Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/469)
  • Patent number: 10239854
    Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: March 26, 2019
    Assignee: ARTHROSI THERAPEUTICS, INC.
    Inventors: Shunqi Yan, Li-Tain Yeh, Robert Orr
  • Patent number: 10213464
    Abstract: The present invention provides a novel method for enhancing engraftment of haematopoetic stem cells by an ex-vivo pretreatment comprising the steps of obtaining a sample containing haematopoetic stem cells and admixing a prostacyclin analog to obtain a mixture, incubating said mixture for a period of time sufficient to stimulate G alphas-signalling in said cells and optionally and isolating said stimulated cells. Further, a composition comprising a prostacyclin analog for use in the treatment of individuals undergoing haematopoetic stem cell transplantation is provided.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: February 26, 2019
    Assignee: SCIPHARM SARL
    Inventors: Michael Freissmuth, Eva-Maria Zebedin-Brandl, Christian Bergmayr, Filza Hussain
  • Patent number: 10196342
    Abstract: The present disclosure provides regioselective methods for synthesizing intermediates useful in making prostacyclin derivatives, such as treprostinil.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: February 5, 2019
    Assignee: United Therapeutics Corporation
    Inventors: Hitesh Batra, Sudersan M. Tuladhar, David A. Walsh
  • Patent number: 10189783
    Abstract: The present invention relates to a an imide compound according to anyone of formulas Ia, Ib, Ic, or Ie wherein R1 is H or a C1-C20 optionally substituted hydrocarbon group; both R2 and R5 are a COOH group or one of R2 and R5 is a COOH group while the other substituent is H, methyl or ethyl group; R3 and R4 are independently H, or C1-C20 optionally substituted hydrocarbon group; R6 is H or a methyl group; R7 and R8 are independently H, methyl or ethyl.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: January 29, 2019
    Assignee: DSM IP ASSETS B.V.
    Inventors: Cornelis Eme Koning, Paulus Franciscus Anna Buijsen, Adrianus Jozephus Hendricus Lansbergen, Alwin Papegaaij, Douglas Hayden
  • Patent number: 10179119
    Abstract: Embodiments of the invention relate to the treatment of sleep disturbances in individuals with Smith-Magenis Syndrome (SMS).
    Type: Grant
    Filed: August 29, 2015
    Date of Patent: January 15, 2019
    Assignee: VANDA PHARMACEUTICALS INC.
    Inventors: Christian Lavedan, Mihael H. Polymeropoulos
  • Patent number: 10017487
    Abstract: The present invention relates to a condensed heterocyclic compound that has an enteropeptidase inhibitory effect, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like. Specifically, the present invention relates to a compound represented by the formula (I) or a salt thereof, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like [in the formula, each symbol is as defined in the specification].
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: July 10, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Keiko Kakegawa, Zenichi Ikeda, Minoru Sasaki, Fumiaki Kikuchi, Yoichi Nishikawa
  • Patent number: 9920036
    Abstract: Compounds of Formula (I), including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: (I).
    Type: Grant
    Filed: March 20, 2015
    Date of Patent: March 20, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, John F. Kadow
  • Patent number: 9913823
    Abstract: The present invention relates to a compound of Formula 1, and an SIRT 1 activator including, as an active ingredient, derivatives thereof or pharmaceutically acceptable salts thereof. The present invention also relates to a composition including the SIRT 1 activator for detoxification, for the improvement of metabolic disorders, for the prevention or improvement of eye diseases, or the prevention or improvement of immune diseases.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: March 13, 2018
    Assignee: AMOREPACIFIC CORPORATION
    Inventors: Byung Gyu Kim, Hyun Woo Jeong, Su Kyung Kim, Si Young Cho, Chan Woong Park, Dae Bang Seo, Wan Gi Kim, Sang Jun Lee
  • Patent number: 9895340
    Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: February 20, 2018
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards
  • Patent number: 9782383
    Abstract: It is already known that 1-(benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable acid addition salt thereof exhibits an excellent effect as an antidepressant, a psychotropic drug, an antiparkinsonian drug, and an anti-Alzheimer's disease drug. However, it has not been known at all that the compound is effective for the prevention or therapy of attention-deficit/hyperactivity disorder (ADHD). The present invention has newly found that 1-(benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable acid addition salt thereof is effective for the prevention or therapy of ADHD, and has been accomplished.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: October 10, 2017
    Assignee: FUJIMOTO CO., LTD.
