Patents Issued in May 12, 2016
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Publication number: 20160130260Abstract: Tert-butyl sulphoxide method for producing festinavir is set forth.Type: ApplicationFiled: June 11, 2014Publication date: May 12, 2016Inventors: Adrian Ortiz, Tamas Benkovics, Martin D. Eastgate
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Publication number: 20160130261Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.Type: ApplicationFiled: July 9, 2014Publication date: May 12, 2016Inventors: Joelle Lorraine BURGESS, Steven David KNIGHT
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Publication number: 20160130262Abstract: The present invention relates to novel N-substituted azetidine derivatives<of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, >to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancerType: ApplicationFiled: December 16, 2011Publication date: May 12, 2016Inventors: Fredericus Antonius Dijcks, Scott James Lusher, Herman Thijs Stock, Arthur Oubrie, Gerrit Herman Veeneman
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Publication number: 20160130263Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 11, 2014Publication date: May 12, 2016Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates
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Publication number: 20160130264Abstract: The present invention relates to methods and strategies for large-scale synthesis of compounds having the chemical structure: The R substituents are H, methyl, isopropyl, benzyl, cyclohexyl, cyclopropylmethyl, methoxy, tert-butyloxycarbonyl, methanesulfonyl, p-toluenesulfonyl, quinolinesulfonyl, or thiophenesulfonyl groups. The method comprises condensing prothionamide with a halo nitroacetophenone to form a nitrophenyl substituted thiazole, reducing the nitro group to form an amine and derivatizing the amine to produce the compound.Type: ApplicationFiled: November 6, 2015Publication date: May 12, 2016Inventor: William R. Cantrell, JR.
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Publication number: 20160130265Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: December 29, 2015Publication date: May 12, 2016Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
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Publication number: 20160130266Abstract: The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an ?-oxoacyl amino-caprolactam that is represented by formula (I) (in formula (I), X represents N or CH, Y represents O or CH2, and Z represents S or CH2); and a bone resorption inhibitor containing the ?-oxoacyl amino-caprolactam.Type: ApplicationFiled: June 13, 2014Publication date: May 12, 2016Inventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii, Mizuho Ishikawa, Daisuke Morita
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Publication number: 20160130267Abstract: The present invention is directed to novel inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.Type: ApplicationFiled: November 5, 2015Publication date: May 12, 2016Applicant: H. LUNDBECK A/SInventors: Karsten Juhl, Lena Tagmose, Mauro Marigo
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Publication number: 20160130268Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: May 7, 2014Publication date: May 12, 2016Inventors: Kenneth Albert BRAMELD, Erik VERNER
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Publication number: 20160130269Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.Type: ApplicationFiled: January 5, 2016Publication date: May 12, 2016Applicant: MERCK PATENT GmbHInventors: Dieter DORSCH, Christian SIRRENBERG, Thomas J.J. MUELLER, Eugen MERKUL, Gnuni Amatunu KARAPETYAN
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Publication number: 20160130270Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: ApplicationFiled: January 19, 2016Publication date: May 12, 2016Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Publication number: 20160130271Abstract: A redox-active triangular prism is provided. The redox-active triangular prism includes a plurality of pure enantiomers selected from a group consisting of (?)-NDI-? and (+)-NDI-?. Methods for their preparation as solvent-templated supramolecular structures and a characterization of their redox-active behavior are provided.Type: ApplicationFiled: September 3, 2015Publication date: May 12, 2016Inventors: James Fraser Stoddart, Severin T. Schneebeli, Marco Frasconi, Zhichang Liu
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Publication number: 20160130272Abstract: Crystalline form, Form N-2, of N,Ndicyclopropyl-4-(1,5-dimethyl-1Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising Form N-2 of Compound I as well as a method of using the Form N-2 of Compound I in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.Type: ApplicationFiled: May 28, 2014Publication date: May 12, 2016Applicant: BRISTOL-MYERS SQUIBB COMPANYInventor: Shella Tameze
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Publication number: 20160130273Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.Type: ApplicationFiled: September 15, 2015Publication date: May 12, 2016Applicant: MERCK SHARP & DOHME CORP.Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyoshi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch, Teresa Andreani
