Sulfur Is Part Of A Substituent Which Contains Additional Nitrogen Patents (Class 514/593)
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Patent number: 11951085Abstract: The present technology is related to reducing or treating neurological swelling and related conditions with SUR1-TRPM4 channel inhibitors. In some embodiments, the methods include: reducing late neurological deterioration or preventing death, reducing cerebral midline shift, reducing the degree of disability in a subject, counteracting blood glucose levels in a subject receiving a SUR1-TRPM4 channel inhibitor, preventing brain swelling, monitoring liver enzyme activity along with treating injury or conditions related to CNS edema, or monitoring cardiac activity along with treating injury or conditions related to CNS edema.Type: GrantFiled: September 29, 2021Date of Patent: April 9, 2024Assignee: REMEDY PHARMACEUTICALS, INC.Inventor: Sven Martin Jacobson
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Patent number: 11623922Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.Type: GrantFiled: October 3, 2018Date of Patent: April 11, 2023Assignee: INFLAZOME LIMITEDInventors: David Miller, Stephen Thom, Stephen St-Gallay, Jonathan Shannon, Paul Leeson
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Patent number: 11236045Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions as well as treatment of disease states mediated by NLRP3 as well as treatment of diseases or conditions in which interleukin 1? activity and interleukin-18 (IL-18) is implicated.Type: GrantFiled: June 8, 2018Date of Patent: February 1, 2022Assignee: Cadila Healthcare LimitedInventors: Rajiv Sharma, Pravin Iyer, Sameer Agarwal
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Patent number: 11166966Abstract: Compounds including vitamins and aspirin are disclosed. The compounds are provided in dosage form and preferably include selected amounts of folic acid, vitamin D, calcium, vitamin C, thiamine, and riboflavin with the aspirin. A protective coating is preferably provided between the aspirin and the other vitamin and mineral constituents. The dosages are effective in the treatment and prevention of pre-natal conditions.Type: GrantFiled: November 3, 2017Date of Patent: November 9, 2021Inventor: Roxane Handal-Orefice
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Patent number: 9962371Abstract: Disclosed in certain embodiments is a pharmaceutical composition for parenteral administration comprising: an aqueous solution comprising ketorolac or a pharmaceutically acceptable salt thereof in an amount from about 0.1 mg/mL to about 10 mg/mL; and a pharmaceutically acceptable excipient; wherein the formulation is substantially free of alcohol.Type: GrantFiled: July 15, 2016Date of Patent: May 8, 2018Assignee: RTU PHARMACEUTICALS, LLCInventors: Joseph V. Pergolizzi, Alexander Mironov, Chad James Pickens, Douglas Giles Johnson
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Patent number: 9675289Abstract: A system and method for monitoring individual metabolic response and for generating nutritional feedback involve monitoring of a glucose level in a qualified subject. The method comprises the step of consecutively performing a plurality of measurements of a glucose level in the qualified subject by a measuring device. In the measuring device first data corresponding to the measured glucose level is generated. This data is further transmitted to an analysis device. There, second data is generated representing at least one measure for variability of a glucose level of the subject from a time-series of glucose measurements represented by the first data. The second data is compared with reference data and a result of the comparison is further processed for generating a conclusion about nutritional quality of foodstuffs consumed by the subject and/or about a risk of long-term health complications of the subject. Finally, feedback is provided corresponding to the conclusion on an output device.Type: GrantFiled: June 6, 2008Date of Patent: June 13, 2017Assignee: Roche Diabetes Care, Inc.Inventor: Kelly Heaton
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Patent number: 9254259Abstract: The present disclosure is drawn to a method of administering glyburide intravenously to a subject over a period of time as a first bolus administration of glyburide; a second bolus administration of glyburide, after the first bolus; and a first continuous infusion administration of glyburide, wherein the first continuous infusion is administered at a first rate of administration for a first period of time, after the second bolus administration of glyburide.Type: GrantFiled: October 28, 2014Date of Patent: February 9, 2016Assignee: Remedy Pharmaceuticals, Inc.Inventor: Sven Martin Jacobson
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Publication number: 20150141516Abstract: The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pH values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) freeze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.Type: ApplicationFiled: October 7, 2014Publication date: May 21, 2015Inventor: Sven Jacobson
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Publication number: 20150140092Abstract: The invention relates generally to methods of making formulations for delivering biological agents to a patient. In one aspect, proliposomal drug-delivery systems for medicaments are provided. In another aspect, coated proliposomal formulations for poorly water soluble drugs, and methods for making the same, are provided. Certain embodiments of the present invention provide enhanced stability and bioavailability for pharmaceutical formulations.Type: ApplicationFiled: November 17, 2014Publication date: May 21, 2015Inventor: Guru V. BETAGERI
