03rd week of 2022 patent applcation highlights part 23 |
Patent application number | Title | Published |
20220017484 | INHIBITOR OF BRUTON TYROSINE KINASE - Disclosed herein is a compound of Formula (I) with a Btk inhibitory activity, wherein all the variables are as defined herein. The compound can be used for the treatment of diseases such as autoimmune diseases, xenogeneic immune diseases, cancers or thromboembolic diseases. Also disclosed is a pharmaceutical composition comprising a compound of Formula (I). Further provided is a compound capable of inhibiting the activity of Bruton's tyrosine kinase by covalent binding. | 2022-01-20 |
20220017485 | Acyl Sulfonamides that are BCL Family Antagonists for Use in Clinical Management of Conditions Caused or Mediated by Senescent Cells and for Treating Cancer - The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Selected compounds in this class promote apoptosis in senescent cells, and are being developed for treating senescent-related conditions. Selected compounds in this class promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents. | 2022-01-20 |
20220017486 | DOCK1-INHIBITING COMPOUND AND USE THEREOF - Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof: | 2022-01-20 |
20220017487 | DEUTERATED COMPOUNDS AND USES THEREOF - The present invention provides deuterium-enriched CXCR4 inhibitors, pharmaceutical compositions, and methods of using such deuterium-enriched CXCR4 inhibitors and pharmaceutical compositions to treat, prevent, or ameliorate a disease, disorder, or condition such as cancer or WHIM syndrome. | 2022-01-20 |
20220017488 | PLXDC2 LIGANDS - Provided are compounds that target plexin domain containing 2 (PLXDC2). The compounds can be used to treat conditions such as inflammatory or immune-mediated diseases, diabetes, infectious diseases, and cancers. The compounds can be used to treat such specific conditions as systemic lupus erythematosus, rheumatoid arthritis, multiple sclerosis, autoimmune encephalitis, diabetic nephropathy, diabetic retinopathy, psoriasis, and inflammatory bowel disease, among other conditions. | 2022-01-20 |
20220017489 | SOLID DISPERSIONS FOR TREATMENT OF CANCER - Provided herein are amorphous solid dispersions comprising Compound 1 and a polymer. Pharmaceutical compositions comprising the solid dispersions and methods for treating, preventing and managing cancer are also disclosed. | 2022-01-20 |
20220017490 | CO-CRYSTALS OF 2-METHYL-1 -[(4-[6-(TRIFLUOROMETHYL)PYRIDIN-2-YL]-6-{[2-(TRIFLUOROMETHYL) PYRIDIN-4-YL]AMINO}-1,3,5-TRIAZIN-2-YL)AMINO]PROPAN-2-OL, COMPOSITIONS AND METHODS OF USE THEREOF - Provided herein are co-crystals comprising Compound 1 and a coformer. Pharmaceutical compositions comprising the co-crystals and methods for treating, preventing and managing disease are also disclosed. | 2022-01-20 |
20220017491 | COMPOUND INHIBITING YAP-TEAD BINDING, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER, COMPRISING COMPOUND AS ACTIVE INGREDIENT - The present invention relates to a compound which inhibits the binding of Yes associated protein (YAP) and transcriptional enhancer associate domain (TEAD), a prodrug of same, a hydrate of same, a solvate of same or a pharmaceutically acceptable salt of same, and a composition comprising same as an active ingredient, the compound according to the present invention being able to be applied as an inhibitor which can directly inhibit YAP-TEAD binding in the Hippo pathway which plays a crucial role in the occurrence of cancer. | 2022-01-20 |
20220017492 | MMPL3 INHIBITORS, COMPOSITIONS AND USES THEREOF - The present disclosure relates generally to inhibitors of mycobacterial membrane protein MmpL3, compositions comprising the inhibitors, and methods of preparation and use thereof. | 2022-01-20 |
20220017493 | PYRAZOLE COMPOUNDS AND USES THEREOF - The present invention provides pyrazole derivatives, e.g., a compound of Formula (I), and their uses in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders. | 2022-01-20 |
20220017494 | METHODS FOR SYNTHESIZING VINYLIDENES AND ALKENES - The present disclosure provide synthetic methods for the synthesis of N-substituted vinylidene and alkene compounds in addition to compounds formed from such methods. | 2022-01-20 |
20220017495 | CONJUGATES OF BIVALENT EVANS BLUE DYE DERIVATIVES AND METHODS OF USE - A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt, is disclosed. Compositions comprising the compound and methods of use are also disclosed. Those dimeric Evans Blue derivatives, denoted as N(tEB)2, reversibly bind two molecules of albumin via the two albumin binding regions of each NtEB in the dimer, resulting in significantly increased binding affinity to albumin and extended circulation half-life in vivo. Further, when the N(tEB)2 is conjugated to a peptide therapeutic, the in situ formation of the complex of N(tEB)2 with two albumin molecules resulted in increased resistance of the peptide therapeutic from proteolysis. | 2022-01-20 |