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Publication number: 20160130274Abstract: The present invention relates to novel 6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazin-6-yl derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia of the Alzheimer's type, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.Type: ApplicationFiled: June 12, 2014Publication date: May 12, 2016Inventors: Daniel Oehlrich, Henricus Jacobus, Maria Gijsen
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Publication number: 20160130275Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: ApplicationFiled: January 14, 2016Publication date: May 12, 2016Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
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Publication number: 20160130276Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.Type: ApplicationFiled: December 4, 2015Publication date: May 12, 2016Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
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Publication number: 20160130277Abstract: Long-chain alkyl cyclic acetals made from sugars are obtainable by a method that comprises the steps consisting of: dehydrating a hexitol in a monoanhydrohexitol substrate; reacting the monoanhydrohexitol substrate obtained with an alkyl aldehyde reagent containing 5 to 18 carbon atoms, by means of an acetalization reaction with a substrate/reagent ratio of between 5:1 and 1:1, or with a derivative of an alkyl aldehyde reagent containing 5 to 18 carbon atoms, by means of a transacetalization reaction with a substrate/reagent ratio of between 1:1 and 1:3, in the presence of acid catalyst and in an environment that is free of solvent or that consists of non-aqueous polar solvent; collecting the long-chain alkyl acetal of hexitan from the mixture obtained.Type: ApplicationFiled: June 13, 2014Publication date: May 12, 2016Inventors: Charlotte GOZLAN, Nicolas DUGUET, Marc LEMAIRE, Yves QUENEAU, Andreas REDL
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Publication number: 20160130278Abstract: The present invention provides novel compounds of formula [IA] or pharmaceutically acceptable salts thereof: which are useful in the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.Type: ApplicationFiled: June 9, 2014Publication date: May 12, 2016Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Yousuke YAMADA, Hiroshi OHTA, Tomoko TAMITA, Kumi ABE, Shuji YAMAMOTO, Shin-ichi SHIROKAWA, Masahito ABE, Yohei MATSUDA, Yuko ARAKI
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Publication number: 20160130279Abstract: The present invention provides antibodies and methods for preparing antibodies to metabolites in the serotonin, tryptophan, kynurenine pathways. The prepared antibodies have low cross-reactivity to related metabolites, and are useful reagents for specific and sensitive immunoassays The present invention also provides stable derivatives of various metabolites and short chain fatty acids. The derivative can be conjugated to a biomolecule such as a carrier protein and combined with an adjuvant to stimulate an immune response. The derivatives can also be conjugated to other biomolecules.Type: ApplicationFiled: November 11, 2015Publication date: May 12, 2016Applicant: NESTEC S.A.Inventors: FABIYOLA SELVARAJ, Fred Princen, Sharat Singh
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Publication number: 20160130280Abstract: The present invention discloses a process for preparing a chemical compound comprising reacting a nucleophile with an alkyl fluoroalkyl sulfonate in the presence of a base of formula NR1R2R3, wherein R1 and R2 are independently 2-methyipropyl or isopropyl and R3 is —CH(R4)(R5), wherein R4 and R5 are identical or different alkyls that are optionally connected to form a ring. The invention also relates to a process for preparing an alkyl fluoroalkyl sulfonate. The invention further relates to a use of the base in a chemical reaction comprising an alkyl fluoroalkyl sulfonate. The process and uses are suitable for preparing chemical compounds, reactants or intermediates thereof, and in particular for preparing API or reactants, like for example everolimus or reactants for its preparation.Type: ApplicationFiled: June 18, 2014Publication date: May 12, 2016Applicant: Novartis AGInventors: MURAT Acemoglu, Gemma Veitch
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Publication number: 20160130281Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: ApplicationFiled: October 13, 2015Publication date: May 12, 2016Inventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Hauck, Fei Zhou
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Publication number: 20160130282Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: ApplicationFiled: November 6, 2015Publication date: May 12, 2016Inventors: Marlon D. Cowart, Huaqing Liu, Robert Altenbach
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Publication number: 20160130283Abstract: The invention relates to the production of zinc trisodium pentetic acid (Zn-DTPA) and to new crystalline forms of said salt.Type: ApplicationFiled: May 23, 2014Publication date: May 12, 2016Inventor: Christian Schickaneder