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Patent number: 8980952Abstract: The present invention is directed to therapeutic compounds, treatment methods, and kits affecting the NCCa-ATP channel of neural tissue, including neurons, glia and blood vessels within the nervous system, and methods of using same. The NCCa-ATP channel is newly expressed in neural tissue following injury such as ischemia, and is regulated by the sulfonylurea receptor SUR1, being inhibited by sulfonylurea compounds, e.g., glibenclamide and tolbutamide, and opened by diazoxide. Antagonists of the NCCa-ATP channel, including SUR1 antagonists, are useful in the prevention, diminution, and treatment of injured or diseased neural tissue, including astrocytes, neurons and capillary endothelial cells, that is due to ischemia, tissue trauma, brain swelling and increased tissue pressure, or other forms of brain or spinal cord disease or injury. Agonists of the NCCa-ATP channel may be are useful in the treatment neural tissue where damage or destruction of the tissue, such as a gliotic capsule, is desired.Type: GrantFiled: February 22, 2006Date of Patent: March 17, 2015Assignees: University of Maryland, Baltimore, The United States of America as represented by the Dept. of Veterans AffairsInventors: J. Marc Simard, Mingkui Chen
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Publication number: 20150051289Abstract: The present invention relates to a liquid pharmaceutical formulation of hypoglycaemic sulfonamide, intended for oral or ophthalmic administration. The present invention relates in particular to an oral formulation particularly suitable for paediatric use.Type: ApplicationFiled: February 28, 2013Publication date: February 19, 2015Inventor: Marianne Berdugo Polak
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Patent number: 8946293Abstract: Methods of administering glyburide, or other drug, are disclosed. The novel methods disclosed herein include intravenous methods of administering glyburide, or other drug, over periods of more than an hour, preferably over periods of about 72 hours. The novel methods include administering a bolus of glyburide, or other drug, followed by a first continuous infusion administration of glyburide, or other drug; and optionally a second or further bolus administration of glyburide, or other drug, and/or a second or further continuous infusion administration of glyburide, or other drug. These methods are effective to rapidly achieve a desired level of glyburide, or other drug, and to provide a substantially steady level of glyburide, or other drug, over a desired period of time. The methods disclosed herein may be useful for treating a subject in need of treatment for, e.g.Type: GrantFiled: July 18, 2011Date of Patent: February 3, 2015Assignee: Remedy Pharmaceuticals, Inc.Inventor: Sven Martin Jacobson
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Publication number: 20140378548Abstract: The invention relates to a compound which is effective in inhibiting the function of the TRPM4 ion channel and the use of such compound in treating or preventing a neurodegenerative disease, such as Multiple Sclerosis, Parkinson's disease, Alzheimer's disease, or a myotrophic lateral sclerosis, in a subject. The invention also provides a pharmaceutical composition comprising a TRPM4 inhibitory compound. The invention further relates to in vitro methods for identifying pharmaceutically active compounds that are useful for treating or preventing a neurodegenerative disease.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Inventors: Manuel Friese, Benjamin Schattling, Karin Steinbach, Marc Freichel, Veit Flockerzi, Rudi Vennekens, Doron Merkler
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Patent number: 8883852Abstract: Provided herein are methods, for reducing, preventing, mitigating and treating damage caused by radiation. The methods comprise delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation or to mitigate apoptosis. The compounds comprise glyburide or other sulfonylurea hypoglycemic compounds or potassium channel inhibitors.Type: GrantFiled: October 21, 2009Date of Patent: November 11, 2014Assignee: University of Pittburgh—Of the Commonwealth System of Higher EducationInventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
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Publication number: 20140323423Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.Type: ApplicationFiled: May 2, 2014Publication date: October 30, 2014Applicant: Chrono Therapeutics, Inc.Inventors: Guy DiPierro, Steven A. Giannos
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Publication number: 20140314746Abstract: The invention includes novel methods of treating or preventing fibrosis in a subject afflicted with scleroderma, comprising administering to the subject a therapeutically effective amount of an agent that inhibits formation of at least one inflammasome signaling product in the subject.Type: ApplicationFiled: March 11, 2014Publication date: October 23, 2014Applicant: Philadelphia Health and Education Corporation, d/b/a Drexel University College of MedicineInventors: CAROL M. ARTLETT, PETER D. KATSIKIS
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Publication number: 20140235564Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: ApplicationFiled: February 20, 2014Publication date: August 21, 2014Inventors: J. Marc Simard, Mingkui Chen
