12th week of 2020 patent applcation highlights part 24 |
Patent application number | Title | Published |
20200087263 | 5-CARBOXAMIDE-2-THIOBARBITURIC ACIDS AND USE THEREOF AS MEDICAMENTS - The invention relates to a class of 5-carboxamide-2-thiobarbituric acid derivatives which inhibits human type II topoisomerase (topoII) enzyme and to use thereof as medicaments especially for blocking the proliferation of cancer cells and treating cancer. The invention also provides a method for the manufacture of the 5-carboxamide-2-thiobarbituric acid derivatives. | 2020-03-19 |
20200087264 | NOVEL SELECTIVE LIGAND FOR DOPAMINE D3 RECEPTOR, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATION THEREOF - The present invention provides a novel ligand for the dopamine D3 receptor and a preparation method therefor. The compound, and a pharmaceutically acceptable salt and a pharmaceutical composition or a pharmaceutical preparation thereof are used for the treatment and prevention of schizophrenia, neurodegenerative diseases, particularly Parkinson's disease, drug dependence, drug addiction, anxiety, depression, etc. The novel ligand of the dopamine D3 receptor features a high affinity, a high specificity, and a high functional selectivity. The compound and the pharmaceutically acceptable salt and the pharmaceutical composition or the pharmaceutical preparation thereof can be used to study the distribution and function of dopamine D2 subtype receptors and mechanism of diseases associated with dysfunction of dopamine D2-like receptors, and can also be used for the disease modification of hyperprolactinemia, extrapyramidal symptoms, and levodopa-associated movement disorder or dyskinesia. | 2020-03-19 |
20200087265 | HEPATITIS C VIRUS NS3/4A PROTEASE INHIBITORS - The invention provides novel classes of HCV therapeutics that are orally available, safe and effective HCV NS3/4A protease inhibitors and are less susceptible to drug resistance than existing therapeutics. The invention also relates to pharmaceutical composition of these compounds and methods of preparation and use thereof. | 2020-03-19 |
20200087266 | TRIAZINE COMPOUNDS AND PHARMACEUTICAL USE THEREOF - Provided is a compound having an mPGES-1 inhibitory activity and useful for the prophylaxis or treatment of pain, rheumatism, osteoarthritis, fever, Alzheimer's disease, multiple sclerosis, arteriosclerosis, glaucoma, ocular hypertension, ischemic retinal disease, systemic scleroderma and cancer including colorectal cancer. | 2020-03-19 |
20200087267 | COMPOSITIONS AND METHODS FOR TREATING CANCER - This invention is directed to compositions and methods for treating cancer in a patient. | 2020-03-19 |
20200087268 | HALOGENATED BENZOXAZINE FOR USE IN THE SYNTHESIS OF POLYBENZOXAZINE - A halogenated benzoxazine compound, which can be used in particular as monomer in the synthesis of polybenzoxazine, corresponds to the formula: | 2020-03-19 |
20200087269 | PROCESS FOR THE PRODUCTION OF OZANIMOD - The present invention relates a new process for the preparation of ozanimod of the formula and acid addition salts, via new intermediates and a new polimop form of ozanimod base. | 2020-03-19 |
20200087270 | COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY - In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: | 2020-03-19 |
20200087271 | N-CYCLOBUTYL-THIAZOL-5-CARBOXAMIDES WITH NEMATICIDAL ACTIVITY - The present invention relates to compounds of the formula (I), in which the substituents are as defined in claim | 2020-03-19 |
20200087272 | TREATMENT OF MULTIPLE SCLEROSIS AND PSORIASIS USING PRODRUGS OF METHYL HYDROGEN FUMARATE - Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed. | 2020-03-19 |
20200087273 | NEW PREPARATION METHOD FOR ESCITALOPRAM PAMOATE - The present invention relates to a new preparation method for escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisob enzofuran pamoate), wherein the method is environmentally friendly and pollution-free, and the escitalopram pamoate prepared by means of the method has a high purity and a good repeatability. | 2020-03-19 |
