Patents Issued in April 13, 2017
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Publication number: 20170101416Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: formula (I).Type: ApplicationFiled: May 19, 2015Publication date: April 13, 2017Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Tao WANG, Zhongxing Zhang, John F. Kadow
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Publication number: 20170101417Abstract: Polyols stabilize polymorphous form of rifaximin, in particular the ? form. When polyols having at least two hydroxy groups are added to rifaximin powder, polymorph ? is stable and remains stable in time independently from the environment humidity. In this invention a method to prepare formulations constituted by pure and stable polymorphous forms able to give a pharmaceutical product is described.Type: ApplicationFiled: May 12, 2016Publication date: April 13, 2017Inventors: Paola MAFFEI, Milena BACHETTI, Giuseppe BOTTONI, Giuseppe Claudio VISCOMI
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Publication number: 20170101418Abstract: The invention relates to methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infection, atheroscleosis, Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder including by modulating biological processes by the inhibition of PI3 kinase and/or bromodomain protein binding to substrates comprising the administration of a compound(s) of Formula I-IX (or pharmaceutically acceptable salts thereof) as defined herein.Type: ApplicationFiled: October 19, 2016Publication date: April 13, 2017Applicant: SignalRx Pharmaceuticals, Inc.Inventors: Donald L. Durden, Guillermo A. Morales, Joseph R. Garlich
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Publication number: 20170101419Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.Type: ApplicationFiled: December 14, 2016Publication date: April 13, 2017Applicant: SignalRx Pharmaceuticals, Inc.Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
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Publication number: 20170101420Abstract: The present invention relates to compounds of general formula (I) having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.Type: ApplicationFiled: June 2, 2015Publication date: April 13, 2017Inventors: Marina VIRGILI-BERNADO, Monica ALONSO-XALMA, Carlos ALEGRET-MOLINA, Carmen ALMANSA-ROSALES, Monica GARCIA LOPEZ
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Publication number: 20170101421Abstract: A method of forming a compound of formula (IIIa): wherein: R1 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C1-5 alkenyl and C1-5 alkynyl; R2 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C1-5 alkenyl and C1-5 alkynyl; R4 is C1-5 alkyl; and R6 is a C1-5 fluoroalkyl; and PG is a protecting group, the method comprising the step of reacting a compound of formula (IIa) with a compound of formula (VIII):Type: ApplicationFiled: May 14, 2015Publication date: April 13, 2017Applicant: Allecra Therapeutics SASInventors: Andrea Faini, Marco Forzatti, Giovanni Fogliato, Stefano Biondi
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Publication number: 20170101422Abstract: The present application relates to novel bicyclic compounds, to their use for controlling animal pests and to processes and intermediates for their preparation.Type: ApplicationFiled: June 2, 2015Publication date: April 13, 2017Inventors: SILVIA CEREZO-GALVEZ, THOMAS BRETSCHNEIDER (DECEASED), REINER FISCHER, MARTIN FUESSLEIN, JOERG GREUL, PETER JESCHKE, JOACHIM KLUTH, ARND VOERSTE, KERSTIN ILG, Olga MALSAM, PETER LOESEL, Ulrich GOERGENS
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Publication number: 20170101423Abstract: The present invention is a mono-functional branched organosiloxane compound that is liquid and shown by the following general formula (1) Ma-1MRa-2Db-1DRb-2Tc-1TRc-2Qd-1??(1) wherein M=R13SiO0.5, MR=R12R2SiO0.5, D=R12SiO, DR=R2R1SiO, T=R1SiO1.5, TR=R2SiO1.5, and Q=SiO2, where R1 represents a group selected from an alkyl group having 1 to 30 carbon atoms, and so on, R2 represents a hydrogen atom, and so on, a-1 represents an integer of 1 or more, b-1 and c-1 each represent an integer of 0 or more, and a-2, b-2, c-2, and d-1 each represent 0 or 1, provided that c-1, c-2, and d-1 are not simultaneously 0, a total of a-2, b-2, and c-2 is 1, and when b-1 is 0, a-1 is 2 or more and a total of c-1 and d-1 is 1 or more. There can be provided a novel mono-functional branched organosiloxane compound having a branched structure, and a method for producing the same.Type: ApplicationFiled: September 20, 2016Publication date: April 13, 2017Applicant: SHIN-ETSU CHEMICAL CO., LTD.Inventors: Emi AKABANE, Tomoyuki GOTO
