34th week of 2022 patent applcation highlights part 26 |
Patent application number | Title | Published |
20220267294 | SMALL MOLECULE INHIBITORS OF SRC TYROSINE KINASE - Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof. Also disclosed herein are methods of using the compounds of Formula (I) in the treatment of certain diseases (e.g., cancer). | 2022-08-25 |
20220267295 | CRYSTALLINE FORMS OF SOMATOSTATIN MODULATORS - Described herein are pharmaceutically acceptable salts of a somatostatin modulator, crystalline forms of the pharmaceutically acceptable salts of the somatostatin modulator, methods of making such salts and crystalline forms, pharmaceutical compositions and medicaments comprising such salts and crystalline forms, and methods of using such salts and crystalline forms in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity. | 2022-08-25 |
20220267296 | METHODS FOR THE PREPARATION OF 5-BROMO-2-(3-CHLORO-PYRIDIN-2-YL)-2H-PYRAZOLE-3-CARBOXYLIC ACID - Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)-2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives. Also described herein are novel reaction intermediates. | 2022-08-25 |
20220267297 | 2-SUBSTITUTED IMIDAZOLIDINE DERIVATIVE CONTAINING ARYL BIPYRIDYLOXY STRUCTURE AND PREPARATION METHOD AND USE THEREOF - The present disclosure relates to a 2-substituted imidazolidine derivative containing an aryl bipyridyloxy structure, and a preparation method and use thereof, which is obtained by the reaction of 2-substituted imidazolidine and aryl bipyridyloxy compound. The 2-substituted imidazolidine derivative containing an aryl bipyridyloxy structure has a good insecticidal effect on harmful insects, and the compound can be used to prepare insecticides in the fields of agriculture, horticulture, etc. | 2022-08-25 |
20220267298 | QUINAZOLIN-4-ONE DERIVATIVES USEFUL AS GRK2 INHIBITORS - The present invention is directed to quinazolin-4-one derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GRK2, including the treatment of for example, cardiac failure, cardiac hypertrophy, hypertension, Type II diabetes Mellitus, NASH, NAFLD, End-stage kidney disease, kidney failure, etc. | 2022-08-25 |
20220267299 | NEW CRYSTALLINE FORMS OF N-(3-(2-(2-HYDROXYETHOXY)-6-MORPHOLINOPYRIDIN-4-YL)-4-METHVLPHENYL)-2 (TRIFLUOROMETHYL)ISONICOTINAMIDE AS RAF INHIBITORS FOR THE TREATMENT OF CANCER - The present invention relates to crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinanmide and to processes for their preparation. Furthermore, the invention relates to a N pharmaceutical composition comprising said crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-trifluoromethyl)isonicotinamide, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition CA of the present invention can be used as a medicament, in particular for the treatment of cancers. | 2022-08-25 |
20220267300 | SULFONAMIDE DERIVATIVES AND USES THEREOF - The present disclosure relates to compounds of Formula (I) or (II): | 2022-08-25 |
20220267301 | NOVEL SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS D-AMINO ACID OXIDASE (DAAO) INHIBITORS - The present invention provides novel substituted benzimidazole derivatives used as DAAO inhibitors and for treatment and/or prevention of neurological disorders. | 2022-08-25 |
20220267302 | THERAPEUTIC COMPOUNDS - The invention provides compounds having Formula (I): | 2022-08-25 |
20220267303 | Compounds and Methods for Treating or Preventing Bacterial Infections - The disclosure relates, in certain aspects, to compounds that can be used to inhibit β-lactamases, such as but not limited to OXA enzymes, such as but not limited to OXA-24, OXA-48, and/or OXA-58. In certain embodiments, these compounds can be used to inhibit activity of β-lactamases in vitro and in vivo. | 2022-08-25 |
20220267304 | INDAZOLE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATION THEREOF - An indazole derivative, a preparation method therefor, and a pharmaceutical application thereof. In particular, the present invention relates to an indazole derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and a use of the derivative as an estrogen receptor modulator in the prevention and/or treatment of an estrogen receptor mediated or dependent disease or condition, the disease being particularly preferably breast cancer. The definition of each substituent in the general formula (I) is the same as that in the description. | 2022-08-25 |
20220267305 | MODULATORS OF ESTROGEN RECEPTOR PROTEOLYSIS AND ASSOCIATED METHODS OF USE - The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. | 2022-08-25 |
20220267306 | HETEROCYCLIC PROLINAMIDE DERIVATIVES - This invention is directed to novel heterocyclic prolinamide derivatives of Formula I, | 2022-08-25 |
20220267307 | ANTI-CANCER COMPOUNDS - This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent. | 2022-08-25 |