20200087274 | SULFONAMIDE ANALOGUES OF GALIELLALACTONE - Disclosed are sulfonamide analogues of galiellactone of formula (I) as STAT3-inhibitors for use in the treatment of a STAT3 signaling related disorder, e.g. solid cancers, hematological cancers, benign tumors, hyperproliferative diseases, inflammations, autoimmune diseases, graft or transplant rejections, delayed physiological function of grafts or transplants, neurodegenerative diseases and viral infections. The sulfonamide comprises a cyclic substituent. | 2020-03-19 |
20200087275 | GIBBERELLIC ACID COMPOSITIONS - The present disclosure provides an anhydrous solution that includes between 5% and 15% w/w of gibberellic acid (GA3) in a solvent, where the solvent consists of: (a) isopropanol; (b) up to 10% w/w of methanol, ethanol, or a combination thereof; (c) up to 10% w/w of dimethyl sulfoxide (DMSO); and (d) up to 50% w/w of n-propanol, tetrahydrofurfuryl alcohol (THFA), or a combination thereof. The disclosure also provides methods of making such solutions. | 2020-03-19 |
20200087276 | CHEMICAL PROCESS TO MANUFACTURE BRANCHED-CAPROLACTONE - Synthesizing an alkyl-caprolactone includes hydrogenating an alkyl-phenol to yield a first mixture comprising an alkyl-cyclohexanone and an alkyl-cyclohexanol; separating the alkyl-cyclohexanone from the first mixture to yield a first portion of a purified alkyl-cyclohexanone; oxidizing the first portion of the purified alkyl-cyclohexanone to yield a second mixture comprising an alkyl-caprolactone, the alkyl-cyclohexanone, and the alkyl-cyclohexanol; separating the alkyl-caprolactone from the second mixture to yield a third mixture comprising the alkyl-cyclohexanone and the alkyl-cyclohexanol; combining the third mixture and the first mixture in to yield a fourth mixture; separating the alkyl-cyclohexanone from the fourth mixture to yield a second portion of the purified alkyl-cyclohexanone; oxidizing the second portion of the purified alkyl-cyclohexanone to yield a fifth mixture comprising the alkyl-caprolactone, the alkyl-cyclohexanone, and the alkyl-cyclohexanol; separating the alkyl-caprolactone from the fifth mixture; and combining the alkyl-caprolactone from the fifth mixture with the alkyl-caprolactone from the second mixture. | 2020-03-19 |
20200087277 | NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES - The invention provides certain nicotine salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, certain nicotine salt-co-crystals are described, including nicotine and two different coformers. The invention further provides methods of preparation and characterization of nicotine salts, co-crystals, and salt co-crystals. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided. | 2020-03-19 |
20200087278 | METHOD OF PREPARING N-ACYL ANTHRANILAMIDE - Disclosed herein is a method of preparing N-acyl anthranilamide (I), including: reacting a substituted anthranilic acid (II) with pyrazolecarboxylic acid (III) under the action of a phosphorus reagent and a base to obtain an intermediate benzoxazinone (IV); and subjecting the intermediate benzoxazinone (IV) and a protonic acid salt of methylamine to a ring-opening reaction to obtain N-acyl anthranilamide (I), as shown in the following reaction scheme: | 2020-03-19 |
20200087279 | COMPOSITIONS AND METHODS RELATED TO PYRIDINOYLPIPERDINE 5-HT1F AGONISTS - The present invention provides new pseudo-polymorphs of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide which are useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine headache. | 2020-03-19 |
20200087280 | QUINAZOLINONES AND AZAQUINAZOLINONES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS - The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: | 2020-03-19 |
20200087281 | FUSED BICYCLIC COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF - Fused bicyclic compounds are inhibitors of GPR91. The compounds, their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of GPR91. | 2020-03-19 |
20200087282 | SALT OF SUBSTITUTED PIPERIDINE COMPOUND - An object of the present invention is to provide a salt of the compound 1-(2,3-dichlorobenzoyl)-4((5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid, useful as an antitumor agent, and crystals thereof which are excellent in solubility, stability, and oral absorption and can be produced in large quantities. The present invention relates to a hydrochloride salt of 1-(2,3-dichlorobenzoyl)-4-((5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid and crystals of the hydrochloride salt having characteristic peaks at particular diffraction angles in powder X-ray diffraction spectrum. | 2020-03-19 |
