Patents Assigned to Neurogen Corporation
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Patent number: 8759361Abstract: 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: GrantFiled: August 22, 2011Date of Patent: June 24, 2014Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Patent number: 8334382Abstract: 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: GrantFiled: February 15, 2010Date of Patent: December 18, 2012Assignee: Neurogen CorporationInventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
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Publication number: 20120208829Abstract: 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: ApplicationFiled: August 22, 2011Publication date: August 16, 2012Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Patent number: 8003656Abstract: 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: GrantFiled: August 22, 2007Date of Patent: August 23, 2011Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Publication number: 20110160187Abstract: 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: ApplicationFiled: May 6, 2005Publication date: June 30, 2011Applicant: Neurogen CorporationInventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
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Patent number: 7935702Abstract: 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: GrantFiled: October 12, 2005Date of Patent: May 3, 2011Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Kevin J. Hodgetts, Scott Michael Capitosti
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Publication number: 20110002855Abstract: 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: ApplicationFiled: June 25, 2008Publication date: January 6, 2011Applicant: NEUROGEN CORPORATIONInventors: Timothy M. Caldwell, Yang Gao, Linghong Xie, Yuelian Xu
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Patent number: 7851474Abstract: 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: GrantFiled: July 28, 2006Date of Patent: December 14, 2010Assignee: Neurogen CorporationInventors: Linghong Xie, Joseph W. Ochterski, Yang Gao, Bingsong Han, Timothy M. Caldwell, Yuelian Xu, John M. Peterson, Ping Ge, Robert Ohliger
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Patent number: 7795262Abstract: 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: GrantFiled: March 8, 2007Date of Patent: September 14, 2010Assignee: Neurogen CorporationInventors: Yang Gao, Bingsong Han, Linghong Xie
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Publication number: 20100217012Abstract: 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: ApplicationFiled: March 26, 2008Publication date: August 26, 2010Applicant: NEUROGEN CORPORATIONInventors: Zhe-qing Wang, Andrew J. Staab, Christopher K. Seekamp, George P. Luke
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Patent number: 7728009Abstract: 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: GrantFiled: February 16, 2006Date of Patent: June 1, 2010Assignee: Neurogen CorporationInventors: Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
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Patent number: 7662830Abstract: 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: GrantFiled: August 13, 2005Date of Patent: February 16, 2010Assignee: Neurogen CorporationInventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
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Publication number: 20100008866Abstract: 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: ApplicationFiled: May 6, 2009Publication date: January 14, 2010Applicant: Neurogen CorporationInventors: Charles A. Blum, Manuka Ghosh, Isamir Martinez, Xuechun Zhang, Xiaozhang Zheng
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Patent number: 7642267Abstract: 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: GrantFiled: November 19, 2007Date of Patent: January 5, 2010Assignee: Neurogen CorporationInventors: 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
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Publication number: 20090286767Abstract: 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: ApplicationFiled: February 9, 2009Publication date: November 19, 2009Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Stéphane De Lombaert, Kevin J. Hodgetts
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Patent number: 7566712Abstract: 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: GrantFiled: July 16, 2004Date of Patent: July 28, 2009Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles A. Blum, Stéphane De Lombaert, Taeyoung Yoon, Xiaozhang Zheng
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Publication number: 20090069347Abstract: 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: ApplicationFiled: August 22, 2007Publication date: March 12, 2009Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Patent number: 7488740Abstract: 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: GrantFiled: July 14, 2004Date of Patent: February 10, 2009Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Stéphane De Lombaert, Kevin J. Hodgetts
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Patent number: 7482350Abstract: 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: GrantFiled: May 6, 2005Date of Patent: January 27, 2009Assignee: Neurogen CorporationInventors: George D. Maynard, Manuka Ghosh, Jun Yuan, Kevin S. Currie, Scott Mitchell, Qin Guo, He Zhao
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Publication number: 20090023737Abstract: 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: ApplicationFiled: February 9, 2005Publication date: January 22, 2009Applicant: NEUROGEN CORPORATIONInventors: Yuelian Xu, Bingsong Han, Linghong Xie, George D. Maynard