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Publication number: 20160130284Abstract: The present invention discloses a new modality of photodynamic therapy (PDT) through the design of the present invention's truly dual-functional—PDT and imaging—gadolinium complex (Gd-N) with a molecular formula of: which can target cancer, cells specifically. The present invention provides a PDT drug that can specifically localize on the anionic cell membrane of cancer cells in which its laser-excited photoemission signal can be monitored without triggering the phototoxic generation of reactive oxygen species—singlet oxygen—prior to due excitation. The present invention also provides the use of Gd-N as a tumor selective PDT photosensitizer modality.Type: ApplicationFiled: November 5, 2015Publication date: May 12, 2016Inventors: Ka-Leung WONG, Wai-Kwok WONG, Rongfeng LAN, Tao ZHANG
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Publication number: 20160130285Abstract: The invention relates to a method for producing alkali metal salts having monohydrido-tricyanoborate anions from alkali metal monofluorotricyanoborates, and to a method for producing alkali metal salts having dihydrido-dicyanoborate anions from alkali metal difluorodicyanoborates.Type: ApplicationFiled: June 6, 2014Publication date: May 12, 2016Applicant: MERCK PATENT GMBHInventors: Nikolai (Mykola) IGNATYEV, Jan Arke Peter SPRENGER, Johannes LANDMANN, Maik FINZE
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Publication number: 20160130286Abstract: The invention relates to a method for producing alkali metal salts having monofluoro-tricyanoborate anions from alkali metal tetrafluoroborates.Type: ApplicationFiled: June 6, 2014Publication date: May 12, 2016Applicant: MERCK PATENT GMBHInventors: Nikolai (Mykola) IGNATYEV, Jan Arke Peter SPENGER, Johannes LANDMANN, Maik FINZE
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Publication number: 20160130287Abstract: The present invention provides multi-thiol mercaptoalkoxysilane compositions and methods of making multi-thiol mercaptoalkoxysilane compositions having the formula: wherein the R3 group, and the R4 group are independently an alkoxy, a halogen, an alkyl, an aryl, a heteroaryl, a heterocycle or derivatives thereof and n is an integer between 1 and 30.Type: ApplicationFiled: December 17, 2015Publication date: May 12, 2016Inventors: David Y. Son, Abby R. Jennings
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Publication number: 20160130288Abstract: The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.Type: ApplicationFiled: May 9, 2014Publication date: May 12, 2016Applicant: MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIEInventors: Thomas Kapsner, Axel Dalhoff, Thomas Gramatte
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Publication number: 20160130289Abstract: A method of manufacturing cyclophosphazenes PFPE derivatives to be used in the lubrication of magnetic recording media is herein provided. The method comprises: a) a (per)fluoropolyether (PFPE) polyol [PFPE (Ppol)] comprising a fluoropolyoxyalkylene chain (Rf) having two chain ends, each chain end comprising at least one hydroxy group, and b) the corresponding alkoxide of perfluoropolyether (Ppol) [PFPE (Palk)] wherein the equivalent concentration of PFPE (Palk) in PFPE (Ppol) is lower than 30%, preferably ranging from 5% to 15%; 2) contacting mixture (M) with a perhalocyclophosphazene (CPhalo) to provide a mixture (M1) containing an equivalent ratio of PFPE (Palk)/(CPhalo) of at least 1; 3) allowing mixture (M1) to react until complete disappearance of P—Cl groups to provide a mixture (M2); 4) submitting mixture (M2) to hydrolysis to provide a mixture (M3); 5) optionally removing (Ppol) from mixture (M3) to provide a mixture (M4). A method of purifying mixture (M4) is also herein provided.Type: ApplicationFiled: June 3, 2014Publication date: May 12, 2016Applicant: SOLVAY SPECIALTY POLYMERS ITALY S.P.A.Inventors: Roberto VALSECCHI, Rosaldo PICOZZI, Pier Antonio GUARDA
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Publication number: 20160130290Abstract: The invention relates to a process for producing preparations including one or more mononuclear platinum complex compounds of formula (X), one or more compounds comprising carbon atoms, hydrogen atoms and at least two oxygen atoms as compound(s) from compound class II, and one or more olefinically unsaturated compound(s) selected from olefin1 and olefin2 as compound(s) from compound class III, by contacting at least one compound from each of compound classes II and III with one or more dinuclear platinum (II) compound(s) as compound(s) from compound class I.Type: ApplicationFiled: November 12, 2015Publication date: May 12, 2016Applicant: Evonik Degussa GmbHInventors: Wilfried Knott, Klaus-Dieter Klein, Horst Dudzik
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Publication number: 20160130291Abstract: Compounds comprising a Pt(II) metal center and S-containing ligands in accordance to Formula I as anticancer agents. Methods of treating cancer comprising administering the compounds are also provided.Type: ApplicationFiled: November 12, 2014Publication date: May 12, 2016Applicant: King Fahd University of Petroleum and MineralsInventors: Ahmed Zainelabdeen Abdalla Mustafa, Muhammad Monim-Ul-Mehboob, Muhammad Altaf, Anvarhusein Abdulkadir Isab