20200087283 | COMPOUNDS FOR TREATING CERTAIN LEUKEMIAS - Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. | 2020-03-19 |
20200087284 | [4-(PHENYLSULFONYL)PIPERAZIN-1-YL](1H-1, 2, 3-TRIAZOL-4-YL)METHANONES - The present invention covers [4-(phenylsulfonyl)piperazin-1-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I), in which Q, R | 2020-03-19 |
20200087285 | NOVEL GLUTAMINYL CYCLASE INHIBITORS AND THE USE THEREOF IN TREATMENT OF VARIOUS DISEASES - The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) | 2020-03-19 |
20200087286 | PYRIMIDINE DERIVATIVE COMPOUND, OPTICAL ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION FOR PREVENTING OR TREATING TYRO 3 RELATED DISEASE COMPRISING SAME AS ACTIVE INGREDIENT - The present invention relates to a pyrimidine derivative compound, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the same as an active ingredient. The pyrimidine derivative compound, the optical isomer thereof, or the pharmaceutically acceptable salt thereof according to the present invention has an excellent selective inhibitory effect especially against TYRO 3 among TAM receptor inhibitory effects, and thus can be used as an excellent composition of preventing or treating cancer without adverse effects resulting from the inhibition of Axl and Mer. | 2020-03-19 |
20200087287 | CRYSTALLINE PHARMACEUTICAL AND METHODS OF PREPARATION AND USE THEREOF - Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention. | 2020-03-19 |
20200087288 | ORAL CANNABINOID RECEPTOR MODULATOR FORMULATIONS - Oral formulations of benzofuran compounds which modulate cannabinoid receptors are presented. Methods of using these formulations for treatment of cannabinoid receptor-mediated disease, including neuropathic pain and addition, are also described. | 2020-03-19 |
20200087289 | CRYSTALLINE FORMS OF POSACONAZOLE INTERMEDIATE AND PROCESS FOR THE PREPARATION OF AMORPHOUS POSACONAZOLE - The present invention provides an industrial method production of amorphous posaconazole. The present invention also relates to a method for production of the posaconazole via and novel crystalline forms of posaconazole intermediate. More particularly the present invention relates to novel crystalline forms of posaconazole intermediate and methods for production of novel crystalline forms of posaconazole intermediate represented by the following structural formula III Which is key intermediate in the production of posaconazole. The present invention also provides for the one pot process for the preparation of amorphous posaconazole using novel crystalline forms of benzyl posaconazole. | 2020-03-19 |
20200087290 | METHOD FOR PRODUCING GLYCERIC ACID ESTER - The present invention relates to providing a novel glyceric acid ester which can be produced in a high yield and is expected to be applied as a synthetic intermediate, and a method of producing the same. In addition, the present invention relates to providing a novel glyceric acid ester which exhibits a high recovery in a water-washing step after the reaction and a small work load at the time of production, and is expected to be applied as a synthetic intermediate, and a method of producing the same. The present invention provides a method of producing a compound represented by the following formula (II), including a step of oxidatively esterifying a compound represented by the following formula (I): | 2020-03-19 |
20200087291 | NEW QUINOLINE AND ISOQUINOLINE DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS - The present invention relates to new compounds of formula (I): | 2020-03-19 |
20200087292 | PESTICIDALLY ACTIVE AZETIDINE SULFONES AMIDE ISOXAZOLINE DERIVATIVES - Compounds of formula (I) wherein the substituents are as defined in claim | 2020-03-19 |
20200087293 | COMPOUNDS AND METHOD FOR TREATING AUTOIMMUNE DISEASES - Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I | 2020-03-19 |