    Inventors: Hiroko Togashi, Sachiko Hiraide, Fumio Yoneda, Kazue Takahata
  • Patent number: 9745319
    Abstract: Irreversible inhibitors of K-Ras, H-Ras or N-ras protein comprising a G12C mutation are provided. Also disclosed are methods to regulate the activity of K-Ras, H-Ras or N-ras protein comprising G12C mutation and methods to disease mediated by K-Ras, H-Ras or N-ras G12C.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 29, 2017
    Assignee: ARAXES PHARMA LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng
  • Patent number: 9700540
    Abstract: The invention relates to dronedarone or one of its pharmaceutically acceptable salts for the treatment of leishmaniasis, formulations and associations comprising dronedarone or one of its pharmaceutically acceptable salts for the treatment of leishmaniasis.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: July 11, 2017
    Assignee: SANOFI
    Inventors: Stephane Beilles, Sandra Chambonnet, Jean-Pierre Collaveri
  • Patent number: 9642828
    Abstract: The present invention relates to a stable, sterile, ready to administer parenteral dosage form of amiodarone or its pharmaceutically acceptable salt. Particularly, the present invention provides a stable, sterile, ready to administer parenteral dosage form of amiodarone comprising an aqueous solution comprising amiodarone or its pharmaceutically acceptable salt, an acid, and a polyol, wherein the pH of the solution is in the range of about 2.0 to 4.0, wherein the solution is filled in a plastic container and wherein the solution is free of a solubilizer.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: May 9, 2017
    Assignee: SUN PHARMACEUTICAL INDUSTRIES LIMITED
    Inventors: Amar Kishorbhai Rana, Shantaram Pawar, Prashant Kane, Subhas Balaram Bhowmick, Maheshkumar Parasmal Soni, Milan Mohanbhai Vasoya, Samarth Kumar
  • Patent number: 9624189
    Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: April 18, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards
  • Patent number: 9604952
    Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: March 28, 2017
    Assignee: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan, Ji-Hye Kang
  • Patent number: 9549913
    Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: January 24, 2017
    Assignee: Vanda Pharmaceuticals, Inc.
    Inventors: Marlene Michelle Dressman, Louis William Licamele, Mihael H. Polymeropoulos
  • Patent number: 9517232
    Abstract: The invention is directed to the use of a compound of formula I, as defined herein, to a pharmaceutically acceptable salt thereof; to a pharmaceutical composition containing a compound of formula I, and to a combination of a compound of formula I with a pharmacologically effective cholinesterase inhibitor to treat a mammal, including a human, for a disorder or condition selected from the list including Alzheimer's disease, Huntington's disease, Parkinson's disease, non-Alzheimer's dementias and ALS.
