Patents Assigned to Neurogen Corporation
-
Publication number: 20080267887Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention 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 pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.Type: ApplicationFiled: October 5, 2005Publication date: October 30, 2008Applicant: Neurogen CorporationInventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
-
Patent number: 7432275Abstract: Acid-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: GrantFiled: December 12, 2003Date of Patent: October 7, 2008Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Timothy M. Caldwell, Stéphane DeLombaert, Kevin J. Hodgetts, Xiaozhang Zheng
-
Publication number: 20080175794Abstract: Substituted pyridazinyl- and pyrimidinyl-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: ApplicationFiled: January 25, 2006Publication date: July 24, 2008Applicant: NEUROGEN CORPORATIONInventors: Timothy M. Caldwell, Bertrand L. Chenard, Kevin J. Hodgetts
-
Publication number: 20080153857Abstract: Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol 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: ApplicationFiled: December 10, 2007Publication date: June 26, 2008Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Stephane De Lombaert, Xiaozhang Zheng
-
Publication number: 20080139580Abstract: Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, 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: ApplicationFiled: September 14, 2007Publication date: June 12, 2008Applicant: Neurogen CorporationInventors: Linghong Xie, Bingsong Han, Yuelian Xu, George Maynard, Bertrand L. Chenard, Kenneth Shaw, Yang Gao
-
Publication number: 20080132509Abstract: Substituted biaryl 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 localizations studies.Type: ApplicationFiled: December 13, 2005Publication date: June 5, 2008Applicant: Neurogen CorporationInventors: Charles A. Blum, Bertrand L. Chenard, Kevin J. Hodgetts, Xiaozhang Zheng
-
Publication number: 20080125466Abstract: Aryl-substituted benzo[d]isothiazol-3-ylamine 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: ApplicationFiled: July 9, 2004Publication date: May 29, 2008Applicant: NEUROGEN CORPORATIONInventors: Charles A. Blum, Xiaozhang Zheng
-
Patent number: 7371752Abstract: Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are 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, Down Syndrome, 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: GrantFiled: December 3, 2004Date of Patent: May 13, 2008Assignee: Neurogen CorporationInventors: Guolin Cai, Pamela Albaugh, Jun Yuan
-
Publication number: 20080090845Abstract: Haloalkyl-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: ApplicationFiled: August 22, 2007Publication date: April 17, 2008Applicant: Neurogen CorporationInventors: Charles Blum, Xiaozhang Zheng, Isamir Martinez, Bertrand Chenard
-
Publication number: 20080085901Abstract: Heteroaryl substituted 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: ApplicationFiled: January 13, 2006Publication date: April 10, 2008Applicant: Neurogen CorporationInventors: Timothy Caldwell, Bertrand Chenard, Kevin Hodgetts
-
Patent number: 7351826Abstract: The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables 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.Type: GrantFiled: February 16, 2004Date of Patent: April 1, 2008Assignee: Neurogen CorporationInventors: Linghong Xie, Bingsong Han, Yuelian Xu
-
Patent number: 7348326Abstract: 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: GrantFiled: December 6, 2005Date of Patent: March 25, 2008Assignee: Neurogen CorporationInventors: Robert DeSimone, Alan Hutchison, Kenneth Shaw, Daniel Rosewater
-
Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I 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 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
-
Patent number: 7329664Abstract: Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol 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.Type: GrantFiled: July 16, 2004Date of Patent: February 12, 2008Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Stéphane De Lombaert, Xiaozhang Zheng
-
Publication number: 20080032975Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. 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, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: ApplicationFiled: October 15, 2007Publication date: February 7, 2008Applicant: Neurogen Corporation, A Corporation of the State of DelawareInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
-
Patent number: 7326709Abstract: 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: GrantFiled: May 30, 2006Date of Patent: February 5, 2008Assignee: Neurogen CorporationInventors: Jun Yuan, Pamela A. Albaugh, Kenneth Shaw, Alan J. Hutchison
-
Patent number: 7323478Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.Type: GrantFiled: April 8, 2004Date of Patent: January 29, 2008Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
-
Publication number: 20080015183Abstract: 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: ApplicationFiled: September 29, 2007Publication date: January 17, 2008Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles Blum, Harry Brielmann, Timothy Caldwell, Stephane De Lombaert, Kevin Hodgetts, Xiaozhang Zheng, James Krause, Uri Herzberg, Taeyoung Yoon
-
Publication number: 20080015196Abstract: Novel aryl substituted imidazopyrazines, imidazopyrimidines, and imidazopyridines are provided. Such compounds can act as selective modulators of CRF receptors. The imidazopyrazines, imidazopyrimidines, and imidazopyridines 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: ApplicationFiled: April 15, 2005Publication date: January 17, 2008Applicant: NEUROGEN CORPORATIONInventors: Dario Doller, Lu Zhang, Ping Ge, Yasuchika Yamaguchi, Raymond Horvath, Xuechun Zhang
-
Publication number: 20080009477Abstract: CB1 antagonists are provided. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 receptor modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using ligands for receptor localization studies and various in vitro assays.Type: ApplicationFiled: November 1, 2005Publication date: January 10, 2008Applicant: NEUROGEN CORPORATIONInventors: Alan Hutchison, Jun Yuan