20200087294 | COMPOSITIONS AND METHODS FOR TREATING DISEASES AND CONDITIONS - A compound of Formula II, or a salt, ester, solvate, hydrate or prodrug thereof: | 2020-03-19 |
20200087295 | INHIBITORS OF C-JUN-N-TERMINAL KINASE (JNK) - The present invention provides novel compounds according to Formula (I): | 2020-03-19 |
20200087296 | AMINOPYRIMIDINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF - The present invention relates to an aminopyrimidine compound, a preparation method therefor and use thereof. The aminopyrimidine compound has the structure as shown in formula I: | 2020-03-19 |
20200087297 | QUATERNARY AMINE COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF - This invention relates to quaternary amine linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer. | 2020-03-19 |
20200087298 | Imidazo[4,5-c] Ring Compounds Containing Guanidine Substituted Benzamide Groups - Imidazo[4,5-c] ring compounds of formula I, (particularly imidazo4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridine compounds) having a guanidine substituted benzamide that is attached at the N−1 position by a linking group, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed. | 2020-03-19 |
20200087299 | INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN - Disclosed are small molecule inhibitors of av136 integrin, and methods of using them to treat a number of diseases and conditions. | 2020-03-19 |
20200087300 | Deuterated Imidazo[4,5-c]quinolin-2-one Compounds and Their Use in Treating Cancer - The specification generally relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, where R | 2020-03-19 |
20200087301 | PYRAZOLOPYRIDINE COMPOUNDS AND USES THEREOF - Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer. | 2020-03-19 |
20200087302 | NITROGEN-CONTAINING HETEROCYCLE AND CARBOCYCLE DERIVATIVES HAVING TRKA INHIBITORY ACTIVITY - The present invention provides a compound having TrkA inhibitory activity, or a pharmaceutically acceptable salt thereof. The present invention relates to a compound represented by Formula (I): | 2020-03-19 |
20200087303 | JAK Kinase Inhibitor Compounds for Treatment of Respiratory Disease - The invention provides compounds of formula (I): | 2020-03-19 |
20200087304 | PYRAZOLE MAGL INHIBITORS - Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain. | 2020-03-19 |
20200087305 | SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SYNTHESIS - The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines. | 2020-03-19 |
20200087306 | 2,6-DISUBSTITUTED-9-CYCLOPENTYL-9H-PURINES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS - The present invention relates to novel 2,6-disubstituted-9-cyclopentyl-9H-purines of general formula I, capable of inhibiting the activity of kinases such as FLT3, CDKs and PDGFRs in cancer and other related proliferative diseases. The invention further includes pharmaceutical compositions containing the 2,6-disubstituted-9-cyclopentyl-9H-purines. Compounds of the present invention can be used as active ingredients of a pharmaceutical compositions for treating acute myeloid leukemia (AML). | 2020-03-19 |
20200087307 | BICYCLIC COMPOUNDS AS ATX INHIBITORS - The invention provides novel compounds having the general formula (I) | 2020-03-19 |
20200087308 | NITROGEN-CONTAINING CYCLIC COMPOUNDS AND METHODS FOR PRODUCING THE SAME - There are provided novel glycolurils, and methods for producing the same. A nitrogen-containing cyclic compound of following formula (1): | 2020-03-19 |
20200087309 | ACTIVATING PYRUVATE KINASE R AND MUTANTS THEREOF - The disclosure provides chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD). | 2020-03-19 |
20200087310 | Ectonucleotidase Inhibitors and Methods of Use Thereof - The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention. | 2020-03-19 |
20200087311 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - Organic electroluminescent materials and devices are disclosed. The organic electroluminescent materials are novel benzodithiophene or its analogous structure compounds, which can be used as charge transporting materials, hole injection materials, or the like in an electroluminescent device. These novel compounds can offer excellent performance compared with existing materials, for example, to further improve the voltage, efficiency and/or lifetime of the OLEDs. | 2020-03-19 |