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Publication number: 20160130292Abstract: A fructoside-containing product is manufactured from a glucose-rich feedstock, in a process where glucose to fructose is isomerized by contacting the glucose-rich feedstock with a basic isomerization catalyst in an alcoholic medium at a temperature of at least 75° C., to yield a fructose-containing product; and where at least part of the fructose-containing product obtained therefrom is reacted with an alcohol in the presence of an acid catalyst to yield a fructoside-containing product.Type: ApplicationFiled: June 6, 2014Publication date: May 12, 2016Inventors: Benjamin McKay, Ana Sofia Vagueiro De Sousa Dias, Sarwat Iqbal, Gerardus Johannes Maria Gruter, Robert-Jan Van Putten
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Publication number: 20160130293Abstract: The present invention provides a novel compound isolated from a plant of the genus Quamoclit and a method for preparing a novel compound isolated from a plant of the genus Quamoclit through chemical synthesis, and relates to a novel compound and a composition containing the novel compound as an active ingredient for preventing or treating diabetes and diabetic complications. The compound derived from a plant of the genus Quamoclit and the composition containing the compound as an active ingredient according to the present invention have an excellent effect of promoting insulin secretion, thereby exhibiting efficacies in preventing or treating diabetes and the resulting various complications.Type: ApplicationFiled: May 26, 2014Publication date: May 12, 2016Applicant: KOREA RESEARCH INSTITUTE BIOSCIENCEInventors: Bong Hyun CHUNG, Ui Jin LEE, So Yeon YI
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Publication number: 20160130294Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R4, R5a, R5b, Rb5, Rb6 and D are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.Type: ApplicationFiled: November 5, 2015Publication date: May 12, 2016Inventors: Jay R. Luly, Bin Wang, Guoqiang Wang, Yat Sun Or
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Publication number: 20160130295Abstract: A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures.Type: ApplicationFiled: November 13, 2015Publication date: May 12, 2016Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Nagichettiar Satyamurthy, Jorge R. Barrio, Bernard Amarasekera, R. Michael Van Dam, Sebastian Olma, Dirk Williams, Mark Eddings, Clifton Kwang-Fu Shen
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Publication number: 20160130296Abstract: Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.Type: ApplicationFiled: December 22, 2015Publication date: May 12, 2016Inventors: Pasit Phiasivongsa, Sanjeev Redkar
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Publication number: 20160130297Abstract: The present invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4, R5, R6, R7, R8 and m are as defined herein, pharmaceutical compositions comprising these compounds and methods of use of these compounds for treating a TGR5 mediated disease or condition.Type: ApplicationFiled: November 5, 2015Publication date: May 12, 2016Inventors: Yat Sun Or, Guoqiang Wang, Ruichao Shen, Xuechao Xing
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Publication number: 20160130298Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: January 5, 2016Publication date: May 12, 2016Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
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Publication number: 20160130299Abstract: Tubulysin analogs of the formula (I) where R1, R2 R3, R4, R5, R6, R7, and Y are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.Type: ApplicationFiled: August 24, 2015Publication date: May 12, 2016Inventors: Heidi L. PEREZ, Donna WEI, Robert M. BORZILLERI, Sanjeev GANGWAR, Gretchen M. SCHROEDER, Heng CHENG, Robert J. SCHMIDT
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Publication number: 20160130300Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.Type: ApplicationFiled: January 15, 2016Publication date: May 12, 2016Inventors: Kyla Bjornson, Eda Canales, Jeromy J. Cottell, Kapil K. Karki, Ashley A. Katana, Darryl Kato, Tetsuya Kobayashi, John O. Link, Ruben Martinez, Barton W. Phillips, Hyung-jung Pyun, Michael Sangi, Adam J. Schrier, Dustin Siegel, James G. Taylor, Chinh V. Tran, Teresa A. Trejo Martin, Randall W. Vivian, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20160130301Abstract: This present invention provides a novel peptide for inhibiting growth of microorganisms, a pharmaceutical composition, an antimicrobial composition comprising such novel peptide, and a method for inhibiting growth of microorganisms. The novel peptide for inhibiting growth of microorganisms has amino acid sequence: KX1LRX2X3X4RRWX5, wherein X1, X2, and X5 are selected from the group of W and R, respectively; X3 is selected from the group of V and P; and X4 is selected from the group of R and methylated W. The method for inhibiting growth of microorganisms disclosed in this present invention comprises administering the novel peptide, the pharmaceutical composition, or the antimicrobial composition.Type: ApplicationFiled: November 6, 2015Publication date: May 12, 2016Inventor: Feng-Di Lung
