24th week of 2021 patent applcation highlights part 27 |
Patent application number | Title | Published |
20210179525 | FORMATION OF ALPHA,BETA-UNSATURATED CARBOXYLIC ACIDS AND SALTS THEREOF FROM METALALACTONES AND ANIONIC POLYELECTROLYTES - This disclosure provides processes for forming acrylic acid and other α,β-unsaturated carboxylic acids and their salts, including catalytic processes, and catalyst systems for effecting the processes. For example, there is provided a catalyst system for producing an α,β-unsaturated carboxylic acid or a salt thereof, the catalyst system comprising: (a) a transition metal precursor compound comprising a Group 8-11 transition metal and at least one first ligand; (b) optionally, at least one second ligand; and (c) an anionic polyaromatic resin with associated metal cations. The catalyst system can further comprise (d) an olefin; (e) carbon dioxide (CO | 2021-06-17 |
20210179526 | Electrochemical Reduction of Carbon Dioxide to Upgrade Hydrocarbon Feedstocks - A system and method with a solid oxide electrolysis cell (SOEC), including feeding carbon dioxide and an olefin to the SOEC and discharging carbon monoxide and an olefin oxide from the SOEC, wherein the olefin oxide corresponds to the olefin. | 2021-06-17 |
20210179527 | METHOD FOR OXIDIZING A 1,1,-BIS-(3,4-DIMETHYLPHENYL)-ALKANE TO 3,3',4,4'-BENZOPHENONE TETRACARBOXYLIC ACID - In a method for oxidizing 1,1-bis-(3,4-dimethylphenyl)-alkane with nitric acid in a pressure vessel to produce 3,3′,4,4′-benzophenone tetracarboxylic acid with concurrent formation of nitric oxide, passing nitric oxide from the pressure vessel into an absorption vessel and reacting nitric oxide in the absorption vessel with molecular oxygen and water to produce an aqueous nitric acid solution prevents discharge of nitric oxide, avoids the risk of oxygen inhibiting the nitric acid oxidation and reduces nitric acid consumption when the nitric acid from the absorption vessel is used for oxidizing the 1,1-bis-(3,4-dimethylphenyl)-alkane. | 2021-06-17 |
20210179528 | SALTS OF TREPROSTINIL - Provided are novel treprostinil salts as well as methods for making treprostinil salts. | 2021-06-17 |
20210179529 | PREPARATION OF (METH)ACRYLIC ACID ESTERS - The invention relates to a method for preparation of (meth)acrylic acid esters from (meth)acrylic acid anhydrides. | 2021-06-17 |
20210179530 | METHOD OF PREPARING ESTER-BASED COMPOSITION - The present invention relates to a method of preparing an ester-based composition, which includes mixing a dibenzoic acid and a carboxylic acid to prepare an acid mixture and reacting the acid mixture with an alcohol, wherein a product of the reaction includes a benzoic acid ester-based material and a carboxylic acid ester-based material. The preparation method can improve a reaction rate and a temperature rising rate, and can also reduce energy, by adding a carboxylic acid and/or a carboxylic acid ester-based material in a preparation process. | 2021-06-17 |
20210179531 | PREPARATION OF DIESTERS OF (METH)ACRYLIC ACID FROM EPOXIDES - The invention relates to a method for preparation of diesters from anhydrides of carboxylic acids. | 2021-06-17 |
20210179532 | ALKOXYCARBONYLATION OF TRIVINYLCYCLOHEXANE - Process for the alkoxycarbonylation of trivinylcyclohexane. | 2021-06-17 |
20210179533 | SALICYL FUMARATE DERIVATIVE AND ITS APPLICATION IN THE TREATMENT OF PARKINSON'S DISEASE AND OTHER NEURODEGENERATIVE DISEASES - A salicyl fumarate derivative, and its general structural formula (A) is: | 2021-06-17 |
20210179534 | TRIESTERS OF CYCLOHEXANETRIPROPIONIC ACID - The invention relates to triesters of cyclohexanetripropionic acid, preparation thereof and use thereof as plasticizers for polymers. | 2021-06-17 |
20210179535 | ALPHA-TRUXILLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure: Formula (I) | 2021-06-17 |
20210179536 | METHOD OF SYNTHESIZING (1R,2R)-NITROALCOHOL COMPOUND - Disclosed is a method of synthesizing a (1R,2R)-nitroalcohol compound of formula (I), as shown in the following reaction scheme, including: subjecting a compound of formula (II) and a compound of formula (III) to a condensation reaction in an organic solvent in the presence of a copper complex generated in situ from a chiral (1S,2R)-amino alcohol ligand and a cupric salt to produce the (1R,2R)-nitroalcohol compound of formula (I), where R | 2021-06-17 |
