Plural Ring Oxygens In The Hetero Ring Patents (Class 514/452)
  • Patent number: 8986683
    Abstract: The invention discloses a kit which comprises a formulation containing artemisinin or the derivatives thereof, a formulation containing ribonuclease, and a specification.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: March 24, 2015
    Assignees: Shanghai Biomodel Organism Science & Technology Co., Ltd., Shanghai Research Center for Model Organisms
    Inventors: Qingcheng Wang, Ruling Shen, Jun Li, Jian Fei, Zhugang Wang
  • Publication number: 20150080348
    Abstract: Pharmaceutical compositions including combinations of protective agents selected from isosilybin B, methylsulfonylmethane (MSM), phosphatidylcholine, cysteine (Cys), seleno-cysteine (Se-Cys), ribose-cysteine (RibCys), N-acetylcysteine (NAC), N-acetylcysteine-amide (AD4), methionine (Met) and S-adenosylmethionine (SAM) for reducing and/or preventing drug-induced toxicity, such as acetaminophen-induced toxicity. The compositions may be formulated with or without acetaminophen, and accordingly may be used as safe formulations of acetaminophen with reduced risk of causing liver damage, or as an antidote for the treatment of acetaminophen overdose. Methods for treating acetaminophen intoxication.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Josef Mograbi, Yaron Ilan
  • Publication number: 20150079189
    Abstract: In one embodiment, the present application discloses synthetic LDL nanoparticles comprising mixtures of components selected from the group consisting of phospholipids, triglycerides, cholesterol ester and free cholesterol; optionally further comprising an agent selected from the group consisting of natural antioxidants, ubiquinol and vitamin E, and methods for preparing the synthetic nanoparticles. The disclosed synthetic LDL nanoparticles are capable of selectively delivering lipophilic drugs and prodrugs to cellular targets expressing LDL receptors after intra venous injection.
    Type: Application
    Filed: September 13, 2014
    Publication date: March 19, 2015
    Applicant: Arbor Therapeutics, LLC
    Inventors: James D. McChesney, Igor Nikoulin, Steve J. Bannister, Douglas L. Rodenburg
  • Publication number: 20150080460
    Abstract: There is disclosed a method for administration of a formulation of resiniferatoxin (RTX) to provide cardiac sympathetic afferent denervation when applied in an amount and concentration sufficient to chemically denervate vanilloid 1 receptor (TRPV1)-expressing CSAR (cardiac sympathetic afferent reflex) afferents. There is further disclosed a method for treating heart failure or hypertension and its related indications selected from the group consisting of increased sympatho-excitation, cardiac hypertrophy, increased left ventricular end diastolic pressure (LVEDP), lung edema, and combinations thereof, comprising administering an effective amount of RTX directly to a tissue site selected from the group consisting of epicardium, a T1-T4 dorsal root ganglion and intrathecally to the T1-T4 region of the spinal column.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 19, 2015
    Applicant: Board of Regents of the University of Nebraska
    Inventors: Irving H. Zucker, Hanjun Wang
  • Publication number: 20150064124
    Abstract: Personal care formulations containing alkyl ketal esters having the structure wherein a is 0 or an integer of 1 to 12; b is 0 or 1; R2 is a divalent C1-8 group optionally substituted with up to 5 hydroxyl groups; and R1 is C1-6 alkyl.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Applicant: SEGETIS, INC.
    Inventors: Dorie J. YONTZ, Lee Richard RIETH, Nicholas MORANTE, Irwin PALEFSKY
  • Patent number: 8969405
    Abstract: In one aspect, the invention relates to compounds having anticancer activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended to be used as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: March 3, 2015
    Assignee: St. Jude Children's Research Hospital
    Inventors: Thomas R. Webb, Chandraiah Lagisetti
  • Publication number: 20150051271
    Abstract: The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 19, 2015
    Inventors: Michael J. IADAROLA, Zoltan OLAH, Laszlo KARAI
  • 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: 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: 20150045420
    Abstract: The present invention generally relates to topical skin care compositions having at least one cyclic diester. More specifically, the present invention relates to novel topical skin care compositions having at least one cyclic diester of an alpha hydroxy acid, and at least one polar non-aqueous solvent.
    Type: Application
    Filed: August 8, 2014
    Publication date: February 12, 2015
    Inventors: WILLIAM R. CAHILL, JR., Robert Ray Burch, Jeffrey Jon Horsager, Jessica Linda Reisack, Jennifer Marie Altland
  • Publication number: 20150045421
    Abstract: The present invention generally relates to topical skin care compositions having at least one cyclic diester. More specifically, the present invention relates to novel topical skin care compositions having at least one cyclic diester of an alpha hydroxy acid, and at least one polar non-aqueous solvent.
    Type: Application
    Filed: August 8, 2014
    Publication date: February 12, 2015
    Inventors: William R Cahill, JR., Jessica Linda Reisack, Robert Ray Burch, Jennifer Marie Altland, Jeffrey Jon Horsager
  • Publication number: 20150045409
    Abstract: An amide compound represented by formula (I) has an excellent pest control effect. (In the formula, Y represents a 3-7 membered saturated heterocyclic ring which contains, as ring-forming components(s), one or more atoms or groups that are selected from the group consisting of an oxygen atom and —S(O)t—, the saturated heterocyclic ring may have one to three atoms or groups selected from group D and t represents 0 or the like; X represents a C1-C10 chain hydrocarbon group which may have one or more atoms or groups that are selected from group A, or the like; W represents —CR8— or the like; r represents 1 or the like; R1, R2, R3, R4, R5, R6, R7 and R8 may be the same or different and each represents a hydrogen atom or the like; and n represents 1 or the like.
    Type: Application
    Filed: February 5, 2013
    Publication date: February 12, 2015
    Inventors: Hideki Ihara, Tomotsugu Awano, Jun Ohshita, Noritada Matsuo
  • Patent number: 8952075
    Abstract: Bioactive liquid formulations are formed of combinations of absorbable, segmented aliphatic polyurethane compositions and liquid polyether for use as vehicles for the controlled release of at least one active agent for the conventional and unconventional treatment of different forms of cancer and the management of at least one type of bacterial, fungal, and viral infection.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: February 10, 2015
    Assignee: Poly-Med, Inc.
    Inventor: Shalaby W. Shalaby
  • Patent number: 8952053
    Abstract: The present invention relates to prodrugs of compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: February 10, 2015
    Assignee: Evolva SA
    Inventors: Peteris Alberts, Alexandra Santana Sorensen
  • Publication number: 20150031714
    Abstract: Embodiments of the invention include methods of preventing and/or reducing the risk or severity of an allergic reaction in an individual. In some embodiments, particular small molecules are employed for prevention and/or reduction in the risk or severity of anaphylaxis. In at least particular cases, the small molecules are inhibitors of STAT3. In some cases, the small molecule comprises N-(1?,2-dihydroxy-1,2?-binaphthalen-4?-yl)-4-methoxybenzenesulfonamide.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 29, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Josh Milner
  • Publication number: 20150031663
    Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
    Type: Application
    Filed: October 13, 2014
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
  • Publication number: 20150025130
    Abstract: The present disclosure discloses a sterol derivative, a preparation method therefor and a use thereof. The sterol derivative includes a sterol compound with Structural Formula (I) or a pharmaceutically acceptable salt thereof, or an extract containing the sterol compound, or a composition containing the sterol compound, wherein Structural Formula (I) is as follows: where R1 is —OH, ?O, H or C1-C3 alkyl; R2 is —OH, H or C1-C3 alkyl; R3 is —OH, ?O, H or C1-C3 alkyl; R4 is —OH, H or C1-C3 alkyl, and at least one of R1, R2, R3 and R4 is —OH. The compound with Structural Formula (I) can be used for preparing a drug having inhibitory effect on 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity and the prepared drug can effectively inhibit the HMG-CoA reductase activity or be used for preparing an anti-cancer drug.
    Type: Application
    Filed: February 4, 2013
    Publication date: January 22, 2015
    Inventors: Zhenwen Duan, Shuren Guo, Xuemei Li
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20150025129
    Abstract: Certain embodiments of the invention include compositions comprising a compound of Formula (I), and salts, isomers, and derivatives thereof. Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I), and salts, isomers, and derivatives thereof. Other embodiments of this invention include methods for treating disease (e.g., cancer) and methods for administering a compound of Formula (I), and salts, isomers, and derivatives thereof.
    Type: Application
    Filed: November 16, 2012
    Publication date: January 22, 2015
    Inventors: Gerald B. Hammond, Zhuang Jin, Paula J. Bates, Elsa Merit Reyes-Reyes, Abraham Vaisberg
  • Patent number: 8937085
    Abstract: The present invention relates to a pharmaceutical carrier composition and a pharmaceutical composition comprising said pharmaceutical carrier composition. The pharmaceutical composition comprises: (a) at least 20% (w/w) of the composition of a sugar or a sugar alcohol; (b) one or more pharmaceutically acceptable excipients; (c) one or more pharmaceutically active ingredients in their base form; and (d) water up to 100% (w/w). The present pharmaceutical composition is especially resistant against flocculation, clumping and/or precipitation at room temperature during prolonged time-periods such as one or more years.
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: January 20, 2015
    Assignee: Dafra Pharma N.V.
    Inventor: Frans Herwig Jansen
  • Patent number: 8937096
    Abstract: The present invention is a method for the treatment of mania and/or bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: January 20, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Virginia L. Smith-Swintosky, Allen B. Reitz
  • Publication number: 20150011617
    Abstract: A therapy for renal diseases characterized by alterations of the kidney function, such as Chronic Kidney Disease (CKD), acute and chronic renal impairment, and renal diseases that develop in diabetic patients or in patients who underwent an anticancer chemotherapic treatment with a platinum derivative. The invention is a combination of compounds selected from mono- or diamide of a C12-C20 monocarboxylic acid, saturated or monounsaturated, or a C4-C14 dicarboxylic acid, saturated or monounsaturated, with an aminoalkanol, and compounds selected from Silymarin, derivatives thereof or conjugates or complexes thereof, for use in the treatment of renal diseases.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Applicant: Epitech Group S.r.l.
    Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Salvatore Cuzzocrea
  • Publication number: 20150005256
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: April 16, 2014
    Publication date: January 1, 2015
    Inventors: Robert Eugene HORMANN, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Patent number: 8921413
    Abstract: The present invention discloses ?-diketones, ?-diketones or ?-hydroxyketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: December 30, 2014
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Patent number: 8916607
    Abstract: The present invention relates to the use of piperphentonamine or pharmaceutically acceptable salts thereof to prevent/treat encephalopathy in mammals, and the use of a combination of piperphentonamine or pharmaceutically acceptable salts thereof and other medicines in manufacture a medicine to prevent/treat encephalopathy in mammals. The mammals include human beings, and the encephalopathy includes cerebral injury related diseases or cerebrovascular diseases. The cerebrovascular diseases refer to cerebral ischemia, cerebral ischemia/reperfusion-induced injury or cerebral hemorrhage. The cerebral hemorrhage includes hypertensive cerebral hemorrhage, cerebral hemorrhage secondary to infarction, tumor cerebral hemorrhage or cerebral hemorrhage caused by arteritis. The cerebral ischemia means carotid system cerebral ischemia or vertebrobasilar cerebral ischemia.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: December 23, 2014
    Assignee: Guangzhou Municipal Zhongwei Biotechnology Limited Company
    Inventors: Huayin Wan, Rubing Li, Lijian Zhou, Tieqiu Liu, Yangshu Chen, Yonghe Li
  • Publication number: 20140363395
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.
    Type: Application
    Filed: July 24, 2014
    Publication date: December 11, 2014
    Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laquerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
  • Patent number: 8906955
    Abstract: A method for treating an aging-related disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor agonist.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: December 9, 2014
    Inventors: Shuguang Lin, Meng Zheng
  • Patent number: 8901165
    Abstract: Described are alkoxylated glycerol acetals according to Formulas (Ia) and (Ib) wherein R1 represents a linear or branched, saturated or unsaturated and optionally substituted hydrocarbyl residue comprising 6 to 22 carbon atoms and 0 or 1 to 3 double bonds, a benzyl or furfuryl radical, R2 is selected from hydrogen, an alkyl, alkenyl or hydroxyalkyl group having 6 to 22 carbon atoms or an acyl group having 6 to 22 carbon atoms and 0 or 1 to 3 double bonds, AO represents an ethylene oxide, a propylene oxide, a butylene oxide unit, or their mixtures, and n is an integer of about 1 to about 100.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: December 2, 2014
    Assignee: Cognis IP Management GmbH
    Inventors: Ingo Fleute-Schlachter, Sandra Mack, Peter Kempers, Ulrich Schörken, Eckhard Paetzold, Udo Kragl
  • Patent number: 8895584
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Publication number: 20140336174
    Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.
    Type: Application
    Filed: April 17, 2014
    Publication date: November 13, 2014
    Applicant: Genzyme Corporation
    Inventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
  • Publication number: 20140303241
    Abstract: The present invention provides a series of derivatives of stilbenoid which are useful as new inhibitory agents against head and neck squamous cell carcinoma (HNSCC) and hepatoma.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 9, 2014
    Applicant: AnnCare Bio-Tech Center Inc.
    Inventors: Sheng-Chu Kuo, Jai-Sing Yang, Min-Tsang Hsieh, Tian-Shung Wu, Kuo-Hsiung Lee, Huei-Wen Chen, Li-Jiau Huang, Hsin-Yi Hung, Tzong-Der Way, Ling-Chu Chang, Hui-Yi Lin, Yung-Yi Cheng, Chin-Yu Liu
  • Patent number: 8853263
    Abstract: The present invention is directed to co-therapy for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, co-therapy with a therapeutically effective amount of a benzo-fused heterocycle sulfamide derivative and a therapeutically effective amount of one or more anticonvulsant and/or anti-epileptic agents.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: October 7, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Virginia L. Smith-Swintosky, David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
  • Publication number: 20140296223
    Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Publication number: 20140296183
    Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Masatoshi KIUCHI, Kaoru MARUKAWA, Nobutaka KOBAYASHI
  • Publication number: 20140296270
    Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.
    Type: Application
    Filed: April 15, 2014
    Publication date: October 2, 2014
    Applicant: Baylor College of Medicine
    Inventors: David J. Tweardy, Xuejun Xu, Moses M. Kasembeli
  • Publication number: 20140288110
    Abstract: 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections.
    Type: Application
    Filed: March 24, 2014
    Publication date: September 25, 2014
    Applicant: EVOLVA SA
    Inventors: Karsten KRISTIANSEN, Prathama S. MAINKAR, Jean-Philippe MEYER, Alexandra Santana SORENSEN
  • Patent number: 8841290
    Abstract: Disclosed is a tetrahydronapthalene compound having Formula I the variables of which are as described herein, methods of preparing same and their use.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: September 23, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Publication number: 20140275037
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: December 19, 2013
    Publication date: September 18, 2014
    Applicant: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
  • Publication number: 20140275172
    Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • Publication number: 20140271955
    Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: The Scripps Research Institute, The California Institute for Biomedical Research
    Inventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
  • Publication number: 20140275134
    Abstract: The disclosed subject matter provides certain N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or development of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: October 16, 2012
    Publication date: September 18, 2014
    Inventors: John P. Toscano, Daryl A. Guthrie
  • Patent number: 8835376