20220267308 | Modulators of Excitatory Amino Acid Transporters and Methods Using Same - The present disclosure provides in one aspect compounds of Formula I. In certain embodiments, the compounds of the disclosure are useful for treating, ameliorating or preventing a disease or disorder that is caused, induced or characterized by abnormal reduction in glutamate transporter activity or abnormal increase in extracellular CNS glutamate concentration in a subject. In certain embodiments, the compounds of the disclosure stimulate a glutamate transporter. | 2022-08-25 |
20220267309 | DIMERIC OR POLYMERIC FORM OF MUTANT IDH INHIBITOR - The present invention provides a mutant IDH inhibitor in dimeric or multimeric form. Specifically, the present invention provides a compound of formula I, | 2022-08-25 |
20220267310 | QUINAZOLINE AND CINNOLINE DERIVATIVES AS DNA-PK INHIBITOR - Disclosed in the present invention are a compound as represented by formula (I), and an isomer or pharmaceutically acceptable salt thereof, and disclosed is an application thereof in preparing drugs for treating DNA-PK inhibitor-related diseases. | 2022-08-25 |
20220267311 | BICYCLO[1.1.1]PENTANE INHIBITORS OF DUAL LEUCINE ZIPPER (DLK) KINASE FOR THE TREATMENT OF DISEASE - Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain). | 2022-08-25 |
20220267312 | AMINO BENZOTHIAZOLE COMPOUNDS FOR TREATMENT OF ANTIBIOTIC RESISTANT BACTERIA - Provided herein are compounds of the formula: | 2022-08-25 |
20220267313 | DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES - Provided herein are dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof. | 2022-08-25 |
20220267314 | METHODS FOR MAKING THIAZOLYPYRAZOLE CARBOXYLIC ACIDS AND INTERMEDIATES THEREFOR - This disclosure relates generally to improved methods of preparing pyrazolylthiazole-containing compounds and their intermediates. | 2022-08-25 |
20220267315 | N-(PYRIDIN-2-YL)-4-(THIAZOL-5-YL)PYRIMIDIN-2-AMINE DERIVATIVES AS THERAPEUTIC COMPOUNDS - A novel class of inhibitors of protein kinates that are useful in the treatment of cell proliferative diseases and conditions, and especially those characterised by over-expression of CDK4, CDK6 and/or cyclin D, including certain cancers of lung, breast, brain, central nervous system, colorectal cancer and leukaemias. The inhibitors have the general structure I: | 2022-08-25 |
20220267316 | COMPOUNDS FOR DEGRADING TAU PROTEIN AGGREGATES AND USES THEREOF - Disclosed herein are novel compounds for degrading Tau protein aggregates, pharmaceutical acceptable salts, enantiomers, non-enantiomers, tautomers, racemates, solvates, metabolic precursors, or prodrugs thereof. Also disclosed herein are uses of the compounds, pharmaceutical acceptable salts, enantiomers, non-enantiomers, tautomers, racemates, solvates, metabolic precursors, or prodrugs thereof in manufacture a medicament for treating a tauopathy, as well as method for aiding in the treatment of a tauopathy or treating a tauopathy in a subject. | 2022-08-25 |
20220267317 | 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. | 2022-08-25 |
20220267318 | Tetrahydro-Pyrido-Pyrimidine Derivatives - The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), | 2022-08-25 |
20220267319 | HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DIODE COMPRISING SAME - The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same. | 2022-08-25 |
20220267320 | 4-(IMIDAZO[1,2-A]PYRIDIN-3-YL)-PYRIMIDINE DERIVATIVES - Compounds of the formula I | 2022-08-25 |
20220267321 | AZAINDOLE PYRAZOLE COMPOUNDS AS CDK9 INHIBITORS - The present invention discloses new azaindole pyrazole compounds as CDK9 inhibitors, in particular, compounds as represented by formula (I), pharmaceutically acceptable salts and isomers thereof, and the use of compounds represented by formula (I), pharmaceutically acceptable salts and isomers thereof, and the pharmaceutical composition containing them in the preparation of cancer drugs. | 2022-08-25 |
20220267322 | OXAZOLE COMPOUND AS MULTI-TARGETED INHIBITOR OF IRAK4 AND BTK - Provided are a class of multi-targeted inhibitors of IRAK4 and BTK, and the use thereof in preparing a drug for treating IRAK4- and BTK-related diseases. The present invention specifically relates to the compounds represented by formula (II), isomers thereof or pharmaceutically acceptable salts thereof. | 2022-08-25 |
20220267323 | SYNTHESIS OF BICYCLIC INHIBITORS OF HISTONE DEACETYLASE - Provided herein are synthetic methods for the preparation of compounds having the Formula: (I) and (I′) and salts thereof. | 2022-08-25 |
20220267324 | PYRIDINE DERIVATIVE AS FGFR AND VEGFR DUAL INHIBITORS - FGFR and VEGFR dual inhibitors, specifically being a compound represented by formula (I) or a pharmaceutically acceptable salt. | 2022-08-25 |
20220267325 | PGDH INHIBITORS AND METHODS OF MAKING AND USING - Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels. | 2022-08-25 |
20220267326 | CRYSTALLINE FORM OF VALBENAZINE DITOSYLATE, PROCESSES FOR PREPARATION THEREOF AND USE THEREOF - A crystalline form of valbenazine ditosylate, processes for preparation thereof, a pharmaceutical composition containing the crystalline form, use of the crystalline form for preparing vesicular monoamine transporter 2 inhibitor drugs, and use of the crystalline form for preparing drugs treating tardive dyskinesia. | 2022-08-25 |