20210179537 | Non-Coordinating Anion Type Activators Containing Cation Having Aryldiamine Groups and Uses Thereof - The present disclosure provides borate or aluminate activators comprising cations having linear alkyl groups, catalyst systems comprising, and methods for polymerizing olefins using such activators. | 2021-06-17 |
20210179538 | METHOD FOR PRODUCING 2-OCTYLGLYCINE ESTER HAVING OPTICAL ACTIVITY - A method for producing a 2-octylglycine ester having optical activity from a racemic 2-octyl-DL-glycine ester and, more particularly, to a method for producing a 2-octyl-L-glycine ester or a 2-octyl-D-glycine ester by using a chiral mandelic acid as an optical resolution agent. | 2021-06-17 |
20210179539 | METAL SALTS AND USES THEREOF - The present invention relates to metal salts of 2-[3-[(3R)-3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]butoxy]phenyl]acetic acid which exhibit improved physical properties and stability. The invention also relates to pharmaceutical compositions including an effective amount of the metal salts, as well as methods of treating cancer including administration of a pharmaceutical composition including a salt of the invention to a subject in need thereof. | 2021-06-17 |
20210179540 | TRISAMIDE COMPOUNDS AND COMPOSITIONS COMPRISING THE SAME - A trisamide compound has the structure of Formula (I) | 2021-06-17 |
20210179541 | Method for Producing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylb- utanoyl]amino}phenyl)-3-cyclo-propylpropanoic Acid and the Crystalline Form Thereof for Use as a Pharmaceutical Ingredient - The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders. | 2021-06-17 |
20210179542 | 4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES - Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed. | 2021-06-17 |
20210179543 | CALPAIN-2 SELECTIVE INHIBITOR COMPOUNDS FOR TREATMENT OF GLAUCOMA - Compounds of Formula (I) are provided including for treatment of disorders such as glaucoma. | 2021-06-17 |
20210179544 | TRISAMIDE COMPOUNDS AND COMPOSITIONS COMPRISING THE SAME - A trisamide compound has the structure of Formula (I) | 2021-06-17 |
20210179545 | COMPOSITIONS OF OLIGOANILINES AND METHODS OF MAKING AND USING - Compositions of oligoanilines with higher purity, methods of making and using thereof, are provided. The compositions are produced in large scale with larger yield using simple purification techniques such as washing. Methods have been developed that allow large scale synthesis of oligoaniline compounds with the following benefits: (i) higher purity; (ii) larger yield of oligoaniline compounds; (iii) simple purification that does not require complicated techniques such as liquid chromatograph; (iv) lower cost; and (v) full characterization. The highly pure oligoaniline compositions can be used as reducing or oxidizing agent in a redox reaction. The oligoaniline compositions have colors and can be used as dyes, i.e. redox active dyes in a redox reaction, as intermediates for the development of conductive elastomers, or as catalysts. | 2021-06-17 |
20210179546 | METHODS AND COMPOSITIONS FOR TERPENOID TRICYCLOALKANE SYNTHESIS - In one aspect, the disclosure relates to methods for preparation of intermediates useful for the preparation of terpenoid cores. In a further aspect, the disclosed methods pertain to the preparation of compounds comprising a terpenoid core or scaffold, such as 6/7/5 tricycloalkanes. The disclosed methods utilize abundant starting materials and simple reaction sequences that can be used to tunably and scalably assemble common terpenoid cores. In various aspects, the present disclosure pertains to compounds prepared using the disclosed methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. | 2021-06-17 |
20210179547 | PLANT AND METHOD FOR PURIFYING AN ISOMERIC MONOMER - A plant for preparing a purified isomeric methylene diphenyl diisocyanate monomer from a mixture of different isomeric monomers is disclosed herein. The plant can comprise a distillation apparatus, which comprises: a) a distillation column including a structured packing, b) a source for a mixture of different isomeric methylene diphenyl diisocyanate monomers, c) an evaporator, d) an overhead vapor condenser, e) optionally, an overhead vacuum system and f) a flow-controlled reflux system. The overhead vapor condenser comprises a shell and tube arrangement and is embodied so as to directly subcool the condensate to less than 47° C. The flow-controlled reflux system comprises a heater, which is embodied so as to reheat a partial stream of the condensate formed in the overhead vapor condenser up to 190° C. | 2021-06-17 |
