C=x Bonded Directly Or Indirectly By An Acyclic Carbon Or Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring (e.g., Tryptophan, Etc.) (x Is Chalcogen) Patents (Class 514/419)
  • Patent number: 10265300
    Abstract: Methods of treating a seizure disorder with a maxi-K channel opener or a pharmaceutically acceptable salt thereof are provided. In embodiments, suitable maxi-K channel openers are be fluoro-oxindole or chloro-oxindole compounds. In some embodiments, the maxi-K channel opener may be (3S)-(+)-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6 -(trifluoromethyl)-2H-indole-2-one or pharmaceutically acceptable salts thereof. The methods provide therapeutic compositions that may be used to improve one or more symptoms of a seizure disorder.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: April 23, 2019
    Assignee: OVID THERAPEUTICS INC.
    Inventor: Matthew During
  • Patent number: 10206903
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: February 19, 2019
    Assignee: BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIVERSITY OF NEVADA, RENO
    Inventors: Dean Burkin, Ryan Wuebbles
  • Patent number: 10029984
    Abstract: The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: July 24, 2018
    Assignees: Janssen Pharmaceuticals, Inc., Katholieke Universiteit Leuven
    Inventors: Bart Rudolf Romanie Kesteleyn, Jean-François Bonfanti, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Dorothée Alice Marie-Eve Bardiot, Arnaud Didier M Marchand
  • Patent number: 9980943
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: May 29, 2018
    Assignee: BOARD OF REGENTS OF THE NEVADA SYSTEMS OF HIGHER EDUCATION ON BEHALF OF THE NEVADA, RENO
    Inventors: Dean Burkin, Ryan Wuebbles
  • Patent number: 9925170
    Abstract: Provided herein are pharmacologically active compositions suitable for topical application or injection directly for fat treatment without the need for surgical intervention.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: March 27, 2018
    Assignee: Kythera Biopharmaceuticals, Inc.
    Inventors: Serge Lichtsteiner, Alain Vasserot, Neil Poloso
  • Patent number: 9910047
    Abstract: Biomarkers relating to insulin resistance and insulin resistance-related disorders are provided, as well as methods for using such biomarkers as biomarkers for insulin resistance, dysglycemia, type-2 diabetes, and cardiovascular disease. In addition, methods for monitoring the respective disorders or conditions of a subject are also provided. Also provided are suites of small molecule entities as biomarkers for insulin resistance, dysglycemia, type-2 diabetes, and cardiovascular disease.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: March 6, 2018
    Assignee: Metabolon, Inc.
    Inventors: Walter Gall, Jeffery Edmond Cobb, Kirk Lane Pappan
  • Patent number: 9901559
    Abstract: Composition comprising leucine, isoleucine, valine threonine and lysine for treating angiogenic disorders in elderly subjects.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: February 27, 2018
    Assignee: Determinants of Metabolism Research Laboratory S.r.l.
    Inventors: Franco Conti, Isabella Arborio Mella, Edoardo Carlo Marla Conti, Giovanni Federico Maria Conti, Francesco Saverio Dioguardi
  • Patent number: 9861612
    Abstract: The invention relates to compounds of formula (I), wherein R1 and R2 are as defined herein. The compounds of the invention are inhibitors of ROR?t and are useful in the treatment of diseases and conditions mediated by ROR?t.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: January 9, 2018
    Assignee: ORCA PHARMACEUTICALS LIMITED
    Inventors: Clive McCarthy, Naomi Went, Roine Inge Olsson
  • Patent number: 9744122
    Abstract: Described herein are topical pain compositions comprising between 15 and 90% mannitol, for use in the treatment of pain, itch and other cutaneous nerve conditions. The resulting compositions may be in the form of creams, gels, lotions, ointments, foams, suppositories, and sprays.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: August 29, 2017
    Inventors: Helene Bertrand, Marylene Kyriazis
  • Patent number: 9700501
    Abstract: The invention relates to a compound of formula I wherein R1, R2 and R3 are identical or different and each is H or alkyl of 1-6 carbon atoms, R4 is H or methyl, R5 is phenyl or chlorophenyl, and/or physiologically acceptable salts thereof and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said compound.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: July 11, 2017
    Assignee: Merck Patent GmbH
    Inventors: Soheila Anzali, Francis Contard, Jean Jacques Zeiller
  • Patent number: 9668691
    Abstract: The invention relates to a method of measuring the elasticity and firmness of skin. The invention also relates to methods of measuring improvements in a person's skin health by measuring firmness and elasticity before, during and after a cosmetic treatment. The invention further relates to methods of measuring the improvement in a person's skin firmness and elasticity that a cosmetic agent may cause when applied on the skin.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: June 6, 2017
    Assignee: LVMH RECHERCHE
    Inventors: Rodolphe Korichi, Marie Baret, Delphine Pelle De Queral, Germaine Gazzano