20220017496 | DISUBSTITUTED PYRAZOLE COMPOUNDS - The present invention provides a compound of Formula I. | 2022-01-20 |
20220017497 | COMPOSITIONS AND METHODS FOR DECREASING, OR PREVENTING OR REVERSING GAIN OF, SKIN PIGMENTATION IN A MAMMALIAN SUBJECT - The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds of the invention treat or prevent skin disorders or diseases associated with hyperpigmentation in the subject. In other embodiments, the compounds of the invention act as antagonist to the non-canonical sex steroid hormone receptor GPRE1 and do not bind to a canonical nuclear estrogen receptor (ER). In yet other embodiments, the compounds of the invention comprise acts as agonists to the non-canonical sex steroid hormone receptor PAQR7 and do not bind to a canonical nuclear progesterone receptor (PR). | 2022-01-20 |
20220017498 | SALT OF SYK INHIBITOR AND CRYSTALLINE FORM THEREOF - Provided is a salt of an Syk inhibitor and a crystalline form thereof, and more specifically, provided are 5-fluoro-1-methyl-3-((5-(4-(oxetan-3-yl)piperazine-1)-yl)pyridin-2-yl)amino)-6-(1H-pyrazol-3-yl)quinoline-2(1H)-ketamine hydrochloride, a crystalline form thereof, a preparation method therefor, a pharmaceutical composition thereof and a use thereof. The hydrochloride of the compound represented by formula I and the crystalline form thereof have good salt-forming properties, high stability and low hygroscopicity, have advantages in terms of physical properties, safety and metabolic stability, and have value in prepared medicines. | 2022-01-20 |
20220017499 | Process for Preparing 1-([3R,4S)-4-Cyanotetrahydropyran-3-YL]-3-[(2-fluoro-6-Methoxy-4-Pyridyl)- Amino]Pyrazole-4-Carboxamide - The application relates to processes for the preparation of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide (I) which include (i) a synthesis for bromo and iodo pyridine intermediates, (ii) a synthesis of a pyrazole ester intermediate which can be obtained in enantiopure form and (iii) the combination of these intermediates into compound (I). | 2022-01-20 |
20220017500 | CRYSTAL FORMS OF CRENOLANIB AND METHODS OF USE THEREOF - The present invention relates to novel crystalline polymorphs of 1-[2-[5-[(3-Methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine monobenzenesulfonate, and to methods for their preparation. The invention further relates to pharmaceutical compositions containing one or more forms and optionally one or more suitable pharmaceutical carriers. The invention also relates to methods of using the crystalline polymorphs of the invention in the treatment of disease. | 2022-01-20 |
20220017501 | MICROBIOCIDAL THIAZOLE DERIVATIVES - Compounds of the formula (I), wherein the substituents are as defined in claim | 2022-01-20 |
20220017502 | MODULATORS OF TREX1 - Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1. | 2022-01-20 |
20220017503 | TRIBENZAZOLE AMINE DERIVATIVE AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING SAME - Provided is a tribenzazole amine derivative represented by Formula 1 that effectively absorbs high energy UV light from an external light source to minimize damage to organic materials present in an organic electroluminescent device, contributing to a substantial improvement in the lifetime of the organic electroluminescent device. Also provided is an organic electroluminescent device using the tribenzazole amine derivative. The organic electroluminescent device includes a first electrode, a second electrode, and an organic layer arranged between the first and second electrodes. The organic layer includes the tribenzazole amine derivative. | 2022-01-20 |
20220017504 | QUINOLINONE AND BENZOXAZINE DERIVATIVES AS MUSCARINIC M1 AND/OR M4 RECEPTOR AGONISTS - This invention related to compounds having activity as muscarinic M | 2022-01-20 |
20220017505 | AMINOQUINAZOLINONE AND AMINOISOQUINOLINONE DERIVATIVES AND APPLICATION THEREOF - Provided by the present disclosure are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present disclosure have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present disclosure can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b are shown as below: | 2022-01-20 |
20220017506 | MORPHOLINYL, PIPERAZINYL, OXAZEPANYL AND DIAZEPANYL O-GLYCOPROTEIN-2-ACETAMIDO-2-DEOXY-3-D-GLUCOPYRANOSIDASE INHIBITORS - Described herein are compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R | 2022-01-20 |
20220017507 | PI-Kinase Inhibitors with Anti-Infective Activity - Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole or a 5-heteroaryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like. | 2022-01-20 |
