The Bicyclo Ring System Consists Of The Five-membered Hetero Ring And A Benzene Ring (e.g., Indole, Etc.) Patents (Class 514/415)
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Publication number: 20130102609Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.Type: ApplicationFiled: December 14, 2012Publication date: April 25, 2013Applicant: LIGAND PHARMACEUTICALS INC.Inventor: Ligand Pharmaceuticals Inc.
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Publication number: 20130096175Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.Type: ApplicationFiled: November 17, 2010Publication date: April 18, 2013Applicants: SOUTHERN RESEARCH INSTITUTE, UNIVERSITY OF ROCHESTERInventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucile White, Krister Wennerberg
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Patent number: 8420677Abstract: Use of DIM and/or its derivatives for prevention, treatment and/or delay of age-related hearing loss in mammals.Type: GrantFiled: February 19, 2009Date of Patent: April 16, 2013Assignee: DSM IP Assets B.V.Inventors: Hubert Hug, Bernd Mussler, Daniel Raederstorff, Ying Wang-Schmidt
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Patent number: 8420830Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: December 19, 2007Date of Patent: April 16, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Peter W. Glunz, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata, Luciano Mueller
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Publication number: 20130085165Abstract: A lozenge is provided that has stable pH and stable levels of active ingredient over time. It comprises a combination of (i) at least one gum and (ii) at least one non-crystallising sugar or non-crystallising sugar alcohol in a matrix designed for controlled buccal delivery of a drug. The lozenge also contains water and optional components selected from flavourings, taste masking agents, colourings, buffer components, pH adjusting agents, excipients, stabilizers and sweeteners. Methods of preparing the lozenge are also provided.Type: ApplicationFiled: November 26, 2012Publication date: April 4, 2013Applicant: ARROW NO. 7 LIMITEDInventors: Anders Dam, Janos Major, Peter Tasko
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Patent number: 8410147Abstract: This invention is directed to methods of preventing or treating diseases or conditions associated with alterations in cellular integrity including alterations in endothelial permeability, excessive cell proliferation or tissue remodeling. Particularly, this invention is directed to methods of treating diabetic nephropathy, malaria, or cancer. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.Type: GrantFiled: June 26, 2009Date of Patent: April 2, 2013Assignee: Inspire Pharmaceuticals, Inc.Inventors: Ward M. Peterson, John W. Lampe, Tomas Navratil, Scott D. Sorensen, Emilee H. Fulcher
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Publication number: 20130078215Abstract: Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described.Type: ApplicationFiled: November 2, 2012Publication date: March 28, 2013Applicant: PHARMACYCLICS, INC.Inventor: PHARMACYCLICS, INC.
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Publication number: 20130072491Abstract: An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula).Type: ApplicationFiled: August 31, 2012Publication date: March 21, 2013Applicant: Ajinomoto Co., Inc.Inventors: Reiko YASUDA, Yuzuru Eto, Yoshiro Kitahara
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Publication number: 20130072539Abstract: A particularly constructed tamoxifen-melatonin hybrid ligand gives new and unexpectedly improved results in the prevention and treatment of cancer, particularly breast cancer. The hybrid ligand comprises either tamoxifen or 4-hydroxy-tamoxifen and also melatonin, with the tamoxifen or 5-hydroxy-tamoxifen and melatonin's being linked by an unsubstituted C2-C4 alkyl liner between the tamoxifen amine and the carbonyl of melatonin.Type: ApplicationFiled: October 12, 2010Publication date: March 21, 2013Inventors: Paula A. Witt-Enderby, Vicki L. Davis, David Lapinsky
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Patent number: 8394847Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.Type: GrantFiled: August 26, 2009Date of Patent: March 12, 2013Assignee: Natrogen Therapeutics International, Inc.Inventors: Longgui Wang, Xiao Mei Liu, Lian Mo, Simon K. Mencher, James P. McCarron, Jr.
