number: 7074799
    Abstract: Substituted quinazolin-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: January 17, 2003
    Date of Patent: July 11, 2006
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Timothy M. Caldwell, Stephane De Lombaert, Kevin J. Hodgetts, Xiaozhang Zheng