20220017508 | METHOD FOR PREPARING A KEY INTERMEDIATE FOR THE SYNTHESIS OF STATINS - Disclosed herein relates to organic synthesis, and more particularly to a method for preparing a key intermediate for the synthesis of statins. The key intermediate is 2-[(4R, 6S)-6-[(benzo[d]thiazol-2-ylthio)methyl]-2,2-di substituted-1,3-dioxan-4-yl] acetate of formula (I): | 2022-01-20 |
20220017509 | GAS41 INHIBITORS AND METHODS OF USE THEREOF - Provided herein are small molecules that bind to GAS41 and inhibit GAS41 activity, and methods of use thereof for the treatment of cancer. | 2022-01-20 |
20220017510 | BIFUNCTIONAL MOLECULES FOR DEGRADATION OF EGFR AND METHODS OF USE - The present application provides bifunctional compounds of Formula (I): | 2022-01-20 |
20220017511 | Bromodomain Inhibitors - The present invention provides for compounds of formula (I) | 2022-01-20 |
20220017512 | SIX-MEMBERED AND SIX-MEMBERED HETEROCYCLIC COMPOUND AND USES THEREOF SERVING AS PROTEIN RECEPTOR KINASE INHIBITOR - Provided are a preparation and applications of a six-membered fused with six-membered heterocyclic compound, specifically, provided in the present invention is a compound as represented by formula I as follows, where the definitions of the groups are as described in the description. The compound has TRK kinase inhibiting activity and can serve as a pharmaceutical composition for treating TRK dysfunction-related diseases. | 2022-01-20 |
20220017513 | AROMATIC RING DERIVATIVE AS IMMUNOREGULATION AND PREPARATION METHOD AND APPLICATION OF AROMATIC RING DERIVATIVE - Relating to a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, and an application of the compound as an S1P1 agonist. | 2022-01-20 |
20220017514 | HETEROCYCLIC COMPOUND - The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. | 2022-01-20 |
20220017515 | sGC STIMULATORS - The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP) might be desirable. Various compounds are disclosed, including those of Formula I: | 2022-01-20 |
20220017516 | LOX INHIBITORS - The disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, Formula (I) as defined herein. Compounds according to Formula I are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer. | 2022-01-20 |
20220017517 | SUBSTITUTED PIPERIDINE COMPOUNDS AND THEIR USE - Provided are compounds represented by the following formulas (I), (II), (III) and (IV) having orexin type 2 receptor-activating activity, or their pharmaceutically acceptable salts. | 2022-01-20 |
20220017518 | Histone Deacetylase Inhibitors and Methods of Use Thereof - The present invention relates to methods of modulating activity of histone deacetylases (HDACs). The present invention also relates to methods of treating HDAC-associated diseases including, but not limited to, cancers, inflammatory disorders, and neurodegenerative disorders. The present invention also provides novel compounds and compositions thereof and methods of preparation of the same. The present invention also includes methods of inhibiting HDACs, and methods of treating HDAC-associated diseases using the compounds of the invention. | 2022-01-20 |
20220017519 | 7-BENZYL-4-(2-METHYLBENZYL)-2,4,6,7,8,9-HEXAHYDROIMIDAZO [1,2-a]PYRIDO[3,4-e]PYRIMIDIN-5(1H)-ONE, ANALOGS THEREOF, AND SALTS THEREOF AND METHODS FOR THEIR USE IN THERAPY - This disclosure relates to methods of treatment using compound (1) or analogs thereof, and pharmaceutically acceptable salts thereof. Also disclosed are compounds of formula (10): | 2022-01-20 |
20220017520 | MACROCYCLIC COMPOUND AS CDK INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE - The present invention relates to a macrocyclic compound as a CDK inhibitor, a preparation method therefor and the use thereof in medicine. Specifically, the present invention relates to a novel macrocyclic compound represented by a general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, the use thereof as a therapeutic agent, particularly as a CDK inhibitor, and the use thereof in treating cancers, inflammation, viral infections, cardiac hypertrophy or HIV, wherein each substituent of the general formula (I) is the same as that defined in the description. | 2022-01-20 |
20220017521 | PYRAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF - Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and/or FGFR activity, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity and/or FGFR activity, such as cancer. | 2022-01-20 |
20220017522 | METHOD FOR PREPARING PYRROLOPYRIMIDINE COMPOUND AND APPLICATION THEREOF - The present invention provides a method for preparing a pyrrolopyrimidine compound and application thereof. Specifically, the present invention provides a compound represented by formula I or pharmaceutically-acceptable salts thereof, a pharmaceutical composition containing the compound or its salts, and a method for preparing the pharmaceutical composition and an application of the pharmaceutical composition as an immunosuppressive drug. | 2022-01-20 |