20200087312 | MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 2020-03-19 |
20200087313 | NUCLEAR TRANSPORT MODULATORS AND USES THEREOF - The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by formula I: | 2020-03-19 |
20200087314 | HISTONE DEACETYLASE INHIBITORS - Provided herein are compounds and methods for inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3). | 2020-03-19 |
20200087315 | TETRAPHENYLPORPHYRIN DERIVATIVE - Provided is a ligand capable of stably bonding together interfaces composed of different types of nanoparticles, different bulk interfaces, or an interface composed of nanoparticles and a bulk interface. A tetraphenylporphyrin derivative represented by the following formula (I): | 2020-03-19 |
20200087316 | PROCESS FOR PREPARING OXYCODONE HYDROCHLORIDE HAVING LESS THAN 25 PPM 14-HYDROXYCODEINONE - In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone. | 2020-03-19 |
20200087317 | Prodrugs of Secondary Amine Compounds - The present invention relates to compounds of Formula I: | 2020-03-19 |
20200087318 | SOMATOSTATIN MODULATORS AND USES THEREOF - Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity. | 2020-03-19 |
20200087319 | Kinase Inhibitors and Uses Thereof - The present disclosure relates generally to compounds and compositions, intermediates, processes for their preparation, and their use as kinase inhibitors. | 2020-03-19 |
20200087320 | 3-OXA-8-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES - A compound of formula Ia, Ib, Ic or Id: | 2020-03-19 |
20200087321 | SULFONAMIDE COMPOUNDS - The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof. | 2020-03-19 |
20200087322 | MACROCYCLIC INDOLE DERIVATIVES - The present invention relates to macrocyclic indole derivatives of general formula (I): | 2020-03-19 |
20200087323 | NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor. | 2020-03-19 |
20200087324 | COMPOUND AND COLOR CONVERSION FILM COMPRISING THE SAME - The present specification relates to a compound, and a color conversion film, a backlight unit, and a display device, including the same. | 2020-03-19 |
20200087325 | Novel Process for the Preparation of Tavaborole, Its Novel Polymorphic Forms and the Polymorphs Thereof - The invention relates to novel process for preparation of Tavaborole. The invention also relates to novel polymorphic forms of Tavaborole and process for preparation of those polymorphic forms. The invention also relates to process for purification of Tavaborole to obtain the Tavaborole in significantly high yield and substantially pure form. | 2020-03-19 |
20200087326 | DEEP RED FLUORESCENT PROBE - A near-infrared fluorescent probe has fluorescence in the near-infrared region. Like CaSiR-1, the probe has rhodamines as the fluorescent mother nucleus and accumulates in the cytoplasm. The probe makes it possible to visualize concentration fluctuations in metal ions, such as calcium ions, within the body. The fluorescent probe includes a compound represented by the following general formula or a salt of the compound: | 2020-03-19 |
20200087327 | METHOD FOR PRODUCING UREIDO GROUP-CONTAINING ORGANOSILICON COMPOUND - A method for producing an ureido group-containing organosilicon compound includes the following steps (I) and (II):
| 2020-03-19 |
20200087328 | A TITANIUM-ORGANIC FRAMEWORK MATERIAL - This patent mentioned the synthesis of new metal-organic framework based on hexameric titanium-oxo cluster. The novel material, termed MOF-902, was successfully synthesized and its crystal structure uncovered the 2-Dimensional (2D) layer structure generated by the link of trigonal prism Ti | 2020-03-19 |
20200087329 | Acyl Germanium Photoinitiators And Process For The Preparation Thereof - Acyl germanium compound according to general formula [R | 2020-03-19 |
20200087330 | METHOD FOR PRODUCING OPTICALLY ACTIVE 2, 3-BISPHOSPHINOPYRAZINE DERIVATIVE AND METHOD FOR PRODUCING OPTICALLY ACTIVE PHOSPHINE TRANSITION METAL COMPLEX - In the method for producing an optically active 2,3-bisphosphinopyrazine derivative of the present invention, an optically active 2,3-bisphosphinopyrazine derivative represented by the following formula (3) is produced by the step of: preparing solution A containing 2,3-dihalogenopyrazine represented by the following formula (1) | 2020-03-19 |