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Publication number: 20170101424Abstract: Hydrosilylation of aliphatically unsaturated compounds (B) with compounds (A) bearing silicon-bonded hydrogen using a metal-containing hydrosilylation catalyst proceeds with higher yields and reduced quantities of byproducts when conducted in the presence of organic salts containing an inorganic or organic anion [Y]? and a heteroatom-containing cation [A]+ in amounts of 0.01 mole % to 10 mole % based on the limiting amount of (A) or (B) in moles present in the reaction.Type: ApplicationFiled: February 20, 2015Publication date: April 13, 2017Inventors: Agnes BASKAKOV, Christine KAES
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Publication number: 20170101425Abstract: A process for the purification of L-?-glycerophosphorylcholine is described, wherein L-?-glycerophosphorylcholine is crystallized from DMSO or from a mixture of DMSO with at least another solvent, preferably selected from water, alcohol, halogenated solvents, ethers, esters and/or amides. Such a process allows to obtain L-?-glycerophosphorylcholine having a purity greater than 99.5%, preferably greater than 99.7%, even more preferably greater than or equal to 99.9%. A method for determining the purity of L-?-glycerophosphorylcholine is also described, comprising the elution of L-?-glycerophosphorylcholine through an HPLC column having an amino stationary phase, and subsequent detection of L-?-glycerophosphorylcholine itself, and any impurity thereof, by means of an Evaporative Light Scattering Detector type.Type: ApplicationFiled: June 9, 2015Publication date: April 13, 2017Inventors: Lorenzo De Ferra, Mauro Anibaldi, Maurizio Zenoni, Fabrizio Cocchi
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Publication number: 20170101426Abstract: The present invention relates to crystallizates of the pure aminoalkylenephosphonic acid DTPMP in three crystal polymorphs and to a process for obtaining solid crystalline DTPMP by a preferably one-stage crystallization from an aqueous product mixture comprising DTPMP, wherein the process comprises the following process steps: (a) introducing seed crystals comprising DTPMP into an aqueous crude product comprising DTPMP with a total proportion in the range from 10 to 65 percent by mass up to a suspension density in the range from 1% to 25%; (b) introducing kinetic energy into the aqueous crude product to precipitate a crystallizate containing DTPMP as pure acid with a total content of at least 75% by mass; and (c) removing the crystallizate formed from the aqueous crude product by sedimentation and/or filtration, such that DTPMP is obtained as a solid end product in the form of a crystallizate.Type: ApplicationFiled: June 2, 2015Publication date: April 13, 2017Applicant: Zschimmer & Schwarz Mohsdorf GmbH & Co. KGInventors: Thomas KREHER, Stephan LIEBSCH, Carsten RUDOLPH
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Publication number: 20170101427Abstract: The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.Type: ApplicationFiled: March 30, 2015Publication date: April 13, 2017Applicant: UNIVERSITEIT ANTWERPENInventors: Jurgen JOOSSENS, Koen AUGUSTYNS, Anne-Marie LAMBEIR, Pieter VAN DER VEKEN, Jeroen VAN SOOM, Viktor MAGDOLEN
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Publication number: 20170101428Abstract: Embodiments of the invention provide a lithium-free metal dichalcogenides functionalization method where a metal dichalcogenide including a surface of predominantly semiconducting 2H phase is reacted with an aryl diazonium salt by exposing at least a portion of transition metal dichalcogenide to the aryl diazonium salt in the absence of alkyl lithium or alkyl lithium. A substantial portion of the reaction of the at least one aryl diazonium salt with the at least one transition metal dichalcogenide occurs with the semiconducting 2H phase. The aryl diazonium salt can be 4-nitrobenzenediazonium tetrafluoroborate or 4-carboxybenzene diazonium tetrafluoroborate, and the metal dichalcogenide can be MoS2. The semiconducting 2H phase of the transition metal dichalcogenide is derived directly from mechanical exfoliation such as mechanical cleaving and/or sonication.Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITYInventors: QING HUA WANG, XIMO CHU, ALEXANDER GREEN, AHMED YOUSAF
