45th week of 2020 patent applcation highlights part 22 |
Patent application number | Title | Published |
20200347045 | CRBN LIGANDS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders. | 2020-11-05 |
20200347046 | NITROGEN-CONTAINING 6-MEMBERED CYCLIC COMPOUND - A novel compound represented by the following general formula (1), or a salt thereof, which has a superior EP | 2020-11-05 |
20200347047 | SOLID STATE FORM OF VALBENAZINE - Salts and solid state forms of Valbenazine, including Valbenazine ditosylate, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed. | 2020-11-05 |
20200347048 | Benzoquinoline Inhibitors of Vesicular Monoamine Transporter 2 - The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. | 2020-11-05 |
20200347049 | 6-5 FUSED RINGS AS C5a INHIBITORS - The present disclosure provides, inter alia, Compounds of Formula (I) | 2020-11-05 |
20200347050 | TETRAHYDROPYRAZOLOPYRIMIDINE COMPOUNDS - Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis. | 2020-11-05 |
20200347051 | SOLID FORMS OF A TOLL-LIKE RECEPTOR MODULATOR - The present disclosure provides solid forms, solvates and hydrates of (R)-2-((2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-1-ol, and methods of making. | 2020-11-05 |
20200347052 | INHIBITORS OF RAF KINASES - Provided herein are heteroaryl inhibitors of receptor tyrosine kinase effector (RAF), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of disease. | 2020-11-05 |
20200347053 | SUBSTITUTED PYRROLOPYRIDINES AS JAK INHIBITORS - The present invention relates to new pyrrolopyridine compounds having the structures of Formula (I)-(IV), wherein the R groups, A, B, C, D and n are as defined in the detailed description, and compositions and their application as pharmaceuticals for the treatment of disease. | 2020-11-05 |
20200347054 | SYNTHETIC METHODS FOR PREPARATION OF (S)-(2R,3R,11BR)-3-ISOBUTYL-9,10-DIMETHOXY-2,3,4,6,7,11B-HEXAHYDRO-1H-PYR- IDO[2,1,-A]lSOQUINOLIN-2-YL 2-AMINO-3-METHYLBUTANOATE DI(4-METHYLBENZENESULFONATE) - Provided herein are processes for the preparation of (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), or a solvate, hydrate, or polymorph thereof. | 2020-11-05 |
20200347055 | SYNTHETIC METHODS FOR PREPARATION OF (S)-(2R,3R,11BR)-3-ISOBUTYL-9,10-DIMETHOXY-2,3,4,6,7,11B-HEXAHYDRO-1H-PYR- IDO[2,1,-A]lSOQUINOLIN-2-YL 2-AMINO-3-METHYLBUTANOATE DI(4-METHYLBENZENESULFONATE) - Provided herein are processes for the preparation of (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), or a solvate, hydrate, or polymorph thereof. | 2020-11-05 |
20200347056 | SYNTHETIC METHODS FOR PREPARATION OF (S)-(2R,3R,11BR)-3-ISOBUTYL-9,10-DIMETHOXY-2,3,4,6,7,11B-HEXAHYDRO-1H-PYR- IDO[2,1,-A]lSOQUINOLIN-2-YL 2-AMINO-3-METHYLBUTANOATE DI(4-METHYLBENZENESULFONATE) - Provided herein are processes for the preparation of (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), or a solvate, hydrate, or polymorph thereof. | 2020-11-05 |
20200347057 | SYNTHETIC METHODS FOR PREPARATION OF (S)-(2R,3R,11BR)-3-ISOBUTYL-9,10-DIMETHOXY-2,3,4,6,7,11B-HEXAHYDRO-1H-PYR- IDO[2,1,-A]lSOQUINOLIN-2-YL 2-AMINO-3-METHYLBUTANOATE DI(4-METHYLBENZENESULFONATE) - Provided herein are processes for the preparation of (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), or a solvate, hydrate, or polymorph thereof. | 2020-11-05 |
20200347058 | S1PR2 ANTAGONISTS AND USES THEREFOR - Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. | 2020-11-05 |
20200347059 | IMIDAZO[4,5-C]PYRIDINE AND PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS SSAO INHIBITORS - A process for the preparation of a compound of formula (Ia) or a pharmaceutically acceptable salt, or N-oxide thereof | 2020-11-05 |
20200347060 | Process for the Preparation of Umeclidinium Bromide - The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed. | 2020-11-05 |
20200347061 | CLASS OF AMINO-SUBSTITUTED NITROGEN-CONTAINING FUSED RING COMPOUNDS, PREPARATION METHOD THEREFOR, AND USE THEREOF - The present invention discloses a class of amino-substituted nitrogen-containing fused ring compounds, a preparation method therefor, and a use thereof. The structure of the amino-substituted nitrogen-containing fused ring compounds of the present invention is as shown in formula (I) below, and each group therein is as defined in the specification. The amino-substituted nitrogen-containing fused ring compounds of the present invention are novel specific FGFR kinase inhibitors, having excellent inhibitory activity for FGFR-related tumor cell proliferation, and is applicable to the treatment of diseases such as tumors associated with FGFR kinase mutations or abnormal expressions. | 2020-11-05 |
20200347062 | PURINE BASED COMPOUNDS AS TOLL-LIKE RECEPTOR 9 ANTAGONIST - The present invention provides novel purine based compounds of formula 1, method of preparation of purine based compounds and its composition useful for inhibiting signalling through Toll-like receptors. These compounds are useful in inhibiting immune stimulation involving toll-like receptor 9 (TLR9). These can be used in treatment of autoimmune disease and inflammation where aberrant activation of TLR9 | 2020-11-05 |