20200087331 | CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES - A chemoselective and reactive Mn(CF | 2020-03-19 |
20200087332 | Complexes - The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). | 2020-03-19 |
20200087333 | PREPARATION OF RHODIUM(III)-2-ETHYLHEXANOATE - The present invention provides a method for preparing rhodium (III) 2-ethylhexanoate solutions which supplies the reaction product with higher space yield, as well as lower sodium and chloride ion content. An aqueous solution of an alkali salt of 2-ethylhexanoate is thereby initially converted with a rhodium (III) precursor. The rhodium (III) precursor is selected from rhodium (III) chloride solution, rhodium (III) chloride hydrate, and rhodium (III) nitrate. The mixture is heated for several hours. After cooling to room temperature, the rhodium (III) 2-ethylhexanoate formed is extracted from the aqueous solution with an alcohol that is immiscible in water or a carboxylic acid that is immiscible in water, and optionally washed with aqueous mineral acid. The rhodium (III) 2-ethylhexanoate solution obtainable in this way may be used directly as catalyst in hydroformylation reactions. | 2020-03-19 |
20200087334 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - Cyclometallated iridium complexes having triphenylene or aza triphenylene and bulky alkyl substitution that can be used as emitters in OLEDs to improve the external quantum efficiency (EQE) and lifetime of OLEDs are disclosed. | 2020-03-19 |
20200087335 | PROCESSES FOR PREPARING MACROLIDES AND KETOLIDES AND INTERMEDIATES THEREFOR - The invention described herein pertains to processes for the preparation of macrolide antibacterial agents. In particular, the invention pertains to processes for preparing macrolides and ketolides from erythromycin A. | 2020-03-19 |
20200087336 | LABELLED NUCLEOTIDES - The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) (wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C | 2020-03-19 |
20200087337 | 2'-CHLORO AMINOPYRIMIDINONE AND PYRIMIDINE DIONE NUCLEOSIDES - Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds. | 2020-03-19 |
20200087338 | NUCLEOTIDE AND OLIGONUCLEOTIDE PRODRUGS - The present invention discloses compounds of formula (I): | 2020-03-19 |
20200087339 | NUCLEOTIDE HEMI-SULFATE SALT FOR THE TREATMENT OF HEPATITIS C VIRUS - A hemi-sulfate salt of the structure: | 2020-03-19 |
20200087340 | LIF/LIFR ANTAGONIST IN ONCOLOGY AND NONMALIGNANT DISEASES - Described herein are methods of using compounds that inhibit leukemia inhibitory factor (LIF) and/or block of the leukemia inhibitory factor receptor for treatment of liver fibrosis, proliferation of spinal tumors, and in combination therapy with an immunotherapeutic agent. | 2020-03-19 |
20200087341 | PROCESS FOR THE PREPARATION OF ALLOPREGNANOLONE - The present invention relates to a method for the preparation of allopregnanolone with a high degree of purity which, eventually, occurs through the formation of 3α-trifluoroacetoxy-5α-pregnan-20-one. | 2020-03-19 |
20200087342 | C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS - The invention relates to C-3 novel triterpenone with C-17 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. | 2020-03-19 |
20200087343 | EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION - The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes. | 2020-03-19 |
20200087344 | COMPOSITION FOR AUTOPHAGY INHIBITING IN CELL, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING TUMOR DISEASE, OR INHIBITING ANTI-CANCER AGENTS RESISTANCE CONTAINING THE SAME - Provided are a polypeptide having the activity of inhibiting autophagy in a cell, a composition for inhibiting autophagy in a cell, and particularly in a tumor cell, containing the polypeptide as an active ingredient, and a pharmaceutical composition containing the polypeptide, and more specifically, a composition for inhibiting autophagy in a cell containing a polypeptide inhibiting the control mechanism of autophagy as an active ingredient, and a pharmaceutical composition for preventing or treating a neoplastic disease or for inhibiting resistance to anticancer agents, containing the polypeptide. | 2020-03-19 |