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Publication number: 20170101429Abstract: The disclosure provides for metal organic frameworks (MOFs) which comprise a plurality of SBUs comprising different metals or metal ions and/or a plurality of organic linking moieties comprising different functional groups.Type: ApplicationFiled: March 27, 2015Publication date: April 13, 2017Inventors: Omar M. Yaghi, Mitsuharu Suzuki, Hexiang Deng, Lisa Wang
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Publication number: 20170101430Abstract: Lignin-rich starting material is suspended in a first medium, which is acidic and aqueous, to form a aqueous acidic suspension, which is heated and allowed to form two continuous phases, a thermoplastic lignin phase and an aqueous phase. The thermoplastic lignin phase is separated from the aqueous phase and passed through a shape giving process into a second medium which is at a temperature lower than that of the thermoplastic lignin phase and in which the thermoplastic lignin phase is essentially insoluble. Solid lignin formed in the second medium is recovered.Type: ApplicationFiled: October 12, 2016Publication date: April 13, 2017Applicant: Valmet Technologies OyInventors: Eric Enqvist, Ville Tarvo, Panu Tikka, Tobias Wittmann, Henrik Wallmo, Anders Littorin
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Publication number: 20170101431Abstract: Provided herein are compounds, compositions, and methods for the treatment of cancer, including leukemia. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-cancer agents.Type: ApplicationFiled: May 27, 2015Publication date: April 13, 2017Applicant: IDENIX PHARMACEUTICALS LLCInventors: Cyril Dousson, David Dukhan, Christophe Claude Parsy, Francois-Rene Alexandre, Rachid Rahali, Jean-Laurent Paparin
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Publication number: 20170101432Abstract: A crystal of free acid of 3?,5?-cyclic diguanylic acid containing no metal salt with cobalt, magnesium or the like is provided. A method is sought for obtaining said crystal in a large amount and with ease. By a manufacturing method comprising a step of adding acid to an aqueous solution of 3?,5?-cyclic diguanylic acid so as to lower pH to 1 to 3, crystals of 3?,5?-cyclic diguanylic acid can be obtained in a large amount with ease. Said crystals are free acid crystals which do not contain a metal salt with cobalt, magnesium or the like.Type: ApplicationFiled: February 27, 2015Publication date: April 13, 2017Inventors: Hisaki TANAKA, Kazuya ISHIGE
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Publication number: 20170101433Abstract: The present invention relates to a cocrystal of progesterone and a coformer selected from the group consisting of vanillic acid, benzoic acid, salicylic acid, cinnamic acid, and vanillin. The present invention also relates to a pharmaceutical composition comprising a cocrystal of the present invention and at least one pharmaceutically acceptable carrier. The present invention further relates to a method of supplementing progesterone in women. This method involves administering to a female subject in need thereof a pharmaceutical composition of the present invention.Type: ApplicationFiled: October 25, 2016Publication date: April 13, 2017Inventors: Ekaterina Albert, Patricia Andres, Melanie Janelle Bevill, Jared Smit, Jennifer Nelson
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Publication number: 20170101434Abstract: The present application provides a compound of formula I: or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1-R10, m, n, p, and are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Inventors: Roberto Pellicciari, Antimo Gioiello
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Publication number: 20170101435Abstract: The present invention relates to an apparatus capable of harvesting a recombinant protein from a bioreactor having a porous container comprised of a chromatography medium capable of binding the recombinant protein and a method of use thereof.Type: ApplicationFiled: October 13, 2015Publication date: April 13, 2017Applicant: THERAPEUTIC PROTEINS INTERNATIONAL, LLCInventor: Sarfaraz K. Niazi