20220017523 | BLOOD-BRAIN BARRIER-PENETRANT DOPAMINE- -HYDROXYLASE INHIBITORS - This invention relates to: (a) compounds of formula I (with R | 2022-01-20 |
20220017524 | ARYL HYDROCARBON RECEPTOR (AHR) ACTIVATOR COMPOUNDS AS CANCER THERAPEUTICS - The present disclosure relates to compositions and methods for the diagnosis and treatment or prevention of cancers, particularly cancers that exhibit elevated expression of FOXA1 and/or FOXA1 gene targets, such as certain breast, liver and/or prostate cancers, including luminal and/or ER-positive forms of breast cancer. Three previously identified adenosine receptor antagonists, CGS-15943, MRS-1220 and SCH-58261, as well as furan ring moiety-possessing derivatives of CGS-15943 are specifically provided for killing cancer cells in a manner that appears to involve activation of the aryl hydrocarbon receptor (AHR) by such compounds. The instant disclosure therefore provides for selecting and/or administering CGS-15943, MRS-1220, SCH-58261 and/or a furan-possessing derivative of CGS-15943, MRS-1220 and/or SCH-58261 as a therapeutic agent to target a cancer cell and/or subject having or at risk of developing a cancer. Methods and compositions for therapies that include such compounds are also provided | 2022-01-20 |
20220017525 | CYCLOBUTYL PYRAZOLOPYRIMIDINE PDE9 INHIBITORS - The present invention is directed to cyclobutyl pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 2022-01-20 |
20220017526 | PYRAZOLOPYRIMIDINE PDE9 INHIBITORS - The present invention is directed to amino and alkyl pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 2022-01-20 |
20220017527 | NOVEL PROCEDURE FOR THE FORMATION OF 2H-BENZOTRIAZOLE BODIES AND CONGENERS - The present invention relates to a process for the preparation of 2H-benzotriazole compounds and congeners, novel 2H-benzotriazole compounds and congeners and their use as UV absorbers in coatings and bulk plastics. | 2022-01-20 |
20220017528 | COMPOUNDS HAVING PDE9A INHIBITORY ACTIVITY, AND PHARMACEUTICAL USES THEREOF - The present invention provides a compound having a specific chemical structure and having PDE9A inhibitory activity, or a pharmaceutically acceptable salt thereof. The present invention provides a composition containing the compound or a pharmaceutically acceptable salt thereof. The present invention provides a pharmaceutical use, for treating or preventing PDE9A-related diseases, of the compound according to the present invention, a salt thereof, and a composition containing the compound or salt. The present invention also provides a method for treating or preventing PDE9A-related diseases, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing the compound or salt to a subject in need of treatment. | 2022-01-20 |
20220017529 | NOVEL L-PROLINE SULFONAMIDE DERIVATIVES COMPRISING PYRAZOLO[4,3- E]TETRAZOLO[4,5-B][1,2,4]TRIAZINE SYSTEM, METHOD OF MANUFACTURING THEREOF, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The subject matter of the invention relates to novel sulfonamide derivatives of 7-methyl-5-phenyl-pyrazolo[4,3-c]tetrazolo[4,5-b] [1,2,4]triazine comprising L-proline or 4-hydroxy-L-proline in the sulfonamide group. The novel compounds exhibit cytostatic activity against gastric cancer cell (AGS) and colorectal cancer cell (DLD-1 and HT-29) lines and may be used as novel medicaments which have anticancer action. The subject matter of the invention also relates to a method of manufacturing such derivatives, as well as uses thereof and a pharmaceutical composition comprising the same. | 2022-01-20 |
20220017530 | HETEROCYCLIC COMPOUND - The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I): | 2022-01-20 |
20220017531 | FLUORESCENT DYES - Automated oligonucleotide synthesis-compatible fluorescent dye phosphoramidite compounds, solid supports, and labeled polynucleotides incorporating the compounds are provided. The compounds allow universal incorporation of the fluorescent label into any position of the polynucleotide. | 2022-01-20 |
20220017532 | MONOHYDRATE POTASSIUM SALT OF A THIENOPYRIDONE DERIVATIVE AND ITS PREPARATION PROCESS - The invention relates to a process for preparing a monohydrate potassium salt of a 5 thienopyridone derivative. It also relates to a monohydrate potassium salt of a thienopyridone derivative and its use in medicine, in particular for treating or preventing metabolic disorders, such as NASH. | 2022-01-20 |
20220017533 | CRYSTALLINE FORMS OF A MCL-1 INHIBITOR, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Crystalline forms of Compound A: | 2022-01-20 |
