The Bicyclo Ring System Consists Of The Five-membered Hetero Ring And A Benzene Ring (e.g., Indole, Etc.) Patents (Class 514/415)
The ring nitrogen is bonded directly to nonshared ring carbons of the five-membered hetero ring (e.g., isoindole, etc.) (Class 514/416)
Chalcogen bonded directly to ring carbon of the five-membered hetero ring (Class 514/418)
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) (Class 514/419)
  • 4-hydroxythiobenzamide derivatives of drugs
    Patent number: 8314140
    Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: November 20, 2012
    Assignee: Antibe Therapeutics Inc.
    Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
  • Treatment of CRTH2-mediated diseases and conditions
    Patent number: 8314257
    Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: November 20, 2012
    Assignee: Oxagen Limited
    Inventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
  • METHODS FOR TREATMENT WITH BUCINDOLOL BASED ON GENETIC TARGETING
    Publication number: 20120289573
    Abstract: The present invention concerns the use of methods for evaluating bucindolol treatment for a patient, particularly one with heart failure. It concerns methods for determining whether to administer or prescribe bucindolol to a patient based on whether the patient is homozygous for the Arg 389 polymorphism in the ?1-adrenergic receptor (AR).
    Type: Application
    Filed: December 1, 2011
    Publication date: November 15, 2012
    Inventors: Stephen B. Liggett, Michael Bristow
  • USE OF JASMONE FOR MODULATING MELATONIN PRODUCTION AND CALCIFICATION OF THE PINEAL GLAND
    Publication number: 20120288485
    Abstract: A formulation, composition or combination of substances comprising jasmonate for modulating melatonin production and/or calcification of a pineal gland and/or modulation and/or treatment of age-related neurodegeneration in a subject, particularly in a mammalian subject and more particularly in a human subject and use of jasmonate for modulating melatonin production and/or calcification of a pineal gland and/or modulation and/or treatment of age-related neurodegeneration is provided.
    Type: Application
    Filed: May 9, 2012
    Publication date: November 15, 2012
    Applicant: Broady Health Sciences, LLC.
    Inventor: Brunde Broady
  • Benzene, pyridine, and pyridazine derivatives
    Patent number: 8309548
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: November 13, 2012
    Assignee: Serenex, Inc.
    Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
  • USE OF BENZO-HETEROCYCLE DERIVATIVES FOR PREVENTING AND TREATING CANCER OR FOR INHIBITING CANCER METASTASIS
    Publication number: 20120283300
    Abstract: This application relates to a novel benzo-heterocycle derivative and more particularly, it relates a composition for preventing and treating cancer or for inhibiting metastasis comprising benzo-heterocycle derivative or pharmaceutically acceptable salts thereof as an active ingredient. The present inventors confirmed that KRS has an effect on cancer metastasis by facilitating cancer (or tumor) cell migration through interaction with 67LR, and also found that a substance inhibiting the interaction between KRS and 67LR can prevent and treat cancer by inhibiting cancer cell metastasis. Accordingly, the composition of the present invention can inhibit cancer metastasis, and thus provide a novel means for prevention and treatment of cancer.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 8, 2012
    Applicant: SNU R&DB FOUNDATION
    Inventors: Sunghoon Kim, Jin Woo Choi, Jin Young Lee, Dae Gyu Kim, Gyoon Hee Han, Jee Sun Yang, Chul Ho Lee
  • Pharmaceutical compositions comprising fluvastatin
    Patent number: 8303987
    Abstract: Pharmaceutical compositions comprising fluvastatin, HPMC and optionally other pharmaceutical excipients which are colour-stable upon prolonged periods of storage.