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Patent number: 8389563Abstract: The present embodiment of the invention is generally directed to compositions comprising suspensions of poorly water soluble compounds recrystallized in nanoparticulate sizes ranging from 0.1 to 5 ?m. In addition, the embodiment of the invention is directed to methods for preparation and administration of these compositions to a patient for prevention and treatment of disease states. In particular, the embodiment of the invention is directed to compositions comprising suspensions of poorly water-soluble compounds, such as antimitotics and antibiotics, in nanoparticulates and methods of prevention and treatment of chronic disease states, such as cancer, by intraperitoneal and intravenous administration of such compositions.Type: GrantFiled: December 2, 2011Date of Patent: March 5, 2013Assignee: The Texas A&M University SystemInventor: Stephen H. Safe
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Publication number: 20130052234Abstract: An edible oral strip composition includes a therapeutically effective amount of active agent(s) to provide at least one effect selected from a stimulating effect, an increased physical endurance, alleviate temporary fatigue, improve nervous system functions, and combinations of any of the foregoing. In additional embodiments, the edible strip composition includes a therapeutically effective amount of active agent(s) to provide sleep aid.Type: ApplicationFiled: August 3, 2012Publication date: February 28, 2013Applicant: Purebrands LLCInventors: Michael Goldberg, Ehud Arbit
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Publication number: 20130052190Abstract: The present invention provides a method for the treatment of allergic and inflammatory diseases or conditions by administering a compound of Formula (I). The invention provides a method of treatment that is particularly suited for patients with a high degree of airway eosinophilia in contrast to those with a lower degree of airway eosinophilia. The invention also provides a method of treatment that is particularly suited for patients with a high atopic status in contrast to those patients with a lower atopic status.Type: ApplicationFiled: February 22, 2012Publication date: February 28, 2013Applicant: Oxagen LimitedInventors: Lisa Pearce Collins, Colin Michael Perkins, Michael Hunter, Eric Roy Pettipher
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Publication number: 20130045217Abstract: The present invention inter alia provides a method, and use thereof, of diagnosing and/or predicting atherosclerosis or CVD by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control and has identified specific lipid markers that are more specific and sensitive in detecting and predicting atherosclerosis and CVD than currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, preventing and/or treating atherosclerosis or CVD. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of atherosclerosis or CVD.Type: ApplicationFiled: May 5, 2011Publication date: February 21, 2013Applicant: ZORA BIOSCIENCES OYInventors: Reijo Laaksonen, Kim Ekroos, Reini Hurme, Minna Janis, Riika Katainen, Kirill Tarasov
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Patent number: 8377928Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives of Formula (I): The invention also relates to compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: November 13, 2008Date of Patent: February 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski
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Patent number: 8377941Abstract: The present invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-2-(trifluoromethyl)-5-pyrimidinecarboxamide.Type: GrantFiled: April 16, 2009Date of Patent: February 19, 2013Assignee: Proximagen LimitedInventors: Kevin Dinnell, Andrew P Lightfoot, Howard Robert Marshall
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Patent number: 8377947Abstract: Use of a composition for treating Alzheimer's disease, osteoporosis, sleep apnea, erectile dysfunction, McArdle disease, or a carbohydrate metabolism disorder, or for reducing aging or fatigue. The composition includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5?-monophosphate-activated protein kinase activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.Type: GrantFiled: March 15, 2010Date of Patent: February 19, 2013Inventor: Chien-Hung Chen
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Patent number: 8377983Abstract: The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.Type: GrantFiled: February 10, 2010Date of Patent: February 19, 2013Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Brian S. Grella, Govindan Subramanian, Murty N. Arimilli, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Xiaochuan Guo, Jeff Zhu
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Publication number: 20130040977Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: August 24, 2012Publication date: February 14, 2013Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20130039998Abstract: The present invention is directed to a composition comprising a modulator of the Wnt/?-catenin pathway, such as a GSK-3 inhibitor, or a pharmaceutically acceptable salt thereof either with a benzamide derivative or a pharmaceutically acceptable salt thereof or with a hydroxamic acid or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method of treating bipolar disorder in a subject by administering either a benzamide derivative or a hydroxamic acid to the subject under conditions effective to treat a bipolar disorder. A modulator of the Wnt/?-catenin pathway, such as a GSK-3 inhibitor, or a pharmaceutically acceptable salt thereof may also be administered to a subject.Type: ApplicationFiled: December 23, 2009Publication date: February 14, 2013Applicants: UNIVERSITY OF WASHINGTON, MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventors: Daniel Fass, Stephen Haggarty, Edward Scolnick, Randall T. Moon, Travis L. Biechele, Nathan D. Camp
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Publication number: 20130040998Abstract: Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (e.g., cancer, neurodegenerative diseases, inflammatory diseases).Type: ApplicationFiled: January 5, 2011Publication date: February 14, 2013Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: James Elliot Bradner, Ralph Mazitschek
