Sulfur Is Part Of A Substituent Which Contains Additional Nitrogen Patents (Class 514/593)
  • Patent number: 11951085
    Abstract: 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: Grant
    Filed: September 29, 2021
    Date of Patent: April 9, 2024
    Assignee: REMEDY PHARMACEUTICALS, INC.
    Inventor: Sven Martin Jacobson
  • Patent number: 11623922
    Abstract: 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: Grant
    Filed: October 3, 2018
    Date of Patent: April 11, 2023
    Assignee: INFLAZOME LIMITED
    Inventors: David Miller, Stephen Thom, Stephen St-Gallay, Jonathan Shannon, Paul Leeson
  • Patent number: 11236045
    Abstract: 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: Grant
    Filed: June 8, 2018
    Date of Patent: February 1, 2022
    Assignee: Cadila Healthcare Limited
    Inventors: Rajiv Sharma, Pravin Iyer, Sameer Agarwal
  • Patent number: 11166966
    Abstract: 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: Grant
    Filed: November 3, 2017
    Date of Patent: November 9, 2021
    Inventor: Roxane Handal-Orefice
  • Patent number: 9962371
    Abstract: 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: Grant
    Filed: July 15, 2016
    Date of Patent: May 8, 2018
    Assignee: RTU PHARMACEUTICALS, LLC
    Inventors: Joseph V. Pergolizzi, Alexander Mironov, Chad James Pickens, Douglas Giles Johnson
  • Patent number: 9675289
    Abstract: 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: Grant
    Filed: June 6, 2008
    Date of Patent: June 13, 2017
    Assignee: Roche Diabetes Care, Inc.
    Inventor: Kelly Heaton
  • Patent number: 9254259
    Abstract: 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: Grant
    Filed: October 28, 2014
    Date of Patent: February 9, 2016
    Assignee: Remedy Pharmaceuticals, Inc.
    Inventor: Sven Martin Jacobson
  • Publication number: 20150141516
    Abstract: 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: Application
    Filed: October 7, 2014
    Publication date: May 21, 2015
    Inventor: Sven Jacobson
  • Publication number: 20150140092
    Abstract: 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: Application
    Filed: November 17, 2014
    Publication date: May 21, 2015
    Inventor: Guru V. BETAGERI
  • Patent number: 8980952
    Abstract: 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: Grant
    Filed: February 22, 2006
    Date of Patent: March 17, 2015
    Assignees: University of Maryland, Baltimore, The United States of America as represented by the Dept. of Veterans Affairs
    Inventors: J. Marc Simard, Mingkui Chen
  • Publication number: 20150051289
    Abstract: 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: Application
    Filed: February 28, 2013
    Publication date: February 19, 2015
    Inventor: Marianne Berdugo Polak
  • Patent number: 8946293
    Abstract: 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: Grant
    Filed: July 18, 2011
    Date of Patent: February 3, 2015
    Assignee: Remedy Pharmaceuticals, Inc.
    Inventor: Sven Martin Jacobson
  • Publication number: 20140378548
    Abstract: 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: Application
    Filed: December 21, 2012
    Publication date: December 25, 2014
    Inventors: Manuel Friese, Benjamin Schattling, Karin Steinbach, Marc Freichel, Veit Flockerzi, Rudi Vennekens, Doron Merkler
  • Patent number: 8883852
    Abstract: 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: Grant
    Filed: October 21, 2009
    Date of Patent: November 11, 2014
    Assignee: University of Pittburgh—Of the Commonwealth System of Higher Education
    Inventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
  • Publication number: 20140323423
    Abstract: 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: Application
    Filed: May 2, 2014
    Publication date: October 30, 2014
    Applicant: Chrono Therapeutics, Inc.