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Publication number: 20140199320Abstract: The invention provides inhibitors capable of binding to a member of the inflammasome group comprised of IL-1?, IL-1 receptor type 1, NLRP3, ASC, Caspase-1 and cathepsin B with a dissociation constant of 10-8 mol/l or smaller for the prevention and treatment of acne, specifically an antibody, an antibody fragment, an antibody-like molecule, an oligopeptide of 6 to 30 amino acid residues, a nucleic acid aptamer molecule of 10 to 75 nucleotides in length or a soluble polypeptide comprising a contiguous amino acid sequence of at least 30 amino acids comprised within the protein sequence of a member of the group comprised of IL-1?, IL-1 receptor type 1, IL-1 receptor type 2, NLRP3, ASC and Caspase-1. Similarly, an interfering RNA or an antisense modulator of gene expression of IL-1?, I L-1? receptor type 1, NLRP3, ASC, Caspase-1 and cathepsin B are provided for the prevention or treatment of acne.Type: ApplicationFiled: July 11, 2012Publication date: July 17, 2014Applicant: UNIVERSITAT ZURICHInventors: Dragana Jankovic, Magdalena Kistowiska, Emmanuel Contassot, Lars E. French, Samuel Gehrke
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Publication number: 20140171467Abstract: Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury. In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SURI and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.Type: ApplicationFiled: September 27, 2013Publication date: June 19, 2014Inventor: J. Marc Simard
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Publication number: 20140080811Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.Type: ApplicationFiled: February 27, 2013Publication date: March 20, 2014Applicant: Remedy Pharmaceuticals, Inc.Inventor: Remedy Pharmaceuticals, Inc.
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Publication number: 20140051761Abstract: The present invention relates to pharmaceutical compositions comprising an ATP-sensitive potassium (K ATP) channel antagonist (e.g., sulfonylureas, meglitinides) and methods for treating hyperglycaemia and/or promoting growth of a premature and/or small for gestational age infant.Type: ApplicationFiled: May 2, 2012Publication date: February 20, 2014Applicant: ASSISTANCE PUBLIQUE - HOPITAUX DE PARISInventors: Michel Polak, Marianne Berdugo Polak
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Patent number: 8569377Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.Type: GrantFiled: December 9, 2010Date of Patent: October 29, 2013Assignees: The United States of America as Represented by the Department of Veteran Affairs, University of Maryland, BaltimoreInventor: J. Marc Simard
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Publication number: 20130273181Abstract: Embodiments herein generally relate to methods and compositions for diagnosing and treating congenital muscle diseases (e.g. muscle myopathy disorders). In certain embodiments, methods and compositions generally relate to treating a subject having a muscle myopathy disorder with a dietary supplement and/or sulfonylurea agent.Type: ApplicationFiled: March 7, 2013Publication date: October 17, 2013Inventors: MARTIN GARTZ HANSON, LEE NISWANDER
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Patent number: 8557867Abstract: Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury. In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SUR1 and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.Type: GrantFiled: June 20, 2008Date of Patent: October 15, 2013Assignees: The United States of America as Represented by the Department of Veterans Affairs, University of Maryland, BaltimoreInventor: J. Marc Simard
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Publication number: 20130245069Abstract: The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pH values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) freeze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.Type: ApplicationFiled: September 11, 2012Publication date: September 19, 2013Applicant: Remedy Pharmaceuticals, Inc.Inventor: Sven Jacobson
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Publication number: 20130203853Abstract: Methods of administering glyburide, or other drug, are disclosed. The novel methods disclosed herein include intravenous methods of administering glyburide, or other drug, over periods of more than an hour, preferably over periods of about 72 hours. The novel methods include administering a bolus of glyburide, or other drug, followed by a first continuous infusion administration of glyburide, or other drug; and optionally a second or further bolus administration of glyburide, or other drug, and/or a second or further continuous infusion administration of glyburide, or other drug. These methods are effective to rapidly achieve a desired level of glyburide, or other drug, and to provide a substantially steady level of glyburide, or other drug, over a desired period of time. The methods disclosed herein may be useful for treating a subject in need of treatment for, e.g.Type: ApplicationFiled: July 18, 2011Publication date: August 8, 2013Applicant: Remedy Pharmaceuticals, Inc.Inventor: Sven Martin Jacobson
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Publication number: 20130184293Abstract: The present invention relates to compositions and methods for treating diabetes mellitus, neuropsychological and neurological disorders in a particular group of patient. More specifically, the invention relates to methods of treating diabetes mellitus, neuropsychological and neurological disorders in patients having defective potassium channels. The invention may be used in human subjects, particularly adults or children, and is appropriate to treat various neurological disorders.Type: ApplicationFiled: December 12, 2012Publication date: July 18, 2013Applicants: UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE HOPITAUX DE PARISInventors: ASSISTANCE PUBLIQUE HOPITAUX DE PARIS, UNIVERSITE PARIS DESCARTES
