Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Type:
Application
Filed:
May 23, 2016
Publication date:
September 15, 2016
Inventors:
Christopher J. BURNS, Denis DAIGLE, Bin LIU, Randy W. JACKSON, Jodie HAMRICK, Daniel McGARRY, Daniel C. PEVEAR, Robert E. Lee TROUT
Abstract: Functionalized F-POSS compounds comprising synthetic blends of at least two feedstocks that produce a distribution of fluorinated polyhedral oligomeric silsesquioxane molecule structures and/or functional groups.
Type:
Application
Filed:
March 9, 2016
Publication date:
September 15, 2016
Inventors:
John C. WARNER, Jean R. LOEBELENZ, Srinivasa Rao CHERUKU, Thomas Woodrow GERO
Abstract: To provide a method for producing a silicon compound, whereby a hydrosilylation reaction of a compound having a 2-propenyl group, can be conducted with high selectivity by a simple and easy method. The method for producing a silicon compound comprises reacting a compound (3) having a group represented by —CH2CH?CH2 and a silicon compound (4) having an H—Si bond in the presence of a transition metal catalyst (C) and a compound (D) having a group represented by —S(?O)— to obtain a compound (5) having a group represented by —CH2CH2CH2Si?.
Abstract: The present invention relates to novel vinylsilane compounds which are useful as modifying monomers in the polymerization of conjugated diene monomers, optionally together with aromatic vinyl monomers, thus producing polymers, specifically elastomeric polymers, which can favorably be used in rubber articles such as tires.
Type:
Application
Filed:
October 18, 2013
Publication date:
September 15, 2016
Inventors:
Michael Rossle, Daniel Heidenreich, Christian Doring, Sven Thiele
Abstract: A manufacturing method of silatrane with thiol group and a preservation method thereof are disclosed. (3-Mercaptopropyl)trimethoxysilane and triethanolamine are reacted for a pre-determined time at a pre-determined temperature under nitrogen atmosphere in presence or absence of catalyst, and then a recrystallization process is performed with a solvent to obtain silatrane with thiol group of formula (1). Silatrane with thiol group is dissolved in an organic solvent to preserve the silatrane with thiol group.
Abstract: Provided are compositions having the formula MnTi(L1)(L2)(L3) wherein L1 is a catecholate, and L2 and L3 are each independently selected from catecholates, ascorbate, citrate, glycolates, a polyol, gluconate, glycinate, hydroxyalkanoates, acetate, formate, benzoates, malate, maleate, phthalates, sarcosinate, salicylate, oxalate, a urea, polyamine, aminophenolates, acetylacetone or lactate; each M is independently Na, Li, or K; n is 0 or an integer from 1-6. Also provided are energy storage systems.
Type:
Application
Filed:
May 23, 2016
Publication date:
September 15, 2016
Inventors:
Arthur J. ESSWEIN, Steven Y. REECE, Evan R. KING, John GOELTZ, Desiree D. AMADEO
Abstract: Provided are novel prodrug salts of selective aquaporin inhibitors, their use as pharmaceuticals, and pharmaceutical compositions comprising them, and novel processes for their synthesis and novel intermediates for use in their synthesis. Also provided is use of a compound for the prophylaxis, treatment, and control of aquaporin-mediated conditions. Aquaporin inhibitors, e.g., inhibitors of AQP4 and/or AQP2, may be of utility in the treatment or control of diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord), hyponatremia, and excess fluid retention, as well as diseases such as epilepsy, retinal ischemia and other diseases of the eye, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines.
Type:
Application
Filed:
November 6, 2014
Publication date:
September 15, 2016
Applicant:
Aeromics, Inc.
Inventors:
Marc F. PELLETIER, Paul Robert MCGUIRK, George William FARR, Robert ZAMBONI, John COLUCCI, Helmi ZAGHDANE
Abstract: The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.