    Type: Grant
    Filed: September 15, 2015
    Date of Patent: December 13, 2016
    Assignee: Medi Synergics, LLC
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Patent number: 9492426
    Abstract: In some embodiments, the present invention provides methods of treating a tumor in a subject. In some embodiments, the methods may include a step of administering to the subject a therapeutic composition that comprises: (a) mycophenolic acid, an analog thereof, or a derivative thereof; and (b) at least one anti-neoplastic agent. In some embodiments, the antineoplastic agent may include at least one of 5-fluouracil (5-FU), paclitaxel, oxaliplatin, doxorubicin, etoposide, irinotecan, bleomycin, imiquimod, 13-cis-retinoic acid, and combinations thereof. In some embodiments, the relative concentrations of the mycophenolic acid, the analog thereof, or the derivative thereof, and the at least one anti-neoplastic agent correspond to their respective IC50 values.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: November 15, 2016
    Assignee: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Robert Y. Tsai, Tao Lin
  • Patent number: 9474733
    Abstract: The object of the invention is the use of compounds comprising one or more free sulphlydryl or amino groups for preparing a pharmaceutical composition for locally binding acetaldehyde in saliva, the stomach or the large intestine, and pharmaceutical compositions comprising the said compounds.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: October 25, 2016
    Assignee: BIOHIT OYJ
    Inventors: Mikko Salaspuro, Martti Marvola
  • Patent number: 9468627
    Abstract: The present invention concerns the treatment of serotonergic dysregulation disorders and/or augmentation of serotonin levels in the brain by add-on treatments to serotonin enhancers, and slow-release formulations of 5-hydroxytryptophan (5-HTP) therefor.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: October 18, 2016
    Assignee: Duke University
    Inventors: Jacob P. R. Jacobsen, Marc G. Caron
  • Patent number: 9434738
    Abstract: Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: September 6, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, John F. Kadow
  • Patent number: 9408816
    Abstract: Provided herein are methods for using at least one histone deacetylase inhibitor to decrease cellular DNA repair activity, methods for monitoring the decrease of cellular DNA repair activity using at least one biomarker, methods of treating cancer by using at least one histone deacetylase inhibitor to decrease cellular DNA repair activity in combination therapy, methods of combination therapy where at least one histone deacetylase inhibitor interferes with a DNA repairing mechanism involving RAD51, methods for predicting a induction time period between a first administration of at least one histone deacetylase inhibitor and a second administration of at least one other therapeutic treatment, and pharmaceutical compositions for combination therapy.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: August 9, 2016
    Assignee: Pharmacyclics LLC
    Inventors: Shanthi Adimoolam, Joseph J. Buggy, Darren Magda, Richard Miller
  • Patent number: 9346842
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: May 24, 2016
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Patent number: 9278947
    Abstract: Serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.
    Type: Grant
    Filed: February 4, 2013
    Date of Patent: March 8, 2016
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Moshe Rehavi, David Gurwitz
  • Patent number: 9155790
    Abstract: Methods for modulating eye damage associated with a disease or disorder, and/or damage incident to trauma including but not limited to trauma associated with ocular surgery are provided. In some embodiments, the methods include administering an effective amount of a modulator of a migration inhibitory factor (MIF) polypeptide biological activity to a subject. Also provided are methods for modulating the severity of delaying the onset of and/or inhibiting and/or preventing the development of an ocular disease, and methods for modulating the severity of delaying the onset of and/or inhibiting and/or preventing the development of scarring and/or other consequence of wound healing incident to ocular surgery, as well as modulating the survival, function, and/or differentiation of engrafted cells that can be employed as part of tissue engineering procedures to correct structural, functional, and/or cellular defects of the eye.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: October 13, 2015
    Assignee: University of Lousiville Research Foundation, Inc.
    Inventors: Tongalp H. Tezel, Henry J. Kaplan, Robert A. Mitchell, John O. Trent
  • Patent number: 9107900
    Abstract: Methods of using dronedarone or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the prevention of cardiovascular hospitalization or of mortality, articles of manufacture and packages related thereto.
    Type: Grant
    Filed: March 19, 2013
    Date of Patent: August 18, 2015
    Assignee: SANOFI
    Inventors: Davide Radzik, Martin Van Eickels, Nacera Hamdani, Christophe Gaudin
  • Patent number: 9102608
    Abstract: Provided is a simple, safe, and industrially practical method for producing a pentafluorosulfanylbenzoic acid.
    Type: Grant
    Filed: December 4, 2012
    Date of Patent: August 11, 2015
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Norimichi Saito, Junichi Chika
  • Patent number: 9066880
    Abstract: This invention relates to cosmetic and pharmaceutical preparations comprising (i) a diastereomer or a mixture of two or more diastereomers of the compound of formula (I) or (ii) a salt of a diastereomer or of a mixture of two or more diastereomers of the compound of formula (I) or (iii) a mixture of two or more salts of a diastereomer or of a mixture of two or more diastereomers of the compound of formula (I), a diastereomer, salt or a mixture as defined above as a drug for topical application and/or for the treatment of lipoatrophy; the non-therapeutic use of a diastereomer, salt or a mixture as defined above for the prevention, treatment or reduction of skin aging, especially skin wrinkles; the use of a diastereomer, salt or a mixture as defined above for the production of an orally administered non-pharmaceutical preparation.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: June 30, 2015
    Assignee: SYMRISE AG
    Inventors: Imke Meyer, Oskar Koch, Jean Krutmann
  • Patent number: 9060995
    Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.
    Type: Grant
    Filed: June 11, 2014
    Date of Patent: June 23, 2015
    Assignee: Vanda Pharmaceuticals, Inc.
    Inventors: Marlene Michelle Dressman, John Joseph Feeney, Louis William Licamele, Mihael H. Polymeropoulos
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Publication number: 20150148353
    Abstract: A method of increasing the insulin sensitivity of a mammalian cell by contacting the cell with a protein phosphatase 2A (PP2A) inhibitor having the structure:
    Type: Application
    Filed: June 28, 2013
    Publication date: May 28, 2015
    Applicant: LIXTE BIOTECHNOLOGY, INC.
    Inventor: John S. Kovach
  • Publication number: 20150148408
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: February 2, 2015
    Publication date: May 28, 2015
    Inventors: Mohamed Naquib Attala, Philippe Diaz
  • Patent number: 9040066
    Abstract: This invention is based upon the discovery that a mixture of ethyl lactate and isoamyl lactate can be used to improve the penetration of active ingredients in skin care formulations through the outer layers of the stratum corneum and viable epidermis and into the dermis layer of the skin structure. The present invention more specifically discloses a method of rejuvenating skin comprising topically applying a topical formulation to the skin, wherein the topical formulation is comprised of ascorbic acid, an amino acid selected from the group consisting of phenylalanine and tyrosine, a non-toxic zinc salt, carnosic acid, ?-tocopherol, 0.01 weight percent to 20 weight percent of a mixture of ethyl lactate and isoamyl lactate, wherein the weight ratio of the ethyl lactate to the isoamyl lactate is within the range of 1:10 to 20:1, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: May 26, 2015
    Assignee: Ad Lunam Labs, Inc.
    Inventors: William H. Beeson, Alvin T. Rockhill
  • Patent number: 9040553
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Publication number: 20150141465
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Calvin W. YEE, Zhe Li
  • Publication number: 20150141380
    Abstract: A method of treating a subject at risk of or suspected of having Fragile X syndrome or autism spectrum disorder associated with abnormalities of ERK includes administering to the subject a therapeutically effective amount of at least one ERK inhibiting compound that prevents abnormalities in neuronal connectivity, a prodrug thereof that is metabolisable to form the compound, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 5, 2011
    Publication date: May 21, 2015
    Applicant: CASE WESTERN RESERVE UNIVERSITY
    Inventors: Mark A. Smith, Michael Snape
  • Patent number: 9034310
    Abstract: A method for pharmacological treatment of cancers and other diseases is presented which includes the novel combination of a statin (Hmg-CoA reductase inhibitor, such as lovastatin, simvastatin, atorvastatin, cerivastatin, fluvastatin, pravastatin, or newer agents), with an interferon (such as interferon alfa-2b or others) and also including concurrent administration of selenium and calcium. The method disclosed in this invention is useful because it can prove more effective than previously known therapies for certain diseases and because its use may be more tolerable, less disfiguring, and less expensive than other methods. The method here disclosed can be readily reproduced by any person skilled in the art of treating disease.
    Type: Grant
    Filed: February 20, 2003
    Date of Patent: May 19, 2015
    Inventor: Stephen B. Cantrell
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Patent number: 9018250
    Abstract: The disclosure relates to a pharmaceutical composition for oral administration, containing, as active principle, a benzofuran derivative having antiarrhythmic activity, in particular dronedarone and the pharmaceutically acceptable salts thereof, and at least one lipid carrier, said pharmaceutical composition being intended to be used in unit dosage form of the capsule type, in particular with a hard shell. This pharmaceutical composition and the dosage form comprising such a composition aim to limit the meal time effect following oral administration in humans. The lipid carrier allows: the solubilization of the active principle of the invention; and the shielding thereof from the negative effects of pH in the intestinal tract, thereby allowing same to be spared from the meal effect to a significant extent.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: April 28, 2015
    Assignee: Sanofi
    Inventors: Bernard Abramovici, Stephane Beilles, Sandra Chambonnet, Jean-Claude Gautier
  • Patent number: 9006284
    Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: April 14, 2015
    Assignee: Bionomics Limited
    Inventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Patent number: 8993619
    Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Sejal Patel, Justin Mao, Qian Liu, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
  • Patent number: 8993620
    Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: March 31, 2015
    Assignee: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Publication number: 20150086480
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
    Type: Application
    Filed: September 26, 2014
    Publication date: March 26, 2015
    Inventors: Emily Catherine D'Amato, Mark Gurney, Xuesheng Mo, Richard A. Nugent
  • Publication number: 20150087676
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: December 9, 2014
    Publication date: March 26, 2015
    Inventors: Michael Eissenstat, Dehui Duan
  • Publication number: 20150087649
    Abstract: Methods and agents are provided for treatment of disorders associated with aberrant adrenocortical cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC) and/or Cushing's syndrome. Such methods involve administration of an agent which exhibits an IC50 value against huACAT1 of less than 10 ?M, and one or more further characteristics including effects on adrenocortical cells, disruption of cholesterol homeostasis, reduction in steroid biosynthesis, reduction of mitochondrial function, and/or preferential binding to by low-density lipoprotein (LDL).
    Type: Application
    Filed: September 26, 2014
    Publication date: March 26, 2015
    Inventors: Stephen Warren Hunt, III, Julia Christine Owens, William E. Rainey, JR., Christopher R. LaPensee, Gary D. Hammer
  • Publication number: 20150080464
    Abstract: Melatonin Agonist, MA-1, is administered at effective doses.
    Type: Application
    Filed: November 27, 2014
    Publication date: March 19, 2015
    Inventors: Gunther Birznieks, Deepak Phadke, Mihael H. Polymeropoulos
  • Patent number: 8980846
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating asthma, the composition containing styraxlignolide A or an aglycone thereof as an active ingredient. More particularly, styraxlignolide A compound is one separated from stems and barks of Styrax japonica, and styraxlignolide A or homoegonol, which is an aglycone of styraxlignolide A and which has improved safety, has the effect of attenuating weight loss and airway hyperresponsiveness, inhibiting the generation of reactive oxygen species in airway, inhibiting generation of IgE, TGF-?1, and IL-17 in the serum and bronchoalveolar lavage fluid, inhibiting endobronchial inflammatory cell infiltration, and inhibiting the formation of a mucous plug and subepithelial fibrosis in an asthma-induced mouse model. Therefore, styraxlignolide or homoegonol can be effectively used as the active ingredient of a pharmaceutical composition for preventing or treating bronchial asthma in which airway remodeling has progressed.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: March 17, 2015
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Kyung Seop Ahn, Ha Young Jang, Sei Ryang Oh, Hyeong Kyu Lee, Ok-Kyoung Kwon, Semi Kim, Jung Hee Kim, Doo-Young Kim
  • Patent number: 8975277
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LQ and Ar are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: March 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf