Plural Ring Oxygens In The Hetero Ring Patents (Class 514/452)
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Patent number: 8986683Abstract: The invention discloses a kit which comprises a formulation containing artemisinin or the derivatives thereof, a formulation containing ribonuclease, and a specification.Type: GrantFiled: September 10, 2012Date of Patent: March 24, 2015Assignees: Shanghai Biomodel Organism Science & Technology Co., Ltd., Shanghai Research Center for Model OrganismsInventors: Qingcheng Wang, Ruling Shen, Jun Li, Jian Fei, Zhugang Wang
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Publication number: 20150080348Abstract: 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: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Josef Mograbi, Yaron Ilan
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Publication number: 20150079189Abstract: 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: ApplicationFiled: September 13, 2014Publication date: March 19, 2015Applicant: Arbor Therapeutics, LLCInventors: James D. McChesney, Igor Nikoulin, Steve J. Bannister, Douglas L. Rodenburg
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Publication number: 20150080460Abstract: 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: ApplicationFiled: September 11, 2014Publication date: March 19, 2015Applicant: Board of Regents of the University of NebraskaInventors: Irving H. Zucker, Hanjun Wang
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Publication number: 20150064124Abstract: 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: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Applicant: SEGETIS, INC.Inventors: Dorie J. YONTZ, Lee Richard RIETH, Nicholas MORANTE, Irwin PALEFSKY
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Patent number: 8969405Abstract: 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: GrantFiled: June 22, 2009Date of Patent: March 3, 2015Assignee: St. Jude Children's Research HospitalInventors: Thomas R. Webb, Chandraiah Lagisetti
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Publication number: 20150051271Abstract: 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: ApplicationFiled: October 24, 2014Publication date: February 19, 2015Inventors: Michael J. IADAROLA, Zoltan OLAH, Laszlo KARAI
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Publication number: 20150051270Abstract: 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 substituenType: ApplicationFiled: February 15, 2013Publication date: February 19, 2015Inventors: Shailesh Mistry, Etíenne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
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Publication number: 20150051257Abstract: 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 andType: ApplicationFiled: March 20, 2013Publication date: February 19, 2015Applicant: ADAMED SP. ZO.OInventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
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Publication number: 20150045420Abstract: 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: ApplicationFiled: August 8, 2014Publication date: February 12, 2015Inventors: WILLIAM R. CAHILL, JR., Robert Ray Burch, Jeffrey Jon Horsager, Jessica Linda Reisack, Jennifer Marie Altland
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Publication number: 20150045421Abstract: 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: ApplicationFiled: August 8, 2014Publication date: February 12, 2015Inventors: William R Cahill, JR., Jessica Linda Reisack, Robert Ray Burch, Jennifer Marie Altland, Jeffrey Jon Horsager
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Publication number: 20150045409Abstract: 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: ApplicationFiled: February 5, 2013Publication date: February 12, 2015Inventors: Hideki Ihara, Tomotsugu Awano, Jun Ohshita, Noritada Matsuo
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Bioactive polymeric liquid formulations of absorbable, segmented aliphatic polyurethane compositions
Patent number: 8952075Abstract: 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: GrantFiled: May 22, 2009Date of Patent: February 10, 2015Assignee: Poly-Med, Inc.Inventor: Shalaby W. Shalaby -
Patent number: 8952053Abstract: 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: GrantFiled: March 6, 2013Date of Patent: February 10, 2015Assignee: Evolva SAInventors: Peteris Alberts, Alexandra Santana Sorensen
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Publication number: 20150031714Abstract: 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: ApplicationFiled: July 18, 2014Publication date: January 29, 2015Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Josh Milner
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Publication number: 20150031663Abstract: 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: ApplicationFiled: October 13, 2014Publication date: January 29, 2015Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
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Publication number: 20150025130Abstract: 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: ApplicationFiled: February 4, 2013Publication date: January 22, 2015Inventors: Zhenwen Duan, Shuren Guo, Xuemei Li
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Publication number: 20150024032Abstract: 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: ApplicationFiled: July 18, 2014Publication date: January 22, 2015Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
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Publication number: 20150025129Abstract: 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: ApplicationFiled: November 16, 2012Publication date: January 22, 2015Inventors: Gerald B. Hammond, Zhuang Jin, Paula J. Bates, Elsa Merit Reyes-Reyes, Abraham Vaisberg
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Patent number: 8937085Abstract: 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: GrantFiled: February 13, 2008Date of Patent: January 20, 2015Assignee: Dafra Pharma N.V.Inventor: Frans Herwig Jansen
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Patent number: 8937096Abstract: 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: GrantFiled: December 18, 2006Date of Patent: January 20, 2015Assignee: Janssen Pharmaceutica NVInventors: Virginia L. Smith-Swintosky, Allen B. Reitz
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Publication number: 20150011617Abstract: 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: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicant: Epitech Group S.r.l.Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Salvatore Cuzzocrea
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Publication number: 20150005256Abstract: 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: ApplicationFiled: April 16, 2014Publication date: January 1, 2015Inventors: Robert Eugene HORMANN, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
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Patent number: 8921413Abstract: 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: GrantFiled: November 21, 2013Date of Patent: December 30, 2014Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Patent number: 8916607Abstract: 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: GrantFiled: October 20, 2009Date of Patent: December 23, 2014Assignee: Guangzhou Municipal Zhongwei Biotechnology Limited CompanyInventors: Huayin Wan, Rubing Li, Lijian Zhou, Tieqiu Liu, Yangshu Chen, Yonghe Li
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Publication number: 20140363395Abstract: 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: ApplicationFiled: July 24, 2014Publication date: December 11, 2014Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laquerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Patent number: 8906955Abstract: 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: GrantFiled: January 30, 2013Date of Patent: December 9, 2014Inventors: Shuguang Lin, Meng Zheng
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Patent number: 8901165Abstract: 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: GrantFiled: September 23, 2010Date of Patent: December 2, 2014Assignee: Cognis IP Management GmbHInventors: Ingo Fleute-Schlachter, Sandra Mack, Peter Kempers, Ulrich Schörken, Eckhard Paetzold, Udo Kragl
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Patent number: 8895584Abstract: 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: GrantFiled: May 12, 2014Date of Patent: November 25, 2014Assignee: Janssen Pharmaceutica NVInventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Publication number: 20140336174Abstract: 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: ApplicationFiled: April 17, 2014Publication date: November 13, 2014Applicant: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
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Publication number: 20140303241Abstract: 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: ApplicationFiled: March 28, 2014Publication date: October 9, 2014Applicant: 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
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Patent number: 8853263Abstract: 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: GrantFiled: May 18, 2007Date of Patent: October 7, 2014Assignee: Janssen Pharmaceutica NVInventors: Virginia L. Smith-Swintosky, David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
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Publication number: 20140296223Abstract: 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: ApplicationFiled: August 31, 2012Publication date: October 2, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
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Publication number: 20140296183Abstract: 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: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Masatoshi KIUCHI, Kaoru MARUKAWA, Nobutaka KOBAYASHI
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Publication number: 20140296270Abstract: 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: ApplicationFiled: April 15, 2014Publication date: October 2, 2014Applicant: Baylor College of MedicineInventors: David J. Tweardy, Xuejun Xu, Moses M. Kasembeli
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Publication number: 20140288110Abstract: 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: ApplicationFiled: March 24, 2014Publication date: September 25, 2014Applicant: EVOLVA SAInventors: Karsten KRISTIANSEN, Prathama S. MAINKAR, Jean-Philippe MEYER, Alexandra Santana SORENSEN
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Patent number: 8841290Abstract: Disclosed is a tetrahydronapthalene compound having Formula I the variables of which are as described herein, methods of preparing same and their use.Type: GrantFiled: February 12, 2010Date of Patent: September 23, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
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Publication number: 20140275037Abstract: 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: ApplicationFiled: December 19, 2013Publication date: September 18, 2014Applicant: Siga Technologies, Inc.Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
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Publication number: 20140275172Abstract: 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: ApplicationFiled: March 7, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Zhihua Sui, Nalin Subasinghe
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Publication number: 20140271955Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicants: The Scripps Research Institute, The California Institute for Biomedical ResearchInventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
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Publication number: 20140275134Abstract: 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: ApplicationFiled: October 16, 2012Publication date: September 18, 2014Inventors: John P. Toscano, Daryl A. Guthrie
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Patent number: 8835376Abstract: 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: GrantFiled: September 24, 2009Date of Patent: September 16, 2014Assignee: Nanomaterials Technology Pte LtdInventors: Zhigang Shen, Jimmy Sung Lai Yun, Jun Hu, Nital Arvind Jugade, Jiyao Zhang, Wenhao Chen, Zhe Wang, Lingyan Gao, William Glover, Jian Feng Chen
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Publication number: 20140255432Abstract: 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: ApplicationFiled: July 27, 2012Publication date: September 11, 2014Applicant: OHIO STATE INNOVATION FOUNDATIONInventors: Robert A. Baiocchi, John Thomas Patton, JR., David M. Lucas, Douglas Kinghorn, Michael Grever
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Patent number: 8828414Abstract: 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: GrantFiled: March 26, 2009Date of Patent: September 9, 2014Assignee: Dow Global Technologies LLCInventors: Kathy J. Ji, Donald J. Love, Jon B. Raymond
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Publication number: 20140249199Abstract: 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: ApplicationFiled: July 19, 2012Publication date: September 4, 2014Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITYInventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
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Publication number: 20140249213Abstract: 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: ApplicationFiled: March 17, 2014Publication date: September 4, 2014Applicant: ARBOR THERAPEUTICS, LLCInventors: James D. McChesney, John T. Henri, Sylesh Kumar Venkataraman, Mahesh Kumar Gundluru
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Publication number: 20140249155Abstract: 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: ApplicationFiled: March 23, 2014Publication date: September 4, 2014Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20140243404Abstract: 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: ApplicationFiled: September 13, 2011Publication date: August 28, 2014Applicant: The Trustees of Columbia University in the City of New YorkInventors: Scott Alan Snyder, Daniel S. Treitler, Alexandria P. Brucks, Andreas Gollner, Maria I. Chiriac, Nathan E. Wright, Jason J. Pflueger, Steven P. Breazzano
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Publication number: 20140243349Abstract: 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: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Publication number: 20140243378Abstract: 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: ApplicationFiled: October 19, 2012Publication date: August 28, 2014Applicants: Tufts Medical Center, Inc., Children's Medical Center CorporationInventors: Isabelle Draper, Louis M. Kunkel, Matthew S. Alexander, Alan S. Kopin