20220017534 | IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS - The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4 A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. | 2022-01-20 |
20220017535 | INHIBITORS OF ALDOSE REDUCTASE - The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, the treatment of ischemic injury, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, cardiomyopathy, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, diabetic cardiomyopathy, infections of the skin, peripheral vascular disease, stroke, galactosemia, asthma, PMM2-CDG and the like. | 2022-01-20 |
20220017536 | Crystal Form of Hepatitis B Surface Antigen Inhibitor - The present invention discloses a crystal form of a hepatitis B surface antigen inhibitor and a preparation method therefor, and also comprises the use of the crystal form in preparing the hepatitis B surface antigen inhibitor. | 2022-01-20 |
20220017537 | COMPOSITIONS AND METHODS FOR REGULATING GLUCOSE HOMEOSTATSIS AND INSULIN ACTION - The present invention encompasses the use of compounds for a novel approach to treat and prevent diseases, conditions, and disorders such as diabetes and ischemic reperfusion injury. Compounds of the invention, including but not limited to BAM15 ((2-fluorophenyl){6-[(2-fluorophenyl)amino](1,2,5-oxadiazolo[3,4-e]pyrazin-5-yl)}amine), a mitochondrial uncoupler, can improve glucose tolerance, increases cellular oxygen consumption, treat or prevent kidney ischemia reperfusion injury reverse insulin resistance, reverse or treat hyperinsulinemia, and reverse or treat hyperlipidemia. The present invention further provides novel compounds as well as methods for identifying compounds with the same or similar properties as BAM15. | 2022-01-20 |
20220017538 | THIOESTER PRODRUGS OF MACROCYCLES AS INHIBITORS OF HISTONE DEACETYLASES - The present invention provides a novel macrocyclic prodrug compound of general Formula (I), a pharmaceutical composition comprising a compound of Formula (I), and a method for treating diseases mediated by HDAC enzymes by administering a compound of Formula (I), wherein R | 2022-01-20 |
20220017539 | SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUND, COMPOSITION CONTAINING THE SAME AND USE THEREOF - The present disclosure provides a substituted pyrazolo[1,5-a]pyridine compound, a composition including the same, and a use thereof. The substituted pyrazolo[1,5-a]pyridine compounds is a compound represented by formula (I) or the tautomers, stereoisomers, prodrugs, crystal forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compound of the present disclosure and composition thereof are useful for treating RET kinase-mediated diseases or conditions and have more excellent pharmacokinetic properties. | 2022-01-20 |
20220017540 | DIAZABICYCLIC SUBSTITUTED IMIDAZOPYRIMIDINES AND THEIR USE FOR THE TREATMENT OF BREATHING DISORDERS - The present invention relates to novel diazabicyclically substituted imidazo[1,2-a]pyrimidine derivatives, to methods for producing the same, to the use thereof either alone or in combinations for the treatment and/or prevention of diseases, as well as to their use for preparing medicaments for the treatment and/or prevention of diseases, especially for treatment and/or prevention of breathing disorders, including sleep-related breathing disorders such as obstructive and central sleep apnoea and snoring. | 2022-01-20 |
20220017541 | INHIBITORS OF ARGINASE - Compounds and compositions as inhibitors of arginase are provided. They may find use as therapeutic agents for the treatment of diseases or conditions associated with expression or activity of arginase. | 2022-01-20 |
20220017542 | PROTEASOME INHIBITORS - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 2022-01-20 |
20220017543 | METHOD FOR PREPARING BORIC ACID ESTER USING UNCATALYZED HYDROBORATION OF CARBOXYLIC ACID - Disclosed is a method for preparing a boric acid ester using non-catalyzed hydroboration of a carboxylic acid. The method includes: in an inert gas atmosphere, mixing pinacolborane and a carboxylic acid and stirring until uniform in a reaction flask subjected to dehydration and deoxygenation treatments, reacting for 6-12 hours to obtain the boric acid ester, then adding silica gel and methanol, and conducting a hydrolysis reaction to prepare an alcohol compound. The carboxylic acid is acetic acid, caproic acid, pentanoic acid, heptanoic acid, trimethylacetic acid, adipic acid, benzoic acid, 4-bromobenzoic acid, 4-fluorobenzoic acid, 1-naphthoic acid, 2-methoxybenzoic acid, 4-tert-butylbenzoic acid, 4-ethoxybenzoic acid, 2-bromobenzoic acid, 4-iodobenzoic acid, 3-phenylpropionic acid, diphenyl acetic acid, 2-phenylbutyric acid, indole-3-acetic acid, o-carboxyl phenylacetic acid or 2-methyl-5-bromobenzoic acid. The present invention utilizes a carboxylic acid to efficiently undergo hydroboration with borane without a catalyst for the first time. | 2022-01-20 |