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: November 6, 2012
    Assignee: Novartis AG
    Inventors: Oskar Kalb, Stephen Valazza
  • Method for the treatment of metabolic disorder containing benzazole derivatives as an active ingredient
    Patent number: 8304448
    Abstract: Disclosed is a composition for the prevention and treatment of metabolic diseases, which comprises a benzazole derivative as an active ingredient. The benzazole derivative has inhibitory activity against DGAT (diacylglycerol acyltransferase), which causes metabolic diseases such as obesity and diabetes in the process of lipid metabolism. With the ability to effectively control lipid metabolism and energy metabolism, thus, the composition is useful in the prevention and treatment of metabolic diseases, such as obesity and diabetes.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: November 6, 2012
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Hyun Sun Lee, Kyeong Lee, Jung Joon Lee, Young Kook Kim, Mun-Chual Rho, Jeong Hyung Lee, Young Soo Hong, Hye-Ran Park, Chul-Ho Lee, Yongseok Choi
  • Bicyclic derivatives of azabicyclic carboxamides, preparation thereof and therapeutic use thereof
    Patent number: 8299114
    Abstract: The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: October 30, 2012
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Catherine Gille, André Malanda
  • Compounds having NPY Y5 receptor antagonistic activity
    Patent number: 8299066
    Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: October 30, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka
  • Treatment of Conditions Through Pharmacological Modulation of the Autonomic Nervous System
    Publication number: 20120270876
    Abstract: Methods are provided for treating a subject for a condition caused by an abnormality in the subject's autonomic nervous system. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is pharmacologically modulated with at least one beta-blocker in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, where such conditions include various disease conditions. Also provided are systems and kits for use in practicing the subject methods.
    Type: Application
    Filed: April 24, 2012
    Publication date: October 25, 2012
    Inventors: Anthony Joonkyoo Yun, Patrick Yuarn-Bor Lee
  • Substituted Indolealkanoic Acids
    Publication number: 20120270912
    Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
    Type: Application
    Filed: June 27, 2012
    Publication date: October 25, 2012
    Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
  • N-substituted benzene sulfonamides
    Publication number: 20120270902
    Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).
    Type: Application
    Filed: February 13, 2012
    Publication date: October 25, 2012
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Martin Neitzel, Jennifer Marugg
  • Heterocyclic Compounds As CCR1 Receptor Antagonists
    Publication number: 20120270879
    Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Daniel Kuzmich
  • Indole derivatives having cPLAinhibiting activity and applications and production methods of the same
    Patent number: 8293781
    Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: October 23, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Toshiyuki Tomoo, Takashi Nakatsuka, Yasuhiro Hayashi, Toyoko Katayama
  • Compound, probe containing the novel compound, and fluorescence-imaging contrast agent containing the novel compound or the probe
    Patent number: 8293782
    Abstract: A compound represented by Formula (1) below, where n is 2 or 3; a is an integer of 1 to 4 and b is an integer of 3 and 5 to 10, or a is 5 and b is an integer of 1 to 10; R1 to R8 each independently represent a hydrogen atom or a sulfonate that is any one of sodium sulfonate, potassium sulfonate, ammonium sulfonate, triethylammonium sulfonate, pyridinium sulfonate, lysine sulfonate, and arginine sulfonate; and R9 to R12 each independently represent a substituted or unsubstituted C1-C3 alkyl group.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: October 23, 2012
    Assignee: Canon Kabushiki Kaisha
    Inventors: Masato Minami, Yoshinori Tomida, Atsushi Takahashi, Kouichi Kato, Fumiko Tomatsu, Sachiko Inoue
  • METHODS OF DIAGNOSING AND TREATING SMALL INTESTINAL BACTERIAL OVERGROWTH (SIBO) AND SIBO-RELATED CONDITIONS
    Publication number: 20120263790
    Abstract: Disclosed is a method of treating small intestinal bacterial overgrowth (SIBO) or a SIBO-caused condition in a human subject. SIBO-caused conditions include irritable bowel syndrome, fibromyalgia, chronic pelvic pain syndrome, chronic fatigue syndrome, depression, impaired mentation, impaired memory, halitosis, tinnitus, sugar craving, autism, attention deficit/hyperactivity disorder, drug sensitivity, an autoimmune disease, and Crohn's disease. Also disclosed are a method of screening for the abnormally likely presence of SIBO in a human subject and a method of detecting SIBO in a human subject. A method of determining the relative severity of SIBO or a SIBO-caused condition in a human subject, in whom small intestinal bacterial overgrowth (SIBO) has been detected, is also disclosed.
    Type: Application
    Filed: December 9, 2011
    Publication date: October 18, 2012
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Henry C. Lin, Mark Pimentel
  • Methods And Compositions For The Treatment Of Anxiety Disorders, Including Post Traumatic Stress Disorder (PTSD) And Related Central Nervous System (CNS) Disorders.