  • Patent number: 9556168
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: January 31, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth J. Barr, Corey E. Bienstock, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Neville J. Anthony, Blair T. Lapointe, Nunzio Sciammetta
  • Patent number: 9522139
    Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphatase (EC:3.1.3.11) enzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: December 20, 2016
    Assignee: University of Houston System
    Inventor: Zhang Weihua
  • Patent number: 9522134
    Abstract: The present invention relates to compounds of formula (I): wherein R1 and R2 are as defined herein. In certain embodiments, the compounds of the present invention are inhibitors of ROR?t and are useful in the treatment of diseases and conditions mediated by ROR?t.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: December 20, 2016
    Assignee: ORCA PHARMACEUTICALS LIMITED
    Inventors: Clive McCarthy, Naomi Went, Roine Inge Olsson
  • Patent number: 9486441
    Abstract: The present invention provides compounds and/or compositions that modulate PP2A methylation and/or activity and methods for preparing the same, which are useful for modulating the demethylation of PP2A, modulating the methylation of PP2A and/or modulating the activity of PP2A.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: November 8, 2016
    Assignee: SIGNUM BIOSCIENCES, INC.
    Inventors: Scott Vafai, Michael Voronkov, Maxwell Stock, Jeffry B. Stock, Seung-Yub Lee, Zhu Li, Haoming Gu
  • Patent number: 9487490
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: November 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth J. Barr, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Dongshan Zhang, Brian M. Andresen, Neville J. Anthony, Blair T. Lapointe, Nunzio Sciammetta
  • Patent number: 9394285
    Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: July 19, 2016
    Assignee: Pfizer Inc.
    Inventors: Samit Kumar Bhattacharya, Kimberly O'Keefe Cameron, Matthew Scott Dowling, David Christopher Ebner, David James Edmonds, Dilinie Prasadhini Fernando, Kevin James Filipski, Daniel Wei-Shung Kung, Esther Cheng Yin Lee, Aaron Christopher Smith, Meihua Mike Tu
  • Patent number: 9376382
    Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: June 28, 2016
    Assignee: Sichuan Guokang Pharmaceutical Co., Ltd.
    Inventors: Luyun Zhang, Fang Yang, Wanqi Shi, Ping Zhang, Ying Li, Shufan Yin
  • Patent number: 9303062
    Abstract: A solid oxidized glutathione salt is produced by heating an oxidized glutathione at 30° C. or higher while the oxidized glutathione is brought into contact with an aqueous medium in the presence of a substance for providing a cation, to produce the salt of the oxidized glutathione and the cation as a solid, wherein the aqueous medium is composed of water and/or a water-soluble medium, and the cation is at least one selected from an ammonium cation, a calcium cation and a magnesium cation.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: April 5, 2016
    Assignee: KANEKA CORPORATION
    Inventors: Taku Mouri, Naoaki Taoka, Tadashi Moroshima, Koichi Kinoshita
  • Patent number: 9301937
    Abstract: The present invention aims to provide an amino acid-containing granule preparation improved in the ease of taking medication than conventional products, which disintegrates rapidly. The amino acid-containing granule preparation of the present invention containing granules having a maximum particle size of substantially not more than 1000 ?m and a bulk density of not less than 0.57 g/mL markedly improves ease of taking medication without impairing disintegration property, as compared to conventional amino acid-containing granule preparations.
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: April 5, 2016
    Assignee: AJINOMOTO CO., INC.
    Inventors: Mitsuyasu Ida, Nobutaka Ninomiya
  • Patent number: 9149450
    Abstract: The invention provides for ischemia/reperfusion protection compositions having one or more ketone bodies and melatonin. The invention also provides for methods of using such compositions to reduce or prevent ischemia/reperfusion injury due to blood loss, stroke or cardiopulmonary arrest or surgery.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: October 6, 2015
    Assignee: Regents of the University of Minnesota
    Inventors: Matthew T. Andrews, Lester R. Drewes, Greg Beilman
  • Publication number: 20150147309
    Abstract: The present invention relates to an allosteric non-inhibitory chaperone of the lysosomal acid alpha-glucosidase (GAA) for use in the treatment of a pathological condition characterized by a deficiency of the lysosomal acid alpha-glucosidase (GAA), to pharmaceutical composition thereof, to a method for increasing the activity of GAA in a subject and to a method for identifying an allosteric non-inhibitory chaperone for GAA.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 28, 2015
    Inventors: Giancarlo Parenti, Caterina Porto, Marco Moracci, Maria Carmina Ferrara, Beatrice Cobucci-Ponzano, Generoso Andria
  • Publication number: 20150148395
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150148360
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.