20220017544 | NOVEL COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME - Provided is a compound of Chemical Formula 1: | 2022-01-20 |
20220017545 | COMPOUND AND ORGANIC LIGHT EMITTING DIODE COMPRISING SAME - A compound of Formula 1 and an organic light emitting device including the same. | 2022-01-20 |
20220017546 | PROCESS FOR REDUCING THE CONTENT OF BORON COMPOUNDS IN HALOSILANE-CONTAINING COMPOSITIONS - The content of boron compounds in a composition containing at least one halosilane is reduced by bringing the composition into contact with at least one phenylsilane and removing the at least one halosilane. The invention further relates to the use of phenylsilanes for removing boron compounds from halosilane-containing compositions. | 2022-01-20 |
20220017547 | ORGANOSILICON COMPOUND, METHOD FOR PRODUCING THEREOF, AND USE THEREOF - An organosilicon compound having not more than 200 silicon atoms per molecule is provided. The organosilicon compound is represented by the following average compositional formula (I): Y | 2022-01-20 |
20220017548 | Compounds and Methods for the Treatment of COVID-19 - The invention relates to compounds of formula I | 2022-01-20 |
20220017549 | PSILOCIN DERIVATIVES AS SEROTONERGIC PSYCHEDELIC AGENTS FOR THE TREATMENT OF CNS DISORDERS - The present application relates to psilocin derivatives of Formula (1), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. | 2022-01-20 |
20220017550 | 3-PYRROLIDINE-INDOLE DERIVATIVES AS SEROTONERGIC PSYCHEDELIC AGENTS FOR THE TREATMENT OF CNS DISORDERS - The present application relates to 3-cyclic amine-indole derivatives of general Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. The diseases, disorders or conditions include, for example, psychosis, mental illnesses, and other neurological diseases, disorders and conditions. | 2022-01-20 |
20220017551 | SELECTIVE DETECTION OF BED BUGS - A device, system, and method of controlling pests are disclosed. A pest control device includes a sensor having a sensor cell and a controller. A surface of the sensor cell is coated with an agent that reacts with a targeted biochemical analyte secreted by pests. The controller is coupled to the sensor and is configured to receive sensor data from the sensor cell indicative of a rate of change in sensor mass detected on the surface of the sensor cell, determine whether the rate of change in the sensor mass based on the received sensor data exceeds a predefined threshold rate, and transmit a pest detection alert notification to a server in response to a determination that the rate of change exceeds the predetermined threshold rate. | 2022-01-20 |
20220017552 | ELECTROLUMINESECENT MATERIAL, METHOD FOR MANUFACTRUING THE SAME, AND LUMINESECENT DEVICE - The present application provides a luminescent material, a method for manufacturing the luminescent material and a luminescent device, the method includes providing a first reactant and a second reactant, reacting the first reactant and the second reactant to generate a mixture containing the luminescent material, separating and purifying the mixture containing the luminescent material to obtain the luminescent material. | 2022-01-20 |
20220017553 | COBALT COMPLEX, METHOD FOR MANUFACTURING SAME, AND METHOD FOR MANUFACTURING COBALT-CONTAINING THIN FILM - To provide a cobalt complex which is liquid at room temperature, useful for producing a cobalt-containing thin film under conditions without using an oxidizing gas. | 2022-01-20 |
20220017554 | COMPOUND, RAW MATERIAL FOR FORMING THIN FILM, METHOD FOR MANUFACTURING THIN FILM, AND AMIDINE COMPOUND - A raw material for forming a thin film, comprising a compound represented by General Formula (1) below. | 2022-01-20 |
20220017555 | IMPROVED PROCESS FOR TREATING LIGNIN - This invention provides improvements to processes for making granular lignin from black liquor. One of the improvements is that the use of a pre-carbonation column reduces the CO | 2022-01-20 |
20220017556 | METHODS FOR PRODUCING STEREOISOMERICALLY ENRICHED CARBOHYDRATE-BASED SURFACTANTS - The present disclosure discusses methods for producing stereoisomerically enriched carbohydrate-based surfactants. In particular, methods of the invention include producing stereoisomerically enriched hydrophobic portion of the carbohydrate-based surfactants. | 2022-01-20 |