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Publication number: 20170101436Abstract: The present invention relates to a method for the crystallization of protein using nanoparticles as nucleation agents. Precisely, the inventors performed the crystallization of such proteins as Bacillus subtilis YesR, chicken egg white lysozyme, bovine serum albumin, Alicyclobacillus acidocaldarius acetyl-CoA carboxylase, and Listeria monocytogenes hypothetical protein which have his-tag at amino terminal by using gold nanoparticles in diverse sizes and shapes in the presence of Ni2+ ions. As a result, it was confirmed that the chance of successful crystallization was higher with the gold nanoparticles than without the gold nanoparticles and the various crystallization conditions were successfully screened. Therefore, the method for inducing nucleation of the invention can be advantageously used for the disclosure of protein structure by increasing the chance of successful crystallization of protein.Type: ApplicationFiled: October 6, 2016Publication date: April 13, 2017Inventors: Jungwoo CHOE, Inhee CHOI
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Publication number: 20170101437Abstract: The present invention provides sequential chromatography steps and conditions for purification of a recombinant protein, especially recombinant darbepoetin alfa.Type: ApplicationFiled: February 17, 2016Publication date: April 13, 2017Inventors: Vamsi Krishna Bandi, Bala Reddy Bheemareddy, Shivu Mokshanath Mugthihalli, Pradeep Kumar Iyer, Prasad Pasupuleti
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Publication number: 20170101438Abstract: A cosmetic or pharmaceutical method for the treatment and/or care of the skin and/or hair which includes administering to the skin and/or hair an effective amount of at least one peptide of general formula (I): R1-AA1-AA2-AA3-R2?? (I) where AA1 and AA2 are independently selected from -Tyr- and -Phe- and AA3 is selected from -Nle- and -Met-, its stereoisomers, mixtures thereof and/or cosmetically or pharmaceutically acceptable salts thereof, in the treatment and/or care of conditions, disorders and/or diseases of the skin and/or hair by stimulating cyclic adenosine monophosphate synthesis (cAMP).Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Inventors: Núria GARCÍA SANZ, Wim VAN DEN NEST, Cristina CARREÑO SERRAÏMA, Antonio Vicente FERRER MONTIEL, Juan CEBRIÁN PUCHE, Núria ALMlÑANA DOMENECH
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Publication number: 20170101439Abstract: STAT3 hyperphosphorylation, dimerization and DNA binding are required for its ability to contribute to malignant transformation. As such, STAT3 has been recognized as a promising target for cancer therapy. Although a number of inhibitors of STAT3-STAT3 dimerization have been reported, molecular ligands that prevent interactions between STAT3 and DNA are very rare. The ?-AApeptide-based one-bead-one-compound (OBOC) combinatorial library was used, and identified ?-AApeptides that can selectively inhibit STAT3/DNA interaction and suppress the expression levels of STAT3 target genes in intact cells. The results not only validate ?-AApeptides as novel inhibitors of STAT3 signaling pathway, but also demonstrate that in addition to the SH2 domain, the DNA binding domain of STAT3 is targetable for the development of new generation of anti-cancer therapeutics. This also validates the approach of OBOC combinatorial library for the identification of ligands targeting traditionally recognized “undruggable targets”.Type: ApplicationFiled: October 24, 2016Publication date: April 13, 2017Applicant: University of South FloridaInventors: Said M. Sebti, Jianfeng Cai
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Publication number: 20170101440Abstract: Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.Type: ApplicationFiled: November 12, 2015Publication date: April 13, 2017Inventors: Mark R. Hellberg, Iok-Hou Pang
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Publication number: 20170101441Abstract: Provided are methods for identifying OP-adducted biomarkers of OP exposure as well as compounds containing OPs that can provide OP adducts and compounds of Formula 1 for eliciting antibodies that specifically and selectively bind to the OP adducts, wherein the Formula 1 compounds have the structure of OP-Peptide-Linker-CP, wherein CP is a carrier protein, OP represents a structure corresponding to that of a reactive organic phosphorous compound covalently modifying a tyrosine residue hydroxyl group of the peptide of Formula I and the other variable groups are as described herein.Type: ApplicationFiled: December 27, 2016Publication date: April 13, 2017Applicant: Human BioMolecular Research FoundationInventors: John R. Cashman, Mary T. MacDonald