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Publication number: 20130035312Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: October 11, 2012Publication date: February 7, 2013Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
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Patent number: 8367665Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: GrantFiled: April 16, 2009Date of Patent: February 5, 2013Assignee: Karo Bio ABInventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
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Patent number: 8367358Abstract: The present disclosure discloses a reagent for differentiating and counting leukocytes which includes: (1) cationic cyanine compounds selected from those having the following general formulae I and II; (2) cationic surfactants selected from those having the following general formulae III, IV and/or V; (3) at least one nonionic surfactant; and (4) optionally, at least one anionic compound selected from those having one or more carboxyl or sulphonyl groups; and optionally includes alcohol compounds. Also disclosed is a kit comprising the reagent for differentiating and counting leukocytes. Further disclosed is a method for differentiating and counting leukocytes using the reagent and kit. Use of the reagent, kit and method disclosed enables the identification of leukocytes in blood samples into five subtypes in a very short time, or at least achieves the differentiation and counting of four leukocyte groupings. Moreover, immature and abnormal cells can be identified.Type: GrantFiled: September 28, 2009Date of Patent: February 5, 2013Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventors: Lei Ting, Xu Bing, Kuang Yuji, Zhang Baohua, Shao Jianhui
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Patent number: 8367711Abstract: A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: GrantFiled: May 30, 2012Date of Patent: February 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Iyassu K. Sebhat, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
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Publication number: 20130029846Abstract: The present invention relates to the use of bicyclic amidine compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to novel bicyclic amidines and processes and intermediates for preparing these compounds.Type: ApplicationFiled: March 28, 2011Publication date: January 31, 2013Applicant: BASF SEInventors: Joachim Rheinheimer, Christian Pilger, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Burghard Liebmann, Wassilios Grammenos
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Publication number: 20130028943Abstract: The present invention provides a pharmaceutical composition for sublingual or buccal administration of actives with low to poor aqueous solubility, e.g. the indole hormone melatonin, which contains a solution of the active in a pharmaceutically acceptable solvent adsorbed or absorbed onto particles of a pharmaceutically acceptable carrier and methods of preparing and using the pharmaceutical composition.Type: ApplicationFiled: October 3, 2012Publication date: January 31, 2013Inventor: John A. McCARTY
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Publication number: 20130029927Abstract: The invention relates to a combination comprising the N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Inventors: Peter Wisdom Atadja, Wenlin Shao, Kapil N. Bhalla
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Patent number: 8362066Abstract: The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, A? protein or ?-synuclein protein aggregation.Type: GrantFiled: November 19, 2007Date of Patent: January 29, 2013Assignee: Treventis CorporationInventors: Michael D. Carter, Donald F. Weaver, Sheila Marie H. Jacobo, Erhu Lu, Fuye Gao
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Patent number: 8362056Abstract: Compounds of Formula I: I in which D1, D2, R1, R2, R7, R8 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: GrantFiled: November 4, 2008Date of Patent: January 29, 2013Assignee: Array BioPharma Inc.Inventor: George A. Doherty
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Publication number: 20130023513Abstract: The invention generally relates to methods of treating a patient having, and/or at risk of, cardiovascular or cerebrovascular disorders. Such methods may include administering a MetAP2 inhibitor at a dose that does not substantially modulate angiogenesis.Type: ApplicationFiled: January 11, 2011Publication date: January 24, 2013Inventor: Thomas E. Hughes
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Patent number: 8357705Abstract: 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 or other conditions.Type: GrantFiled: March 25, 2009Date of Patent: January 22, 2013Assignee: Gruenenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Klaus Linz, Derek John Saunders, Wolfgang Schröder, Werner Englberger, Fritz Theil, Hans Schick, Jens Kaufmann, Julian Gebauer, Helmut Sonnenschein
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Publication number: 20130018026Abstract: The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Inventor: Keith R. Latham
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Publication number: 20130018073Abstract: The present invention provides an indole derivative having a melanin-concentrating hormone receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: January 5, 2011Publication date: January 17, 2013Inventors: Shinichi Masada, Yoshito Terao, Toshiki Murata
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Publication number: 20130017188Abstract: The inventors have made the surprising discovery that SGK1, a serine/threonine kinase previously described as being involved in regulation of cellular sodium homeostasis, has a novel and unexpected function in the differentiation and function of a specific subset of CD4 T cells, the TH17 lineage. Described herein are methods and compositions for modulation of TH17 cell differentiation, proliferation, and/or function that rely upon modulating the activity or expression of SGK1. Such methods and compositions are useful in the treatment of disorders including autoimmune diseases, chronic inflammatory conditions, infectious diseases, and cancer.Type: ApplicationFiled: July 30, 2010Publication date: January 17, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Vijay K. Kuchroo, Hulin Jin