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Patent number: 8318810Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: GrantFiled: September 19, 2007Date of Patent: November 27, 2012Assignees: University of Maryland, Baltimore, The United States of America as represented by the Department of Veterans AffairsInventors: J. Marc Simard, Mingkui Chen
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Publication number: 20120283215Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.Type: ApplicationFiled: September 14, 2010Publication date: November 8, 2012Applicants: The Regents of the University of California, a California Corporation, University of Texas at El Paso, Health and Human ServicesInventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather Balsiger, Robert Fletterick
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Publication number: 20120237449Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Inventors: J. Marc Simard, Mingkui Chen
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Publication number: 20120225947Abstract: The present invention relates to the use of blockers of ion channels regulated by the SUR subunit, for the treatment and/or prevention of eye diseases associated with ischemia and/or retinal excitotoxicity.Type: ApplicationFiled: September 23, 2010Publication date: September 6, 2012Applicant: ASSISTANCE PUBLIQUE - HOPITAUX DE PARISInventors: Michel Polak, Marianne Berdugo Polak, Francine Behar-Cohen, Patricia Crisanti Lassiaz
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Publication number: 20120190618Abstract: The invention provides a method and a pharmaceutical composition in the form of a hydroalcoholic solution in which at least one hypoglycemia-inducing/insulinotropic active principle is dissolved in a stable and complete manner at a dosage that is reduced by 30% to 50% compared with the usual oral unit dosage, for its trans-buccal mucosal application in the spot treatment of postprandial hyperglycemia in type II diabetes in man or animals. The invention also pertains to a method of preparing said formulation and to its specific use in the spot treatment of postprandial hyperglycemia (PPHG) in the context of type II diabetes.Type: ApplicationFiled: July 7, 2010Publication date: July 26, 2012Inventors: Philippe Perovitch, Marc Maury, Jean-Pierre Dumonteix
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Publication number: 20120027879Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: August 3, 2011Publication date: February 2, 2012Inventor: Harry A. DUGGER, III
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Publication number: 20110311594Abstract: The present invention provides a controlled release pharmaceutical composition which exhibits reduced food effect.Type: ApplicationFiled: June 21, 2011Publication date: December 22, 2011Inventors: Shou-Chiung Chen, Shao-Ming Lee, Chaur-Ming Jan
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Publication number: 20110288178Abstract: Provided herein are methods, for reducing, preventing, mitigating and treating damage caused by radiation. The methods comprise delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation or to mitigate apoptosis. The compounds comprise glyburide or other sulfonylurea hypoglycemic compounds or potassium channel inhibitors.Type: ApplicationFiled: October 21, 2009Publication date: November 24, 2011Inventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
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Publication number: 20110263478Abstract: Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN). In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SUR1 and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.Type: ApplicationFiled: September 16, 2009Publication date: October 27, 2011Inventor: J. Marc Simard
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Publication number: 20110250271Abstract: The present invention provides to a method of administration of two or more therapeutically active agents comprising orally administering to a patient a spaced drug delivery system, wherein the time of release of the two or more therapeutically active agents is designed to provide desired control on the disease condition. The present invention also provides a method of administration of two or more therapeutically active agents comprising orally administering to a patient a spaced drug delivery system at a specified time prior to food intake by the patient. The present invention further provides a spaced drug delivery system that releases two or more antidiabetic agents at different times after oral administration, for the treatment of diabetes mellitus or conditions associated with diabetes mellitus.Type: ApplicationFiled: June 17, 2011Publication date: October 13, 2011Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LIMITEDInventors: Dilip Shantilal Shanghvi, Kirti Wardhaman Ganorkar, Yashoraj Rupsinh Zala, Nitin Bhalachandra Dharmadhikari, Satish C. Khanna
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Publication number: 20110092542Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.Type: ApplicationFiled: December 9, 2010Publication date: April 21, 2011Inventor: J. Marc Simard