20210179548 | METHOD FOR PRODUCING CARBAMATE AND METHOD FOR PRODUCING ISOCYANATE - The present invention provides a method for producing a carbamate that includes a step (1) and a step (2) described below:
| 2021-06-17 |
20210179549 | CO-CRYSTAL OF SORAFENIB DERIVATIVES AND PROCESS FOR PREPARATION THEREOF - The present disclosure provides compounds for the inhibition of soluble epoxide hydrolase and associate disease conditions, as well as a method of treating or preventing disorders in a subject by inhibition of soluble epoxide hydrolase. | 2021-06-17 |
20210179550 | PHENYL UREA DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR MODULATORS - The present invention relates to phenyl urea derivatives useful for the treatment of inflammatory diseases, pharmaceutical compositions containing them and their use as tools or as pharmaceuticals as modulators of the N-formyl peptide receptor (FPR), including FPR1 and FPR2, or as selective agonists of the FPR1 receptor. | 2021-06-17 |
20210179552 | METHOD FOR PREPARING POLYTHIOL COMPOSITION - The embodiments relate to a process for preparing a polythiol composition, which comprises reacting a halogen compound or an alcohol compound with thiourea to prepare a thiouronium salt solution; and adding a basic solution to the thiouronium salt solution to hydrolyze it. The hydrolysis reaction is terminated when the area of peak A in the graph measured by gel permeation chromatography of the reactant in the hydrolysis step under certain conditions is 0.5% to 8% based on the total peak area. A tetrafunctional polythiol composition having high purity can be obtained. Thus, an optical lens having excellent color, transparency, and refractive index can be obtained. | 2021-06-17 |
20210179553 | HYDROPERSULFIDE PRECURSORS - A hydropersulfide precursor compound having the formula (I): formula (I) as defined in the specification. A process for preparing the hydropersulfide precursor, and a method of using the precursor to generate hydropersulfide are also described. | 2021-06-17 |
20210179554 | ONIUM SALT COMPOUND, CHEMICALLY AMPLIFIED RESIST COMPOSITION AND PATTERNING PROCESS - An onium salt having formula (1) serving as an acid diffusion inhibitor and a chemically amplified resist composition comprising the acid diffusion inhibitor are provided. When processed by lithography, the resist composition exhibits a high sensitivity, and excellent lithography performance factors such as CDU and LWR. | 2021-06-17 |
20210179555 | METHOD FOR PRODUCING 1-METHYLPYRROLIDIN-3-OL - The invention relates to a method of producing compound (I) | 2021-06-17 |
20210179556 | PRIMARY CARBOXAMIDES AS BTK INHIBITORS - The invention provides compounds of Formula (I) | 2021-06-17 |
20210179557 | SUBSTITUTED TETRAHYDROCYCLOPENTA[C]PYRROLES, SUBSTITUTED DIHYDROPYRROLIZINES, ANALOGUES THEREOF, AND METHODS USING SAME - The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection and/or hepatitis D virus (HDV) infection in a patient. | 2021-06-17 |
20210179558 | CRYSTALLINE FORM OF EB-1020, PROCESSES FOR PREPARATION AND USE THEREOF - The present disclosure relates to a crystalline form of compound I and processes for preparation thereof. The present disclosure also relates to a pharmaceutical composition containing the crystalline form, use of the crystalline form for preparing serotonin, norepinephrine and dopamine triple reuptake inhibitors drugs, and/or use of the crystalline form for preparing drugs treating nervous system disorders. The crystalline form of the present disclosure has one or more improved properties compared with prior art and has significant values for future drug optimization and development. | 2021-06-17 |
20210179559 | PIPERIDINE DERIVATIVES AS HDAC1/2 INHIBITORS - Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity. | 2021-06-17 |
20210179560 | Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer - The present invention provides MDM2 inhibitor compounds of Formula I, | 2021-06-17 |
20210179561 | ACID ADDITION SALTS OF APOMORPHINE, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND METHODS OF USING THE SAME - Acid addition salt of apomorphine glycolate, acid addition salt of apomorphine sulfamate, and acid addition salt of apomorphine isobutyrate salts are disclosed. Also disclosed are pharmaceutical compositions (e.g., unit dosage forms, e.g., films) containing acid addition salt of apomorphine glycolate, acid addition salt of apomorphine sulfamate, or acid addition salt of apomorphine isobutyrate. Further disclosed are methods of use of acid addition salt of apomorphine glycolate, acid addition salt of apomorphine sulfamate, or acid addition salt of apomorphine isobutyrate. | 2021-06-17 |
20210179562 | PROCESS FOR THE SYNTHESIS OF N-SUBSTITUTED LACTAMS AND AMIDES - A process for the synthesis of N-alkylated lactams via reductive alkylation. The process of the present disclosure may be conducted by the addition of an aldehyde to a lactam in the presence of a catalyst under a reducing atmosphere. | 2021-06-17 |
20210179563 | PROCESS FOR THE MANUFACTURE OF IMINIUM COMPOUNDS AND THEIR APPLICATION IN THE MANUFACTURE OF PYRAZOLE DERIVATIVES - Process for the manufacture of iminium compounds and their application in the manufacture of pyrazole derivatives The present invention concerns processes for the manufacture of iminium compounds and their application in the manufacture of pyrazole derivatives, in particular in processes for the manufacture of pharmaceutically or agrochemically active compounds. | 2021-06-17 |
20210179564 | THERAPEUTIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - Compounds of Formula (I): | 2021-06-17 |
20210179565 | PYRIMIDINONE DERIVATIVES AS SHP2 ANTAGONISTS - The invention relates to pyrimidinone derivatives of the general Formula I, | 2021-06-17 |
20210179566 | COMPOSITIONS AND METHODS FOR DELIVERING PHARMACEUTICAL AGENTS - Provided herein are compositions and methods for treating pulmonary arterial hypertension. In particular, provided herein are dry powder formulations of TMP for delivery to the lung. | 2021-06-17 |
20210179567 | SYNTHESIS OF 1,4-DIAZASPIRO[5.5]UNDECAN-3-ONE - This invention provides a process for preparing 1,4-diazaspiro[5.5]undecan-3-one and analogues thereof that are useful in the preparation of pharmaceutical compound, including for the treatment of disorders involving abnormal cellular proliferation. Chemical intermediates in the process are also provided. | 2021-06-17 |
20210179568 | HYDROLYSIS METHOD FOR TERT-BUTYL ESTER IN GADOLINIUM-BASED CONTRAST AGENT - A hydrolysis method for tert-butyl ester in gadolinium-based contrast agent comprises hydrolyzing the tert-butyl ester with a catalyst. The preparation method of the catalyst comprises the following steps: subjecting zirconia and titanium tetrachloride to reaction in the presence of sulfuric acid and water at 60° C. to 90° C. until solids are dissolved, adding silica to perform reaction for 1 to 5 h, filtering to obtain solids, washing and calcining the solids. This hydrolysis method does not introduce other substances that are difficult to remove, such as acids, and provides high hydrolysis efficiency and high purity of the obtained product. | 2021-06-17 |
20210179569 | BENZAMIDE COMPOUNDS AND THEIR USE AS HERBICIDES II - The invention relates to benzamides of formula I, | 2021-06-17 |
20210179570 | PROCESSES AND INTERMEDIATES FOR PREPARING MCL1 INHIBITORS - The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates. | 2021-06-17 |
20210179571 | Small Molecule Inhibitors of Fungal Hyphae and Biofilm Formation - Novel compounds having inhibitory activity on the formation of fungal hyphae and biofilms, and therapeutic formulations and methods based on the novel inhibitors. | 2021-06-17 |
20210179572 | BENZOTHIADIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS - The invention relates to 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases. | 2021-06-17 |
20210179573 | Treatment of Multiple Sclerosis and Psoriasis Using Prodrugs of Methyl Hydrogen Fumarate - Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed. | 2021-06-17 |
20210179574 | ELECTROCHEMICAL, BROMINATION, AND OXYBROMINATION SYSTEMS AND METHODS TO FORM PROPYLENE OXIDE OR ETHYLENE OXIDE - Disclosed herein are methods and systems that relate to various configurations of electrochemical, bromination, oxybromination, bromine oxidation, hydrolysis, neutralization, and epoxidation reactions to form propylene bromohydrin, propanal, and propylene oxide or to form bromoethanol, bromoacetaldehyde, and ethylene oxide. | 2021-06-17 |