    Publication number: 20120264703
    Abstract: The present invention provides novel methods and formulations for treating anxiety disorders, including Post Traumatic Stress Disorder, in human subjects employing coordinate treatment using ? and ? blockers alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce symptomology in treated subjects.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 18, 2012
    Inventors: Arifulla Khan, John Frederick Reinhard, JR.
  • Tetrahydroindole derivatives as NADPH oxidase inhibitors
    Patent number: 8288432
    Abstract: The present invention is related to tetrahydroindole derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: October 16, 2012
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Laetitia Fioraso-Cartier, Bianca Mottironi
  • Diazeniumdiolate compounds, a process for their preparation and pharmaceutical compositions containing them
    Patent number: 8288433
    Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a —COOR group, R2 represents a group G or a linear or branched (C1-C6)alkyl group substituted by a group G, wherein G represents a —(CH2)n-A-(CH2)m—B—(CR4R5)p—(CH2)o—R6 group as defined in the description, R3 represents a hydrogen atom, an alkyl group or an NO2 group. Medicinal products containing the same which are useful in treating hypertension and cardiovascular pathologies.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: October 16, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Alexis Cordi, Laure Haberkorn, Tony Verbeuren, Christine Courchay, Serge Simonet
  • ArylSulfonamide Based Matrix Metalloprotease Inhibitors
    Publication number: 20120258954
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: May 29, 2012
    Publication date: October 11, 2012
    Applicant: NOVARTIS AG
    Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
  • Inhibitors of cytosolic phospholipase A
    Patent number: 8283373
    Abstract: This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLA2?). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: October 9, 2012
    Assignee: Pfizer Inc.
    Inventors: John C. McKew, Katherine L. Lee, Lihren Chen, Richard Vargas, James D. Clark, Cara Williams, Valerie Clerin, Suzana Marusic, Kevin Pong
  • Use of substituted 2-aminotetralins for preventive treatment of parkinson's disease
    Patent number: 8283376
    Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: October 9, 2012
    Assignee: UCB Pharma GmbH
    Inventors: Dieter Scheller, Frank Dressen
  • METHODS AND COMPOSITIONS FOR MODULATING RHO-MEDIATED GENE TRANSCRIPTION
    Publication number: 20120252792
    Abstract: The invention provides methods, compositions, and kits for the inhibition of members of the Rho GTPase family. Specifically, the invention provides methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signalling. The invention finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis, inflammation, inflammatory disease), Rho-mediated biological conditions, and in cell signaling research.
    Type: Application
    Filed: September 17, 2010
    Publication date: October 4, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Richard Neubig, Chris Evelyn, Jenny Ryu, Scott Larsen, Jessica Bell
  • Dissolvable Film Strip Comprising Natural Components
    Publication number: 20120252862
    Abstract: The present invention relates to film strips which comprise natural product formulations and can be absorbed from oral mucosa. The said film strip can be used with the aim of preventing and treating diseases in a short time, by being absorbed rapidly when it is applied from the oral mucosa at lower dosages than the dosage forms known.
    Type: Application
    Filed: September 14, 2010
    Publication date: October 4, 2012
    Applicant: YEDITEPE UNIVERSITES
    Inventors: Erdem Yesilada, Gulengul Duman
  • TRIPTANS FOR THE TREATMENT OF PSORIASIS
    Publication number: 20120252863
    Abstract: The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration.
    Type: Application
    Filed: October 22, 2010
    Publication date: October 4, 2012
    Inventor: Avi Dascalu
  • N-(2-(HETARYL)ARYL)ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL ARYLSULFONAMIDES
    Publication number: 20120245138
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: May 2, 2012
    Publication date: September 27, 2012
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • AMPK modulators
    Patent number: 8273744
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.
    Type: Grant
    Filed: February 4, 2009
    Date of Patent: September 25, 2012
    Assignee: Mercury Therapeutics, Inc.
    Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
  • TREATMENT OF CANCER
    Publication number: 20120238601
    Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.
    Type: Application
    Filed: December 12, 2011
    Publication date: September 20, 2012
    Applicant: BiPar Sciences, Inc.