20220267327 | METHOD FOR PRODUCING MORPHINAN DERIVATIVE - Provided is, for example, a method for producing a morphinan derivative represented by General Formula (II), including the step of: allowing metal sodium and ethylenediamine to act on a morphinan derivative represented by General Formula (I) in presence of an auxiliary solvent. | 2022-08-25 |
20220267328 | AZABICYCLO AND DIAZEPINE DERIVATIVES - The present invention provides in one aspect azabicyclo and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator. | 2022-08-25 |
20220267329 | Dihydro-Spiro[Indoline-3:1'-Isoquinolin]-2-Ones and Their Analogues and Derivatives and Methods of Treating Cancer and Other Diseases - The present invention is directed to various 3′,4′-dihydro-2′H-spiro[indoline-3:1′-isoquinolin]-2-one compounds and methods for treating disease states and/or conditions which are mediated through sphingosine-1-phosphate receptor(s). The present invention is also directed to the use of these compounds as anticancer agents and as modulators of sphingosine-1-phosphate receptor function in the treatment of disease states and/or conditions which are mediated through these receptors. In addition, the invention relates to pharmaceutical compositions comprising one or more of these compounds alone or in combination with other therapeutic agents. The invention is also directed to methods of treatment of cancer and/or conditions that may respond to the modulation of sphingosine-1-phosphate receptor function and which employ compounds of the present invention or pharmaceutical compositions comprising one or more of the compounds of this invention. | 2022-08-25 |
20220267330 | NEAR-INFRARED FLUORESCENT MOLECULE ACTIVE TARGETING FOLATE RECEPTOR AND PREPARATION METHOD THEREOF - The present disclosure relates to the fields of near-infrared surgical navigation fluorescent molecules, cell marker imaging and so on, and in particular discloses an active targeting near-infrared fluorescent small molecule structure and a preparation method thereof. The present disclosure prepares the active targeting near-infrared fluorescent small molecule with pemetrexed disodium and derivatives thereof as active targeting groups by utilizing an organic total synthesis method. Such active targeting near-infrared fluorescent molecule has the advantages of high active targeting property, strong specificity, good water solubility, high fluorescence quantum yield and so on. | 2022-08-25 |
20220267331 | DOPAMINE-B-HYDROXYLASE INHIBITORS - This invention relates to: (a) compounds of formula I (with R | 2022-08-25 |
20220267332 | SUBSTITUTED FUSED HETEROAROMATIC BICYCLIC COMPOUNDS AS KINASE INHIBITORS AND THE USE THEREOF - The disclosure provides novel substituted fused heteroaromatic compounds as represented in Formula I, wherein A | 2022-08-25 |
20220267333 | PYRROLO[2,3-b]PYRAZINES AS HPK1 INHIBITOR AND THE USE THEREOF - Disclosed herein is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating HPK1 related disorders or diseases by using the compound disclosed herein. | 2022-08-25 |
20220267334 | CRYSTALLINE FORMS OF AN ORALLY AVAILABLE, SELECTIVE KIT AND PDGFR KINASE INHIBITOR - The present invention relates to crystalline avapritinib, polymorphs and hydrates thereof as well as to processes for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising crystalline avapritinib and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment of patients with gastrointestinal stromal tumors (GIST) and advanced systemic mastocytosis (AdvSM), including aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematologic neoplasm (SM-AHN) and mast cell leukemia (MCL). | 2022-08-25 |
20220267335 | PYRAZOLO[3,4-D]PYRROLO[1,2-B]PYRIDAZINYL COMPOUNDS USEFUL AS IRAK4 INHIBITORS - Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein R | 2022-08-25 |
20220267336 | PYRROLOPYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND APPLICATION THEREOF IN MEDICINE - Disclosed are a pyrrolopyrazole derivative, a preparation method therefor, and the medical use thereof. In particular, disclosed are a novel class of pyrrolopyrazole derivatives represented by general formula (I), a preparation method therefor, and the use of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives in biomedicine as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blochers (P-CABs). The definitions of various substituent (R | 2022-08-25 |
20220267337 | PYRROLIDINE-PYRAZOLES AS PYRUVATE KINASE ACTIVATORS - The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia. | 2022-08-25 |
20220267338 | HYDRATES OF POLYMORPHS OF 6-(1H-INDAZOL-6-YL)-N-(4-MORPHOLINOPHENYL)-2,3-DIHYDROIMIDAZO[1,2-A]PYRAZ- IN-8-AMINE BIS-MESYLATE AS SYK INHIBITORS - Polymorphs of a bis-mesylate salt of a compound of Formula IA: | 2022-08-25 |