Abstract: A method for the purification of lecithin, comprising the steps of: a. reducing the viscosity of lecithin to a viscosity of less than about 10 Pa·s; then b. mixing the lecithin with granulated active carbon; then c. separating the lecithin from the granulated active carbon and recover purified lecithin. Lecithin substantially free of poly-aromatic hydrocarbons, and a food or feed product comprising said lecithin.
Type:
Application
Filed:
April 7, 2016
Publication date:
September 15, 2016
Applicant:
Cargill, Incorporated
Inventors:
Bassam Farid JIRJIS, Jeff MOLNAR, Christoph SCHAEFER, Arnulf SCHOEPPE
Abstract: Compounds having the following formula (E): Formula E or a pharmaceutically acceptable salt thereof, wherein R, R?, R?, X and n are as defined herein are provided. Methods comprising use of such compounds for the treatment of neurologic disorders, such as pantothenate kinase-associated neurodegeneration, and pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders are also provided.
Type:
Application
Filed:
October 27, 2014
Publication date:
September 15, 2016
Inventors:
Andrew Vaino, Marek Biestek, Martin Shkreli
Abstract: The present invention is related to a method for the synthesis of ethane-1-hydroxy-1,1-diphosphonic acid or its salt which includes the steps of reacting tetraphosphorus hexaoxide and acetic acid under controlled reaction conditions; hydrolyzing the formed ethane-1-hydroxy-1,1-diphosphonic acid condensates to form ethane-1-hydroxy-1,1-diphosphonic acid; further processing the ethane-1-hydroxy-1,1-diphosphonic acid solution. The process according to the method of the present invention is highly controllable and further is characterized by a high selectivity.
Abstract: The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.
Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
Type:
Application
Filed:
May 23, 2016
Publication date:
September 15, 2016
Inventors:
Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
Abstract: The application discloses compounds of Formula I wherein the variable substituents are as defined herein. The compounds of Formula I and pharmaceutical compositions comprising compounds of Formula I are useful for the treatment of diseases mediated by RSV.
Abstract: This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3?-position of the deoxyribose.
Type:
Application
Filed:
May 27, 2016
Publication date:
September 15, 2016
Inventors:
Jingyue Ju, Zengmin Li, John Robert Edwards, Yasuhiro Itagaki
Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.
Abstract: The sulfated oxysterol 5-cholesten-3?, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.
Abstract: Regulator of G Protein Signaling (RGS) proteins modulate the complex signaling pathways elicited by G protein coupled receptor activation. Recent studies have implicated RGS proteins in the development and progression of multiple cancers. Provided herein are inhibitors of RGS17, compositions thereof and methods of treating diseases using the inhibitors.
Abstract: Disclosed herein is an integrated approach to purification process development and execution, including processes comprising particular capture and fine purification steps; processes that employ of a minimal number of buffer systems, and processes that make use of minimally-corrosive buffer systems, as well as combinations thereof.
Type:
Application
Filed:
October 14, 2015
Publication date:
September 15, 2016
Inventors:
Diane D. Dong, Stephen M. Lu, Natarajan Ramasubramanyan, Wen-Chung Lim
Abstract: The present invention relates to a method for separating antibody isoforms using cation exchange chromatography and, more specifically, to a method for separating and purifying several isoforms, which are generated during an antibody production procedure, using a washing buffer for cation exchange chromatography.
Type:
Application
Filed:
October 24, 2014
Publication date:
September 15, 2016
Inventors:
Dong Woo LEE, Mi Na SONG, Byoung Oh KWON, Ki Sung KWON, Dong Rim YEOM, Yeon Jung KIM
Abstract: The present invention relates to a method or process for the manufacture of a virus and prion save native fibrinogen concentrate of high purity and low amounts of fibrinopeptide A and fibronectin.