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Publication number: 20110046187Abstract: Methods are provided for assessing a patient being treated with a peroxisome-proliferator-activator-receptor-? (PPAR-?) agonist or a thiazolidinedione (TZD), or having a condition treatable with a peroxisome-proliferator-activator-receptor-?agonist or a thiazolidinedione. Methods include measuring a galectin-3 concentration or a change in a galectin-3 concentration in a body fluid of a patient being treated with a peroxisome-proliferator-activator-receptor-? agonist or a thiazolidinedione. A comparison to galectin-3 levels or changes in comparable patients provides information indicative of congestive heart risk.Type: ApplicationFiled: September 16, 2008Publication date: February 24, 2011Applicant: BG MEDICINE, INC.Inventors: Robert Nicholas McBurney, Shunguang Wang, Tom Plasterer, Pieter Muntendam
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Publication number: 20110034560Abstract: The invention provides liquid formulations of compounds that act at sulfonylurea receptors that are suitable for intra-venous and intra-arterial infusion. Compounds active at a sulfonylurea receptor include glibenclamide, tolbutamide, repaglinide, nateglinide, meglitinide, midaglizole, LY397364, LY389382, glyclazide, and glimepiride. Liquid formulations may be concentrated solutions suitable for storage; may be diluted (e.g., dilution of 1:1 or 1:1.2) suitable for bolus injections, and may be further diluted (e.g., dilution of 1:10 or 1:20 or more) for intravenous and intra-arterial infusion over an extended period of time. For example, a liquid formulation may include at least about 0.05 mg/ml glibenclamide in a water-based solution including 40% polyethylene glycol 300, 10% Ethanol, 50% water, at about pH 9. The solution may include a buffer, and is suitable for storage in refrigerator or at room temperature. This solution may be diluted 1:1, or more (e.g., 1:20) without precipitation of the glibenclamide.Type: ApplicationFiled: January 29, 2009Publication date: February 10, 2011Inventors: Sven Jacobson, Gillian Clarke, Rajinder Matharu
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Patent number: 7872048Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.Type: GrantFiled: September 16, 2005Date of Patent: January 18, 2011Assignee: University of Maryland, BaltimoreInventor: J. Marc Simard
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Publication number: 20100311639Abstract: Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury. In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SUR1 and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.Type: ApplicationFiled: June 20, 2008Publication date: December 9, 2010Inventor: J. Marc Simard
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Publication number: 20100273703Abstract: Methods of treating diseases such as diabetes are disclosed. Methods of modulating elevated fructosamine levels, elevated HbA1c levels, impaired glucose tolerance, and impaired fasting glucose are also disclosed. In some embodiments, methods include co-administration of a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide, a sulfonylurea and insulin, or pharmaceutically acceptable salts thereof. Drug products including a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide, a sulfonylurea and insulin, or pharmaceutically acceptable salts thereof, in combination are also disclosed.Type: ApplicationFiled: June 16, 2010Publication date: October 28, 2010Applicant: Daiichi Sankyo, Inc.Inventor: Michael R. Jones
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Publication number: 20100273886Abstract: The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pH values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) freeze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.Type: ApplicationFiled: December 3, 2008Publication date: October 28, 2010Inventor: Sven Jacobson
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Publication number: 20100209541Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: January 22, 2010Publication date: August 19, 2010Inventor: Harry A. DUGGER, III
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Publication number: 20100143347Abstract: The present invention concerns protection of an organ or tissue following an ischemic episode In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth In specific embodiments, the organ is subjected to an inhibitor of an NCCa-ATP channel that is regulated by SUR1 Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for exampleType: ApplicationFiled: January 11, 2008Publication date: June 10, 2010Inventor: J. Marc Simard
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Patent number: 7674827Abstract: Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds for combating animal pests The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.Type: GrantFiled: November 15, 2006Date of Patent: March 9, 2010Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20100056444Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.Type: ApplicationFiled: October 11, 2007Publication date: March 4, 2010Inventors: Sven Martin Jacobson, Robert Ang
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Publication number: 20080139659Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: ApplicationFiled: September 19, 2007Publication date: June 12, 2008Applicant: University of MarylandInventors: J. Marc Simard, Mingkui Chen
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Patent number: 7285574Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: GrantFiled: April 5, 2005Date of Patent: October 23, 2007Assignee: University of Maryland, BaltimoreInventors: J. Marc Simard, Mingkui Chen