20200087345 | MODULATION OF P53 FOR THE TREATMENT OF CANCER - The invention provides compositions and methods for preventing or treating cancer in a subject. In some embodiments, the compositions comprise isolated peptides and/or isolated oligonucleotides. In other embodiments, peptides of the present invention are conjugated with cell-penetrating peptides. Vectors, cells, and kits for preventing or treating cancer are also provided herein. | 2020-03-19 |
20200087346 | PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) TARGETING PEPTIDES - Described herein is the discovery of novel PSMA-specific peptides, which were identified through a novel combinatorial biopanning method. One of the novel PSMA-specific peptides discovered, GTIQPYPFSWGY (or GTI) (SEQ ID NO: 2), exhibits high binding affinity and selectivity to PSMA and PSMA-positive prostate cancer cells. It was found that GTI can mediate internalization of the apoptotic KLA peptide to PSMA-positive LNCaP cells and induce cell death. Moreover, a FAM-labeled GTI peptide shows a high and specific tumor uptake in nude mice bearing human prostate cancer xenografts. It was demonstrated that the GTI peptide can be employed as a PSMA-specific ligand for prostate cancer diagnosis and/or for targeted drug delivery to prostate cancer cells. | 2020-03-19 |
20200087347 | LIGANDS FOR INTEGRIN αVβ8, SYNTHESIS AND USES THEREOF - Disclosed are compounds represented by the following general formula (I): Cyclo-(Arg-Gly-Asp-X | 2020-03-19 |
20200087348 | MODIFIED MICROCYSTINS AND NODULARINS - A compound includes cytotoxic agents such as microcystin and nodularin. More specifically, a modified microcystin and/or nodularin compound contains one or more modified substrates, wherein one or more modified substrates include an anchor group directly accessible or transformable for use in conjugation chemistry (incl. click chemistry), for the attachment of a targeting moiety. This compound is useful for cancer treatment. | 2020-03-19 |
20200087349 | BROAD-SPECTRUM ANTI-INFECTIVE PEPTIDES - Provided herein are anti-infective peptides and uses thereof. Such anti-infective peptides are useful against bacteria and viruses. Also provided herein are compositions comprising said anti-infective peptides. | 2020-03-19 |
20200087350 | Divalent Nucleobase Compounds and Uses Therefor - Described herein are novel divalent nucleobases that each bind two nucleic acid strands, matched or mismatched when incorporated into a nucleic acid or nucleic acid analog backbone (a genetic recognition reagent, or genetic recognition reagent). In one embodiment, the genetic recognition reagent is a peptide nucleic acid (PNA) or gamma PNA (γPNA) oligomer. Uses of the divalent nucleobases and monomers and genetic recognition reagents containing the divalent nucleobases also are provided. | 2020-03-19 |
20200087351 | RECOMBINANT VECTOR COMPRISING PORCINE FC FRAGMENT AND PREPARATION METHOD OF RECOMBINANT PROTEIN USING THEREOF - Provided is a recombinant vector including a porcine Fc fragment. By fusing the porcine Fc fragment with various target proteins by using the recombinant vector of the present invention, not only target proteins may be expressed using various hosts including plants, but the productivity and stability of target proteins may also be increased. | 2020-03-19 |
20200087352 | ASSEMBLY ACTIVATING PROTEIN (AAP) AND ITS USE FOR THE MANUFACTURE OF PARVOVIRUS PARTICLES ESSENTIALLY CONSISTING OF VP3 - The present invention relates to nucleic acids encoding the novel parvoviral protein “assembly activating protein” (AAP), the encoded polypeptides, methods of producing the polypeptides, antibodies specific for AAP, the use of the nucleic acids for the preparation of the polypeptides, the use of the nucleic acids or the polypeptides for the preparation of the parvoviral particle and methods of producing parvoviral particles essentially consisting of VP3 by providing in addition to the coding sequence of the parvoviral structural protein VP3 a sequence fragment Z/a nucleic acid encoding AAP in the cell and expressing VP3 and fragment Z under control of a rep-independent promoter. Furthermore, the present invention relates to parvoviral particles essentially consisting of VP3 and/or obtainable by the above method as well as expression cassettes comprising (i) a heterologous promoter and (ii) VP3 coding sequence and/or fragment Z. The present invention further relates to a medicament, particularly a vaccine, comprising the parvoviral particles or expression cassettes and their use. | 2020-03-19 |