    Inventors: Jerome MOORE, Bruce KEYT, John BURNIER, Barry SHERMAN, Max TOTROV, Valeria S. OSSOVSKAYA
  • Alkylglycoside compositions for drug administration
    Patent number: 8268791
    Abstract: The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject. The compositions include at least one alkyl glycoside and at least one therapeutic agent, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: September 18, 2012
    Assignee: Aegis Therapeutics, LLC.
    Inventor: Edward T. Maggio
  • P2X7R antagonists and their use
    Patent number: 8268861
    Abstract: The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 18, 2012
    Assignee: Affectis Pharmaceuticals AG
    Inventor: Michael C Boes
  • COMPOSITIONS AND METHODS FOR DIABETES TREATMENT
    Publication number: 20120232003
    Abstract: The present invention relates to methods and compositions for the treatment or prevention of type 2 diabetes by administering an effective amount of a melatonin receptor agonist to a human subject in need of such treatment or prevention.
    Type: Application
    Filed: March 15, 2010
    Publication date: September 13, 2012
    Inventors: Joseph S. Takahashi, Steve A. Kay
  • Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease
    Publication number: 20120232070
    Abstract: Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.
    Type: Application
    Filed: March 9, 2012
    Publication date: September 13, 2012
    Applicant: Laboratoires Fournier SA
    Inventors: Jerome Amaudrut, Benaissa Boubia, Maria Johanna Petronella Van Dongen, Fabrice Guillier, Olivia Poupardin-Olivier
  • INJECTABLE FORMULATIONS FOR INTRA-ARTICULAR OR PERI-ARTICULAR ADMINISTRATION
    Publication number: 20120232031
    Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.
    Type: Application
    Filed: October 19, 2010
    Publication date: September 13, 2012
    Applicant: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Petpiboon Peppi Prasit, Isabelle Marguerite Dearmond
  • Matrix metalloproteinase inhibitors
    Patent number: 8263602
    Abstract: The present invention relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: September 11, 2012
    Assignee: Glaxo Group Limited
    Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20120225846
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • COMPOUNDS FOR ALZHEIMER'S DISEASE
    Publication number: 20120225873
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: April 13, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • COMPOUNDS FOR DISEASES AND DISORDERS
    Publication number: 20120225845
    Abstract: The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: May 4, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Christine Klein, Andrew D. Gassman, Leena Bhoite, John Manfredi
  • Method of inhibiting apoptosis
    Patent number: 8258174
    Abstract: The invention disclosed is drawn to a method of inhibiting apoptosis comprising administration an effective amount of an indole derivative represented by formula (1) as described herein.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: September 4, 2012
    Inventors: Yoshikazu Mikami, Masanori Somei
  • Melatonin derivatives and their use as antioxidants
    Patent number: 8258173
    Abstract: The present subject matter relates generally to antioxidant compounds having the formula (I): wherein each of R1, R2, R3, and R4 are as defined below. These compounds are potentially useful as, for example, antioxidants.
    Type: Grant
    Filed: November 19, 2007
    Date of Patent: September 4, 2012
    Assignee: University of Sunderland
    Inventors: Rosaleen Joy Anderson, Paul William Groundwater, David Antony Philip Small, Yu Gong
  • METHODS AND COMPOSITIONS FOR ENHANCING POLYPEPTIDE PRODUCTION
    Publication number: 20120207707
    Abstract: Methods of increasing production, stability or activity of a target polypeptide are provided herein. The method includes increasing the level of an antioxidant in a cell comprising a polynucleotide encoding the target polypeptide. Also provided are cells and transgenic organisms produced using the methods described herein. Methods of treating a subject with a condition treatable by administration of the target polypeptide are also disclosed. Finally methods and compositions for transiently increasing antioxidants in plant cells are provided.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 16, 2012
    Inventors: Maureen C. Dolan, Argelia Lorence, Giuliana Medrano
  • Pyrone-indole derivatives and process for their preparation
    Patent number: 8242163
    Abstract: The present invention relates to a method for treating insulin resistance, neuronal loss associated with stroke, ischemia, central nervous system trauma, a central nervous system disorder, a neurodegenerative disease, the adverse consequences of the over-stimulation of excitatory amino acids, a psychiatric disease, epilepsy or other convulsive disorder, chronic pain, CMV retinitis, urinary incontinence, or for inducing anesthesia; which comprises administering to an animal or human in need thereof an effective amount of a pharmaceutical formulation comprising an effective amount of a pyrone-indole derivative of formula (I): Ar—B—Ar???(I) wherein Ar represents an indole nucleus ring system: Ar? represents an alpha-, beta- or gamma-pyrone nucleus ring system: and each of B, R1-4, and R1-2? are one of the groups as defined herein.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: August 14, 2012
    Assignee: Neurim Pharmaceuticals (1991) Ltd.