20220267339 | SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS - The invention relates to substituted bicyclic heterocyclic compounds of formula (I), pharmaceutically acceptable salts thereof and pharmaceutical compositions for treating diseases, disorders or conditions associated with the overexpression of PRMT5 enzyme. The invention also relates to methods of treating diseases, disorders or conditions associated with the overexpression of PRMT5 enzyme. | 2022-08-25 |
20220267340 | DOSAGE FORM COMPOSITIONS COMPRISING AN INHIBITOR OF BRUTON'S TYROSINE KINASE - The invention relates generally crystalline mesylate salts, crystalline chloride salts and crystalline sulfate salts of the compound (S)-2-(3′-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4′-bipyridin]-2′-yl)-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one that is an inhibitor of Bruton's tyrosine kinase. In some aspects, the crystalline salts are single polymorphs. | 2022-08-25 |
20220267341 | SOLID FORMS OF TERT-BUTYL (S)-2((2S,3R)-1-AMINO-3-HYDROXY-1-OXOBU TAN-2-YL)-1-OXO-2, 5-DIAZASPIRO [3.4] OCTAN E-5-CARBOXYLATE AND METHODS OF PREPARING THEM - Solid state forms of tert-buty 1 (S)-2-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-1-oxo-2,5-diazaspiro[3.4] octane-5-carboxylate, pharmaceutical compositions, preparation, and uses thereof. | 2022-08-25 |
20220267342 | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2- -TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF - The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS). | 2022-08-25 |
20220267343 | SUBSTITUTED PYRIDOTRIAZINE COMPOUNDS AND USES THEREOF - The present disclosure relates generally to certain tricyclic compounds, pharmaceutical compositions comprising said compounds, and methods of making said compounds and pharmaceutical compositions. The compounds of the disclosure are useful in treating or preventing human immunodeficiency virus (HIV) infection. | 2022-08-25 |
20220267344 | COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, COMPOSITION FOR ORGANIC OPTOELECTRONIC DEVICE AND ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE - The present invention relates to a compound for an organic optoelectronic element, the compound being represented by a combination of Chemical Formula 1 to Chemical Formula 3; a composition for an organic optoelectronic element, the composition including the compound; an organic optoelectronic element; and a display device. | 2022-08-25 |
20220267345 | CDK Inhibitors And Their Use As Pharmaceuticals - The disclosure is directed to compounds of Formula I | 2022-08-25 |
20220267346 | THIENOPYRIMIDINE DERIVATIVES HAVING STEREO CONFIGURATIONS AND USE THEREOF IN MEDICINE - Thienopyrimidine derivative having stereo configurations and use thereof in medicine. Also included are pharmaceutical compositions of the compounds. The compounds or pharmaceutical compositions may be used to inhibit acetyl-CoA carboxylase (ACC). A method for preparing the compounds and the pharmaceutical compositions, and use thereof in treatment or prevention of diseases associated with ACC regulation of mammals, in particular, humans. | 2022-08-25 |
20220267347 | SUBSTITUTED PYRIMIDINEDIONE COMPOUNDS AND USES THEREOF - Substituted pyrimidinedione compounds and uses thereof, as well as pharmaceutical compositions containing such compounds, which can be used as gonadotropin releasing hormone receptor antagonists and a method for preparing such compounds and pharmaceutical compositions and their uses in the prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis, hysteromyoma, precocious puberty and other diseases. | 2022-08-25 |
20220267348 | THIENOPYRIDINYL AND THIAZOLOPYRIDINYL COMPOUNDS USEFUL AS IRAK4 INHIBITORS - Disclosed are compounds of Formula (I) [INSERT CHEMICAL STRUCTURE HERE] (I) or a salt or prodrug thereof, wherein: X is CR4 or N; and R | 2022-08-25 |
20220267349 | HETEROCYCLIC COMPOUNDS - The invention provides new heterocyclic compounds having the general formula (I) | 2022-08-25 |
20220267350 | ADENOSINE RECEPTOR ANTAGONIST - A compound represented by formula (I) and a pharmaceutical composition thereof. The compound represented by formula (I) can be used as an adenosine receptor inhibitor, in particular, A2A and/or A2B inhibitors, for example, can be used for preventing or treating diseases related to A2A and/or A2B activity or expression level. | 2022-08-25 |
20220267351 | SUBSTITUTED BENZOXAZOLE AND BENZOFURAN COMPOUNDS AS PDE7 INHIBITORS - Substituted benzoxazole and benzofuran chemical entities of Formula (I): wherein, V, W, X, Y, Z, and m have any of the values described herein and compositions comprising such chemical entities; processes for making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; and the treatment of one or more disorders, including neurological, cognitive, immunological, and inflammatory disorders, as well as other conditions and diseases involving PDE7 or cyclic nucleotide signaling. | 2022-08-25 |
20220267352 | RAPAMYCIN ANALOGS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 2022-08-25 |
