Patents by Inventor Helen Jane Szekeres
Helen Jane Szekeres 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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Publication number: 20240076269Abstract: Small molecule potentiatiors to potassium channels (such as Kv7 potentiators—which are also called KCNQ potentiators), compositions including such compounds, and methods of using such compounds for the treatment of Amyotrophic Lateral Sclerosis and other neurological diseases caused by changes in motor neuron excitability, including, but not limited to, primary lateral sclerosis, pseudobulbar palsy, progressive bulbar palsy, progressive muscular atrophy and epilepsy.Type: ApplicationFiled: November 9, 2023Publication date: March 7, 2024Applicant: EIi Lilly and CompanyInventors: Helen Jane Szekeres, Maria Ann Whatton, Andrew Caerwyn Williams
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Patent number: 11840516Abstract: Small molecule potentiatiors to potassium channels (such as Kv7 potentiators—which are also called KCNQ potentiators), compositions including such compounds, and methods of using such compounds for the treatment of Amyotrophic Lateral Sclerosis and other neurological diseases caused by changes in motor neuron excitability, including, but not limited to, primary lateral sclerosis, pseudobulbar palsy, progressive bulbar palsy, progressive muscular atrophy and epilepsy.Type: GrantFiled: November 19, 2021Date of Patent: December 12, 2023Assignee: Eli Lilly and CompanyInventors: Helen Jane Szekeres, Maria Ann Whatton, Andrew Caerwyn Williams
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Publication number: 20220073464Abstract: Small molecule potentiatiors to potassium channels (such as Kv7 potentiators—which are also called KCNQ potentiators), compositions including such compounds, and methods of using such compounds for the treatment of Amyotrophic Lateral Sclerosis and other neurological diseases caused by changes in motor neuron excitability, including, but not limited to, primary lateral sclerosis, pseudobulbar palsy, progressive bulbar palsy, progressive muscular atrophy and epilepsy.Type: ApplicationFiled: November 19, 2021Publication date: March 10, 2022Inventors: Helen Jane Szekeres, Maria Ann Whatton, Andrew Caerwyn Williams
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Patent number: 11208383Abstract: Small molecule potentiatiors to potassium channels (such as Kv7 potentiators—which are also called KCNQ potentiators), compositions including such compounds, and methods of using such compounds for the treatment of Amyotrophic Lateral Sclerosis and other neurological diseases caused by changes in motor neuron excitability, including, but not limited to, primary lateral sclerosis, pseudobulbar palsy, progressive bulbar palsy, progressive muscular atrophy and epilepsy.Type: GrantFiled: February 4, 2020Date of Patent: December 28, 2021Assignee: Eli Lilly and CompanyInventors: Helen Jane Szekeres, Maria Ann Whatton, Andrew Caerwyn Williams
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Publication number: 20200247752Abstract: Small molecule potentiatiors to potassium channels (such as Kv7 potentiators—which are also called KCNQ potentiators), compositions including such compounds, and methods of using such compounds for the treatment of Amyotrophic Lateral Sclerosis and other neurological diseases caused by changes in motor neuron excitability, including, but not limited to, primary lateral sclerosis, pseudobulbar palsy, progressive bulbar palsy, progressive muscular atrophy and epilepsy.Type: ApplicationFiled: February 4, 2020Publication date: August 6, 2020Applicant: Eli Lilly and CompanyInventors: Helen Jane SZEKERES, Maria Ann WHATTON, Andrew Caerwyn WILLIAMS
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Patent number: 8049013Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “-----” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptable sType: GrantFiled: November 15, 2007Date of Patent: November 1, 2011Assignee: Eli Lilly and CompanyInventors: Kevin Matthew Gardinier, David Joseph Garmene, Erik James Hembre, Michael Brunavs, Helen Jane Szekeres
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Publication number: 20100069352Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “ - - - ” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptableType: ApplicationFiled: November 15, 2007Publication date: March 18, 2010Inventors: Kevin Matthew Gardinier, David Joseph Garmene, Erik James Hembre, Michael Brunavs, Helen Jane Szekeres
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Patent number: 7271191Abstract: The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.Type: GrantFiled: April 1, 2004Date of Patent: September 18, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Michela Bettati, Mark Stuart Chambers, Peter Alan Hunt, Philip Jones, Angus Murray MacLeod, Helen Jane Szekeres, Martin Richard Teall
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Patent number: 7153868Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 16, 2003Date of Patent: December 26, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Philip Jones, Helen Jane Szekeres
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Patent number: 7094777Abstract: Compounds of formula I: are antagonists of the human 5-HT2A receptor, and hence useful in treatment or prevention of a variety of neurological conditions.Type: GrantFiled: November 9, 2004Date of Patent: August 22, 2006Assignee: Merk Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Neil Roy Curtis, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
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Patent number: 6936608Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: November 8, 2001Date of Patent: August 30, 2005Assignee: Merck Sharp & Dohme Ltd.Inventors: Michela Bettati, Peter Blurton, William Robert Carling, Mark Stuart Chambers, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Michael Geoffrey Neil Russell, Leslie Joseph Street, Helen Jane Szekeres, Monique Bodil Van Neil
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Patent number: 6900209Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.Type: GrantFiled: November 22, 2001Date of Patent: May 31, 2005Assignee: Merck sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
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Patent number: 6900215Abstract: A class of 3-phenylimidazo[1,2-?]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: March 19, 2002Date of Patent: May 31, 2005Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Philip Jones, Richard Thomas Lewis, Kevin William Moore, Michael Geoffrey Neil Russell, Leslie Joseph Street, Helen Jane Szekeres
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Publication number: 20040043982Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5-or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.Type: ApplicationFiled: May 21, 2003Publication date: March 4, 2004Inventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
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Publication number: 20040023964Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: ApplicationFiled: May 8, 2003Publication date: February 5, 2004Inventors: Michela Bettati, Peter Blurton, William Robert Carling, Mark Stuart Chambers, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Michael Geoffrey Neil Russell, Leslie Joseph Street, Helen Jane Szekeres, Monique Bodil Van Neil
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Publication number: 20040002504Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: 1Type: ApplicationFiled: April 16, 2003Publication date: January 1, 2004Inventors: Mark Stuart Chambers, Philip Jones, Helen Jane Szekeres
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Publication number: 20020193385Abstract: A class of 3-phenylimidazo[1,2-&agr;]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: ApplicationFiled: March 19, 2002Publication date: December 19, 2002Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Philip Jones, Richard Thomas Lewis, Kevin William Moore, Michael Geoffrey Neil Russell, Leslie Joseph Street, Helen Jane Szekeres