Abstract: Provided are a novel compound having a superior inhibitory action on KAT-II, a production method thereof, use thereof, and a pharmaceutical composition containing the aforementioned compound and the like. A compound represented by the formula (I) or a pharmacologically acceptable salt thereof. wherein each symbol is as defined in the DESCRIPTION.
Abstract: Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
Type:
Application
Filed:
January 31, 2019
Publication date:
August 1, 2019
Applicant:
PFIZER INC.
Inventors:
Simon PLANKEN, Hengmiao CHENG, Michael Raymond COLLINS, Jillian Elyse SPANGLER, Alexei BROOUN, Andreas MADERNA, Cynthia PALMER, Maria Angelica LINTON, Asako NAGATA, Ping CHEN
Abstract: Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.
Type:
Application
Filed:
April 2, 2019
Publication date:
August 1, 2019
Applicant:
Genentech, Inc.
Inventors:
Nicholas C. Ray, Yun-Xing Cheng, Christine Edwards, Simon C. Goodacre, Wei Li, Snahel Patel, Matthew W. Cartwright, Mohammed Sajad, Po-wai Yuen, Mark E. Zak
Abstract: The present disclosure relates to orally bioavailable selective estrogen receptor down-regulators (SERDs) and the synthesis of the same. Further, the present disclosure teaches the utilization of the orally bioavailable selective estrogen receptor down-regulators (SERDs) in a treatment for proliferative diseases, including cancer, particularly breast cancer, and especially ER+ breast cancer.
Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, ?-lactamase inhibitors (BLIs).
Type:
Application
Filed:
April 8, 2019
Publication date:
August 1, 2019
Inventors:
Scott J. Hecker, Raja K. Reddy, Tomasz Glinka, Olga Rodny
Abstract: The present disclosure relates to fungicidal active compounds, more specifically to trisubstitutedsilylphenoxyhetero-cycles and analogues thereof, processes and, intermediates for their preparation and use thereof as fungicidal active compound, particularly in the form of fungicide compositions. The present disclosure also relates to methods for the control of phytopathogenic fungi of plants using these compounds or compositions comprising thereof.
Type:
Application
Filed:
October 28, 2016
Publication date:
August 1, 2019
Inventors:
Jérémy DUFOUR, Philippe DESBORDES, Christophe DUBOST, Mathieu GOURGUES, Ruth MEISSNER, Andrew PETTINGER, Philippe RINOLFI, Valérie TOQUIN, Ulrike WACHENDORFF-NEUMANN
Abstract: A process can prepare an isocyanurate compound by hydrosilylation. The compound is a tris[3-(trialkoxysilyl)propyl] isocyanurate, a tris[3-(alkyldialkoxysilyl)propyl] isocyanurate, and/or a tris[3-(dialkylalkoxysilyl)propyl] isocyanurate, The process includes (A) preparing a mixture of at least one carboxylic acid, a platinum catalyst, and 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione; (B) heating the mixture to a temperature in the range of 40 to 140° C.; (C) adding at least one H-silane among a hydrotrialkoxysilane, a hydroalkyldialkoxysilane, and a hydrodialkylalkoxysilane to the mixture; (D) adding at least one alcohol to the mixture prepared in step (C); and (E) isolating the isocyanurate compound.
Abstract: Organoamino-functionalized cyclic oligosiloxanes, which have at least two silicon and two oxygen atoms as well as an organoamino group and methods for making the organoamino-functionalized cyclic oligosiloxanes are disclosed. Methods for depositing silicon and oxygen containing films using the organoamino-functionalized cyclic oligosiloxanes are also disclosed.
Type:
Application
Filed:
April 5, 2019
Publication date:
August 1, 2019
Applicant:
Versum Materials US, LLC
Inventors:
Matthew R. MacDonald, Xinjian Lei, Manchao Xiao, Meiliang Wang
Abstract: Disclosed herein are caged haptens and caged hapten-antibody conjugates useful for enabling the detection of targets located proximally to each other in a sample.
Type:
Application
Filed:
February 25, 2019
Publication date:
August 1, 2019
Inventors:
Yuri Belosludtsev, Traci D. DeGeer, Wendy J. French, Junshan Hao, Brian D. Kelly, Adrian E. Murillo, Nathan W. Polaske
Abstract: The present invention relates to novel crystalline forms of salts and/or co-crystals of tenofovir alafenamide, the pharmaceutical formulations, and the therapeutic uses thereof in treating viral infections.