20220267353 | 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). | 2022-08-25 |
20220267354 | TRICYCLIC COMPOUNDS AS HPK1 INHIBITOR AND THE USE THEREOF - Disclosed herein is a tricyclic compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating HPK1 related disorders or diseases by using the compound disclosed herein. | 2022-08-25 |
20220267355 | PREPARATION METHOD FOR NANO ORGANOMETALLIC CARBOXYLATE - Provided in the present invention is a preparation method for a nano organometallic carboxylate which effectively solves the problems of a complex washing process, and cumbersome, dangerous and uneconomical preparation of lye in traditional methods for producing organometallic carboxylates. A new method for preparing high-quality organometallic carboxylates by using a carboxylic acid, caustic soda, a metal oxide or a hydroxide as starting materials, and using ball milling to assist reaction thereof. The present invention not only efficiently utilizes lye, it also obtains high-quality organometallic carboxylates, which overcomes the technical prejudice that the prior art uses calcium chloride, sodium chloride and other salts for poor reaction efficiency. The problem in environmental pollution caused by the washing waste liquid in the existing process is fundamentally solved. At the same time, addition of non-ionic surfactants makes ball milling more efficient and significantly reduces the particle size of the product. | 2022-08-25 |
20220267356 | ARGINASE INHIBITORS AND METHODS OF USE THEREOF - Disclosed are compounds of formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cancer or a respiratory inflammatory disease using the same: | 2022-08-25 |
20220267357 | Novel Benzimidamides Compounds Comprising an Oxaborinin Ring - The invention relates to 4-(1-hydroxy-3,4-dihydro-1H-benzo[c][1,2]oxaborinin-3-yl)benzimidamide derivatives and their use in treating diseases and conditions of the skin (for example, Netherton syndrome, rosacea, atopic dermatitis, psoriasis and itch) caused by abnormally high levels of protease activity (particularly of serine proteases such as kallikreins). In addition, the invention relates to compositions containing the derivatives and processes for their preparation. | 2022-08-25 |
20220267358 | CYCLIC GERMANIUM COMPOUNDS AND APPLICATIONS THEREOF - The present disclosure provides a new series of compounds exhibiting high fluorescence quantum yields in the solid state. In one embodiment, the compounds include a series of 2,3,4,5-tetraphenylgermoles with the same or different 1,1-substituents. In another embodiment, substituted germafluorenes, germa-fluoresceins/rhodamines, and germapins are described. These germanium heterocycles possess ideal photophysical and thermostability properties, which makes them excellent candidates for chemical or biological sensors, host materials for electroluminescent devices and solar cells, and emissive and/or electron-transport layer components in organic light emitting diode devices. | 2022-08-25 |
20220267359 | PROCESS FOR THE PREPARATION OF THE POLYMORPH F OF SODIUM NERIDRONATE - The present invention relates to a new process for the preparation of the crystalline polymorph of sodium neridronate in form hemihydrate F, comprising the following steps: a) reacting the 6-aminohexanoic acid with a mixture of phosphorous acid and methanesulfonic acid at a temperature in the range from 60 to 80° C., under stirring, until a clear solution is obtained; b) adding rl phosphorus trichloride to said solution of step (a) under stirring at a temperature in the range of 60 to 80° C.; c) diluting with water the reaction mixture obtained from the previous step (b) and heating said water diluted mixture at a temperature in the range from 80 to 120° C.; d) cooling the heated mixture obtained in step (c) up to room temperature, diluting it with water, then slowly adding an aqueous sodium hydroxide solution up to a pH in the range from 4.2 to 4.6, to obtain a neutralized solution; e) bringing the neutralized solution of step (d) up to a temperature of about 70° C., then subjecting it to a temperature increase in the range from 70 to 140° C., until evaporation of at least 70% of the initial volume of the neutralized solution of step (d), thus obtaining a suspension to be kept under stirring for at least 1 hour; f) cooling the suspension of step (e) up to a temperature in the range from around 5 to 25° C.; and g) recovering the crystalline sodium neridronate in hemihydrate form F by filtering the suspension of the previous step (f). The process is particularly simple, scalable and environmentally sustainable | 2022-08-25 |
20220267360 | METAL COMPLEX AND COMPOSITION COMPRISING THE SAME - A metal complex (1) is useful for producing a light emitting device having excellent external quantum efficiency. | 2022-08-25 |