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Publication number: 20170101442Abstract: Methods and compositions for identifying and using polypeptides that target hepatic stellate cells are described. Embodiments include a targeting composition that may include one or more polypeptides including an amino acid sequence that binds to an insulin-like growth factor 2 receptor. Other embodiments relate to targeting systems that may include a one or more polypeptides including an amino acid sequence that binds to an insulin-like growth factor 2 receptor of hepatic stellate cells. Further embodiments relate to methods for treating health disorders in which the methods include the targeting composition or targeting systems as well as an agent capable of treating the disorder.Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Inventors: Kun Cheng, Zhijin Chen
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Publication number: 20170101443Abstract: Disclosed is a crystalline powder of a cyclic peptide compound, represented by formula I is the structure of same, and, also disclosed are a preparation method for same and uses thereof.Type: ApplicationFiled: May 29, 2015Publication date: April 13, 2017Applicant: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.Inventors: Shidong LIU, Xiusheng WANG, Zhijun TANG, Xiaoming JI
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Publication number: 20170101444Abstract: The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.Type: ApplicationFiled: October 24, 2016Publication date: April 13, 2017Applicant: Aurigene Discovery Technologies LimitedInventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
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Publication number: 20170101445Abstract: The present invention relates to a compound of the formula (I), (II), (III), (IV), (V), or (VI): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection using the same.Type: ApplicationFiled: December 20, 2016Publication date: April 13, 2017Inventors: Zhuang SU, Zhengyu LONG, Suizhou YANG
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Publication number: 20170101446Abstract: The present invention relates to a polypeptide comprising a mutant fragment of an outer surface protein A (OspA), a nucleic acid coding the same, a pharmaceutical composition (particularly for use as a medicament of in a method of treating or preventing a Borrelia infection) comprising the polypeptide and/or the nucleic acid, a method of treating or preventing a Borrelia infection and a method of immunizing a subject.Type: ApplicationFiled: September 22, 2016Publication date: April 13, 2017Applicant: Valneva Austria GmbHInventors: Pär Comstedt, Urban Lundberg, Andreas Meinke, Markus Hanner, Wolfgang Schüler, Benjamin Wizel, Christoph Reinisch, Brigitte Grohmann, Robert Schlegl
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Publication number: 20170101447Abstract: Compositions and methods for conferring pesticidal activity to bacteria, plants, plant cells, tissues and seeds are provided. Compositions comprising a coding sequence for a delta-endotoxin polypeptide are provided. The coding sequences can be used in DNA constructs or expression cassettes for transformation and expression in plants and bacteria. Compositions also comprise transformed bacteria, plants, plant cells, tissues, and seeds. In particular, isolated delta-endotoxin nucleic acid molecules are provided. Additionally, amino acid sequences corresponding to the polynucleotides are encompassed, and antibodies specifically binding to those amino acid sequences. In particular, the present invention provides for isolated nucleic acid molecules comprising nucleotide sequences encoding the amino acid sequence shown in SEQ ID NO:61-121 and 133-141, or the nucleotide sequence set forth in SEQ ID NO:1-60, 124-132, and 142-283, as well as variants and fragments thereof.Type: ApplicationFiled: December 20, 2016Publication date: April 13, 2017Inventors: Kimberly S. Sampson, Daniel J. Tomso