Type:
Application
Filed:
March 21, 2019
Publication date:
August 1, 2019
Inventors:
Chiajen Lai, Bing Shi, Robert G. Strickley
Abstract: A compound, enantiomer, prodrug, diastereomer, or salt is provided which is an activator of the enzyme glucokinase and thus is believed to be useful in as treating diabetes and related diseases, which compound has the structure (I). A method for treating diabetes and related disease employing the compound, enantiomer, prodrug, diastereomer, or salt is also provided.
Type:
Application
Filed:
July 21, 2017
Publication date:
August 1, 2019
Applicant:
BRISTOL-MYERS SQUIBB COMPANY
Inventors:
Peter T.W. CHENG, Wei Meng, Mark Liu, Bei Wang, Rulin Zhao
Abstract: The invention provides compounds suitable for use as contrast agents in magnetic resonance imaging (MRI). The compounds of the present invention are manganese (II) complexes having advantageous properties as compared with similar known compounds.
Type:
Application
Filed:
June 20, 2017
Publication date:
August 1, 2019
Inventors:
Andreas Richard MEIJER, Mikkel Jacob THANING, Brian Christopher BALES, Michael James RISHEL
Abstract: A compound including a first ligand LA of Formula I is disclosed. In the structure of Formula I, one of L1 and L2 is C, and the other is N; Y1 to Y14 are each C or N; at least two adjacent Y7, Y8, Y9, and Y10 are carbon atoms that are fused to a structure of Formula II Z1 and Z2 are each O, S, Se, NR, CRR?, or SiRR?; and each R, R?, RA, RB, RC, and RD is hydrogen or a substituent; and any two substituents may be joined or fused together to form a ring. In the compound, LA is complexed to a metal M by L1 and L2, and M has an atomic weight greater than 40. Organic light emitting devices and consumer products containing the compounds are also disclosed.
Type:
Application
Filed:
January 14, 2019
Publication date:
August 1, 2019
Applicant:
UNIVERSAL DISPLAY CORPORATION
Inventors:
Zhiqiang JI, Jui-Yi TSAI, Alexey Borisovich DYATKIN, Chun LIN
Abstract: The present invention relates to improved processes for the preparation of ruthenium or osmium complexes comprising P and N donor ligands, in particular, ruthenium complexes.
Abstract: The present invention relates to the field of blue light phosphorescent tetradentate ring metal platinum complex luminescent material, discloses a blue light phosphorescent tetradentate ring metal platinum complex based on 4 aryl pyrazole, and its preparation method and application. The complex can be a delayed fluorescent and/or phosphorescent emitter with characteristics such as high thermal decomposition temperature, high quantum effect, being equipped with blue luminescence and narrow emission spectrum. Therefore, it has great application prospect in the field of blue light, especially dark blue phosphorescent material.
Abstract: The present invention relates to the field of luminescent material which is blue light phosphorescent tetradentate ring metal platinum complex, discloses a blue light phosphorescent tetradentate ring metal platinum complex based on trisubstituted pyrazole, and its preparation method and application. The complex can be a delayed fluorescent and/or phosphorescent emitter with characteristics such as high thermal decomposition temperature, high quantum effect, being equipped with blue luminescence and narrow emission spectrum. Therefore, it has great application prospect in the field of blue light, especially dark blue phosphorescent material.
Abstract: The present invention relates to the field of blue light phosphorescent tetradentate ring metal platinum complex luminescent material, publishes a blue light phosphorescent tetradentate ring metal platinum complex based on 4-aryl-3, 5-disubstituted pyrazole, its preparation method and application. The complex can be a delayed fluorescent and/or phosphorescent emitter with characteristics such as high thermal decomposition temperature, high quantum effect, being equipped with blue luminescence and narrow emission spectrum. Therefore, it has great application prospect in the field of blue light, especially dark blue phosphorescent material.
Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-?3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
Abstract: The present invention pertains to methods of extracting cardiac glycosides from cardiac glycoside containing plant material, such as Nerium oleander, through use of aloe. It further provides for compositions resulting from such extractions, pharmaceutical compositions, cosmetic compositions, and methods of treating skin conditions.
Abstract: Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are dessorbed and pharmaceutical compositions comprising at least one of the same.
Type:
Application
Filed:
October 6, 2017
Publication date:
August 1, 2019
Applicant:
GLYCOMIMETICS, INC.
Inventors:
John L. MAGNANI, John M. PETERSON, Myung-Gi BAEK
Abstract: The present disclosure discloses the chemical synthesis method of the Plesiomonas shigelloides serotype O51 O-antigen oligosaccharide, belonging to the field of chemistry. Source-abundant D-glucose, L-fucose, D-glucosamine and the like are used as raw materials to prepare three glycosylation building blocks, the synthetic route composed of 11 reaction modules is designed, and through the optimization of protecting group and the optimization of the time of introducing functional group, the preparation of the target oligosaccharide chain is successfully achieved. The oligosaccharide chain prepared in the present disclosure has the advantages of cheap and easy-to-get raw materials, and simple and easy-to-repeat preparation method. The present disclosure will have good application prospects in the aspects of development of new drugs and vaccines of Plesiomonas shigelloides, and the like.
Type:
Application
Filed:
December 10, 2018
Publication date:
August 1, 2019
Inventors:
Jian YIN, Jing HU, Peter Seeberger, Chunjun QIN
Abstract: The invention relates to bola-amphiphilic compounds and their uses for biomedical application. The invention particularly relates to the use of bola-amphiphilic compounds for providing low molecular weight gels (LMWG), useful, in particular, as culture media for animal or human cells, or as biocompatible material for biomedical applications.
Type:
Application
Filed:
January 18, 2019
Publication date:
August 1, 2019
Inventors:
Philippe BARTHELEMY, Michael RAMIN, Laurent LATXAGUE, Ananda APPAVOO, Olivier CHASSANDE, Camille EHRET
Abstract: The present disclosure relates to the field of nucleic acid chemistry, specifically to 5-position modified uridines as well as phosphoramidite and triphosphate derivatives thereof. The present disclosure also relates to methods of making and using the same.
Type:
Application
Filed:
January 22, 2019
Publication date:
August 1, 2019
Inventors:
John Rohloff, Nebojsa Janjic, Jeffrey D. Carter, Catherine Fowler
Abstract: To provide an easy and practical iron ion removal method, as a method for purifying P1,P4-di(uridine 5?-)tetraphosphate from a solution containing iron ions. Purification is performed by a purification method including a method for purifying P1,P4-di(uridine 5?-)tetraphosphate by removing iron ions from an aqueous solution or hydrophilic solvent solution containing P1,P4-di(uridine 5?-)tetraphosphate and iron ions, including (1) a step of purification using a chelating resin packed column, and (2) a step of adjusting the pH of the solution after said purification step using the chelating resin packed column to 5.5 or less, and then crystallizing P1,P4-di(uridine 5?-)tetraphosphate, or a step of treating the solution after said purification step using the chelating resin packed column with zinc chloride-activated activated carbon.
Abstract: The present invention relates to Cyclic Phosphate Substituted Nucleoside Compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein in A, B, R1, R2, R3, Q and V are as defined herein. The present invention also relates to compositions comprising a Cyclic Phosphate Substituted Nucleoside Compound, and methods of using the Cyclic Phosphate Substituted Nucleoside Compounds for treating or preventing HCV infection in a patient.
Abstract: The present invention relates to a method for detecting a target molecule, comprising forming a capturing complex comprising the target molecule; and binding the capturing complex with a signal amplifier, wherein the capturing complex has a net electrical charge; the signal amplifier has affinity to the capturing complex and has a like net electrical charge of the net electrical charge of the capturing complex. The invention improves the detection sensitivity and sensing limit of the detection.
Abstract: Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R2, R3, R4, R5, R6, R7, R11a, R11b, R12, R16, R17, R19, and are as herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
Type:
Application
Filed:
July 11, 2017
Publication date:
August 1, 2019
Applicant:
Sage Therapeutics, Inc.
Inventors:
Albert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison, Francesco G. Salituro, Andrew Griffin, Maria Jesus Blanco-Pillado
Abstract: The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body.
Abstract: A reaction cell for an automated peptide synthesizer consists of a body having adjacent first and second reaction wells for simultaneous reactions. The first reaction well is in fluid communication with the second reaction well for reagent pre-activation simultaneously with an amino acid addition for solid state peptide production.
Abstract: Provided herein are methods relating to the purification of a polypeptide comprising an Fc region (e.g., an antibody) via protein A chromatography; methods relating to the use of a wash solution comprising a benzoate salt and/or benzyl alcohol during protein A chromatography; and methods of adjusting a harvest using sodium benzoate prior to protein A chromatography.
Abstract: The invention provides a washing method for affinity chromatography in which a wash solution comprising arginine, or an arginine derivative, and a nonbuffering salt, preferably at high pH, greater than 8.0, is effective in removing impurities, such as high molecular weight species and host cell proteins, while also increasing product concentration in the eluate and maintaining a high percent yield of recovered product.
Abstract: Useful chiral specific boron-containing compounds, such as boronate, boronate esters, boranamines, borane diamines, boranamine thioesters, and boronic mono/di-thioesters, have been prepared. These compounds and compositions containing them are useful as anti-cancer or anti-amyloidosis agents.
Abstract: The present invention provides one or more compounds of formula (I) for conjugation to small molecules, polymers, peptides, proteins, antibodies, antibody fragments etc.
Abstract: A self-assembling peptide is provided that is enzymatically oxidized to form a polymeric pigment. The monomeric peptide has three amino acids (tyrosine (Y), one phenylalanine (F), and one aspartic acid (D) or one lysine (K)) and, following self-assembly and treatment with a tyrosinase enzyme oxidizes and polymerizes into a material with predetermined properties.
Type:
Application
Filed:
September 11, 2017
Publication date:
August 1, 2019
Inventors:
Rein V. Ulijn, Ayala Lampel, Tell Tuttle, Gary Scott, Scott McPhee, Christopher Bettinger
Abstract: Disclosed are crystalline forms of the bis- and tris-(hydrochloride) salts of D-Arg-Tyr(2,6-DiMe)-Lys-Phe-NH2, which is also known as MTP-131.
Abstract: The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are specific for the human and rat protease plasma kallikrein and are modified in one or two peptide loops to enhance potency and/or protease resistance.
Type:
Application
Filed:
January 3, 2019
Publication date:
August 1, 2019
Inventors:
Daniel Teufel, Catherine Stace, Edward Walker
Abstract: Reported herein are presumptively de-attenuating mutations that are useful, either individually or in combinations that may include other known mutations, in producing recombinant strains of human respiratory syncytial virus (RSV) exhibiting attenuation phenotypes. Also described herein is a novel RSV construct, Min_L-NPM2-1(N88K)L, which exhibits an attenuated phenotype, is stable and is as immunogenic as wild type RSV. The recombinant RSV strains described here are suitable for use as live-attenuated RSV vaccines. Exemplary vaccine candidates are described. Also provided are polynucleotide sequences capable of encoding the described viruses, as well as methods for producing and using the viruses.
Type:
Application
Filed:
September 22, 2017
Publication date:
August 1, 2019
Inventors:
Cyril LENOUEN, Ursula J. BUCHHOLZ, Peter L. COLLINS, Steffen MUELLER
Abstract: The present invention relates to a method to improve the production of a secondary metabolite catalyzed by a non-ribosomal peptide synthetase comprising contacting in a eukaryotic host a eukaryotic non-ribosomal peptide synthetase with an MbtH-like protein. The present invention further relates to a composition comprising a eukaryotic non-ribosomal peptide synthetase that is not a hybrid and a prokaryotic MbtH and to a eukaryotic host cell comprising a non-ribosomal peptide synthetase and a polynucleotide allowing the expression of an MbtH-like protein.
Abstract: The present invention relates to compositions comprising improved flagellin derived constructs and methods of using the same in the treatment of various diseases.
Abstract: Disclosed herein are a recombinant Streptomyces S27S5 hemagglutinin (SHA), and homologues thereof, and a fusion protein of a fluorescent protein (such as GFP and mCherry1) and SHA or a homologue thereof, which specifically bind to carbohydrates, including oligomeric sugars that terminate in L-rhamnose or D-galactose. The SHA, SHA homologues, and fusion proteins can be used to detect a variety of microorganisms or cancer or tumor antigens.
Type:
Application
Filed:
October 19, 2018
Publication date:
August 1, 2019
Inventors:
Markus KALKUM, Yoko FUJITA-YAMAGUCHI, Karine BAGRAMYAN, Teresa B. HONG, Sarah SHUCK
Abstract: The invention provides methods for improving plant yield, biomass accumulation and stress tolerance. According to the invention applications have discovered that a novel AP2-like transcription factor MPG1, which when modulated impacts grain yield, biomass and abiotic and biotic stress tolerance when compared to non-modulated plants. The invention further provides methods using recombinant expression cassettes, host cells, transgenic plants and breeding methods using the same.
Type:
Application
Filed:
July 6, 2017
Publication date:
August 1, 2019
Inventors:
Daniel R. Bush, Amanda K. Broz, Bettina E. Broeckling, Michael M. Friedman
Abstract: The present invention relates to a modified fibroin including a domain sequence represented by Formula 1: [(A)n motif-REP]m, in which the domain sequence has an amino acid sequence locally containing a region with locally high hydropathy index equivalent to an amino acid sequence in which one or a plurality of amino acid residues in REP are substituted with amino acid residues with a high hydropathy index and/or one or a plurality of amino acid residues with a high hydropathy index are inserted into REP, as compared to naturally occurring fibroin. In Formula 1, (A)n motif represents an amino acid sequence consisting of 4 to 20 amino acid residues and the number of alanine residues relative to the total number of amino acid residues in the (A)n motif is 83% or more. REP represents an amino acid sequence consisting of 10 to 200 amino acid residues. m represents an integer of 10 to 300, A plurality of (A)n motifs and the like may be the same amino acid sequence or different amino acid sequences.
Type:
Application
Filed:
June 23, 2017
Publication date:
August 1, 2019
Applicants:
Spiber Inc., KOJIMA INDUSTRIES CORPORATION
Abstract: The present disclosure provides isolated nucleic acid sequences encoding a monomeric green/yellow fluorescent proteins, and fragments and derivatives thereof. Also provided is a method for engineering the nucleic acid sequence, a vector comprising the nucleic acid sequence, a host cell comprising the vector, and use of the vector in a method for expressing the nucleic acid sequence. The present invention further provides an isolated nucleic acid, or mimetic or complement thereof, that hybridizes under stringent conditions to the nucleic acid sequence. Additionally, the present invention provides a monomeric green/yellow fluorescent protein encoded by the nucleic acid sequence, as well as derivatives, fragments, and homologues thereof. Also provided is an antibody that specifically binds to the green/yellow fluorescent protein.
Type:
Application
Filed:
January 24, 2019
Publication date:
August 1, 2019
Inventors:
Nathan C. Shaner, Gerard G. LAMBERT, Yuhui NI, Jiwu WANG
Abstract: The invention concerns derivatives of CMAP27, which have a good antimicrobial activity and a low haemolytic activity as compared to the wild-type CMAP27 peptide. These derivatives can be used for antibiotic therapy or in a bacteriocidal composition. Further comprised in the invention is the use of CMAP27 and/or its derivatives as adjuvant.
Type:
Application
Filed:
April 10, 2019
Publication date:
August 1, 2019
Applicant:
Universiteit Utrecht Holding B.V.
Inventors:
Floris Jacob Bikker, Albert van Dijk, Rosalia Mars-Groenendijk, Edwin Johannes Adrianus Veldhuizen, Desiree van der Kleij, Hendrik Haagsman, Elisabeth Margaretha Molhoek
Abstract: The present invention provides a method for diagnosing and detecting diseases associated with kidney. The present invention provides one or more proteins or fragments thereof, peptides or nucleic acid molecules differentially expressed in kidney diseases (KCAT) and antibodies binds to KCATs. The present invention provides that KCATs are used as targets for screening agents that modulates the KCAT activities. Further the present invention provides methods for treating diseases associated with kidney.
Type:
Application
Filed:
December 5, 2018
Publication date:
August 1, 2019
Inventors:
Elizabeth Joseloff, Steve Ruben, Tao He
Abstract: The technology relates in part to compositions and methods for inducing an immune response against a Bob1 antigen. Provided are methods for treating hyperproliferative diseases by inducing an immune response against a Bob1 antigen; the immune response may be induced using a Bob1 polypeptide fragment, or by specifically targeting Bob1-expressing cells using T cell receptors directed against Bob1.
Type:
Application
Filed:
December 7, 2018
Publication date:
August 1, 2019
Inventors:
Mirjam H.M HEEMSKERK, J.H. Frederik FALKENBURG
Abstract: In certain aspects, the present disclosure provides compositions and methods for increasing red blood cell and/or hemoglobin levels in vertebrates, including rodents and primates, and particularly in humans. In some embodiments, the compositions of the disclosure may be used to treat or prevent sideroblastic anemias and myelodysplastic syndromes or one or more complications associated sideroblastic anemias and myelodysplastic syndromes.
Type:
Application
Filed:
December 5, 2018
Publication date:
August 1, 2019
Inventors:
Kenneth M. Attie, Christopher Robert Rovaldi
Abstract: Peptide analogues of ?-amyloid and methods of using said analogues for neuroprotection are described herein. The ?-amyloid peptide analogues have a sequence that is at least 50% identical to an N-terminal ?-amyloid core fragment. A pharmaceutical composition of the ?-amyloid peptide analogues in a pharmaceutically acceptable carrier can be administered to a subject for neuromodulation. The ?-amyloid peptide analogues, while lacking neurotoxicity, effectively provides for protective activity against ?-amyloid toxicity.
Type:
Application
Filed:
August 15, 2017
Publication date:
August 1, 2019
Inventors:
Robert A. Nichols, Kelly Forest, Victor J. Hruby