20200087353 | SELECTIVE RECOVERY - Provided herein are methods of selective screening. In addition, various targeting proteins and sequences, as well as methods of their use, are also provided. | 2020-03-19 |
20200087354 | INHIBITORS OF CRISPR-CAS9 - Cas9-inhibiting polypeptide compositions and methods are provided. | 2020-03-19 |
20200087355 | CATALYTICALLY ACTIVE PROTEIN AGGREGATES AND METHODS FOR PRODUCING THE SAME - Disclosed are catalytically active water-insoluble protein aggregates comprising fusion proteins which comprise a coiled-coil domain and a catalytic domain, methods of manufacturing such protein aggregates, and their use. | 2020-03-19 |
20200087356 | Mosquitocidal Xenorhabdus, Lipopeptide and Methods - Provided is a bacterial strain which produces a family of mosquitocidal toxins, Xenorhabdus MT, on deposit with the American Type Culture Collection, PTA-6826, insecticidal compositions comprising the mosquitocidal toxin(s) produced by Xenorhabdus MT, a mosquitocidal toxin preparation prepared from spent culture medium, whole culture or cells or a mixture thereof, of Xenorhabdus MT and method of insect control, especially mosquito control. Also provided are microbial compounds (same as mosquitocidal toxins) compositions comprising them and use in formulating therapeutic and other antimicrobial compositions, and methods of use for inhibiting microbial growth and for treating infection. | 2020-03-19 |
20200087357 | STRAIN OF BACTERIA PRODUCING DHA AND EPA, SIX GENE FRAGMENTS IN THE BACTERIAL GENOME AND THEIR APPLICATIONS - The present invention discloses a strain of bacteria producing DHA and/or EPA, six gene fragments in the bacterial genome, and uses thereof. The strain is | 2020-03-19 |
20200087358 | ENGINEERED LIGHT-SENSITIVE PROTEINS - Disclosed herein are engineered light-sensitive proteins, for example channelrhodopsins and variants thereof. Also disclosed are compositions for expressing the light-sensitive proteins in cells, tissues, organs and subjects, and methods for using the light-sensitive proteins to, for example, enable minimally-invasive neuronal circuit interrogation in living organism, and treat neuronal and ocular disorders. | 2020-03-19 |
20200087359 | GRIFFITHSIN MUTANTS - The invention provides modified griffithsin polypeptides comprising the amino acid sequence of SEQ ID NO: 1, as well as corresponding nucleic acids, vectors, cells, fusion proteins, constructs, conjugates, and methods of inhibiting viral infection. | 2020-03-19 |
20200087360 | Method of treating a diarrhea disorder using a novel polypeptide - The present invention provides for a recombinant or isolated polypeptide comprising the amino acid sequence of an enhancer polypeptide associated with a diarrhea disorder; a transgenic non-human mammal, wherein the mammal is deleted or knocked out for one or more of an intestine-critical region (ICR); a pharmaceutical composition comprising the polypeptide of the present invention and a pharmaceutical acceptable carrier; and, a method of treating or preventing a subject suffering or at risk or suspected of suffering from a diarrhea disease or disorder, the method comprising administrating a pharmaceutical composition of the present invention to a subject in need of such treatment. | 2020-03-19 |
20200087361 | PNEUMOCOCCAL FUSION PROTEIN VACCINES - Technologies for the prevention and/or treatment of pneumococcal infections. | 2020-03-19 |
20200087362 | FUSION PROTEIN SLIT2D2(C386S)-HSA AND USE THEREOF IN PREVENTION AND/OR TREATMENT OF LUNG INFLAMMATION - The present invention provides a recombinant fusion protein. The fusion protein is formed by the fusion of D2 domain of Slit2 protein and HSA protein, and the position 386 amino acid of the Slit2 protein molecule is serine. | 2020-03-19 |