20220267361 | CORROLE-BASED FRAMEWORKS AND METHODS OF USE THEREOF - Described herein are corrole-based frameworks and methods for making the same. The corrole-based frameworks have unique structural and physical properties, which lends them to be versatile in a number of different applications and uses such as in gas storage/separation, proton conduction, biomedicine, sensing, and catalysis. In one aspect, the corrole-based frameworks are organic frameworks. In other aspects, the corrole-based frameworks are metal-organic frameworks. | 2022-08-25 |
20220267362 | Methods for Glycosylation - Provided herein are methods of glycosylation in the formation of disaccharides, trisaccharides, and oligosaccharides using fluoroglycosides, silyl ether glycosides and a triaryl borane catalyst. | 2022-08-25 |
20220267363 | SIALIDASE-RESISTANT SACCHARIDE AND METHOD OF MAKING AND USING THE SAME - Disclosed are a method of preparing a saccharide that contains a 3-fluoro-sialic acid and a method of bonding it to a homogeneous antibody. Also within the scope of this invention are compounds each containing a 3-fluoro-sialic acid, monoclonal antibodies bonded to α2,6-linked 3-fluoro-sialo-side terminated N-glycans, and treatment of cancer with such monoclonal antibodies. | 2022-08-25 |
20220267364 | HETEROCYCLIC AMIDE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF - Disclosed in the present invention are a compound shown in formula (IA), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a STING agonist. | 2022-08-25 |
20220267365 | NOVEL PHOSPHATE ESTER COMPOUND HAVING PYRROLOPYRIMIDINE SKELETON OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - There is provided a novel phosphate ester compound having a pyrrolopyrimidine skeleton having an excellent antitumor effect or a pharmaceutically acceptable salt thereof, and a method for preventing and/or treating a tumor in combination with an alkylating agent and/or a radiation therapy. According to one aspect of the present invention, there is provided a compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, and a method for preventing and/or treating a tumor in combination with an alkylating agent and/or a radiation therapy. | 2022-08-25 |
20220267366 | BETA-D-2'-DEOXY-2'-ALPHA-FLUORO-2'-BETA-C-SUBSTITUTED-2-MODIFIED-N6-SUBSTI- TUTED PURINE NUCLEOTIDES FOR HCV TREATMENT - A compound of the structure: | 2022-08-25 |
20220267367 | COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF PARKINSON'S DISEASE - Methods of preventing or retarding or reversing or abolishing the onset of Parkinson's and other neurodegenerative diseases are discussed. | 2022-08-25 |
20220267368 | METHOD FOR PREPARING BOTULINUM TOXIN - The present invention relates to a | 2022-08-25 |
20220267369 | METHODS OF SEPARATING HOST CELL LIPASES FROM A PRODUCTION PROTEIN IN CHROMATOGRAPHIC PROCESSES - Provided herein are methods of separating host cell lipases from a production protein in chromatographic processes and methods of improving polysorbate-80 stability in a production protein formulation by separating host cell lipases from the production protein using chromatographic processes. Also provided are pharmaceutical compositions comprising less than 1 ppm of a host cell lipase. | 2022-08-25 |
20220267370 | Process for Separating Antigen-Binding Polypeptide Monomers Comprising One or More Immunoglobulin Single Variable Domains from Aggregates of Said Monomers - A method that uses Protein A chromatography to separate antigen-binding polypeptide monomers comprising one or more immunoglobulin single variable domains (ISVDs) from aggregates of said monomers is disclosed. | 2022-08-25 |
20220267371 | METHODS FOR ANTIBODY DRUG CONJUGATION, PURIFICATION, AND FORMULATION - Methods of producing, purifying, and formulating antibody drug conjugates (ADCs) are provided herein. The methods use continuous conjugation processes, single-pass tangential flow filtration, countercurrent diafiltration, and/or in-line process automation technologies. The methods decrease process times and costs and improve product consistency. | 2022-08-25 |
20220267372 | COMPOUNDS FOR PROTEASOME ENZYME INHIBITION - Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Nn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. | 2022-08-25 |
20220267373 | SELF-ASSEMBLING PEPTIDES AND HYDROGELS - Novel self-assembling pentapeptides and peptides containing such self-assembling pentapeptides, self-assembled hydrogels, and methods of making and using the same are described. These pentapeptides, and peptides containing such pentapeptides, self-assemble under physiological conditions (e.g., in a physiological buffer under biologically acceptable conditions (e.g., pH≈6-11)) into long fibrils with sequence-dependent fibrillary morphologies. The hydrogels comprise one or more these pentapeptides which make up the 3-dimensional nanofibrous network of the hydrogel structure. The hydrogels are shear-thinning hydrogels that have high storage moduli and high rates of recovery after destruction. These hydrogels are useful in various applications, including but not limited to, scaffolds for tissue engineering, 2-dimensional (2-D) and 3-dimensional (3-D) cell cultures, drug delivery and encapsulation of therapeutic agents (cells, molecules, drugs, compounds), injectables (including those that gel in situ, such as hemostatic compositions), hemostatic agents, wound dressings, pharmaceutical carriers or vehicles, cell transplantation, cell storage, virus culture, and virus storage. | 2022-08-25 |
20220267374 | IMMUNITY INDUCER AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING AGING-RELATED DISEASES - An immunity inducer contains, as an active ingredient, any of a peptide (a) or (b) below, or an expression vector having a structural gene including a region encoding the peptide. (a) A peptide including an amino acid sequence represented by SEQ ID NO: 1 or 2; (b) a peptide having immunity induction activity and including an amino acid sequence in which one or several amino acids are deleted, substituted or added in the amino acid sequence represented by SEQ ID NO: 1 or 2. A pharmaceutical composition for preventing or treating aging-related diseases includes the immunity inducer and an adjuvant. | 2022-08-25 |
20220267375 | NOVEL PEPTIDE - Provided are a novel peptide, a polynucleotide encoding the peptide, an expression vector including the polynucleotide, and a pharmaceutical composition including the peptide, a quasi-drug composition including the peptide, and a health functional food composition including the peptide. | 2022-08-25 |
20220267376 | P53 ACTIVATOR PEPTIDOMIMETIC MACROCYCLES - Peptidomimetic macrocycles that comprise all-D configuration ?-amino acids and bind mouse double minute 2 (MDM2 aka E3 ubiquitin-protein ligase) and MDMX (aka MDM4) are described. These all-D configuration α-amino acid peptidomimetic macrocycles are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy. | 2022-08-25 |
20220267377 | COMPOSITIONS COMPRISING CHEMERIN ANALOGS AND METHODS OF USE - The present disclosure relates to peptide compositions and methods for treating an inflammatory condition such as ocular inflammation, retinal inflammation, dry eye, uveitis, allergic conjunctivitis, and inflammation resulting from nerve injury or nerve degeneration. The peptide compositions disclosed herein can also be used for treating pain such as neuropathic pain, ocular pain, chronic pain, pain resulting from chemotherapy or radiation, pain resulting from nerve injury or nerve degeneration, and pain resulting from an inflammatory condition, dysesthesia, or allodynia. | 2022-08-25 |
20220267378 | PEPTIDES AS INHIBITORS OF FIBROTIC MATRIX ACCUMULATION - The present invention relates to peptides that inhibit overproduction and/or excess accumulation of extracellular matrix in an organ or tissue. The inventive peptides have the general sequence Xa-Leu-Gln-Gly-Xb (SEQ ID NO: 1), wherein Xa is selected from Pro-Gly, Gly and Ac-Gly and Xb is selected from Glu and Glu-NH | 2022-08-25 |
20220267379 | NOVEL INHIBITORS OF KALLIKREIN PROTEASES AND USES THEREOF - The present invention relates to a cyclic inhibitor of a kallikrein protease comprising or consisting of (I) the peptide (X | 2022-08-25 |
20220267380 | Glycopeptides Increasing Lipid Synthesis - The present invention relates to a glycopeptide of the following formula I: or a tautomer, a stereoisomer or a mixture of stereoisomers thereof in any proportions, in particular a mixture of enantiomers, and particularly a racemate mixture, and/or a physiologically acceptable salt and/or solvate thereof, in which:—n represents an integer from 1 to 6,—m represents 0 or 1,10—p represents 0 or 1—R represents H, F, CH | 2022-08-25 |
20220267381 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING AUTOIMMUNE INDUCED CARDIAC LONG QT SYNDROME - Disclosed herein, are decoy peptides or polypeptides capable of neutralizing and/or inhibiting the binding of anti-Ro antibodies to a hERG potassium channel extracellular pore region, and pharmaceutical compositions containing the decoy peptides or polypeptides and methods of use. | 2022-08-25 |
20220267382 | CHIMERIC HEMAGGLUTININ PROTEIN AND A VACCINE COMPOSITION COMPRISING THE SAME - Provided is a chimeric hemagglutinin (HA) protein including an HA1 subunit and an HA2 subunit, in which the HA1 subunit is composed of a first domain derived from a parental HA1 subunit of a first subtype influenza virus and a second domain derived from a parental HA1 subunit of a second subtype influenza virus. The chimeric HA protein has improved thermal stability and can be used in a vaccine composition for preventing influenza virus infection. Also provided is a method of inducing an immune response against an influenza virus in a subject in need thereof that includes administering the chimeric HA protein to the subject, thereby conferring protection against the influenza virus infection on the subject. | 2022-08-25 |
20220267383 | MODIFIED AAV CAPSID PROTEINS AND USES THEREOF - Adeno associated viral (AAV) particles are emerging as a useful vehicle for gene delivery to various organs and tissues, one of them being the retina. Provided here are variant AAV (e.g., variant serotype 2 (AAV2)) capsid proteins and variant capsid protein containing particles with enhanced ability to transduce retinal cells. | 2022-08-25 |