Type:
Application
Filed:
May 25, 2016
Publication date:
September 15, 2016
Applicant:
OCTAPHARMA AG
Inventors:
Petra Schulz, Rainer Pape, Werner Gehringer
Abstract: Provided is a separation and purification method for vancomycin hydrochloride of high purity. The method comprises the following steps: (1) obtaining a vancomycin hydrochloride solution from a crude vancomycin product by ion exchange chromatography and obtaining a concentrate by nanofiltration desalination and concentration; (2) adjusting the concentrate with a hydrochloric acid solution and then performing a column chromatography using a reverse chromatography column for the adjusted concentrate; (3) collecting the chromatographic solution of vancomycin to obtain a mixed chromatographic solution; (4) adjusting the mixed chromatographic solution, and separating the solution and the salts by nanofiltration desalination and concentration to obtain a concentrate; and (5) obtaining a vancomycin dry powder with a chromatographic purity of up to 99% and a pure white appearance by dehydrating and drying the concentrate of step (4), or by solvent crystallization or salting-out crystallization.
Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
Type:
Application
Filed:
March 9, 2016
Publication date:
September 15, 2016
Applicant:
AGIOS PHARMACEUTICALS, INC
Inventors:
Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy M. Travins, Shunqi Yan
Abstract: The present invention relates to compositions comprising a substantially pure compound represented by Structural Formula I: and methods of using such compounds to activate cytoprotective kinases. The values and preferred values of the variables in Structural Formula I are defined herein.
Type:
Application
Filed:
October 20, 2015
Publication date:
September 15, 2016
Inventors:
Alexander Baguisi, Reinier Beeuwkes, Ralph Casale, Steven A. Kates, Alan S. Lader
Abstract: The present invention is to provide a method for the efficient production on an industrial scale of SS-31 (D-Arg-Dmt-Lys-Phe-NH2), which is an SS peptide. According to the present invention, the desired SS-31 is produced by efficiently synthesizing a tetrapeptide compound as a precursor of SS-31 and improving the tetrapeptide purity by crystallization.
Abstract: Tubulysin compounds of the formula (I) where R1, R2 R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.
Abstract: The subject invention provides advantageous new salts of mu-opiate receptor peptides. These salts have been found to have excellent properties in terms of their activity.
Abstract: An object of the present invention is to provide a method for producing a peptide thioester compound, a peptide hydrazide compound, and a peptide amide compound. The present invention provides a method for producing a peptide hydrazide compound or a peptide amide compound by using a compound represented by Formula (2): wherein R1, R2, R3, and X are as defined in the specification, and using a hydrazine compound or an ammonia compound as a reaction reagent. The present invention also provides a method for producing a peptide thioester compound from the peptide hydrazide compound.
Abstract: Cyclic peptides represented by (Formula 1) selectively bind the oncoprotein K-Ras G12D in vitro and in cellulo, where Z1 and Z2 are each L-propargylglycine (Pra), azidoornithine (OrnN3), or L-azidolysine (Az4), and V1-V2-V3-V4-V5 is an amino acid variable region having a sequence selected from the group consisting of SEQ ID NOs: 1-20.
Type:
Application
Filed:
March 11, 2016
Publication date:
September 15, 2016
Inventors:
Ryan K. Henning, Ashwin N. Ram, Samir Das, Arundhati Nag, James R. Heath
Abstract: The present invention relates to the preparation of compounds, in particular to the preparation of compounds of formula (I), which may be used with a compound of formula (VI), or a salt thereof as intermediates for the preparation of antifungal agents, preferably micafungin (MICA) or a salt thereof.
Type:
Application
Filed:
May 23, 2016
Publication date:
September 15, 2016
Inventors:
Roland Barth, Kerstin Knepper, Hubert Sturm
Abstract: Provided is a Titi Monkey Adenovirus (TMAdV) that can infect both human and non-human primates. Further provided are nucleic acid sequences, proteins, expression vectors and host cells, anti-TMAdV antibodies, vaccines, compositions, methods of detecting TMAdV, methods for assaying for anti-TMAdV compounds, and methods for treating or preventing a TMAdV infection.
Type:
Application
Filed:
January 14, 2016
Publication date:
September 15, 2016
Inventors:
Charles CHIU, Eunice CHEN, Nicholas W. LERCHE, Karen Lisa BALES
Abstract: Protein kinase inhibitors and more specifically inhibitors of the protein kinase c-Jun amino terminal kinase are herein described. Additionally, JNK inhibitor sequences, chimeric peptides, nucleic acids encoding same as well as pharmaceutical compositions for treating pathophysiologies associated with JNK signaling are herein provided.
Abstract: The present invention provides proteins that are suitable to be used as the active ingredient in subunit vaccine against Mycoplasma spp. The present invention also provides a subunit vaccine made therefrom. Said proteins have been experimentally proved to have the capability of inducing sufficient immune response to avoid pigs from Mycoplasma spp. infection. Said vaccine may have one of said proteins as active ingredient; or may have two or more of said proteins and is formulated as a cocktail vaccine. The present vaccine not only is safer than the conventional vaccines but also has equal or even better immune efficiency than the conventional ones. Furthermore, fusion partners suitable for producing said proteins of high solubility are also proved, which can significantly reduce production cost.
Type:
Application
Filed:
November 21, 2013
Publication date:
September 15, 2016
Applicant:
AGRICULTURAL TECHNOLOGY RESEARCH INSTITUTE
Abstract: The invention provides proteins from group B streptococcus (Streptococcus agalactiae) and group A streptococcus (Streptococcus pyogenes), including amino acid sequences and the corresponding nucleotide sequences. Data are given to show that the proteins are useful antigens for vaccines, immunogenic compositions, and/or diagnostics. The proteins are also targets for antibiotics.
Type:
Application
Filed:
May 26, 2016
Publication date:
September 15, 2016
Inventors:
John TELFORD, Vega MASIGNANI, Maria SCARSELLI, Guido GRANDI, Herve TETTELIN, Claire FRASER
Abstract: A novel peptide analogue of the Heterometrus spinnifer toxin HsTX1 is disclosed along with its application as, for example, a therapeutic agent for treating an autoimmune disease such as multiple sclerosis (MS) or rheumatoid arthritis (RA). The analogue comprises a peptide with an amino acid substitution at amino acid position 14 of the wild-type (WT) peptide sequence (or a position corresponding to position 14 of the WT peptide sequence). The analogue exhibits selectivity for Kv1.3 over Kv1.1 and other potassium channels relative to the WT peptide.
Type:
Application
Filed:
October 28, 2013
Publication date:
September 15, 2016
Inventors:
Raymond S. NORTON, Serdar KUYUCAK, M Harunur RASHID, Michael PENNINGTON, Christine BEETON
Abstract: The field of this invention relates to methods for combining genetic elements such that the activity of one of the elements provides a means for identifying, enriching, selecting for, or enhancing the activity of a second element. The invention also includes specific elements and combinations of elements.
Abstract: The invention relates to an isolated peptide inhibitor of the interaction between the TEAD and YAP or TAZ proteins and a derived chimeric peptide linked to a cell-penetrating peptide. These peptides which have a cytotoxic activity are useful, in particular for the treatment of hyperproliferative disorders such as cancer.
Abstract: The present invention relates to a chimeric protein comprising at least one human amyloid P component and at least one fragment of an Fc region of a human antibody, the human amyloid P component and the fragment of an Fc region with which it is associated being bound to each other by means of a hinge region.
Type:
Application
Filed:
October 31, 2014
Publication date:
September 15, 2016
Applicants:
LABORATOIRE FRANCAIS DU FRACTIONNEMENT ET DES BIO- TECHNOLOGIES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE LIMOGES
Abstract: This invention provides WT1 peptides and methods of treating, reducing the incidence of, and inducing immune responses against a WT1-expressing cancer, comprising same.
Type:
Application
Filed:
January 8, 2016
Publication date:
September 15, 2016
Applicant:
SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH
Inventors:
David A. Scheinberg, Javier Pinilla-Ibarz, Rena May
Abstract: This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.