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Publication number: 20170101448Abstract: The present invention relates to a novel fusion protein comprising the transcription modulation domain of the transcription factor NF-?B subunit p65 and a protein transduction domain and to the use thereof. The fusion protein of the present invention has the effects of inhibiting the transcription of NF-?B and IL-2 by competitive inhibition and inhibiting the LPS-induced secretion of inflammatory cytokines and also inhibiting the production of IL-2, IFN-?, IL-4, IL-17A and IL-10 in splenocytes, and thus is effectively used as a composition for the prevention or treatment of a disease related to NF-?B overactivity.Type: ApplicationFiled: November 3, 2016Publication date: April 13, 2017Inventor: Sang-Kyou Lee
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Publication number: 20170101449Abstract: The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF 19 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the ?Klotho-FGF receptor complex involving the use of chimeric proteins of the present invention.Type: ApplicationFiled: October 10, 2016Publication date: April 13, 2017Inventors: Moosa MOHAMMADI, Regina GOETZ
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Publication number: 20170101450Abstract: Expression vector systems are provided for increased production of a recombinant GDF-5 (rhGDF-5) protein. Also provided are transformed host cells that were engineered to produce and express high levels of rhGDF-5 protein. Methods for production and high expression of rhGDF-5 protein are disclosed herein. The methods of enhancing production and protein expression of rhGDF-5 protein as disclosed are cost-effective, time-saving and are of manufacturing quality.Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Inventors: David S. Scher, Roger E. Harrington
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Publication number: 20170101451Abstract: The present invention is directed stromal cell derived factor-1 peptides that have been mutated to make them resistant to digestion by the proteases dipeptidyl peptidase IV (DPPIV) and matrix metalloproteinase-2 (MMP-2) but which maintain the ability of native SDF-1 to attract T cells. The mutants may be attached to membranes formed by self-assembling peptides and then implanted at sites of tissue damage to help promote repair.Type: ApplicationFiled: December 9, 2016Publication date: April 13, 2017Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Richard T. LEE, Vincent SEGERS
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Publication number: 20170101452Abstract: Embodiments relate to peptide antagonists of ?c-family cytokines, which is associated with important human diseases, such as leukemia, autoimmune diseases, collagen diseases, diabetes mellitus, skin diseases, degenerative neuronal diseases and graft-versus-host disease (GvHD). Thus, inhibitors of ?c-cytokine activity are valuable therapeutic and cosmetic agents as well as research tools. Traditional approaches to inhibiting ?c-cytokine activity involve raising neutralizing antibodies against each individual ?c-cytokine family member/receptor subunit. However, success has been limited and often multiple ?c-cytokine family members co-operate to cause the disease state. Combinatorial use of neutralizing antibodies raised against each factor is impractical and poses an increased risk of adverse immune reactions. The present embodiments overcome these shortcomings by utilizing peptide antagonists based on the consensus ?c-subunit binding site to inhibit ?c-cytokine activity.Type: ApplicationFiled: October 6, 2016Publication date: April 13, 2017Inventor: Nazli Azimi
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Publication number: 20170101453Abstract: The present invention refers to a method of purification of HMG (human menopausal gonadotropin) by multimodal chromatography in order to obtain HMG-UP (human menopausal gonadotropin with ultra-purity grade) composition.Type: ApplicationFiled: May 21, 2015Publication date: April 13, 2017Inventors: Liliana BALANIÁN, Mariana CANCELA, Claudio WOLFENSON, José GROISMAN
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Publication number: 20170101454Abstract: The present invention relates to novel glucagon derivatives which are GLP-1/glucagon receptor co-agonists, and to the use of said glucagon derivatives in medicine, such as in the treatment of diabetes, obesity and related diseases and conditions.Type: ApplicationFiled: June 3, 2015Publication date: April 13, 2017Inventors: Ulrich Sensfuss, Jesper F. Lau, Thomas Kruse