20220267384 | PROTEINS COMPRISING BINDING REGIONS, SHIGA TOXIN A SUBUNIT EFFECTOR REGIONS, AND CARBOXY-TERMINAL, ENDOPLASMIC RETICULUM LOCALIZATION SIGNAL MOTIFS - The present invention provides proteins comprising binding regions for cell-type specific targeting, Shiga toxin effector regions derived from A Subunits of members of the Shiga toxin family for providing Shiga toxin effector functions (e.g. cellular internalization and cytotoxicity), and carboxy-terminal endoplasmic reticulum localization signal motifs. The presently disclosed proteins can comprise additional exogenous materials, such as, e.g., antigens, cytotoxic agents, and detection-promoting agents, and are capable of targeted delivery of these additional exogenous materials into the interiors of target cells. The proteins of the present invention have uses in methods such as, e.g., methods involving targeted killing of target cells, delivering exogenous materials into target cells, labeling subcellular compartments of target cells, and diagnosing and/or treating a variety of conditions including cancers, tumors, other growth abnormalities, immune disorders, and microbial infections. | 2022-08-25 |
20220267385 | IMMUNOGENIC FUSION PROTEIN - The present invention relates to an immunogenic fusion protein comprising a first amino acid sequence having at least 80% sequence identity with the amino acid sequence of the N-terminal region of a first group B | 2022-08-25 |
20220267386 | SELF-COMPATIBILITY IN CULTIVATED POTATO - The invention relates to an isolated nucleic acid molecule comprising a nucleic acid sequence encoding a protein having the amino acid sequence as depicted in SEQ ID NO:10, and sequences having at least 70% sequence identity with said amino acid sequence and conferring self-compatibility to a potato plant. The invention further relates to a transformed plant that comprises the nucleic acid sequence, and parts thereof. The invention further related to methods for the selection and methods for the production of a plant comprising the nucleic acid sequence, and to a plant that is obtainable by these methods. Said plant may further comprise at least one allele of each of a Phytophtera infestance resistance gene selected from | 2022-08-25 |
20220267387 | FLAVIN MONONUCLEOTIDE-BINDING PROTEIN VARIANTS HAVING IMPROVED FLUORESCENCE INTENSITY DERIVED FROM ARABIDOPSIS THALIANA - The present invention relates to flavoprotein improved LOV (iLOV) variants that exhibit enhanced fluorescence intensity compared to iLOV. The present invention also relates to a method for screening any of the iLOV variants. The iLOV variants of the present invention are useful in determining whether target proteins are expressed, irrespective of the presence of oxygen, and isolating and purifying the expressed target proteins due to their enhanced fluorescence intensity and quantum yield compared to existing LOV or iLOV proteins. | 2022-08-25 |
20220267388 | ENGINEERED Fc CONSTRUCTS - The present disclosure relates to engineered IgG Fc constructs and uses thereof. | 2022-08-25 |
20220267389 | NANOSPHERES OF SEC14-LIKE PROTEINS AND COGNATE LIGANDS - The present invention relates to a nanosphere comprising an equal number of a human SEC 14-like protein and a cognate ligand of said SEC 14-like protein as well as to methods of producing the same and uses of said nanospheres. | 2022-08-25 |
20220267390 | MPS MODIFIED PEPTIDES AND USE THEREOF - This disclosure provides an isolated polypeptide therapeutics, polynucleotides encoding the polypeptides and antibodies that bind to the polypeptides are also provided. Therapeutic and diagnostic uses are further provided. | 2022-08-25 |
20220267391 | NOVEL PEPTIDES AND COMBINATION OF PEPTIDES FOR USE IN IMMUNOTHERAPY AGAINST LUNG CANCER, INCLUDING NSCLC, SCLC AND OTHER CANCERS - 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. | 2022-08-25 |
20220267392 | NOVEL PEPTIDES AND COMBINATION OF PEPTIDES FOR USE IN IMMUNOTHERAPY AGAINST LUNG CANCER, INCLUDING NSCLC, SCLC AND OTHER CANCERS - 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. | 2022-08-25 |
20220267393 | A Method for Producing An Active Hepatocyte Growth Factor (HGF) - The present invention provides a method for producing active hepatocyte growth factor activator (HGFA) and active hepatocyte growth factor (HGF) without using animal serum. The present invention relates to a method for producing active HGFA without using animal serum. The method is characterized in that it comprises a step of obtaining a culture supernatant comprising pro-HGFA by culturing mammalian cells expressing inactive hepatocyte growth factor activator (pro-HGFA) in a medium without serum, and a step of adjusting the culture supernatant comprising pro-HGFA obtained in the above step to weakly acidic to convert pro-HGFA into active HGFA. The present invention also relates to a method for producing active HGF with HGFA produced by said method. | 2022-08-25 |