Type:
Application
Filed:
November 5, 2014
Publication date:
September 15, 2016
Applicant:
Trophogen Inc.
Inventors:
Mariusz Szkudlinski, Bruce D. Weintraub
Abstract: The present invention discloses cryopreserved recombinant cells for screening drug candidates that transiently overexpress one or more drug transporter proteins and/or drug metabolizing enzymes. Advantageously, such cells provide a cost-efficient consumable product that streamlines the process of screening whether drug candidates are substrates or inhibitors of drug transporter proteins and/or drug metabolizing enzymes.
Abstract: The present invention relates to a method for producing a cell line expressing a stabilized functional single chain-antigen-recognizing genetic construct (scARC), comprising a genetic construct of the human scARC to be expressed, comprising the domains huV1/2-Li-huV2/1-C4/3 and a genetic construct comprising the corresponding hetero-/(homo-)dimeric domain C3/4, containing xenogenic, in its special case murine amino acid exchanges in the domains C4/3 and C3/4, wherein co-expression of the genetic constructs of the scARC-fragments occurs through the cell. Preferably, the scARCs are single chain-TCRs (scTCRs) or antibody-scFv-fragments, which further preferably recognize tumor associated peptide antigens (TAA). The present invention further relates to a gp100-protein-specific T-cell response mediated ?/? T-cell receptor rationally mutated by means of the method of the present invention and its uses.
Type:
Application
Filed:
May 30, 2016
Publication date:
September 15, 2016
Inventors:
Ralf-Holger VOSS, Matthias THEOBALD, Ratna Sari Intan PÖNDL, Renate ENGEL, Simone THOMAS
Abstract: The present invention provides variant activin IIB soluble receptor polypeptides and proteins capable of binding and inhibiting the activities of activin A, myostatin, or GDF-11. The present invention also provides polynucleotides, vectors and host cells capable of producing the variant polypeptides and proteins. Compositions and methods for treating muscle-wasting and other diseases and disorders are also provided.
Type:
Application
Filed:
June 2, 2016
Publication date:
September 15, 2016
Inventors:
Jeonghoon Sun, Lei-Ting Tony Tam, Hui-Quan Han, Keith Soo-Nyung Kwak, Xiaolan Zhou
Abstract: The present invention relates to modified coagulation factors. In particular, the present invention relates to stabilized Factor VIII molecules conjugated with a half life extending moiety as well as use of such molecules.
Type:
Application
Filed:
June 1, 2016
Publication date:
September 15, 2016
Inventors:
Henrik Oestergaard, Marianne Kjalke, Ole Hvilsted Olsen, Lars Thim, Henning Ralf Stennicke
Abstract: The invention is directed to a method of producing pulmonary surfactant protein-B (SP-B) isoforms fragments and analogues thereof in a plant cell, and to expression cassettes for expression of the SP-B proteins in plants. The expression cassettes may include various elements for improved expression, stability of the expressed protein or efficient purification of the expressed protein, including signal sequences, protease cleavage sites for release of the target protein, trafficking peptides for trafficking of the expressed protein to various plant compartments, and/or various tags.
Type:
Application
Filed:
May 16, 2014
Publication date:
September 15, 2016
Applicant:
AZARGEN BIOTECHNOLOGIES (PTY) LTD
Inventors:
Mauritz Venter, Jacobus Petrus Zwiegelaar
Abstract: The invention provides polypeptides (e.g., antibodies) and fusion proteins that target a epitope in the receptor binding domain (RBD) of the spike (S) glycoprotein of the Middle East Respiratory Syndrome Coronavirus (MERS-CoV). The polypeptides and fusion proteins can be used to treat and prevent MERS-CoV infection in mammals.
Type:
Application
Filed:
October 16, 2014
Publication date:
September 15, 2016
Inventors:
Dimiter S. Dimitrov, Tianlei Ying, Tina W. Ju, Kwok Yung Yuen