20200347063 | SOLVATED FORMS OF A BRUTON?S TYROSINE KINASE INHIBITOR - Described herein are solvates of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the solvates, as well as methods of using the solvates, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2020-11-05 |
20200347064 | SYNTHESIS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the synthesis of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. | 2020-11-05 |
20200347065 | SALTS OF TAM INHIBITORS - The present application provides salt forms of N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-(pyridin-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide and N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxamide, which are useful as inhibitors of TAM kinases, as well as processes and intermediates related thereto. | 2020-11-05 |
20200347066 | TRICYCLIC AMINE COMPOUNDS AS CDK2 INHIBITORS - The present application provides tricyclic amine compounds, which are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same. | 2020-11-05 |
20200347067 | TRICYCLIC AMINE COMPOUNDS AS CDK2 INHIBITORS - The present application provides tricyclic amine compounds, which are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same. | 2020-11-05 |
20200347068 | SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE - The present disclosure provides novel heteroaryl compounds of formula (IV). Such compounds are useful for the treatment of cancers. | 2020-11-05 |
20200347069 | NOVEL CRYSTAL FORM OF ACALABRUTINIB AND PREPARATION METHOD AND USE THEREOF - The present disclosure relates to novel crystalline forms of acalabrutinib and processes for preparation thereof. The present disclosure also relates to pharmaceutical compositions containing acalabrutinib, use of acalabrutinib for preparing Bruton's tyrosine kinase inhibitor drug, and use of acalabrutinib for preparing drugs treating mantle cell lymphoma. The crystalline forms of the present disclosure have one or more improved properties compared with prior art, and have significant value for future drug optimization and development. | 2020-11-05 |
20200347070 | HETEROCYCLIC COMPOUND, PREPARATION METHOD AND USE THEREOF IN MEDICINE - Provided are a heterocyclic compound, a preparation method and the use thereof in medicine, and particularly involved are a heterocyclic compound for preventing and/or treating hypemricemia and gout, a preparation method and the use thereof in medicine. In particular, provided are a compound as shown in formula (I) and/or formula (II) or a tautomer thereof and a pharmaceutically acceptable salt thereof, a preparation method therefor and a method and the use thereof for treating hypemricemia and gout. | 2020-11-05 |
20200347071 | AMINOPYRROLOTRIAZINES AS KINASE INHIBITORS - The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications. | 2020-11-05 |
20200347072 | Tricyclic Compounds Useful to Treat Orthomyxovirus Infections - The present invention provides a compound of Formula (I) including pharmaceutically acceptable salts thereof: (I) and therapeutic uses of these compounds. The invention further provides pharmaceutical compositions comprising these compounds, compositions comprising these compounds with a therapeutic co-agent, and methods of using the compounds and compositions to treat viral infections. | 2020-11-05 |
20200347073 | SELECTIVE ESTROGEN RECEPTOR DEGRADERS - Novel selective estrogen receptor degraders (SERDs) according to the formula: | 2020-11-05 |
20200347074 | COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF - The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for ex ample through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein such as CEP250. These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of the target protein. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of target protein activity. | 2020-11-05 |
20200347075 | BIOACTIVE CONJUGATE, PREPARATION METHOD THEREFOR AND USE THEREOF - The disclosure relates to a bioactive molecule conjugate, preparation methods and use thereof, particularly relates to a novel bioactive molecule conjugate obtained by improving coupling of the drug and the targeting moiety in an ADC or SMDC, as well as its preparation method and use in the manufacture of a medicament for the treatment of a disease associated with an abnormal cell activity. | 2020-11-05 |
20200347076 | Biologically Active Taxane Analogs and Methods of Treatment by Oral Administration - The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents. | 2020-11-05 |
20200347077 | THIOPHENE END GROUPS OF NON-FULLERENE ACCEPTORS FOR ELECTRONIC AND PHOTONIC APPLICATIONS - Provided herein are small molecular acceptor compounds containing thiophene end groups, methods for their preparation and intermediates used therein, the use of formulations containing the same as semiconductors in organic electronic devices, especially in organic photovoltaic and organic field-effect transistor devices, and to organic electronic and organic photovoltaic devices made from these formulations. | 2020-11-05 |
20200347078 | HETEROCYCLYLMETHYLIDENE DERIVATIVES AND THEIR USE AS MODULATORS OF mGluR5 RECEPTORS - This invention relates to compounds of formula (I) and their use as allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction, such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related directly or indirectly to glutamate dysfunction. | 2020-11-05 |
20200347079 | NOVEL PTEFB INHIBITING MACROCYCLIC COMPOUNDS - The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). | 2020-11-05 |
20200347080 | NOVEL PROBE COMPOUNDS FOR FLUORESCENCE AND/OR CIRCULAR DICHROISM SENSOR FOR AMINE COMPOUNDS INCLUDING AMINO ALCOHOLS, AND SIMULTANEOUS ANALYSIS METHOD OF FLUORESCENCE AND CIRCULAR DICHROISM - The present disclosure relates to a novel probe compound, i.e., 1-(ortho-benzophenylaminoalkyl)-phenylboric acid, or its derivative for a fluorescence and/or circular dichroism (CD) sensor for amine compounds containing aminoalcohols. Also, the present disclosure relates to a simultaneous analysis method of fluorescence and CD of amine compounds containing aminoalcohols using the novel probe compound. | 2020-11-05 |
20200347081 | COMPOUND, DISPLAY PANEL AND DISPLAY APPARATUS - A compound according to Formula (1), | 2020-11-05 |
20200347082 | METHOD FOR PRODUCING TETRAALKOXYSILANE - An object of the present invention is to provide a method capable of producing a tetraalkoxysilane with a high energy efficiency and with a high yield. The present invention provides a method for producing a tetraalkoxysilane, the method including: a first step of reacting an alcohol with a silicon oxide; and a second step of bringing a vaporized component of the reaction mixture obtained in the first step into contact with a molecular sieve. | 2020-11-05 |
20200347083 | FUNCTIONALIZED ALUMINUM REAGENTS - The invention is directed to functionalized aluminum reagents of formula 1 | 2020-11-05 |
20200347084 | METHOD FOR THE MANUFACTURE OF ALKOXYSILYL-CONTAINING THIOCARBOXYLIC ACID ESTERS - There is provided herein a method for the manufacture of alkoxysilyl-containing thiocarboxylic acid ester which comprises reacting a thioester with a mercapto-functional alkoxysilane and/or an alkali metal salt, an alkaline earth metal salt, a trisubstituted ammonium salt of an alkoxysilyl-functional thiolate which uses economical and readily available reagents, avoids the use of phosgene or thionyl chloride reagents and produces byproducts that may be recycled. | 2020-11-05 |
20200347085 | Organic electroluminescent materials and devices - A compound comprising a first ligand L | 2020-11-05 |
20200347086 | ORGANOMETALLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME - Provided are an organometallic compound represented by Formula 1 and an organic light-emitting device including the same. The organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; an organic layer between the first electrode and the second electrode and including an emission layer; and at least one organometallic compound represented by Formula 1. | 2020-11-05 |
20200347087 | SYNTHESIS OF DESOSAMINES - The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof. | 2020-11-05 |
20200347088 | CO-CRYSTAL FORMS OF A NOVOBIOCIN ANALOG AND PROLINE - Disclosed are co-crystal forms of N-(2-(5-(((2R,3R,4S,5R)-3,4-dihydroxy-5-methoxy-6,6-dimethyltetra-hydro-2H-pyran-2-yl)oxy)-3′-fluoro-[1,1′-biphenyl]-2-yl)ethyl)-acetamide and L-proline or D-proline, their pharmaceutical compositions, processes of manufacture, and methods of use for treating neurodegenerative disorders such as diabetic peripheral neuropathy. | 2020-11-05 |
20200347089 | NOVEL GALACTOSIDE INHIBITOR OF GALECTINS - An α-D-galactopyranose compound of the general formula (1). The α-D-galactopyranose compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human. Furthermore, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human. | 2020-11-05 |
20200347090 | CD73 INHIBITORS - Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases. | 2020-11-05 |
20200347091 | METHOD FOR PREPARING CHOLIC ACID COMPOUND - The present application belongs to the field of pharmaceutical chemistry, and relates to a method for preparing a cholic acid compound. Specifically, the present application provides a process for preparing a compound as shown in formula I, comprising subjecting a compound of formula 2 to an oxidization reaction to obtain a compound of formula 3; attaching a trimethylsilyl group to the compound of formula 3 to obtain a compound of formula 4; reacting the compound of formula 4 with acetaldehyde to obtain a compound of formula 5; subjecting the compound of formula 5 to a catalytic hydrogenation reaction to obtain a compound of formula 6; and converting a cyano group of the compound of formula 6 to a carboxyl group to give the compound of formula I. The preparation method has high yield, requires less purification operations, and is suitable for industrial application. | 2020-11-05 |
20200347092 | BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF - The present invention provides compounds of Formula I, | 2020-11-05 |
20200347093 | IMPROVED METHOD FOR PURIFICATION OF IMMUNOGLOBULIN - The present invention relates to an improved method of purifying an immunoglobulin, and more particularly to a method of purifying an immunoglobulin which is capable of sufficiently removing impurities from an immunoglobulin-containing plasma protein sample through a simple process, comprising a single anion-exchange chromatography and a single cation-exchange chromatography. | 2020-11-05 |
20200347094 | Preparation Method of Activated or Solubilized Mutated Enzyme - A method for producing an active-form mutant enzyme, by specifying a protein of which a native form exhibits an enzyme activity but which has 10% or less enzyme activity of the native form when a gene of the protein is expressed to provide an inactive-form enzyme; determining a sequence conservation of amino acid residues in an amino acid sequence of the inactive-form enzyme and specifying amino acid residue(s) for which sequence conservation in the inactive-form enzyme is lower than sequence conservation of other amino acid(s) of the same residue; preparing a gene having a base sequence that codes for the amino acid sequence of the inactive-form enzyme in which at least one said specified amino acid residue is substituted by another amino acid with a higher sequence conservation; and expressing the gene to obtain an enzyme that exhibits an enzyme activity of the native form protein. | 2020-11-05 |
20200347095 | Methods for Treating Cancer - The invention relates to novel peptides having an HDM-2 targeting sequence that target the human minute binding protein-2. The invention also relates to fusion proteins comprising a HDM-2 targeting sequence. The invention also relates to methods of using the peptides to treat cancer. | 2020-11-05 |
20200347096 | CYCLIC PEPTIDE AND A MEDICAMENT, EXTERNAL PREPARATION AND COSMETIC COMPRISING SAID CYCLIC PEPTIDE - The present invention is aimed for providing a novel peptide with a high drug efficacy and strong effect, a medicament or external preparation comprising it, specifically a prophylactic or therapeutic for dermatitis, rhinitis or alopecia, or a hair growth stimulant, a hair growing agent, an antipruritic or a skin-care product. The present invention achieved said aim by providing a cyclic peptide having an amino acid sequence expressed by the Formula I or a derivative thereof or a pharmaceutically acceptable salt thereof, wherein the amino acid sequence does not have a peptide bond that is not between the amino acids constituting the amino acid sequence. | 2020-11-05 |
20200347097 | Process for the Preparation of Cyclic Depsipeptides - Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R | 2020-11-05 |
20200347098 | POLYPEPTIDE COMPRISING CELL-PENETRATING SEQUENCE AND COMPOSITION COMPRISING SAME - The present application provides: a polypeptide characterized by having an ability of penetrating into a cell and the structure represented by Formula (I) | 2020-11-05 |
20200347099 | Synthetic Beta-Amyloid Peptides Capable of Forming Stable Antigenic Oligomers - Synthetic Aβ peptides, oligomers, their methods of synthesis, and their applications are provided. The Aβ peptides can form stable, soluble oligomers important for the advancement of knowledge, detection, and treatment of Alzheimer's disease. Antibodies specific to oligomeric Aβ and their methods of synthesis are also described. | 2020-11-05 |
20200347100 | NON-NATURALLY OCCURRING CAPSIDS FOR DELIVERY OF NUCLEIC ACIDS AND/OR PROTEINS - Provided herein are non-naturally occurring self-assembling polypeptides for transferring nucleic acids and/or proteins to a cell, pharmaceutical compositions comprising such polypeptides, and methods for treatment comprising use of such compositions. The methods for producing polypeptide compositions may include combining in a solution, unassembled recombinant GAG-like proteins, nucleic acids and/or proteins in low salt conditions; and increasing the ionic strength of the solution. | 2020-11-05 |
20200347101 | CONJUGATABLE DESMOGLEIN 2 (DSG2) BINDING PROTEINS AND USES THEREFOR - The disclosure provides polypeptide compositions that open a tumor tight junction, comprising an adenovirus fiber polypeptide shaft domain motif; a sequence that opens a tumor tight junction; a multimerization domain; and a conjugatable moiety. In another aspect, the multimerization domain comprises a conjugatable moiety. | 2020-11-05 |
20200347102 | COMPOSITIONS COMPRISING RECOMBINANT BACILLUS CELLS AND ANOTHER BIOLOGICAL CONTROL AGENT - The present invention relates to a composition comprising a) recombinant exosporium-producing | 2020-11-05 |
20200347103 | MHC MULTIMERS IN TUBERCULOSIS DIAGNOSTICS, VACCINE AND THERAPEUTICS - The present invention relates to MHC peptide complexes and uses thereof in the diagnosis of, treatment of or vaccination against a disease in an individual. More specifically the invention discloses MHC complexes comprising | 2020-11-05 |
20200347104 | WHEAT COMPRISING MALE FERTILITY RESTORER ALLELES - A wheat transgenic plant carrying restorer of fertility genes specific to | 2020-11-05 |
20200347105 | GENOME ENGINEERING WITH CRISPR-CAS SYSTEMS IN EUKARYOTES - Disclosed herein are Type I Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)/CRISPR-associated (Cas) programmable systems and methods of using said Type I CRISPR/Cas programmable systems for activating gene expression, repressing gene expression, and gene editing. The disclosure relates to compositions that include Type I CRISPR-Cas fusion proteins designed for transcriptional activation, transcriptional repression, and/or gene editing of target genes in eukaryotic cells. The disclosure relates to Type I Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)/CRISPR-associated (Cas) transcriptional activation system related compositions and methods of using said Type I CRISPR/Cas transcriptional activation system related compositions for activating gene expression. The disclosure relates to compositions that include a Type I CRISPR-Cas fusion protein designed for transcriptional activation of target genes in eukaryotic cells. | 2020-11-05 |
20200347106 | COMPOSITIONS AND METHODS OF USING ISLET NEOGENESIS PEPTIDES AND ANALOGS THEREOF - The invention provides peptides and analogs of INGAP and HIP peptides. The peptides and analogs can be used in methods for treating various diseases and conditions. Such diseases and conditions can include impaired pancreatic function, treating a metabolic disease, for example, diabetes, both type 1 and type 2 diabetes, islets induction, expansion and proliferation for transplantation, promoting neuroprotection or nerve regeneration, promoting liver regeneration or inhibiting inflammation. | 2020-11-05 |
20200347107 | PACAP STABILIZED PEPTIDE - The purpose of the present invention is to provide a PACAP peptide having increased stability. The problem is solved by the discovery that substituting a carboxy group of the position 3 and/or position 8 aspartic acid in the PACAP sequence by tetrazole significantly enhances stability. | 2020-11-05 |
20200347108 | Peptide Conjugates Incorporating Urea Elements and Their Use as Vaccines - The present invention provides compounds that may be useful for provoking an immune response against an epitope in a subject in need thereof | 2020-11-05 |
20200347109 | De Novo Design of Potent and Selective Interleukin Mimetics - De novo designed polypeptides that bind to IL-2 receptor βγ | 2020-11-05 |
20200347110 | Composition and Methods for Stimulating Gastrointestinal Motility - The present invention relates to a method of treating a transient impairment of the motility of the gastrointestinal system resulting from postoperative ileus in a patient wherein said method includes the step of administering a therapeutically effective amount of a peptidyl analog of ghrelin to said patient. | 2020-11-05 |
20200347111 | N-TERMINAL FUSION PARTNER FOR PRODUCING RECOMBINANT POLYPEPTIDE, AND METHOD FOR PRODUCING RECOMBINANT POLYPEPTIDE USING SAME - Disclosed are a novel N-terminal fusion partner, a fusion polypeptide including the fusion partner and a target polypeptide, and a method for producing a target polypeptide using the same. The novel fusion partner can enhance the yield of a target polypeptide (recombinant polypeptide) compared to the conventional fusion partners. Using the novel fusion partner is particularly beneficial in producing a target polypeptide having a relatively low molecular weight and an easily degradable amino terminus based on genetic recombination technologies. Further, the novel fusion polypeptide including the fusion partner can be expressed as inclusion bodies in a host cell and protected against proteases or the like in a host cell, which makes the target polypeptide produced stably. Therefore, in comparison to the conventional fusion partners, the novel fusion partner can be used to provide a method for producing a recombinant peptide with improved stability and yield. | 2020-11-05 |
20200347112 | COMPOSITIONS OF ENGINEERED EXOSOMES AND METHODS OF LOADING LUMINAL EXOSOMES PAY-LOADS - The present invention relates to methods of preparing a therapeutic exosome using proteins newly identified to be enriched in the lumen of exosomes. Specifically, the present invention provides methods of localizing a therapeutic peptide or protein in exosomes. The methods involve generation of lumen-engineered exosomes that include one or more of the exosome proteins at higher concentrations, a modification or a fragment of the exosome protein, or a fusion protein of the exosome protein and a therapeutic or cargo protein. | 2020-11-05 |
20200347113 | EPHA3 AND MULTI-VALENT TARGETING OF TUMORS - Provided herein is a construct comprising, in combination: an EphA3, EphA2 and/or EphB2 binding ligand; and at least one effector molecule. In some embodiments, the at least one effector molecule comprises a therapeutic agent, a nanoparticle, a detectable group, a lipid, or a liposome. In some embodiments, the construct is a fusion protein and/or a covalent conjugate. Further provided is a construct comprising, in combination: a ligand that binds to EphA2, EphA3 and/or EphB2; a ligand that binds to IL-13Rα2; and at least one effector molecule. Also provided are methods of use thereof for treating cancer. | 2020-11-05 |
20200347114 | MHC Peptide Complexes and Uses Thereof in Infectious Diseases - Novel compounds carrying ligands capable of binding to counter receptors on relevant target cells are disclosed. The compounds possess a number of advantageous features, rendering them very suitable for a wide range of applications, including use as detection systems, detection of relevant target cells as well as a number of other methods. In particular, novel MHC complexes comprising one or more MHC molecules are disclosed. The affinity and specificity of the MHC-peptide complexes are surprisingly high. The possibility of presenting to the target cells a plurality of MHC-peptide complexes makes the MHC complexes according to the present invention an extremely powerful tool e.g. in the field of therapy and diagnosis. The invention generally relates to the field of therapy, including therapeutic methods and therapeutic compositions. Also comprised by the present invention is the sample-mounted use of MHC complexes and MHC multimers. | 2020-11-05 |