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Patent number: 8349822Abstract: This invention relates to compositions and methods utilizing a chemotherapeutic drug and 6-bromoindirubin3?-oxime (BIO) for the treatment of cancer, including glioblastoma multiforme. The present invention demonstrates that BIO works synergistically with chemotherapeutic drugs to increase the cytotoxic effects of these drugs in glioma cells.Type: GrantFiled: February 25, 2008Date of Patent: January 8, 2013Assignee: Cedars-Sinai Medical CenterInventor: John S. Yu
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Patent number: 8349886Abstract: The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: April 15, 2009Date of Patent: January 8, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Osamu Ujikawa
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Publication number: 20130004577Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: NIPPON SHINYAKUInventors: Hironobu KATO, Hirokazu SAKAMOTO
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Patent number: 8343964Abstract: The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.Type: GrantFiled: January 31, 2008Date of Patent: January 1, 2013Assignees: Universite Joseph Fourier, Centre National de la Recherche ScientifiqueInventors: Jean-Noel Marie Leon Denis, Xavier Jean Georges Marie Guinchard, Nicole Jeanne Moreau born Laffont, Luc Neuville, Yannick Vallee
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Patent number: 8338416Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: GrantFiled: March 16, 2007Date of Patent: December 25, 2012Assignee: Pharmacylics, Inc.Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
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Publication number: 20120322800Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).Type: ApplicationFiled: October 14, 2010Publication date: December 20, 2012Inventor: Julian Blagg
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Patent number: 8334109Abstract: A reagent for blood analysis includes: (1) a compound having the general formula I; and (2) at least one surfactant selected from cationic surfactants and nonionic surfactants. In another aspect a method for differentiating and counting blood cells is provided, the method includes the following steps: (a) mixing a blood sample with the reagent for blood analysis according to the present disclosure to form a cell suspension; (b) detecting scattered light signals and fluorescence signals of cells in the blood sample; and (c) differentiating and counting the cells in the blood sample based upon the scattered light signals and fluorescence signals. The reagent for blood analysis may be effective for identifying and counting erythroblasts and/or basophils in a blood sample to be detected, and meanwhile counting leukocytes therein.Type: GrantFiled: December 8, 2009Date of Patent: December 18, 2012Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventors: Zhang Baohua, Xu Bing, Kuang Yuji, Lei Ting, Shao Jianhui, Bao Dequan
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Publication number: 20120316215Abstract: Disclosed are methods for treating a subject suffering from phenylketonuria and/or phenylalanemia. The methods include, in part, enterally administering to the subject a LNAA supplement in which the weight ratio of Leu to Val is greater than 2:1; in which the weight ratio of Leu to iLeu is greater than 3:1; or which includes one or more LNAAs and which further includes Lys. LNAA supplements are also disclosed. Also disclosed are methods for treating a subject suffering from a condition involving a metabolic disorder involving the metabolism of a first amino acid X. The method includes enterally administering to the subject a composition which (i) is substantially free from the first amino acid X and (ii) which includes a second amino acid Y that competes with amino acid X at a gastrointestinal tract transporter.Type: ApplicationFiled: August 20, 2012Publication date: December 13, 2012Applicant: PreKUlab Ltd.Inventor: Reuben Matalon
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Publication number: 20120309757Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120309769Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120309808Abstract: Provided herein are pharmaceutical compositions and methods for treating disorders characterized by reduced expression of anti-oxidative stress enzymes in a subject. In one aspect, the present invention provides a method for inducing expression of anti-oxidative stress enzymes in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of a demethylating agent. The demethylating agent includes a phytochemical that induces expression of Nrf2 and Nrf2-mediated genes expressing anti-oxidative stress. Such phytochemicals include indoles, such as 3,3?-diindolylmethane (DIM) and indole-3-carbinol (I3C), and isothiocyanates, such as phenethyl isothiocyanate (PEITC) and sulforaphane (SFN).Type: ApplicationFiled: May 31, 2012Publication date: December 6, 2012Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventor: Ah-Ng T. Kong
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Publication number: 20120309809Abstract: A method of processing an active ingredient, the method comprising submitting a pharmaceutically active ingredient in the absence of excipients and/or additives to compression and shearing forces. The invention also relates to compositions comprising an active prepared by the method.Type: ApplicationFiled: December 8, 2010Publication date: December 6, 2012Applicant: VECTURA LIMITEDInventors: Matthew Michael James Green, Richard Michael Poole
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Patent number: 8324258Abstract: The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.Type: GrantFiled: September 11, 2008Date of Patent: December 4, 2012Assignee: The Regents of the University of MichiganInventors: Gary D. Glick, Gina Ney
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Patent number: 8324267Abstract: The present invention relates to protein kinase inhibitors and to the use thereof for the treatment of diseases induced by pathological signal transduction cascades.Type: GrantFiled: July 12, 2002Date of Patent: December 4, 2012Assignee: Forschungzentrum Karlsruhe GmbHInventors: Vladimir Chirchin, Giannis Athanassios, Ralph Mazitschek, Jonathan Sleemann
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Publication number: 20120302576Abstract: 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: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet