Patents by Inventor Kenneth J. Kellar
Kenneth J. Kellar 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).
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Patent number: 11278522Abstract: Previous studies (Xiao et al., 2001) have identified two metabolites of methadone, EMDP (2-ethyl-5-methyl-3,3-diphenyl-1-pyrroline) and EDDP (2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine), which are considered to be inactive at opiate receptors, as relatively potent noncompetitive channel blockers of ?3?4 nAChRs. We have now evaluated these compounds in rats and mice in preclinical behavioral models predictive of potential anxiolytic and antidepressant efficacy. We found that EMDP, but not EDDP, displayed robust effects predictive of anxiolytic and antidepressant efficacy without significant effects on locomotor activity. Moreover, EMDP at behaviorally active doses, unlike mecamylamine, did not produce eyelid ptosis, suggesting it may produce fewer autonomic side effects than mecamylamine. Thus, the methadone metabolite EMDP may represent a novel therapeutic avenue for the treatment of some affective disorders.Type: GrantFiled: July 13, 2020Date of Patent: March 22, 2022Assignee: Georgetown UniversityInventors: Kenneth J. Kellar, Yingxian Xiao, Patrick A. Forcelli
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Publication number: 20210161861Abstract: Previous studies (Xiao et al., 2001) have identified two metabolites of methadone, EMDP (2-ethyl-5-methyl-3,3-diphenyl-1-pyrroline) and EDDP (2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine), which are considered to be inactive at opiate receptors, as relatively potent noncompetitive channel blockers of ?3?4 nAChRs. We have now evaluated these compounds in rats and mice in preclinical behavioral models predictive of potential anxiolytic and antidepressant efficacy. We found that EMDP, but not EDDP, displayed robust effects predictive of anxiolytic and antidepressant efficacy without significant effects on locomotor activity. Moreover, EMDP at behaviorally active doses, unlike mecamylamine, did not produce eyelid ptosis, suggesting it may produce fewer autonomic side effects than mecamylamine. Thus, the methadone metabolite EMDP may represent a novel therapeutic avenue for the treatment of some affective disorders.Type: ApplicationFiled: July 13, 2020Publication date: June 3, 2021Inventors: Kenneth J. Kellar, Yingxian Xiao, Patrick A. Forcelli
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Patent number: 10709685Abstract: Disclosed are methods of treating anxiety or depression, comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of 2-ethyl-5-methyl-3,3-diphenyl-1-pyrroline (EMDP), 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP), and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 31, 2016Date of Patent: July 14, 2020Assignee: Georgetown UniversityInventors: Kenneth J. Kellar, Yingxian Xiao, Patrick A. Forcelli
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Patent number: 10407406Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: GrantFiled: February 13, 2018Date of Patent: September 10, 2019Assignee: Georgetown UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu
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Publication number: 20180305335Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: ApplicationFiled: February 13, 2018Publication date: October 25, 2018Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu
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Publication number: 20180169065Abstract: Disclosed are methods of treating anxiety or depression, comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of 2-ethyl-5-methyl-3,3-diphenyl-1-pyrroline (EMDP), 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP), and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: May 31, 2016Publication date: June 21, 2018Inventors: Kenneth J. Kellar, Yingxian Xiao, Patrick A. Forcelli
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Patent number: 9993465Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: GrantFiled: April 5, 2016Date of Patent: June 12, 2018Assignees: Georgetown University, Duke UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
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Patent number: 9994548Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: GrantFiled: May 23, 2016Date of Patent: June 12, 2018Assignees: Georgetown University, Duke UniversityInventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Patent number: 9890137Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: GrantFiled: March 26, 2014Date of Patent: February 13, 2018Assignee: Georgetown UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu
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Publication number: 20170107197Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: ApplicationFiled: May 23, 2016Publication date: April 20, 2017Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Publication number: 20170035743Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: ApplicationFiled: April 5, 2016Publication date: February 9, 2017Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
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Patent number: 9346784Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: GrantFiled: November 9, 2012Date of Patent: May 24, 2016Assignees: Georgetown University, Duke UniversityInventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Patent number: 9303017Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: GrantFiled: November 9, 2012Date of Patent: April 5, 2016Assignees: Georgetown University, Duke UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
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Publication number: 20160031853Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: ApplicationFiled: March 26, 2014Publication date: February 4, 2016Applicant: Georgetown UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu
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Publication number: 20140378428Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: ApplicationFiled: November 9, 2012Publication date: December 25, 2014Applicants: Georgetown University, Duke UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
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Publication number: 20140323461Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: ApplicationFiled: November 9, 2012Publication date: October 30, 2014Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Patent number: 8729103Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.Type: GrantFiled: May 26, 2009Date of Patent: May 20, 2014Assignee: Georgetown UniversityInventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar
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Patent number: 8642612Abstract: The present invention discloses nicotinic desensitizers and methods of selecting, testing, and using them. The present invention provides methods for selecting nicotinic desensitizers from one or more compounds by using receptor, cell, and tissue models; and methods for testing one or more nicotinic desensitizers for their therapeutic utility by using animal models. The present invention also provides compounds of formula (I) and (II) as nicotinic desensitizers. Nicotinic desensitizers of the present invention are useful for the treatment of a wide range of conditions, diseases, and disorders.Type: GrantFiled: July 18, 2007Date of Patent: February 4, 2014Assignee: Potomac Pharmaceuticals, Inc.Inventors: Yingxian Xiao, Kenneth J. Kellar
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Publication number: 20110281836Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.Type: ApplicationFiled: November 19, 2010Publication date: November 17, 2011Applicant: PSYCHOGENICS, INC.Inventors: Joel R. Walker, Milton Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar
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Publication number: 20110269733Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.Type: ApplicationFiled: May 26, 2009Publication date: November 3, 2011Applicant: Georgetown UniversityInventors: Milton I. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar