Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/469)
  • 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: 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
  • 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
  • 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: 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: 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: 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
  • Publication number: 20150065494
    Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
  • Publication number: 20150065554
    Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventor: Cristina Fernandez-Valle
  • Publication number: 20150057320
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina of a mammal afflicted therewith comprising administering to the mammal an effective amount of a transthyretin (TTR) ligand.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: The Trustees of Columbia University in the City of New York
    Inventor: Konstantin PETRUKHIN
  • Publication number: 20150057325
    Abstract: The present invention relates to novel uses of compounds that protect the endothelium, particularly prostacyclin and variants and derivatives thereof in the treatment or prevention of acute traumatic coagulopathy (ATC) and of patients resuscitating from cardiac arrest. The invention also relates to a method of identifying individuals at risk of developing ATC.
    Type: Application
    Filed: March 26, 2013
    Publication date: February 26, 2015
    Applicant: Rigshospitalet
    Inventors: Pär Johansson, Sisse Rye Ostrowski
  • Publication number: 20150057238
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Publication number: 20150051270
    Abstract: A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein either Q1, CR6a and optionally R6b together form a cyclic moiety wherein: Q1 is selected from C1-2 alkylene, C1-2 alkenylene, OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo; R6a is a single bond and R6b is H; or R6a and R6b together form a double bond; and Q2 and Q3 are independently selected from H, R1 and R2; or Q2 and Q3 together form a cyclic moiety in which one of Q2 and Q3 is a cyclic moiety selected from OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo or a group R5 as here in below defined for R2 and the other of Q2 and Q3 is a cyclic moiety selected from C1-2 alkylene, C1-2 alkenylene and OC1 alkylene optionally substituted by oxo; R6a and R6b are each H or a cyclic moiety as defined above; and Q1 is selected from H, R1 and R2 and a cyclic moiety as defined above; and R1-4 are H or substituen
    Type: Application
    Filed: February 15, 2013
    Publication date: February 19, 2015
    Inventors: Shailesh Mistry, Etíenne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20150045373
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Application
    Filed: July 10, 2014
    Publication date: February 12, 2015
    Inventors: John S. KOVACH, Francis JOHNSON
  • Publication number: 20150038518
    Abstract: Described herein are combinations of ACK inhibitors and HDAC inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 5, 2015
    Inventor: Sriram BALASUBRAMANIAN
  • Publication number: 20150038507
    Abstract: The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.
    Type: Application
    Filed: August 4, 2013
    Publication date: February 5, 2015
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Publication number: 20150033418
    Abstract: A first aspect of the invention is an agricultural composition comprising nanoparticles, an agrochemical active ingredient in the nanoparticles, and optionally (but in some embodiments preferably) a carrier for the nanoparticles. In some embodiments, the nanoparticles are viral particles or capsids, particularly plant viral particles or capsids. In some embodiments, the carrier comprises an inert or biodegradable carrier (e.g., a solid carrier) to which the nanoparticles are bound or in which the nanoparticles are suspended. In some embodiments, the carrier comprises inert or biodegradable polymer fibers.
    Type: Application
    Filed: April 16, 2013
    Publication date: January 29, 2015
    Inventors: Steven A. Lommel, Julie Willoughby, Richard Guenther
  • Publication number: 20150025086
    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: Application
    Filed: October 9, 2014
    Publication date: January 22, 2015
    Inventors: Marlene Michelle Dressman, John Joseph Feeney, Louis William Licamele, Mihael H. Polymeropoulos
  • Publication number: 20150024040
    Abstract: N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy}-benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, alone or in association with surgery, chemotherapy or hormone therapy treatment or radiotherapy, for use in the treatment of cancer, characterised in that it is administered for 4 consecutive days, that period being followed by 3 consecutive days without any administration of compound of formula (I), with the proviso that the chemotherapy is not FOLFOX.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 22, 2015
    Inventors: Ioana Kloos, Renata Robert, Anne Jacquet-Bescond, Stéphane Depil, Marylore Chenel, Sylvain Fouliard, Sriram Balasubramanian
  • Publication number: 20150017242
    Abstract: The present invention relates to multi component composition of dronedarone or pharmaceutically acceptable salts, esters, metabolites, prodrugs or enantiomers thereof and controlled release polymers. The use of multi component composition of Dronedarone would improve the bioavailability and the patient compliance with reduction in number of dosages to be taken per day.
    Type: Application
    Filed: February 14, 2013
    Publication date: January 15, 2015
    Inventors: Ashish Ashokrao Deshmukh, Hemant Bhalerao, Pravin Meghrajji Bhutada, Sajeev Chandran, Shirishkumar Kulkarni
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8927594
    Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: January 6, 2015
    Assignees: National Sun Yat-Sen University, National Museum of Marine Biology & Aquarium
    Inventors: Jyh-Horng Sheu, Wei-Hsien Wang, Zhi-Hong Wen, Bo-Wei Chen, Ping-Jyun Sung
  • Publication number: 20150005282
    Abstract: Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
    Type: Application
    Filed: December 27, 2012
    Publication date: January 1, 2015
    Inventors: Fanglong Yang, Qing Dong, Jihui Han, Chunfei Wang, Ling Zhang, Yang Wang
  • Patent number: 8921416
    Abstract: A dronedarone solid dispersion and preparation method thereof are disclosed. The solid dispersion is composed of active ingredient dronedarone or its pharmaceutically acceptable salt and a carrier material, wherein the carrier material is povidone, copovidone, hydroxypropyl cellulose, or a mixture thereof.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: December 30, 2014
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Piaoyang Sun, Kai Pan, Yuxia Wu
  • Publication number: 20140371307
    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: Application
    Filed: October 18, 2012
    Publication date: December 18, 2014
    Applicant: 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
  • Publication number: 20140357710
    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: Application
    Filed: January 25, 2013
    Publication date: December 4, 2014
    Inventors: Marlene Michelle Dressman, Louis William Licamele, Mihael H. Polymeropoulos