    Type: Application
    Filed: July 19, 2013
    Publication date: May 28, 2015
    Inventors: Jung-Hsin Lin, Jim-Min Fang, Ting-Rong Chen, Jhih-Bin Chen, Ching-Chow Chen, Tzu-Tang Wei
  • Publication number: 20150147320
    Abstract: An ophthalmic drug delivery system that contains phospholipid and cholesterol for prolonging drug lifetime in the eyes.
    Type: Application
    Filed: December 16, 2014
    Publication date: May 28, 2015
    Inventors: SHEUE-FANG SHIH, PO-CHUN CHANG, YUN-LONG TSENG, LUKE S.S. GUO, KEELUNG HONG
  • Publication number: 20150140080
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140079
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140078
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140077
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140075
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140081
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150133499
    Abstract: This invention relates to novel pharmaceutical compositions comprising a therapeutically effective amount of a slow-release formulation of 5-hydroxytryptophan (5-HTP) and a serotonin-enhancing compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating CNS disorders, including depressive disorders, bipolar disorders, anxiety disorders, obesity and pain.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 14, 2015
    Inventors: Jacob Pade Ramsoe Jacobsen, Brian Frostrup
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150133370
    Abstract: The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 14, 2015
    Inventor: Valter Longo
  • Publication number: 20150125548
    Abstract: The present invention is directed to nutritional and nutraceutical compositions which comprise novel mixtures of two or more indole-based dietary supplements such as L-tryptophan and melatonin, together with selected minerals and vitamins that stimulate tryptophan metabolism in the direction of serotonin and melatonin, and to their use in a preferred embodiment of the invention in a readily ingested beverage form, optionally combined with a range of other natural ingredients designed to improve the health and state of mind of human subjects. Alternative dosage forms, such as tablets for oral dosing, and dosage forms for buccal and sublingual administration, including thin films, are also incorporated in the present invention. Health improvements include the treatment of disorders of circadian rhythm, such as shift work disorder and jet lag, the induction of relaxation and a restful frame of mind, as well as providing restorative sleep function.
    Type: Application
    Filed: November 13, 2012
    Publication date: May 7, 2015
    Applicant: Requis Pharmaceuticals Inc.
    Inventors: Lars Jacob Stray Knutsen, Judi Lois Knutsen
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Publication number: 20150126462
    Abstract: The present invention relates to a new pharmaceutical composition containing nicotinic acid, nicotinamide, tryptophanor related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.
    Type: Application
    Filed: June 14, 2013
    Publication date: May 7, 2015
    Applicant: CONARIS RESEARCH INSTITUTE AG
    Inventors: Georg Waetzig, Dirk Seegert
  • Patent number: 9023871
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: May 5, 2015
    Assignee: The University of Toledo
    Inventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
  • Publication number: 20150119414
    Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.
    Type: Application
    Filed: January 2, 2015
    Publication date: April 30, 2015
    Applicant: PIVOTAL THERAPEUTICS INC.
    Inventors: George JACKOWSKI, Rachelle MACSWEENEY, Nisar Ahmad SHAIKH, Jason YANTHA, Valerie B. SCHINI-KERTH
  • Publication number: 20150111942
    Abstract: Indole-3-propionic acid as a marker and for treatment for Huntington Disease.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 23, 2015
    Inventor: Wayne R. Matson
  • Publication number: 20150105439
    Abstract: A pharmaceutical composition, a method of producing same, and a method of providing cancer therapy therein comprising a pharmaceutically acceptable excipient or carrier and a compound Formula 3 as follows: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are optionally substituted and are hydrogen, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, C1-10 alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, nitroalkyl, cyanoalkyl, acetamidoalkyl, acyloxyalkyl, hydroxyl, alkoxy, acetoxy, amino, alkylamino, acetamido.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 16, 2015
    Inventors: Alexander V. Akensov, Snezna Rogelj, Liliya Frolova, Alexander Kornienko, Gabriel Avilucea
  • Publication number: 20150099691
    Abstract: A dipeptide derivative as formyl peptide receptor 1 (FPR1) antagonist is provided. The dipeptide derivative is represented by formula (I), wherein: the chiral centers in formula (I) are S and R configurations respectively; each of RK and RT is selected from a group consisting of a hydrogen, a hydroxyl group, a C1-C4 alkyl-substituted hydroxyl group, a C1-C4 alkoxyl group, a carboxylic acid group, a C1-C4 alkyl nitrile-substituted, C1-C4 alkyl-substituted or C1-C4 alkoxyl-substituted amido group, a C1-C4 alkyl-substituted ester group and a benzoyl group having a C1-C4 alkyl-substituted benzene ring; and each of RM and RS is selected from a group consisting of a hydrogen, a hydroxyl group, a phenyl group, a pyridinyl group, a carboxylic acid group, a C1-C4 alkoxyl substituted ester group, and a benzoyl group having a hydroxyl-substituted, a halogen-substituted, a C1-C4 alkoxyl-substituted or a C1-C4 alkyl-substituted benzene ring.
    Type: Application
    Filed: April 9, 2014
    Publication date: April 9, 2015
    Applicant: CHANG GUNG UNIVERSITY
    Inventors: Tsong-Long Hwang, Pei-Wen Hsieh, Yin-Ting Huang, Chih-Hao Hung
  • Publication number: 20150099790
    Abstract: Disclosed herein are methods and compositions for the diagnosis and treatment of conditions associated with aberrant pyruvate metabolism, and symptoms thereof, in a subject. Disclosed herein are methods of detecting an aberrant pyruvate metabolism-associated condition, and symptoms thereof, in a subject, by the expression level of MPC1 or MPC2. Disclosed herein are methods of detecting an aberrant pyruvate metabolism-associated condition, and symptoms thereof, in a subject, by the activity level of MPC1 or MPC2. Disclosed herein are methods of determining responsiveness to a treatment for an aberrant pyruvate metabolism associated condition, and symptoms thereof, in a subject.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Inventors: Jared Rutter, Carl Thummel, Daniel K. Bricker, Thomas Orsak
  • Publication number: 20150094330
    Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20150087605
    Abstract: Disclosed are compositions and methods for treating anthrax, inhibiting anthrax toxins and inhibiting anthrax toxin-induced cytotoxicity. Carboxylic acid-containing small molecules can be used in the methods and compositions disclosed herein, for example, sulindac and derivatives thereof may be used. Methods of screening for carboxylic acid-containing small molecules that can be used to treat anthrax are disclosed. Targeting the anthrax toxin reduces the risks of anthrax spores.
    Type: Application
    Filed: September 19, 2014
    Publication date: March 26, 2015
    Inventors: J. Manuel Perez Figueroa, Oscar Santiesteban, Charalambos Kaittanis
  • Publication number: 20150087617
    Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 26, 2015
    Inventors: Abraham Nudelman, Marta Weinstock-Rosin
  • Patent number: 8987474
    Abstract: Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erk 1/2 activation pathway. Additionally, a number of analogs of NSC-117199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and are found to be potent and/or selective inhibitors of Shp1 and/or Shp2 protein tyrosine phosphatases.
    Type: Grant
    Filed: April 9, 2007
    Date of Patent: March 24, 2015
    Assignees: University of South Florida, H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Jie Wu, Nicholas J. Lawrence, Said M. Sebti, Harshani R. Lawrence
  • Patent number: 8987321
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: March 24, 2015
    Assignee: University of Virginia Patent Foundation
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Publication number: 20150080328
    Abstract: The present invention relates to compounds and compositions and their application as pharmaceuticals for treating, preventing, or reversing injury to skeletal or cardiac muscles, for treating or preventing diseases relating to the structure and function of skeletal or cardiac muscle, and for inducing regeneration or restructuring of skeletal or cardiac muscle as a means of treating diseases relating to abnormalities in skeletal or cardiac muscle structure and function in a human or animal subject.
    Type: Application
    Filed: March 22, 2013
    Publication date: March 19, 2015
    Inventors: Francisco Villarreal, George F. Schreiner, Guillermo Ceballos
  • Publication number: 20150072963
    Abstract: The invention relates to compositions and methods for regulating hair growth. Specifically, the invention relates to regulating hair growth by regulating the activity one of the prostaglandin D2 (PGD2) receptors, DP-2 (GPR44). Compositions and methods for regulating hair growth include inhibiting hair growth by administering a DP-2 agonist, or stimulating hair growth by administering a DP-2 antagonist.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 12, 2015
    Inventors: George Cotsarelis, Garret Fitzgerald, Luis Garza