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Publication number: 20170101455Abstract: The present invention relates to an insulin analog that has reduced insulin receptor binding affinity for the purpose of increasing the blood half-life of insulin, and long-acting insulin, a conjugate, and a method of preparing long-acting insulin using the same.Type: ApplicationFiled: January 20, 2015Publication date: April 13, 2017Applicant: HANMI PHARM. CO., LTD.Inventors: Sung Youb JUNG, Sang Youn HWANG, Euh Lim OH, Sung Hee PARK, Hyun Uk KIM, Chang Ki LIM, Se Chang KWON
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Publication number: 20170101456Abstract: An insulin analogue comprises a B-chain polypeptide containing a cyclohexanylalanine substitution at position B24 and optionally containing additional amino-acid substitutions at positions A8, B28, and/or B29. A proinsulin analogue or single-chain insulin analogue containing a B domain containing a cyclohexanylalanine substitution at position B24 and optionally containing additional amino-acid substitutions at positions A8, B28, and/or B29. The analogue may be an analogue of a mammalian insulin, such as human insulin. A nucleic acid encoding such an insulin analogue is also provided. A method of lowering the blood sugar of a patient comprises administering a physiologically effective amount of the insulin analogue or a physiologically acceptable salt thereof to a patient. A method of semi-synthesis using an unprotected octapeptide by means of modification of an endogenous tryptic site by non-standard amino-acid substitutions.Type: ApplicationFiled: September 27, 2016Publication date: April 13, 2017Inventor: Michael A. Weiss
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Publication number: 20170101457Abstract: Fusion proteins containing active agonist or antagonist fragments of parathyroid hormone (PTH) and parathyroid hormone related peptide (PTHrP) coupled to a collagen-binding domain are presented. The fusion proteins can be used to promote bone growth, to promote hair growth, to prevent cancer metastasis to bone, to promote immune reconstitution with a bone marrow stem cell transplant, to promote mobilization of bone marrow stem cells for collection for autologous stem cell transplant, and to treat renal osteodystrophy. Pharmaceutical agents comprising a collagen-binding polypeptide segment linked to a non-peptidyl PTH/PTHrP receptor agonist or antagonist are also presented.Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Applicants: OCHSNER CLINIC FOUNDATION, NATIONAL UNIVERSITY CORPORATION KAGAWA UNIVERSITY, THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSASInventors: Robert C. Gensure, Joshua Sakon, Osamu Matsushita, Tulasi Ponnapakkam
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Publication number: 20170101458Abstract: A recombinant vector having an expression cassette is provided which comprises a modified human low density lipoprotein receptor (hLDLR) gene is provided, wherein said hLDLR gene encodes a modified hLDLR comprising (a) one or more of the following amino acid substitutions: L318H, N295D, H306D, V307D, N309A, D310N, L318H, and/or L318D; or (b) an amino acid substitution of any of (a) in combination with one or more of the following amino acid substitutions: K796, K809R and/or C818A. Also provided are pharmaceutical compositions containing this vector and uses therefor in lowering cholesterol and/or treating familial hypercholesterolemia.Type: ApplicationFiled: April 24, 2015Publication date: April 13, 2017Inventors: James M. Wilson, Daniel J. Rader, Suryanrayan SOMANATHAN
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Publication number: 20170101459Abstract: In one aspect, the disclosure relates to major histocompatibility complex (MHC) molecules comprising a ligand in the peptide binding groove of the MHC molecule, whereby the ligand comprises an azobenzene (Abc), and at least two amino acid residues separated by the azo-group of the Abc, and wherein the amino acid residues are positioned to interact with the peptide binding groove of the MHC molecule. The disclosure also relates, among others, to means and methods for producing and using such MHC molecules, and the ligands therefor.Type: ApplicationFiled: June 5, 2015Publication date: April 13, 2017Inventors: Gijsbert Marnix Grotenbreg, Steven Hendrik Leonard Verhelst, Ai Ling Joanna Choo, Sock Yue Thong, Jiawei Yap, Wilhelmus Johannes Elisabeth Van Esch