    Inventors: Moshe Laudon, Tal Peleg-Shulman
  • SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES
    Publication number: 20120202810
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 9, 2012
    Applicant: Grunenthal GmbH
    Inventors: Bert NOLTE, Wolfgang SHRÖDER, Klaus LINZ, Werner ENGLBERGER, Hans SCHICK, Heinz GRAUBAUM, Birgit ROLOFF, Sigrid OZEGOWSKI, József BÁLINT, Helmut SONNENSCHEIN
  • Diindolylmethane for the treatment of HPV infection
    Patent number: 8236848
    Abstract: New methods and compositions are disclosed that comprise the phytochemical Diindolylmethane, alone or in combination with immune potentiating steroids. These methods and compositions are utilized to treat subjects suffering from common cutaneous warts (verrucae) and Human Papilloma Virus (HPV) related conditions of the oropharynx, larynx, genitalia, and uterine cervix.
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: August 7, 2012
    Assignee: BioResponse, L.L.C.
    Inventor: Michael A. Zeligs
  • Model for glutamate racemase inhibitors and glutamate racemase antibacterial agents
    Patent number: 8236849
    Abstract: The increase in antibacterial resistance has created the demand for new antibiotics. The present invention relates to a more potent antibiotic that targets the enzyme glutamate racemase from known glutamate racemase inhibitors. Glutamate racemase catalyses the interconversion of L-glutamate to D-glutamate, making D-glutamate available, which is required for bacterial peptidoglycan biosynthesis. Knockout mutations have shown glutamate racemase to be necessary for bacterial cell survival and, before the present invention, no antibiotic on the market targeted this enzyme. The present invention relates to new, ligand based glutamate racemase inhibitors, developed using software to extract a pharmacophore model from a group of known glutamate racemase inhibitors. Forty-seven (47) known inhibitors were collected from the literature and several pharmacophore models were extracted therefrom.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: August 7, 2012
    Assignee: Ohio Northern University
    Inventors: Tarek M. Mahfouz, Kyle W. Skidmore, Amy Stockert, Corey Scherer
  • CONTROLLED-RELEASE MELATONIN COMPOSITIONS AND RELATED METHODS
    Publication number: 20120195968
    Abstract: This disclosure relates to controlled-release melatonin compositions and related methods. In one embodiment, a controlled-release medicament composition comprises melatonin dispersed in a controlled melatonin release portion comprising a polymer matrix, the polymer matrix adapted to encapsulate the melatonin in a melatonin solubility enhancing pH environment and to maintain the melatonin solubility enhancing pH environment when the composition is located in a melatonin solubility diminishing pH environment for allowing an effective amount of melatonin to be released into the melatonin solubility diminishing pH environment.
    Type: Application
    Filed: January 27, 2012
    Publication date: August 2, 2012
    Inventors: SYED M. SHAH, DANIEL HASSAN
  • Acyl Guanidine Derivatives Modulating The Hedgehog Protein Signaling Pathway
    Publication number: 20120196865
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Application
    Filed: July 19, 2010
    Publication date: August 2, 2012
    Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Substituted arylsulphonylglycines, the preparation thereof and the use thereof as pharmaceutical compositions
    Patent number: 8232312
    Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Targeting of EWS-FLI1 as anti-tumor therapy
    Patent number: 8232310
    Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: July 31, 2012
    Assignee: Georgetown University
    Inventors: Jeffrey A. Toretsky, Aykut Üren, Milton Lang Brown, Yali Kong
  • METHODS TO IDENTIFY TARGETS AND MOLECULES REGULATING PURINOSOMES AND THEIR USES
    Publication number: 20120190620
    Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 26, 2012
    Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier