30th week of 2021 patent applcation highlights part 25 |
Patent application number | Title | Published |
20210230151 | Crystalline Forms of 4-(5-(4,7-Dimethylbenzofuran-2-YL)-1,2,4-Oxadiazol-3-YL)Benzoic Acid and Processes for Their Preparation - The present invention pertains generally to the field of therapeutic compounds, and more specifically to crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (referred to herein as “BHBA-001”), which, inter alia, is a (selective) retinoic acid receptor beta (RΛRβ) (e.g., RΛRβ2) agonist. The present invention also pertains to pharmaceutical compositions comprising such crystalline forms, and the use of such crystalline forms and compositions, both in vitro and in vivo, to (selectively) activate RΛRβ (e.g., RΛRβ2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RARβ (e.g., RΛRβ2), that are ameliorated by the activation of RΛRβ (e.g., RΛRβ2), etc., including, e.g., neurological injuries such as spinal cord injuries. | 2021-07-29 |
20210230152 | ADDITION SALT OF S1P1 RECEPTOR AGONIST AND CRYSTAL FORM THEREOF, AND PHARMACEUTICAL COMPOSITION - Disclosed in the present application are a salt form and a crystal form of an S1P1 receptor mediated disease or symptom drug 1-{2-fluoro-4-[5-(4-isobutylphenyl)-1,2,4-oxadiazole-3-yl]benzyl}-3-azetidinecarboxylic acid (formula A). Also disclosed in the present invention are a preparation method for the salt form or the crystal form, a pharmaceutical composition of the salt form or the crystal form, and use of the salt form or the crystal form in the preparation of a drug for treating and/or preventing an S1P1 receptor mediated disease or symptom. | 2021-07-29 |
20210230153 | ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS AND USES THEREOF - The present invention provides AHR agonists, compositions thereof, and methods of using the same. | 2021-07-29 |
20210230154 | COMPOUNDS AND USES THEREOF - The present disclosure features compounds useful for the treatment of BAF complex-related disorders. | 2021-07-29 |
20210230155 | PROCESS FOR PREPARATION OF ((3R,11BR)-1,3,4,6,7,11B-HEXAHYDRO-9,10-DI(METHOXY-D3)-3-(2-METHYLPROPYL)- -2H-BENZO[A]QUINOLIZIN-2-ONE - The present invention provides a process for preparation of deutetrabenazine using tetrabenazine as starting material. | 2021-07-29 |
20210230156 | NOVEL HUMAN DIHYDROOROTATE DEHYDROGENASE (hDHODH) INHIBITORS AND THEIR USE IN TARGETING ONCOLOGICAL DISEASES SENSITIVE TO PYRIMIDINE STARVATION - Compounds of formulae (I) and (II) | 2021-07-29 |
20210230157 | PAIN TREATING COMPOUNDS AND USES THEREOF - The present invention relates to compounds useful in the modulation of ion channel activity in cells. The invention also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation. | 2021-07-29 |
20210230158 | INHIBITORS OF RORgamma - The present disclosure relates to processes for the production of salts and crystalline forms of a compound having the formula. | 2021-07-29 |
20210230159 | 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE COMPOUNDS - The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders. | 2021-07-29 |
20210230160 | PHOSPHODIESTERASE INHIBITORS - Provided herein are compounds and methods for modulating the phosphodiesterase PDE4. More particularly, provided are selective inhibitors PDE4 and the uses of such inhibitors in regulating diseases and disorders, e.g., to treat cancer, inflammatory diseases, neurological diseases, neurodegenerative diseases, and addiction. | 2021-07-29 |
20210230161 | COMPOUNDS FOR INHIBITING EGFR KINASE, PREPARATION METHODS AND USES THEREOF - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. The compounds can selectively inhibit the activity of epidermal growth factor receptor (EGFR) mutants, and shows good inhibitory effect towards mutant EGFR and anti-proliferative activity against cancer cells. Thus they can be used for treating tumors and related diseases. | 2021-07-29 |
20210230162 | SPIRO COMPOUNDS AS INHIBITORS OF KRAS - Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer. | 2021-07-29 |
20210230163 | TYK2 INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders. | 2021-07-29 |
20210230164 | IMIDAXOPYROLONE COMPOUND AND APPLICATION THEREOF - Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof. (I-1), (I-2) | 2021-07-29 |
20210230165 | MODULATORS OF ION CHANNEL RECEPTORS AND USES THEREOF - Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation. | 2021-07-29 |
20210230166 | 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AS BTK INHIBITORS - The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) | 2021-07-29 |
20210230167 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - The present invention includes novel organic materials comprising indolo[2,3-c]carbazole linked to an aromatic heterocycle via a carbazole linker. These materials may be useful as host materials for PHOLED devices. | 2021-07-29 |
20210230168 | PRC2 INHIBITORS - The present invention relates to compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention. | 2021-07-29 |
20210230169 | COMPOUNDS FOR USE IN THE TREATMENT OF FASCIOLIASIS - The present invention relates to compounds and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of | 2021-07-29 |
20210230170 | KRAS G12C INHIBITORS - The present invention relates to compounds that, inhibit KRas G12C, In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor. | 2021-07-29 |
20210230171 | SELECTIVE A2A RECEPTOR ANTAGONIST - The present invention relates to a selective A | 2021-07-29 |
20210230172 | SYNTHETICALLY MODIFIABLE ION CHANNELS - A new class of ordered functional nanoporous material (OFNMs) with a unique combination of electronic conductivity, gas transport ability, and ion transport properties are provided. The OFNM provided is highly ordered and contains nanometer scale pores lined with nitrogen atoms. The pores have dimensions of from 1.2 nm to 82 nm of longest linear extent across the pore. The functionality within the pore is controlled through selection of groups that extend into the pore. The degree of conjugated aromaticity is readily controlled to adjust the electrical conductivity properties of the resulting structure. By adjusting the groups external to the pore, three-dimensional structures are formed that are organic mimics of zeolites, metal organic frameworks (MOF), or perovskites. | 2021-07-29 |
20210230173 | HETEROCYCLIC LSF INHIBITORS AND THEIR USES - The present invention is directed to heterocyclic SV40 Factor (LSF) inhibitors and their uses. In some implementations, the present invention discloses small-molecule compounds of Formula (I). In some implementations, the compounds of Formula (I) are used in methods for inhibiting LSF in a subject. In some implementations, the compounds of Formula (I) are used in methods for treating cancer in a subject. | 2021-07-29 |
20210230174 | SPIROCYCLIC TETRAHYDROQUINAZOLINES - The present disclosure provides compounds represented by Formula I: | 2021-07-29 |
20210230175 | METHODS OF MAKING LOW ODOR CHOLINE SALTS OF AN ORGANIC COMPOUND - Methods of making low odor choline salts of an organic compound, for example, choline ellagate compound(s), and uses and formulations thereof. | 2021-07-29 |
20210230176 | HEPATITIS B ANTIVIRAL AGENTS - The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: | 2021-07-29 |
20210230177 | SYNTHESIS OF HALICHONDRINS - The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A) | 2021-07-29 |
20210230178 | TRIOXACARCIN ANALOGS AND DIMERS AS POTENT ANTICANCER AGENTS - In one aspect, the present disclosure provides trioxacarcin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein as well as dimers of the compounds described herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. | 2021-07-29 |
20210230179 | THIENO[2,3-B]PYRIDINE DERIVATIVES AS EPAC INHIBITORS AND THEIR PHARMACEUTICAL USES - The present invention relates to thieno[2,3-b]pyridine derivatives for use in the treatment and/or the prevention of a disease selected from the group consisting of inflammation, cancer, vascular diseases, kidney diseases, cognitive disorders, pain, infections, obesity, and cardiac diseases. Indeed, the inventors found that thieno[2,3-b]pyridine derivatives of the invention are inhibitors of the Epac protein and can thus be useful for the prevention and/or treatment of diseases wherein the Epac protein is involved. Particularly, the inventors showed that thieno[2,3-b]pyridine derivatives of the invention are potent and non-competitive inhibitors of Epac and demonstrated that they also inhibit the activation of Epac downstream effectors such as Rap1 in cells. | 2021-07-29 |
20210230180 | POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 - Described are positive allosteric modulators of muscarinic acetylcholine receptor M | 2021-07-29 |
20210230181 | CRYSTAL FORMS OF THIOPHENE DERIVATIVES - Disclosed are polymorph, crystal form III and crystal form IV of compound (S)-N-[5-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4,6-dioxo-5,6-dihydro-4H-thieno[3,4-c]pyrrole-1-yl]acetamide. | 2021-07-29 |
20210230182 | NOVEL COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME - A novel compound of the following Chemical Formula 1, and an organic light emitting device comprising the same. | 2021-07-29 |
20210230183 | COMPOSITIONS AND METHODS FOR TREATING CANCER - K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer. | 2021-07-29 |
20210230184 | MCL-1 INHIBITORS AND METHODS OF USE THEREOF - Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 | 2021-07-29 |
20210230185 | 7-PHENYLETHYLAMINO-4H-PYRIMIDO[4,5-D][1,3]OXAZIN-2-ONE COMPOUNDS AS MUTANT IDH1 AND IDH2 INHIBITORS - A compound, as defined herein, or pharmaceutical composition containing the compound, for use in treating IDH1 or IDH2 mutant cancer and having the structure: (I). | 2021-07-29 |
20210230186 | COMPOSITIONS AND METHODS FOR THE DELIVERY OF THERAPEUTICS - The present invention provides compositions and methods for the delivery of antivirals to a cell or subject. | 2021-07-29 |
20210230187 | PROCESS FOR PREPARING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVE AND CRYSTAL THEREOF - The present invention provides a process for preparing a compound of the formula (II): | 2021-07-29 |
20210230188 | CRYSTAL FORM OF TRI-CYCLE COMPOUND AND APPLICATION THEREOF - Disclosed are crystal form A and crystal form B of a compound represented by formula (I), and application thereof in the preparation of medicaments for treating HBV-related diseases. | 2021-07-29 |
20210230189 | COMPOUNDS THAT INHIBIT MCL-1 PROTEIN - Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, | 2021-07-29 |
20210230190 | COMPOUNDS AND USES THEREOF - The present disclosure features compounds useful for the treatment of BAF complex-related disorders. | 2021-07-29 |
20210230191 | FORMATION OF METAL-ORGANIC FRAMEWORKS - In some embodiments, the present disclosure pertains to a method of forming metalorganic frameworks. In some embodiments, the method includes exposing a plurality of zerooxidation state metal atoms to an oxidizing agent. In some embodiments, the exposing facilitates oxidation of the plurality of zero-oxidation state metal atoms to a plurality of metallic ions. In some embodiments, the plurality of metallic ions react with a plurality of ligands to form the metal-organic frameworks. In some embodiments, the formed metal-organic frameworks comprise one or more metals and one or more ligands coordinated with the one or more metals. | 2021-07-29 |
20210230192 | METHOD FOR PREPARING 18F-BPA AND INTERMEDIATE - A method for preparing | 2021-07-29 |
20210230193 | PRECURSOR COMPOUNDS FOR ATOMIC LAYER DEPOSITION (ALD) AND CHEMICAL VAPOR DEPOSITION (CVD) AND ALD/CVD PROCESS USING THE SAME - The present invention relates to precursor compounds, and more particularly to nonpyrophoric precursor compounds suitable for use in thin film deposition through atomic layer deposition (ALD) or chemical vapor deposition (CVD), and to an ALD/CVD process using the same. | 2021-07-29 |
20210230194 | SILOXANE DERIVATIVES OF AMINO ACIDS HAVING SURFACE-ACTIVE PROPERTIES - The present disclosure provides siloxane derivatives of amino acids that have surface-active properties. The amino acid can be naturally-occurring or synthetic, or they may be obtained via a ring-opening reaction of a lactam, such as caprolactam. The amino acid may be functionalized with a siloxane group to form a compound that is surface-active and has surfactant characteristics. The compounds have low critical micelle concentrations (CMC) as well as the ability to lower the surface tension of a liquid. | 2021-07-29 |
20210230195 | PRODRUG MODULATORS OF THE INTEGRATED STRESS PATHWAY - Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions. | 2021-07-29 |
20210230196 | Cyclopentane-Based Modulators of STING (Stimulator of Interferon Genes) - Compounds of the general formula (I): | 2021-07-29 |
20210230197 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - Provided are organometallic compounds. Also provided are formulations comprising these organometallic compounds. Further provided are OLEDs and related consumer products that utilize these organometallic compounds. | 2021-07-29 |
20210230198 | Metal Complexes, Methods, and Uses Thereof - Disclosed herein are metal complexes that exhibit multiple radiative decay mechanisms, together with methods for the preparation and use thereof. | 2021-07-29 |
20210230199 | SIMPLE METHOD FOR THE PURIFICATION OF LACTO-N-NEOTETRAOSE (LNnT) FROM CARBOHYDRATES OBTAINED BY MICROBIAL FERMENTATION - Provided is a method for the purification of lacto-N-neotetraose from other carbohydrates, characterized in that the method comprises the steps of subjecting an aqueous solution containing lacto-N-neotetraose to two membrane filtration steps using different membranes or of subjecting an aqueous solution containing lacto-N-neotetraose to a membrane filtration step and a continuous chromatography. | 2021-07-29 |
20210230200 | INDUSTRIAL METHOD FOR SIMULTANEOUSLY PREPARING STEVIA REBAUDIANA CHLOROGENIC ACID AND STEVIOSIDE - Disclosed is an industrial method for simultaneously preparing | 2021-07-29 |
20210230201 | CARBOHYDRATE BINDERS AND MATERIALS MADE THEREWITH - A binder comprising a polymeric binder comprising the products of a carbohydrate reactant and nucleophile is disclosed. The binder is useful for consolidating loosely assembled matter, such as fibers. Fibrous products comprising fibers in contact with a carbohydrate reactant and a nucleophile are also disclosed. The binder composition may be cured to yield a fibrous product comprising fibers bound by a cross-linked polymer. Further disclosed are methods for binding fibers with the carbohydrate reactant and polyamine based binder. | 2021-07-29 |
20210230202 | DITHIOLSACCHARIDE MUCOLYTIC AGENTS AND USES THEREOF - There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a dithiolsaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods. | 2021-07-29 |
20210230203 | Amphiphilic Kanamycin Compositions and Methods - The present relates to novel bioactive amphiphilic kanamycin compounds having the general formula of: | 2021-07-29 |
20210230204 | INDUSTRIAL UTILIZATION METHOD FOR STEVIA REBAUDIANA AND STEVIOSIDE AND CHLOROGENIC ACID OF STEVIA REBAUDIANA - An industrialization method for comprehensive utilization of | 2021-07-29 |
20210230205 | COMPOUNDS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS - Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory/infections disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugate which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eye, ocular surface or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders. | 2021-07-29 |
20210230206 | METHOD FOR SEPARATING NATURAL SUBSTANCE MIXTURES BY MEANS OF SCPC - The invention relates to a method for separating natural substance mixtures, in particular those consisting of plant extracts, and for isolating and purifying and obtaining same, by means of sequential centrifugal partition chromatography (sCPC). | 2021-07-29 |
20210230207 | NOVEL ALL-TRANS POLYENE AMPHOTERIC MACROLIDE - The present invention is directed to a process for purifying natamycin, to an all-trans polyene amphoteric macrolide, to a composition comprising said polyene amphoteric macrolide and to a process for preparing said polyene amphoteric macrolide. | 2021-07-29 |
20210230208 | INORGANIC SALTS OF NICOTINAMIDE MONONUCLOETIDE AS ANTI-AGING AGENTS - The present invention relates to inorganic salts of nicotinamide mononucleotides and compositions of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD | 2021-07-29 |
20210230209 | AMP-ACTIVATED PROTEIN KINASE ACTIVATING COMPOUNDS AND USES THEREOF - The present invention relates to pharmaceutical compounds, compositions and methods, especially as they relate to the treatment and/or prevention of conditions associated with activation of AMP-activated protein kinase, wherein the compound is of Formula (I): as described herein, including pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising such compounds, as well as methods to use these positions for treating indications including cancer, diabetes, ischemic injury, obesity, hyperlipidemia, and cardiac conditions. | 2021-07-29 |
20210230210 | METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS - The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. | 2021-07-29 |
20210230211 | 3-(4'-SUBSTITUTED)-BENZYL-ETHER DERIVATIVES OF PREGNENOLONE - The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO | 2021-07-29 |
20210230212 | METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER - In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. | 2021-07-29 |
20210230213 | ARAMCHOL SALTS - The present invention relates to salts of arachidyl amido cholanoic acid (Aramchol), pharmaceutical compositions comprising Aramchol salts, methods for their preparation, and methods of use thereof in medical treatment. | 2021-07-29 |
20210230214 | Potent aromatase inhibitors through fungal transformation of anti-cancer drug testolactone: An approach towards treatment of breast cancer - Biotransformation of an aromatase inhibitor, testolactone (1), yielded five new metabolites, 7α-hydroxy-3-oxo-13,17-secoandrosta-1,4-dieno-17,13α-lactone (2), 7β-hydroxy-3-oxo-13,17-seco-5β-androsta-1-eno-17,13α-lactone (3), 3α,11β-dihydroxy-13,17-seco-5β-androsta-17,13α-lactone (4), 4β,5β-epoxy-3β-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (5), and 4β,5β-epoxy-3α-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (6). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+ (estrogen-positive) breast-cancers and several other diseases caused by overexpression of aromatase enzyme. Metabolites 3 (IC | 2021-07-29 |
20210230215 | Thiophosphorodichloridate Reagents for Chemoselective Histidine Bioconjugation - Proteins are labeled by contacting the protein with a thiophosphorodichloridate reagent under conditions to effect chemoselective histidine conjugation. | 2021-07-29 |
20210230216 | METHOD FOR PURIFYING LONG CHAIN POLYPEPTIDE - A method for purifying a long chain polypeptide includes: 1) purification step: connecting two chromatographic columns in series to separate a crude product, in which the particle size of a packing in an upstream chromatographic column is larger than that in a downstream chromatographic column; optionally, the method further includes step 2): using the upstream chromatographic column in step 1) for a salt conversion, loading the target peak product obtained in step 1) and rinsing with 95-85% of the A2 and 5-15% of the B for 15-30 min for a desalination, wherein A2 phase is an acetic acid aqueous solution with a volume ratio of 0.05%-0.2%; B phase is an organic phase acetonitrile, and the detection wavelength is 230 nm. | 2021-07-29 |
20210230217 | OPTIMISED COMPOUNDS - The present invention relates to TLR2 agonist compounds and their compositions, and the use of such compounds and compositions in the prevention and/or treatment of respiratory infections, or diseases or conditions associated with viral or bacterial infections. | 2021-07-29 |
20210230218 | OLIGOPEPTIDE LINKER INTERMEDIATE AND PREPARATION METHOD THEREOF - The invention provides a new oligopeptide linker intermediate and a preparation method thereof. The preparation method of the oligopeptide intermediate is easily carried out under mild reaction conditions, and since almost no side reactions occur in the reaction, the method produces a high-purity product with fewer impurities and easy to be purified, achieving unexpected technical effects. | 2021-07-29 |
20210230219 | TOLL-LIKE RECEPTOR 2 LIGANDS AND METHODS OF MAKING AND USING THEREOF - Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation. | 2021-07-29 |
20210230220 | METHODS FOR THE SYNTHESIS OF ARGININE-CONTAINING PEPTIDES - Methods for the synthesis of arginine-containing peptides are provided. The methods include a deprotection step that minimizes the transfer of by-products deriving from cleaved sulfonyl-5 based side chain protecting groups from arginine to amino acids carrying electron rich side chains. | 2021-07-29 |
20210230221 | PROTEIN THERAPEUTICS FOR TREATMENT OF SENESCENT CELLS - Methods of generating conditionally active proteins that target senescent cells and which are conditionally active in an extracellular environment of a senescent cell. The methods include discovery methods using libraries of evolved proteins and assays employing physiological concentrations of components of bodily fluids. Also disclosed are conditionally active proteins for killing or removing senescent cells, pharmaceutical compositions employing these conditionally active proteins and methods for treatment of age-related diseases, conditions or disorders using same. The conditionally active proteins may be further evolved, conjugated to other molecules, masked, reduced in activity by attaching a cleavable moiety. | 2021-07-29 |
20210230222 | CYCLOPEPTIDE AND METHOD FOR PREPARING THE SAME - A method for preparing a cyclopeptide and a cyclopeptide preparing by the method are disclosed. The method includes the following steps: (A) providing compounds represented by the following formulas (I-1) and (I-2): | 2021-07-29 |
20210230223 | ARTIFICIALLY SYNTHESIZED PEPTIDE H-473 AND USE THEREOF - The invention discloses an artificially synthesized peptide H-473 and use thereof. The peptide H-473 has an amino acid sequence of RGLRGLR, a molecular weight of 827 Da and a PI of 12.30. The invention further discloses use of the peptide H-473 in anti-cancer, anti-senile dementia, analgesia and the like. The peptide H-473 provides scientific basis and direction for research and development of anti-cancer, anti-asthma, anti-senile dementia and analgesia, provides a valuable resource for studying mechanisms of anti-cancer, anti-asthma, anti-senile dementia, analgesia and anti-psoriasis, and provides a new direction for researching novel means for anti-cancer, anti-asthma, anti-senile dementia, analgesia, anti-psoriasis and anti-age-related macular degeneration (AMD). | 2021-07-29 |
20210230224 | CAR-T CELLS TARGETING GLIOMA STEM CELLS FOR THE TREATMENT OF GLIOBLASTOMA MULTIFORME - Disclosed are compositions and methods for targeted treatment of glioblastoma multiforme (GBM). In particular, chimeric antigen receptor (CAR) polypeptides are disclosed that can be used with adoptive cell transfer to target and kill Glioblastoma Stem Cells (GSCs). Also disclosed are immune effector cells, such as T cells or Natural Killer (NK) cells, that are engineered to express these CARs. Therefore, also disclosed are methods of providing an anti-tumor immunity in a subject with Glioblastoma Stem Cells (GSCs) that involves adoptive transfer of the disclosed immune effector cells engineered to express the disclosed CARs. | 2021-07-29 |
20210230225 | SELENIUM-CHELATING PEA OLIGOPEPTIDE, AND PREPARATION METHOD AND USE THEREOF - A selenium-chelating pea oligopeptide, a preparation method thereof and use thereof. After the selenium-chelating pea oligopeptide is subjected to digestion treatment in at least one of following three ways, a change rate of selenium content not more than 3% with respect to the selenium content before the digestion treatment: hydrolyzing for 4 hours by a pepsin at a pH value of 2 and a temperature of 37° C.; hydrolyzing for 6 hours by a trypsin at a pH value of 7.5 and a temperature of 37° C.; maintaining the temperature constant at 37° C., firstly hydrolyzing for 4 hours by the pepsin at a pH value of 2, and then continuing to hydrolyze for 6 hours by a trypsin at a pH value of 6.8. The preparation method thereof includes mixing and reacting an aqueous solution of pea oligopeptide and sodium selenite, and then being subjected to alcohol precipitation and drying. | 2021-07-29 |
20210230226 | ANTICANCER PEPTIDES - The present invention provides a peptide of formula (I) or a pharmaceutical salt thereof wherein “m”, “n”, “p”, and “q” represent integers and are selected from 0 and 1; and “r” is comprised from 1 to 10; a linker biradical of formula (II), which is connecting an alpha carbon atom of an amino acid located at position “i” in the peptide sequence of formula (I) with an alpha carbon atom of an amino acid located at position “i+4” or “i+7” in the peptide sequence of formula (I); a C-terminal end corresponding to —C(O)R | 2021-07-29 |
20210230227 | PEPTIDE FOR TREATING CANCER - A peptide is disclosed that has an amino acid sequence selected from SEQ ID NO: 22; SEQ ID NO: 23; SEQ ID NO: 24; SEQ ID NO: 25; SEQ ID NO: 26; SEQ ID NO: 27; SEQ ID NO: 28; SEQ ID NO: 29; SEQ ID NO: 30; SEQ ID NO: 31; SEQ ID NO: 32, SEQ ID NO: 33; SEQ ID NO: 34; SEQ ID NO: 35; SEQ ID NO: 36; SEQ ID NO: 37; SEQ ID NO: 38; SEQ ID NO: 39; SEQ ID NO: 40; SEQ ID NO: 41; SEQ ID NO: 42; SEQ ID NO: 43; and/or SEQ ID NO: 44. and retro-inversion peptides thereof. The peptides disclosed herein may be used to inhibit helicase activity and treat cancer, such as liver cancer, lung cancer, breast cancer, pancreatic cancer, or brain cancer. | 2021-07-29 |
20210230228 | HCMV VACCINE STRAIN - The present invention relates to nucleic acid molecules encoding a recombinant human cytomegalovirus (HCMV) strain, dense bodies produced by said HCMV strain and preparations of said dense bodies for use in medicine, particularly as a vaccine against HCMV. | 2021-07-29 |
20210230229 | VIRAL VECTORS EXHIBITING IMPROVED GENE DELIVERY PROPERTIES - The technology described herein provides viral capsid polypeptides bearing mutations that alters tissue tropism of a virus comprising the viral capsid polypeptide. In various embodiments, tissue tropisim to the heart, kidney, liver, lung, spleen, or blood is altered. | 2021-07-29 |
20210230230 | Soluble Forms of Hendra and Nipah Virus G Glycoprotein - This invention relates to soluble forms of G glycoprotein from Hendra and Nipah virus. In particular, this invention relates to compositions comprising soluble forms of G glycoprotein from Hendra and Nipah virus and also to diagnostic and therapeutic methods using the soluble forms of G glycoprotein from Hendra and Nipah virus. Further, the invention relates to therapeutic antibodies including neutralizing antibodies, and vaccines for the prevention and treatment of infection by Hendra and Nipah viruses. | 2021-07-29 |
20210230231 | VARIANT ADENO-ASSOCIATED VIRUSES AND METHODS OF USING - The present disclosure provides AAV variants that exhibit a preference for retrograde movement in neurons and methods of using such variants. | 2021-07-29 |
20210230232 | SITE-SPECIFIC BIO-CONJUGATION METHODS AND COMPOSITIONS USEFUL FOR NANOPORE SYSTEMS - The present disclosure relates to relates methods and associated compositions that provide fast, efficient site-selective conjugation of a protein, such as the pore-forming protein α-hemolysin, to a biomolecule, such as a DNA polymerase, and the use of such site-selective protein-biomolecule conjugates in nanopore devices and methods. | 2021-07-29 |
20210230233 | Method for the Treatment of a Relapsing-Remitting Condition - The present invention relates to a method for the acute treatment of a relapsing-remitting condition, the method comprising the step of administering to a subject in need thereof one or more doses of an effective amount of a peptide molecule as defined in claim | 2021-07-29 |
20210230234 | MALTOSE DEPENDENT DEGRONS, MALTOSE-RESPONSIVE PROMOTERS, STABILIZATION CONSTRUCTS, AND THEIR USE IN PRODUCTION OF NON-CATABOLIC COMPOUNDS - The present disclosure relates to the use of a maltose dependent degron to control stability of a protein of interest fused thereto at the post-translational level. The present disclosure also relates to the use of a maltose dependent degron in combination with a maltose-responsive promoter to control gene expression at the transcriptional level and to control protein stability at the post-translational level. The present disclosure also relates to the use of a stabilization construct that couples expression of a cell-growth-affecting protein with the production of non-catabolic compounds. The present disclosure further relates to the use of a synthetic maltose-responsive promoter. The present disclosure further provides compositions and methods for using a maltose dependent degron, a maltose-responsive promoter, and a stabilization construct, either alone or in various combinations, for the production of non-catabolic compounds in genetically modified host cells. | 2021-07-29 |
20210230235 | COMPOSITIONS AND METHODS FOR PRODUCING HIGH SECRETED YIELDS OF RECOMBINANT PROTEINS - The present disclosure relates to methods for producing recombinant proteins, as well as compositions used in and produced by such methods. Specifically, the present disclosure relates to methods for producing high secreted yields of recombinant proteins, and the compositions provided herein include recombinant host cells that comprise polynucleotide sequences encoding proteins operably linked to at least 2 distinct secretion signals. | 2021-07-29 |
20210230236 | Proteins for the Treatment of Epithelial Barrier Function Disorders - The disclosure relates to therapeutic proteins and pharmaceutical compositions comprising said proteins, which have utility in treating various human diseases. In particular aspects, the disclosed therapeutic proteins are useful for treating human gastrointestinal inflammatory diseases and gastrointestinal conditions associated with decreased epithelial cell barrier function or integrity. Further, the disclosed therapeutic proteins are useful for treating human inflammatory bowel disease, including inter alia, Crohn's disease and ulcerative colitis. | 2021-07-29 |
20210230237 | METHODS AND COMPOSITIONS FOR TREATING INFLAMMATION - This disclosure provides therapeutic compositions and methods for inducing an anti-inflammatory response and/or treating inflammation in the gastrointestinal tract and/or accumulating gut microbial antigen-specific anti-inflammatory T cells in a patient in need thereof. | 2021-07-29 |
20210230238 | THE CORE DOMAIN OF ANNEXINS AND USES THEREOF IN ANTIGEN DELIVERY AND VACCINATION - The present disclosure provides immunogenic compositions, such as vaccines, including DNA vaccines, and uses thereof, e.g., which include an annexin core domain to mediate efficient antigen delivery and antigen presentation in order to induce an antigen-specific immune response and/or to treat or prevent infectious diseases and/or cancer. | 2021-07-29 |
20210230239 | METHODS FOR TREATING MYELODYSPLASTIC SYNDROMES AND SIDEROBLASTIC ANEMIAS - 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. | 2021-07-29 |
20210230240 | B*44 RESTRICTED PEPTIDES FOR USE IN IMMUNOTHERAPY AGAINST CANCERS AND RELATED METHODS - The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules | 2021-07-29 |
20210230241 | MODIFIED NATURAL KILLER CELLS AND NATURAL KILLER CELL LINES HAVING INCREASED CYTOTOXICITY - NK cells and NK cell lines are modified to increase cytotoxicity, wherein the cells and compositions thereof have a use in the treatment of cancer. Production of modified NK cells and NK cell lines is via genetic modification to add mutant (variant) TRAIL ligand expression. | 2021-07-29 |
20210230242 | CYTOKINE FUSION PROTEINS AND USES THEREOF - The present application provides fusion proteins that comprise a cytokine fused to an albumin binding moiety. The fusion proteins may further comprise an antigen binding moiety such as a therapeutic antibody. The present application also provides methods of making and using the fusion proteins. The present application also provides methods of treatment comprises administering a fusion protein comprising a cytokine fused to a half-life extending domain and a second agent. | 2021-07-29 |
20210230243 | PD-1 TARGETED IL-15/IL-15RALPHA FC FUSION PROTEINS WITH IMPROVED PROPERTIES - The present invention relates to fusion proteins comprising variant IL-15 proteins, fusion proteins comprising variant anti-PD-1 antigen binding domains, and fusion proteins comprising variant IL-15 proteins and variant anti-PD-1 antigen binding domains. The present invention also relates to nucleic acid molecules, expression vectors, host cells and methods for making such fusion proteins and the use of such fusion proteins in the treatment of cancer. | 2021-07-29 |
20210230244 | PEPTIDE COMPLEX WITH IMMUNODULATORY AND ANTI-INFLAMMATORY FUNCTION - The present invention relates to compositions that are effective in management of inflammatory diseases. The disclosure provides a peptide complex comprising Abeta 1-42 and undercarboxylated osteocalcin which displays anti-inflammatory and immunomodulatory functions. The disclosure further provides with processes for preparing the compositions. | 2021-07-29 |
20210230245 | CHIMERIC ANTIGEN RECEPTOR AND CAR-T CELLS THAT BIND A HERPES VIRUS ANTIGEN - An isolated chimeric antigen receptor (CAR) polypeptide, wherein the CAR includes an extracellular antigen-binding domain, including an antibody or antibody fragment that binds to a protein encoded by a herpes virus, or to a protein complex including the protein (herpes virus antigen), wherein the herpes virus antigen is present on the surface of a human cell that is latently infected with said herpes virus and supports the lytic phase of viral replication. The invention further relates to a nucleic acid molecule encoding the CAR of the invention, a genetically modified immune cell, preferably a T cell, expressing the CAR of the invention and the use of the cell in the treatment of a medical disorder associated with human herpesvirus, such as herpes virus-associated cancers, chronic active herpes virus infections or primary herpes virus infections. In preferred embodiments the herpes virus is Epstein-Barr virus (EBV) and a preferred herpes virus antigen target of the CAR is the EBV glycoprotein 350/220 (gp350/gp220). | 2021-07-29 |
20210230246 | USE OF INHIBITORY CHIMERIC RECEPTORS TO PREVENT T CELL-INDUCED BLOOD BRAIN BARRIER DAMAGE - Neurotoxicity associated with CD19-targeted CAR-T therapy is reduced by including an inhibitory CAR (iCAR) in the CAR-T cell, wherein the iCAR specifically recognizes an antigen specific for or associated with neurovascular mural cells (e.g. pericytes or vSMC). | 2021-07-29 |
20210230247 | LILRB1-BASED CHIMERIC ANTIGEN RECEPTOR - Provided are chimeric antigen receptors having the hinge, transmembrane region, and/or intracellular domain of LILRB1, or functional fragments or variants thereof. Also provided herein are cells comprising the LILRB1 based receptors, and methods of making and using same. | 2021-07-29 |
20210230248 | Multivalent pharmacophores for high avidity and overexpressed-target specific binding and uses thereof - Overexpression of a variety of cell surface markers in cancer cells and/or non-cancer cells in the tumor microenvironment is an important hallmark for many types of cancers and is associated with cancer progression and poor prognosis. This invention provides multivalent pharmacophores for high avidity and specific binding to these overexpressed markers with much reduced binding to normally-expressed targets in healthy tissues. Further, the pharmacophores will not be interfered by soluble targets present in the circulatory systems and in tumor microenvironment. This new class of targeting therapeutics and diagnostics will provide better efficacy in cancer treatment and higher accuracy in cancer diagnosis than the currently available therapeutic and diagnostic means. This invention will also expand the range of targets that can be targeted in both cancer treatment and diagnosis, and more types of cancers can be treated target-specifically. Other diseases that have overexpressed cell surface markers in diseased cells will also be benefitted from this invention. | 2021-07-29 |
20210230249 | Multi-Specific Molecules - The present disclosure relates to multi-specific molecules which are capable of simultaneously binding at least two different target antigens or epitopes. The molecules comprise at least one binding domain molecule (BDM) which hinds to a first target antigen or epitope, the BDM being modified for selective binding to a heterologous target, coupled to a pharmacologically active protein or peptide which is an antibody or antigen-binding fragment thereof or a non-antibody protein or peptide which binds to a second target antigen or epitope, the BDMs being coupled to a C-terminus of a polypeptide present within the pharmacologically active protein or peptide. | 2021-07-29 |
20210230250 | NOVEL CTLA4-IG IMMUNOADHESINS - The present application relates to CTLA4-Ig immunoadhesins that target CD80 and CD86, and their use, particularly for therapeutic purposes. | 2021-07-29 |