    Abstract: A process for making particles for delivery of drug nanoparticles is disclosed herein. The process comprises the steps of (a) forming a suspension of drug nanoparticles by mixing a precipitant solution with an anti-solvent solution under micro-mixing environment, where the formed nanoparticles have a narrow particle size distribution; (b) providing an excipient to at least one of the precipitant solution, the anti-solvent solution and the suspension of drug nanoparticles, the excipient being selected to maintain said drug nanoparticles in a dispersed state when in liquid form; and (c) drying the suspension of drug nanoparticles containing the excipient therein to remove solvent therefrom, wherein removal of the solvent causes the excipient to solidify and thereby form micro-sized matrix particles, each micro-sized particle being comprised of drug nanoparticles dispersed in a solid matrix of the excipient.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: September 16, 2014
    Assignee: Nanomaterials Technology Pte Ltd
    Inventors: Zhigang Shen, Jimmy Sung Lai Yun, Jun Hu, Nital Arvind Jugade, Jiyao Zhang, Wenhao Chen, Zhe Wang, Lingyan Gao, William Glover, Jian Feng Chen
  • Publication number: 20140255432
    Abstract: Disclosed herein are treatment methods, vaccination methods, compositions, co-therapeutic methods, combination therapeutic compositions and kits comprising silvestrol and silvestrol analogs alone or in combination with therapeutic and preventative therapies. Disclosed herein are also methods, compositions and kits that can be used to treat cancer, viral infections, to modulate the immune system or as preventative therapies.
    Type: Application
    Filed: July 27, 2012
    Publication date: September 11, 2014
    Applicant: OHIO STATE INNOVATION FOUNDATION
    Inventors: Robert A. Baiocchi, John Thomas Patton, JR., David M. Lucas, Douglas Kinghorn, Michael Grever
  • Patent number: 8828414
    Abstract: Provided are biocidal compositions comprising 2,6-dimethyl-m-dioxane-4-ol acetate and a non-formaldehyde releasing biocidal compound selected from the group consisting of: a brominated nitroalkanol, a 2-halo-2-(halomethyl)glutaronitrile, and 2-phenoxyethanol. The compositions are useful for controlling microorganisms in aqueous or water containing systems.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: September 9, 2014
    Assignee: Dow Global Technologies LLC
    Inventors: Kathy J. Ji, Donald J. Love, Jon B. Raymond
  • Publication number: 20140249199
    Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 4, 2014
    Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITY
    Inventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
  • Publication number: 20140249213
    Abstract: The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 4, 2014
    Applicant: ARBOR THERAPEUTICS, LLC
    Inventors: James D. McChesney, John T. Henri, Sylesh Kumar Venkataraman, Mahesh Kumar Gundluru
  • Publication number: 20140249155
    Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.
    Type: Application
    Filed: March 23, 2014
    Publication date: September 4, 2014
    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
  • Publication number: 20140243404
    Abstract: This disclosure is related to halonium compounds useful for cyclization of polyenes, alkenoic acids, and alkenyl alkyl ethers, and halogenation of aromatic compounds. The synthesis of such halonium compounds, compounds made using such halonium compounds, and synthesis of natural compounds, including decalins, using the halonium compounds is also disclosed.
    Type: Application
    Filed: September 13, 2011
    Publication date: August 28, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Scott Alan Snyder, Daniel S. Treitler, Alexandria P. Brucks, Andreas Gollner, Maria I. Chiriac, Nathan E. Wright, Jason J. Pflueger, Steven P. Breazzano
  • Publication number: 20140243349
    Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Application
    Filed: February 21, 2014
    Publication date: August 28, 2014
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Publication number: 20140243378
    Abstract: Disclosed are methods of treating a muscle disease and improving normal muscle function by administering a therapeutically effective amount of an isoprenoid antibiotic. Also disclosed are methods of upregulating hnRNP L and hnRNP L targets by administering a therapeutically effective amount of an isoprenoid antibiotic. Methods of screening compounds for use in treating muscle disease and improving muscle function are also described.
    Type: Application
    Filed: October 19, 2012
    Publication date: August 28, 2014
    Applicants: Tufts Medical Center, Inc., Children's Medical Center Corporation
    Inventors: Isabelle Draper, Louis M. Kunkel, Matthew S. Alexander, Alan S. Kopin