20220017557 | HIGH-PURITY STEVIOL GLYCOSIDES - Methods of preparing highly purified steviol glycosides, particularly steviolmonoside, steviolmonoside A, steviolbioside, steviolbioside D, rubusoside, steviolbioside A, steviolbioside B, rebaudioside B, stevioside, rebaudioside G, stevioside A, stevioside B, stevioside C, rebaudioside A, rebaudioside E, rebaudioside E2, rebaudioside E4, rebaudioside E6, rebaudioside E3, rebaudioside D, rebaudioside 1, rebaudioside AM, rebaudioside D7, rebaudioside M, rebaudioside M4, rebaudioside 1a, rebaudioside 1b, rebaudioside 1c, rebaudioside 1d, rebaudioside 1e, rebaudioside 1f rebaudioside 1g, rebaudioside 1h, rebaudioside 1i, rebaudioside 1j, rebaudioside 1k, rebaudioside 1l, rebaudioside 1m, rebaudioside 1n, rebaudioside 2a and/or SvG7 are described. The methods include utilizing enzyme preparations and recombinant microorganisms for converting various staring compositions to target steviol glycosides. The highly purified steviol glycosides are useful as non-caloric sweetener, flavor enhancer, sweetness enhancer, and foaming suppressor in edible and chewable compositions such as any beverages, confectioneries, bakery products, cookies, and chewing gums. | 2022-01-20 |
20220017558 | NOVEL GALACTOSIDE INHIBITOR OF GALECTINS - A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. | 2022-01-20 |
20220017559 | CYCLIC PEROXIDES AS PRODRUGS FOR SELECTIVE DELIVERY OF AGENTS - Disclosed herein, inter alia, are prodrug compositions and methods of using the same for treatment and detection of disease. Specifically, disclosed herein is a compound of formula (I) having spiro-fused 1,2,4-trioxolane and piperidine rings, namely, 1,2,4-trioxa-8-azaspiro[4.5] decane. Also disclosed is a pharmaceutical composition containing the compound and a pharmaceutically acceptable carrier. | 2022-01-20 |
20220017560 | COMPOSITIONS AND METHODS OF MODULATING THE IMMUNE RESPONSE BY ACTIVATING ALPHA PROTEIN KINASE 1 - The disclosure provides compositions and methods related to activating alpha-kinase 1 (ALPK1) for modulating an immune response and treating or preventing cancer, infection, inflammation and related diseases and disorders as well as potentiating an immune response to a target antigen. The disclosure also provides heterocyclic compounds of formula (I) as agonists of alpha protein kinase 1 (ALPK1) and their use in activating ALPK1, modulating an immune response and treating diseases such as cancer, wherein A | 2022-01-20 |
20220017561 | CYCLIC DINUCLEOTIDES FOR CYTOKINE INDUCTION - A cyclic dinucleotide compound of Formula (I): | 2022-01-20 |
20220017562 | 3beta-(benzyloxy)-17alpha-methyl-pregn-5-en-20-one for use in the treatment of cognitive disorders - The present invention generally relates to a specific pregnenolone derivative for its use for the treatment of a cognitive disorders. More particularly, the invention relates to a compound of Formula (I) | 2022-01-20 |
20220017563 | MOGROSIDE COMPOUNDS AND USES THEREOF - The various aspects presented herein relate to processes for preparing food ingredients, flavors and sweeteners from extracts of plants that contain mogrosides such as | 2022-01-20 |
20220017564 | MOGROSIDE COMPOUNDS AND USES THEREOF - The present disclosure generally relates to various formulations and uses of the compound Isomogroside IV | 2022-01-20 |
20220017565 | STEROID DERIVATIVE REGULATORS, METHOD FOR PREPARING THE SAME, AND USES THEREOF - Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description. | 2022-01-20 |
20220017566 | TERPINOID DERIVATIVES AND USES THEREOF - Described herein are terpinoid derivatives as NRF2 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of inflammatory diseases. | 2022-01-20 |
20220017567 | METHODS OF GENERATING NANOARRAYS AND MICROARRAYS - The methods described herein provide a means of producing an array of spatially separated proteins. The method relies on covalently attaching each protein of the plurality of proteins to a structured nucleic acid particle (SNAP), and attaching the SNAPs to a solid support. | 2022-01-20 |
20220017568 | LINEAR SOLUTION PHASE ROUTES FOR WNT HEXAPEPTIDES - The present disclosure relates generally to the field of polypeptide synthesis, and more particularly, to a linear solution phase synthesis of the Wnt hexapeptide Foxy-5 and protected derivatives and peptide fragments thereof. | 2022-01-20 |
20220017569 | METHODS FOR PREPARING PURIFIED POLYPEPTIDE COMPOSITIONS - The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications. | 2022-01-20 |
20220017570 | METHOD FOR PURIFYING PEGYLATED PROTEIN - This disclosure provides a novel method of purifying PEGylated proteins using ion exchange chromatography by loading PEGylated protein having a high concentration, e.g., at least 6 grams/liter on an ion exchange chromatography matrix, and collecting the PEGylated protein. | 2022-01-20 |