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Publication number: 20160130302Abstract: A peptide composition is provided which specifically inhibits the ability of ?-protein kinase C (?PKC) to phosphorylate pyruvate dehydrogenase kinase (PDK) under ischemic conditions. The peptide composition is useful for treating or reducing tissue damage resulting from ischemia and/or reperfusion.Type: ApplicationFiled: November 17, 2015Publication date: May 12, 2016Inventors: Daria Mochly-Rosen, Nir Qvit, Marie-Helene Disatnik Dziesietnik
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Publication number: 20160130303Abstract: Novel peptide inhibitors of GSK-3, compositions containing same and uses thereof are disclosed. The novel peptide inhibitors are substrate-competitive inhibitors and have an amino acid sequence designed so as to bind to a defined binding site subunit in GSK-3. Also disclosed are GSK-3 substrate competitive inhibitors which bind to the defined binding site subunit in the enzyme. Also disclosed are mutants of GSK-3 and uses thereof for identifying a putative GSK-3 substrate competitive inhibitor.Type: ApplicationFiled: January 12, 2016Publication date: May 12, 2016Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Hagit Eldar-Finkelman, Avital Licht-Murava, Batya Plotkin
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Publication number: 20160130304Abstract: The present invention relates to novel cyclosporine analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporine analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.Type: ApplicationFiled: November 3, 2015Publication date: May 12, 2016Inventors: Guoqiang Wang, In Jong Kim, Yat Sun Or
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Publication number: 20160130305Abstract: Dengue virus (DV) peptides, including T cell epitopes, structural and non-structural (NS) polypeptide sequences, subsequences and modifications thereof, nucleotide sequences encoding such peptides, and compositions including such peptides and encoding nucleotide sequences, and cells expressing such peptides, are provided. Such DV peptides, nucleotide sequences and compositions, can be used to elicit, stimulate, induce, promote, increase, enhance or activate an anti-DV CD8+ T cell response or an anti-DV CD4+ T cell response. Such peptides, nucleotide sequences and compositions can also be used for and in methods of vaccination/immunization of a subject against Dengue virus (DV) (e.g., to provide protection against DV infection and/or pathology), and for treatment of a subject in need thereof, for example, treatment of the subject for a Dengue virus (DV) infection or pathology.Type: ApplicationFiled: July 15, 2015Publication date: May 12, 2016Inventors: Sujan Shresta, Lauren Yauch, Alessandro Sette, Daniela Weiskopf
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Publication number: 20160130306Abstract: The present invention provides, among other things, systems (e.g., comprising compositions and/or methods) for diagnosis, prophylaxis, treatment, prevention, and/or characterization of influenza transmission and/or infection. The present invention also provides methods for monitoring influenza variants for their potential to present a pandemic risk to humans.Type: ApplicationFiled: June 5, 2014Publication date: May 12, 2016Applicant: Massachusetts Institute of TechnologyInventors: Kannan Tharakaraman, Rahul Raman, Akila Jayaraman, Nathan Stebbins, Ram Sasisekharan
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Publication number: 20160130307Abstract: The invention relates to a group of synthetic polypeptides, derived from the pre-S1 region of HBV, that efficiently interfere with early steps of an HBV infection. The peptides of the invention can be used in diagnostics for the detection of antigens and/or antibodies.Type: ApplicationFiled: November 18, 2015Publication date: May 12, 2016Inventors: Philippe Gripon, Stephan Urban
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Publication number: 20160130308Abstract: Provided herein are nucleic acid sequences that encode novel consensus amino acid sequences of herpes virus antigens, as well as genetic constructs/vectors and vaccines expressing the sequences. Also provide herein are methods for generating an immune response against herpes virus using the vaccines that are provided.Type: ApplicationFiled: January 20, 2016Publication date: May 12, 2016Inventors: David B. Weiner, Devon Shedlock
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Publication number: 20160130309Abstract: The disclosure relates to the identification, cloning, and expression of a genetic locus within a Listeria monocytogenes genome that encodes a phage tail-like bacteriocin (PTLB), termed a monocin. Also provided are non-natural monocins, which have been engineered to have altered bactericidal specificity. Nucleic acid molecules encoding natural or non-natural monocins, vector constructs containing such nucleic acids operably linked to a heterologous promoter, producer cells containing such vectors, the encoded monocins, as well as methods of making and using such monocins are described.Type: ApplicationFiled: November 6, 2015Publication date: May 12, 2016Applicant: AvidBiotics Corp.Inventors: Urmi CHAKRABORTY, Grace LEE, Dean SCHOLL