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Publication number: 20170101460Abstract: The transgenic non-human animals are constructed, in whose genome the coding sequences of one of the animal's endogenous immunoglobulin C? constant regions are replaced by human immunoglobulin C? constant region coding sequences. The transgenic animal is mouse, in whose genome the C?1 constant regions are replaced by the human immunoglobulin C? constant regions and the C? constant region is replaced by the human immunoglobulin C? constant region. The transgenic mouse yields humanized IgE-secreting B cells and antigen-specific humanized IgE after immunization. The transgenic animals are employed to prepare serum containing humanized IgE, antiserum containing antigen-specific humanized IgE, and monoclonal antigen-specific humanized IgE antibodies by hybridoma and other technologies.Type: ApplicationFiled: January 12, 2015Publication date: April 13, 2017Applicant: ALLERMABS CO. LTD.Inventors: Alfur Fu-Hsin Hung, Donic Chien-Sheng Lu, Tse-Wen Chang
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Publication number: 20170101461Abstract: The invention relates to an antibody, a fragment or a derivative thereof, for use as an antiretroviral drug targeting a virus belonging to human endogenous retroviruses type W (HERV-W), wherein said antibody, fragment or derivative thereof is directed against HERV-W Envelope protein (HERV-W Env). The invention also relates to a composition comprising said antibody and a retroviral reverse-transcriptase inhibitory drug, for use as an antiretroviral drug targeting a virus belonging to HERV-W.Type: ApplicationFiled: May 27, 2015Publication date: April 13, 2017Inventors: Herve Perron, Francois Curtin, Alois Lang, Raphael Faucard, Julie Medina, Alexandra Madeira, Nadege Gehin
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Publication number: 20170101462Abstract: The present invention provides antibodies or the antigen-binding portion thereof to a tumor-associate carbohydrate antigen. Also disclosed herein are pharmaceutical compositions and methods for the inhibition of cancer cells in a subject in need thereof. The pharmaceutical compositions comprise an antibody or an antigen-binding portion thereof and at least one pharmaceutically acceptable carrier.Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Inventors: Cheng-Der Tony YU, Jiann-Shiun Lai, I-Ju Chen
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Publication number: 20170101463Abstract: The present invention relates to therapeutic agents comprising bispecific recombinant antibody fragments to selectively clear a protein associated with a neurological disease and methods of use of these therapeutic agents to treat neurological diseases.Type: ApplicationFiled: October 24, 2016Publication date: April 13, 2017Applicant: ARIZONA BOARD OF REGENTS, A BODY CORPORATE OF THE STATE OF ARIZONA, ACTING FOR AND ON BEHALF OFInventors: Michael Sierks, Yong Shen
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Publication number: 20170101464Abstract: The present invention provides, inter alia, methods for treating or ameliorating the effects of a disease, such as cancer, in a subject. The methods include: administering to a subject in need thereof (a) a therapeutically effective amount of a monoclonal antibody or antigen binding fragment of the present invention, and (b) a therapeutically effective amount of a combination therapy including bevacizumab and at least one additional therapeutic agent; or a therapeutically effective amount of at least one additional therapeutic agent selected from the group consisting of a COX-2 inhibitor (COXIB), a non-steroidal anti-inflammatory drug (NSAID), a prostaglandin E2 (PGE2) synthase inhibitor, and combinations thereof. Compositions, including pharmaceutical compositions, and kits for treating diseases, such as cancer, are also provided herein.Type: ApplicationFiled: June 9, 2015Publication date: April 13, 2017Inventors: Saurabh Saha, Xiaoyan M. Zhang, Dimiter Dimitrov, Zhongyu Zhu, Brad St. Croix, Enrique Zudaire
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Publication number: 20170101465Abstract: The invention provides methods, uses and compositions for the treatment of hidradenitis suppurativa. The invention describes methods and uses for treating hidradenitis suppurativa, wherein a TNF? inhibitor, such as a human TNF? antibody, or antigen-binding portion thereof, is used to treat hidradenitis suppurativa in a subject. Also described are methods for determining the efficacy of a TNF? inhibitor for treating hidradenitis suppurativa in a subject.Type: ApplicationFiled: May 6, 2016Publication date: April 13, 2017Inventors: Martin M. Okun, Thomas C. Harris