20220017571 | METHODS FOR CHROMATOGRAPHIC PROTEIN EXTRACTION AND PURIFICATION - Disclosed herein are methods and compositions for isolating a protein fraction from a potato sample. The methods include adjusting the potato sample containing the protein fraction to a pH of about 4.0 to 5.2; and loading the potato sample onto a sulfonated epoxy resin, wherein the sulfonated epoxy resin comprising Formula (I) is adjusted to a pH of about 4.0 to 4.5. The methods also include washing the sulfonated epoxy resin and eluting the protein fraction. | 2022-01-20 |
20220017572 | GEMINOID LIPOPEPTIDE COMPOUNDS AND THEIR USES - Disclosed are geminoid peptide-like compound according to Formula I: | 2022-01-20 |
20220017573 | PEPTIDES FOR INDUCING BACTERIOCIN SYNTHESIS AND METHODS TO IDENTIFY AND/OR SELECT AND/OR OPTIMIZE THE SAME - Described herein is a peptide or peptidomimetic with a length of at least 6 residues comprising, consisting essentially of, or consisting of the sequence motif Xaa | 2022-01-20 |
20220017574 | STABILIZED PRE-FUSION RSV F PROTEINS - The present invention provides stable pre-fusion respiratory syncytial virus (RSV) F proteins, immunogenic compositions comprising said proteins and uses thereof for the prevention and/or treatment of RSV infection. | 2022-01-20 |
20220017575 | AAVRH.10 VARIANTS WITH HOST ANTIBODY ESCAPE CAPABILITIES AND ALTERED TISSUE TARGETING PROPERTIES - This disclosure relates to variant AAVrh 10 particles engineered to escape host neutralizing antibodies but retain or improve transduction efficiency, and their use as gene delivery vehicles. | 2022-01-20 |
20220017576 | Recombinant foot-and-mouth disease virus with reduced immunosuppression activity, and preparation method and use thereof - The present disclosure belongs to the technical field of biological products for veterinary medicine, and specifically relates to a recombinant foot-and-mouth disease virus (FMDV) with a reduced immunosuppressive activity, a preparation method and use thereof, and a recombinant vaccine strain. According to the present disclosure, it is firstly discovered that FMDV 3B protein has an immunosuppressive function, and key sites for exerting the immunosuppressive function are found. A recombinant FMDV vaccine strain with a lost immunosuppressive function in FMDV 3B protein is constructed by introducing amino acid mutations into three repeated copies of FMDV 3B protein. | 2022-01-20 |
20220017577 | Proteins for Blocking Neurotransmitter Release - The present invention includes light-controlled and light-independent neurotoxin systems and methods for using such neurotoxin systems for rapidly and locally silencing distinct populations of neurons. | 2022-01-20 |
20220017578 | IMMUNOGENIC COMPOSITIONS COMPRISING MYCOBACTERIUM TUBERCULOSIS POLYPEPTIDES AND FUSIONS THEREOF - The present invention relates to compositions and fusion proteins containing at least two | 2022-01-20 |
20220017579 | ORTHOGONAL PROTEIN HETERODIMERS - Disclosed herein are designed heterodimer proteins, monomeric polypeptides capable of forming heterodimer proteins, protein scaffolds including such polypeptides, and methods for using the heterodimer proteins and subunit polypeptides for designing logic gates. | 2022-01-20 |
20220017580 | ALKALINE PURIFICATION OF SPIDER SILK PROTEINS - The present disclosure relates to methods of producing and purifying synthetic block copolymer proteins, expression constructs for their secretion, recombinant microorganisms for their production, and synthetic fibers comprising these proteins that recapitulate many properties of natural silk. | 2022-01-20 |
20220017581 | ANIMAL-FREE DIETARY COLLAGEN - Provided herein are non-naturally occurring polypeptides comprising a sequence of a fragment of a collagen and recombinant cells containing heterologous nucleic acid sequences encoding the non-naturally occurring polypeptides. Further provided herein are animal-free methods of generating and purifying such non-naturally occurring polypeptides using microorganisms, preferably from bacterial cells. | 2022-01-20 |
20220017582 | COMPOSITION FOR PREVENTING OR TREATING PARKINSON'S DISEASE, COMPRISING AEG-1 S298D AS ACTIVE INGREDIENT - The present invention relates to a composition for preventing or treating Parkinson's disease comprising AEG-1 (S298D) as an active ingredient, and in the present invention, a point mutation was introduced into AEG-1 to induce a constitutively active form of AEG-1 (S298D), to construct AAV-AEG-1 (S298D), and to apply an animal model for Parkinson's disease, and accordingly, it was confirmed that it exhibits a protective effect on brain tissue by preserving dopaminergic neurons and dopamine nerve fibers and thus AEG-1 is useful as a composition for preventing or treating Parkinson's disease, a health food composition for preventing or improving Parkinson's disease, etc. | 2022-01-20 |
20220017583 | AFFINITY SUPPORT AND METHOD FOR TRAPPING SUBSTANCE USING THE SAME - Problems to be Solved | 2022-01-20 |