20200347115 | NOVEL TNF FAMILY LIGAND TRIMER-CONTAINING ANTIGEN BINDING MOLECULES - The invention relates to novel TNF family ligand trimer-containing antigen binding molecules comprising two different fusion polypeptides that comprise a spacer domain, an antigen binding domain and three ectodomains of a TNF ligand member or fragments thereof, wherein two of said ectodomains are separated from each other by a spacer domain comprising at least 25 amino acids and wherein the two fusion polypeptides are covalently associated to each other in the spacer domain | 2020-11-05 |
20200347116 | VON WILLEBRAND FACTOR PROTEINS FOR TREATING BLEEDING DISORDERS - A recombinant von Willebrand Factor (VWF) protein comprising one or more mutations and uses thereof are described. A recombinant protein complex comprising a von Willebrand factor sequence and one artificial Factor VIII sequence is described. A recombinant protein complex comprising a Factor VIII sequence and one artificial von Willebrand sequence is described. A recombinant protein complex is described that includes one artificial von Willebrand factor sequence and one artificial Factor VIII sequence. Also described are nucleic acid sequences and a vector encoding a VWF sequence and a pharmaceutical composition for inducing blood clotting that includes a VWF protein. | 2020-11-05 |
20200347117 | LIBRARIES OF GENETIC PACKAGES COMPRISING NOVEL HC CDR1, CDR2, AND CDR3 AND NOVEL LC CDR1, CDR2, AND CDR3 DESIGNS - Provided are compositions and methods for preparing and identifying antibodies having CDR3s that vary in sequence and in length from very short to very long which in certain embodiments may bind to a carbohydrate moiety or the active site of an enzyme. Libraries coding for antibodies with the CDR3s are also provided. The libraries can be provided by modifying a pre-existing nucleic acid library. | 2020-11-05 |
20200347118 | METHOD TO IMPROVE VIRUS FILTRATION CAPACITY - The present invention relates to the field of protein purification. In particular, the invention concerns methods for increasing the filtration capacity of virus filters, by combined use of endotoxin removal and cation-exchange media in the prefiltration process. | 2020-11-05 |
20200347119 | HYBRIDOMA CELL STRAIN SECRETING NIFURSOLOL RESIDUE MARKER MONOCLONAL ANTIBODY - A hybridoma cell strain secreting a nifursol residue marker monoclonal antibody prepared in the following way: BALB/c mice are subjected to the first immunization with a complete Freund's adjuvant, subjected to booster immunization with an incomplete Freund's adjuvant for four times, and subjected to rush immunization once with nifursol residue marker complete antigen without a Freund's adjuvant so that the BALB/c mice are immunized; the spleen cells of the immunized mice with high titer and low IC50 were fused with mouse myeloma cells by a PEG method, and the fused cells are screened through indirect competitive ELISA and subcloned three times. The monoclonal antibody secreted by this cell strain has good specificity and detection sensitivity (IC50 value of 2 μg/L) to the nifursol residue marker and can be used for residue detection of the nifursol residual marker in food. | 2020-11-05 |
20200347120 | DOSAGE REGIMENS FOR AND COMPOSITIONS INCLUDING ANTI-RSV ANTIBODIES - In one aspect, this disclosure describes methods of treating or preventing RSV infection in a patient in need thereof. The methods including dosing regiments for administering a composition including a fixed dose of an anti-RSV monoclonal antibody or an antigen binding fragment thereof. In another aspect, this disclosure describes pharmaceutical compositions for the treatment or prevention of RSV infection. In yet another aspect, this disclosure describes a pharmaceutical unit dose including nirsevimab. | 2020-11-05 |
20200347121 | COLL2-1 PEPTIDE AND ITS NITRATED FORM AS THERAPEUTIC TARGETS FOR OSTEOARTHRITIS TREATMENT - The present invention provides a medicament comprising as active ingredient an inhibitor of Coll2-1 peptide activity and/or an inhibitor of Coll2-1NO | 2020-11-05 |
20200347122 | CELL CULTURE MEDIA AND METHODS OF ANTIBODY PRODUCTION - Cell culture media are provided herein as are methods of using the media for cell culture and antibody production from cells. Compositions comprising antibodies and fragments thereof, produced by the methods herein are also provided. | 2020-11-05 |
20200347123 | METHODS FOR TREATING SPINAL CORD INJURY AND PAIN - Disclosed herein are anti-RGMa antibodies and methods of using these antibodies to treat spinal cord injury, including promoting axonal regeneration, functional recovery, or both and to treat pain, including neuropathic pain arising from spinal cord injury. | 2020-11-05 |
20200347124 | METHODS AND COMPOSITIONS FOR TREATING LUNG INFLAMMATION - The compositions and methods described herein include agents that inhibit inflammasome signaling in the mammal such as antibodies directed against inflammasome components used alone or in combination with extracellular vesicle uptake inhibitor(s). Also described herein are compositions and methods of use thereof for treating multiple sclerosis. | 2020-11-05 |
20200347125 | POROUS AFFINITY HYDROGEL PARTICLES FOR REDUCING THE BIOAVAILABILITY OF SELECTED BIOLOGICAL MOLECULES - A hydrogel particle that has an average cross-sectional diameter in the range from 1 micrometer (μm) to 1000 μm, wherein the particle includes a first polymer network with an average mesh size that allows diffusion of a molecule with an hydrodynamic radius of 1000 nanometer (nm) or less into the first polymer network and which particle includes one or more binding molecules that are immobilized by the polymer network. The hydrogel particle preferably has wherein the first polymer network has an average mesh size that prevents diffusion of a molecule with an average hydrodynamic radius of more than 1000 nm to diffuse into the first polymer network, preferably the mesh size prevents diffusion of a molecule with an average hydrodynamic radius of more than 100 nm, and preferably more than 5 nm. Methods for reducing the bioavailability of one or more soluble biological molecules in a biological system by using the described hydrogel particle. | 2020-11-05 |
20200347126 | Production of Biosimilar Ustekinumab In CHO Cells - The present invention relates to a method for producing an ustekinumab antibody in CHO cells. It further relates to the use of the produced antibody in the treatment of plaque psoriasis, psoriatic arthritis and inflammatory bowel disease. | 2020-11-05 |
20200347127 | IL-17A BINDING PROTEINS - Binding molecules to IL-17A. The binding molecules are useful in the treatment of disorders, for example psoriasis. | 2020-11-05 |
20200347128 | MODULATING THE EFFECTS OF GAMMA-C-CYTOKINE SIGNALING FOR THE TREATMENT OF ALOPECIA AND ALOPECIA ASSOCIATED DISORDERS - The γc-family cytokines, Interleukin-2 (IL-2), Interleukin-4 (IL-4), Interleukin-7 (IL-7), Interleukin-9 (IL-9), Interleukin-15 (IL-15), and Interleukin-21 (IL-21), are associated with important human diseases, such as alopecia and alopecia associated disorders. Compositions, methods, and kits to modulate signaling by at least one γc-cytokine family member for inhibiting, ameliorating, reducing a severity of, treating, delaying the onset of, or preventing at least one alopecia related disorder are described. | 2020-11-05 |
20200347129 | Anti-Marinobufagenin Antibodies and Uses Thereof - The present disclosure provides chimeric, humanized and human monoclonal antibodies (mAbs) and fragments thereof that specifically bind to marinobufagenin (MBG) with high affinity. The anti-MBG mAbs and fragments thereof can be used to treat MBG-associated disorders, including hypertensive disorders and fibrotic disorders, optionally in combination with an additional therapeutic agent. Furthermore, the anti-MBG mAbs and fragments thereof can be used for diagnostic purposes, including to detect MBG in biological samples and to diagnose MBG-associated disorders. | 2020-11-05 |
20200347130 | CD96 Antibody, Antigen-Binding Fragment and Pharmaceutical use Thereof - Provided are a CD96 antibody, an antigen-binding fragment and a pharmaceutical use thereof. Further provided are a murine antibody, a chimeric antibody and a humanized antibody comprising the CDR region of the CD96 antibody, and a pharmaceutical composition comprising the CD96 antibody and the antigen-binding fragment thereof, and the use of same as a drug. In particular, provided is a use of a humanized CD96 antibody in the preparation of a drug for treating CD96-related diseases or conditions. | 2020-11-05 |
20200347131 | ANTI-LAG-3 ANTIBODY AND USE THEREOF - The present invention relates to the field of treatment of diseases and immunology. Specifically, the present invention relates to an anti-LAG-3 antibody or an antigen-binding fragment thereof, nucleic acid molecules for encoding said antibody and fragment, and method for preparing said antibody and fragment. The anti-LAG-3 antibody or the antigen-binding fragment thereof according to the present invention has high specificity and high affinity to LAG-3, can effectively block the binding of LAG-3 to MHC II and/or FGL1, and can inhibit and/or block intracellular signaling mediated by LAG-3 binding to MHC II and/or FGL1. Therefore, the present invention further relates to a pharmaceutical composition comprising the antibody or the antigen-binding fragment thereof, and use of the pharmaceutical composition in the preparation of drugs. The drugs are used for improving the activity of immune cells and enhancing the immune response, or are used for preventing and/or treating tumors, infections or autoimmune diseases. | 2020-11-05 |
20200347132 | CONSTRAINED CONDITIONALLY ACTIVATED BINDING PROTEINS - The invention relates to COnditional Bispecific Redirected Activation constructs, or COBRAs, that are administered in an active pro-drug format. Upon exposure to tumor proteases, the constructs are cleaved and activated, such that they can bind both tumor target antigens (TTAs) as well as CD3, thus recruiting T cells expressing CD3 to the tumor, resulting in treatment. In some embodiments, the tumor target antigen is B7H3. | 2020-11-05 |
20200347133 | CD33-Binding Polypeptides and Uses Thereof - Provided herein are VHH-containing polypeptides that bind CD33. Uses of the VHH-containing polypeptides are also provided. | 2020-11-05 |
20200347134 | Antibodies Directed Against ICOS and Uses Thereof - The present invention provides antibodies directed against ICOS or a derivative thereof which neutralize ICOS engagement on Treg by inhibiting the fixation between ICOS and ICOS-L and abrogate proliferation of Treg induced by plasmacytoid dendritic cells. The present invention further provides antibodies directed against ICOS or a derivative thereof which induce IL-10 and IFNγ production, induce CD4+ T cells proliferation, reduce Tconv proliferation, and increase the immunosuppressive function of Treg. | 2020-11-05 |
20200347135 | SINGLE-DOMAIN ANTIBODIES AND VARIANTS THEREOF AGAINST PD-1 - Provided are constructs comprising a single-domain antibody (sdAb) moiety that specifically recognizes PD-1. Also provided are methods of making and using these constructs. | 2020-11-05 |
20200347136 | CONSTRAINED CYCLIC PEPTIDES AS INHIBITORS OF THE CD2:CD58 PROTEIN-PROTEIN INTERACTION FOR TREATMENT OF DISEASES AND AUTOIMMUNE DISORDERS - Chemicals and methods of treating autoimmune/inflammatory diseases, comprising administering to a patient the functional groups of a CD58-targeted peptide grafted onto a cyclic scaffold. An additional embodiment includes wherein one or more of the functional groups of the peptide bind to CD58. An additional embodiment includes wherein the scaffold is chosen from the group of sunflower trypsin inhibitor (SFTI) and theta-defensins. | 2020-11-05 |
20200347137 | BISPECIFIC ANTIBODIES AND METHODS OF MAKING AND USING THEREOF - The disclosure provides bispecific antibodies having the binding specificity to at least two of human CTLA4, PD-1 or PD-L1. In one embodiment, the bispecific antibody comprises IgG domains having heavy chains and light chains, and two scFv components being connected to either C-terminal of the heavy chains or N-terminal of the light chains, wherein the IgG domains have the binding specificity to a first antigen, wherein the scFv components have the binding specificity to a second antigen, and wherein the first antigen and the second antigen are different and are independently selected from a-CTLA4, α-PD-1, and α-PD-L1. | 2020-11-05 |
20200347138 | DENDRITIC CELLS-TARGETING VACCINE - The present disclosure relates to recombinant single chain fragment variable (ScFv) binding to DEC-205 of dendritic cells having amino acid sequence selected from a group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, and SEQ ID NO: 9. Also disclosed are ScFv-antigen complex, a method for inducing immune response in a subject using the ScFv-antigen complex and a vaccine composition comprising the ScFv-antigen complex. The ScFv-antigen complex as disclosed herein can be used as immuno-contraceptives for mammals. | 2020-11-05 |
20200347139 | CLEC12a Binding Polypeptides and Uses Thereof - Provided herein are VHH-containing polypeptides that bind CLEC12a. Uses of the VHH-containing polypeptides are also provided. | 2020-11-05 |
20200347140 | COMPOSITIONS AND METHODS FOR TREATING CANCER WITH ANTI-EGFR ANTIBODIES - The present invention provides methods and uses of anti-EGFR antibody compositions for treatment of cancers that are negative for certain mutations in RAS, BRAF, and the EGFR extracellular domain and are resistant to other anti-EGFR therapies. | 2020-11-05 |
20200347141 | MONOCLONAL ANTIBODIES TO FIBROBLAST GROWTH FACTOR RECEPTOR 2 - The present invention is directed toward a monoclonal antibody to fibroblast growth factor receptor 2, a pharmaceutical composition comprising same, and methods of treatment comprising administering such a pharmaceutical composition to a patient. | 2020-11-05 |
20200347142 | CD123-Binding Polypeptides and Uses Thereof - Provided herein are VHH-containing polypeptides that bind CD123. Uses of the VHH-containing polypeptides are also provided. | 2020-11-05 |
20200347143 | NOVEL TNFR AGONISTS AND USES THEREOF - The present invention relates to a new class of TNFR agonist comprising multiple binding portions to two different parts of the same TNFR. The present invention also relates to methods of activating components of the immune system in a patient via the administration of a TNFR agonist according to the present invention as well as the use of such materials for further therapeutic and other purposes. | 2020-11-05 |
20200347144 | 4-1BB ANTIBODY AND PREPARATION METHOD AND USE THEREOF - Provided in the present invention are a 4-1BB antibody and a preparation method and the use thereof. In particular, provided in the present invention are a 4-1BB antibody, which has high affinity to 4-1BB protein, can effectively activate the signal downstream of the 4-1BB and significantly increase expression quantities of IFN-γ and IL-2 in human mixed lymphocytes or T lymphocytes, and can be used to treat cancers and autoimmune diseases. | 2020-11-05 |