    Inventors: Guy DiPierro, Steven A. Giannos
  • Publication number: 20140314746
    Abstract: 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: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Applicant: Philadelphia Health and Education Corporation, d/b/a Drexel University College of Medicine
    Inventors: CAROL M. ARTLETT, PETER D. KATSIKIS
  • Publication number: 20140235564
    Abstract: 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: Application
    Filed: February 20, 2014
    Publication date: August 21, 2014
    Inventors: J. Marc Simard, Mingkui Chen
  • Publication number: 20140199320
    Abstract: 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: Application
    Filed: July 11, 2012
    Publication date: July 17, 2014
    Applicant: UNIVERSITAT ZURICH
    Inventors: Dragana Jankovic, Magdalena Kistowiska, Emmanuel Contassot, Lars E. French, Samuel Gehrke
  • Publication number: 20140171467
    Abstract: 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: Application
    Filed: September 27, 2013
    Publication date: June 19, 2014
    Inventor: J. Marc Simard
  • Publication number: 20140080811
    Abstract: 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: Application
    Filed: February 27, 2013
    Publication date: March 20, 2014
    Applicant: Remedy Pharmaceuticals, Inc.
    Inventor: Remedy Pharmaceuticals, Inc.
  • Publication number: 20140051761
    Abstract: 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: Application
    Filed: May 2, 2012
    Publication date: February 20, 2014
    Applicant: ASSISTANCE PUBLIQUE - HOPITAUX DE PARIS
    Inventors: Michel Polak, Marianne Berdugo Polak
  • Patent number: 8569377
    Abstract: 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: Grant
    Filed: December 9, 2010
    Date of Patent: October 29, 2013
    Assignees: The United States of America as Represented by the Department of Veteran Affairs, University of Maryland, Baltimore
    Inventor: J. Marc Simard
  • Publication number: 20130273181
    Abstract: 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: Application
    Filed: March 7, 2013
    Publication date: October 17, 2013
    Inventors: MARTIN GARTZ HANSON, LEE NISWANDER
  • Patent number: 8557867
    Abstract: 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: Grant
    Filed: June 20, 2008
    Date of Patent: October 15, 2013
    Assignees: The United States of America as Represented by the Department of Veterans Affairs, University of Maryland, Baltimore
    Inventor: J. Marc Simard
  • Publication number: 20130245069
    Abstract: 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: Application
    Filed: September 11, 2012
    Publication date: September 19, 2013
    Applicant: Remedy Pharmaceuticals, Inc.
    Inventor: Sven Jacobson
  • Publication number: 20130203853
    Abstract: 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: Application
    Filed: July 18, 2011
    Publication date: August 8, 2013
    Applicant: Remedy Pharmaceuticals, Inc.
    Inventor: Sven Martin Jacobson
  • Publication number: 20130184293
    Abstract: 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: Application
    Filed: December 12, 2012
    Publication date: July 18, 2013
    Applicants: UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE HOPITAUX DE PARIS
    Inventors: ASSISTANCE PUBLIQUE HOPITAUX DE PARIS, UNIVERSITE PARIS DESCARTES
  • Patent number: 8318810
    Abstract: 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: Grant
    Filed: September 19, 2007
    Date of Patent: November 27, 2012
    Assignees: University of Maryland, Baltimore, The United States of America as represented by the Department of Veterans Affairs
    Inventors: J. Marc Simard, Mingkui Chen
  • Publication number: 20120283215
    Abstract: 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: Application
    Filed: September 14, 2010
    Publication date: November 8, 2012
    Applicants: The Regents of the University of California, a California Corporation, University of Texas at El Paso, Health and Human Services
    Inventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather Balsiger, Robert Fletterick
  • Publication number: 20120237449
    Abstract: 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: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Inventors: J. Marc Simard, Mingkui Chen
  • Publication number: 20120225947
    Abstract: 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: Application
    Filed: September 23, 2010
    Publication date: September 6, 2012
    Applicant: ASSISTANCE PUBLIQUE - HOPITAUX DE PARIS
    Inventors: Michel Polak, Marianne Berdugo Polak, Francine Behar-Cohen, Patricia Crisanti Lassiaz
  • Publication number: 20120190618
    Abstract: 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: Application
    Filed: July 7, 2010
    Publication date: July 26, 2012
    Inventors: Philippe Perovitch, Marc Maury, Jean-Pierre Dumonteix
  • Publication number: 20120027879
    Abstract: 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: Application
    Filed: August 3, 2011
    Publication date: February 2, 2012
    Inventor: Harry A. DUGGER, III
  • Publication number: 20110311594
    Abstract: The present invention provides a controlled release pharmaceutical composition which exhibits reduced food effect.
    Type: Application
    Filed: June 21, 2011
    Publication date: December 22, 2011
    Inventors: Shou-Chiung Chen, Shao-Ming Lee, Chaur-Ming Jan
  • Publication number: 20110288178
    Abstract: 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: Application
    Filed: October 21, 2009
    Publication date: November 24, 2011
    Inventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
  • Publication number: 20110263478
    Abstract: 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: Application
    Filed: September 16, 2009
    Publication date: October 27, 2011
    Inventor: J. Marc Simard
  • Publication number: 20110250271
    Abstract: 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: Application
    Filed: June 17, 2011
    Publication date: October 13, 2011
    Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LIMITED
    Inventors: Dilip Shantilal Shanghvi, Kirti Wardhaman Ganorkar, Yashoraj Rupsinh Zala, Nitin Bhalachandra Dharmadhikari, Satish C. Khanna
  • Publication number: 20110092542
    Abstract: 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: Application
    Filed: December 9, 2010
    Publication date: April 21, 2011
    Inventor: J. Marc Simard
  • Publication number: 20110046187
    Abstract: 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: Application
    Filed: September 16, 2008
    Publication date: February 24, 2011
    Applicant: BG MEDICINE, INC.
    Inventors: Robert Nicholas McBurney, Shunguang Wang, Tom Plasterer, Pieter Muntendam
  • Publication number: 20110034560
    Abstract: 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: Application
    Filed: January 29, 2009
    Publication date: February 10, 2011
    Inventors: Sven Jacobson, Gillian Clarke, Rajinder Matharu
  • Patent number: 7872048
    Abstract: 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: Grant
    Filed: September 16, 2005
    Date of Patent: January 18, 2011
    Assignee: University of Maryland, Baltimore
    Inventor: J. Marc Simard
  • Publication number: 20100311639
    Abstract: 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: Application
    Filed: June 20, 2008
    Publication date: December 9, 2010
    Inventor: J. Marc Simard
  • Publication number: 20100273886
    Abstract: 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: Application
    Filed: December 3, 2008
    Publication date: October 28, 2010
    Inventor: Sven Jacobson
  • Publication number: 20100273703
    Abstract: 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: Application
    Filed: June 16, 2010
    Publication date: October 28, 2010
    Applicant: Daiichi Sankyo, Inc.
    Inventor: Michael R. Jones
  • Publication number: 20100209541
    Abstract: 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: Application
    Filed: January 22, 2010
    Publication date: August 19, 2010
    Inventor: Harry A. DUGGER, III
  • Publication number: 20100143347
    Abstract: 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 example
    Type: Application
    Filed: January 11, 2008
    Publication date: June 10, 2010
    Inventor: J. Marc Simard
  • Patent number: 7674827
    Abstract: 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: Grant
    Filed: November 15, 2006
    Date of Patent: March 9, 2010
    Assignee: BASF SE
    Inventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
  • Publication number: 20100056444
    Abstract: 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: Application
    Filed: October 11, 2007
    Publication date: March 4, 2010
    Inventors: Sven Martin Jacobson, Robert Ang
  • Publication number: 20080139659
    Abstract: 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: Application
    Filed: September 19, 2007
    Publication date: June 12, 2008
    Applicant: University of Maryland
    Inventors: J. Marc Simard, Mingkui Chen
  • Patent number: 7285574
    Abstract: 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: Grant
    Filed: April 5, 2005
    Date of Patent: October 23, 2007
    Assignee: University of Maryland, Baltimore
    Inventors: J. Marc Simard, Mingkui Chen