20210179575 | USE OF PHARMACOLOGICAL CHAPERONES FOR THE TREATMENT OF LYSOSOMAL STORAGE DISEASES - The present invention relates to the use of galactose analogues of formula (I) with the capacity to stabilize the structure of the #-GalA enzyme, for the treatment of lysosomal storage diseases and, in a preferred embodiment, for the treatment of Fabry disease. In addition, the present invention relates to pharmacological compositions having an effective amount of at least one of the galactose analogues described in the present document for the treatment of lysosomal storage diseases and, in a preferred embodiment, for the treatment of Fabry disease. | 2021-06-17 |
20210179576 | MONOETHYLENICALLY UNSATURATED MONOMERS AND USES THEREOF - The invention relates to a monoethylenically unsaturated monomer of formula (I), and to the use thereof for producing a polymer. The invention also relates to the polymer obtained by polymerising said monomer, and to the use thereof in a composition for producing coatings. | 2021-06-17 |
20210179577 | AROMATIC SULFONAMIDE DERIVATIVES FOR THE TREATMENT OF ISCHEMIC STROKE - A compound of formula (I) or an N-oxide, a salt, a hydrate, a solvate, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer for use in the treatment or prophylaxis of brain ischemia, ischemic brain injury, Ischemic Stroke (IS), haemorrhagic stroke, traumatic brain injury, spinal cord injury. | 2021-06-17 |
20210179578 | OX1 ANTAGONISTS - The disclosures herein relate to novel compounds of formula (1) and salts thereof, wherein X; Y; R | 2021-06-17 |
20210179579 | PYRIDAZINONE COMPOUNDS AND USES THEREOF - Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α. | 2021-06-17 |
20210179580 | PYRIMIDINE DERIVATIVES AS INHIBITORS OF PD1/PD-L1 ACTIVATION - The compounds of Formula Ib, Formula Ia, and Formula I are described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The process of preparation of the compounds of Formula Ib, Formula Ia, and Formula I is also described. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are 2-(benzyloxy)pyrimidine derivatives that are inhibitors of PD-1/PD-L1 activation. | 2021-06-17 |
20210179581 | RADICAL COMPOUNDS AND METHODS OF USING THEREOF - Disclosed are methods for performing dynamic nuclear polarization using the polarizing agents described herein. In general, the methods involve (a) providing a frozen sample in a magnetic field, wherein the frozen sample includes a polarizing agent described herein and an analyte with at least one spin half nucleus; (b) polarizing the at least one spin half nucleus of the analyte by irradiating the frozen sample with radiation having a frequency that excites electron spin transitions in the polarizing agent; (c) optionally melting the sample to produce a molten sample; and (d) detecting nuclear spin transitions in the at least one spin half nucleus of the analyte in the frozen or molten sample. In certain embodiments, the polarizing agents can be peptide-based. In these embodiments, the polarizing agents can be readily prepared by solid-phase peptide synthesis. | 2021-06-17 |
20210179582 | Biochemical binding of RET9 and VEGFR2 inhibitors - Provided herein are compounds, compositions, and pharmaceutical compositions of Formula (I). Also provided herein are methods of using compounds of Formula (I) to treat proliferative diseases, ocular diseases, dermatological diseases, inflammatory diseases, autoimmune diseases, autoinflammatory diseases, and metabolic diseases. Also provided herein are methods of using the compounds of Formula (I) as therapeutics, e.g., in the treatment and/or prevention of diseases associated with growth factor activity or angiogenesis. In some embodiments, the disease being treated is a proliferative disease. | 2021-06-17 |
20210179583 | INHIBITORS FOR THE B-CATENIN/B-CELL LYMPHOMA 9 (BCL9) PROTEIN-PROTEIN INTERACTION - Disclosed are inhibitors for the β-catenin/BCL9 interaction. The inhibitors are selective for β-catenin/BCL9 over β-catenin/cadherin interactions. Methods of using the disclosed compounds to treat cancer are also disclosed. | 2021-06-17 |
20210179584 | INHIBITOR OF p38 MAP KINASE - A compound has the following formula: | 2021-06-17 |
20210179585 | CRYSTAL FORM OF ABEMACICLIB MESYLATE, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITION THEREOF - Disclosed is a crystal form of abemaciclib mesylate, which has one or more improved properties compared with the known abemaciclib mesylate. Also involved are a method for preparing the crystal form of abemaciclib mesylate, a pharmaceutical composition and the use of same in the preparation of a drug for treating cancer diseases such as colorectal cancer, breast cancer, lung cancer, prostate cancer, glioblastoma, mantle cell lymphoma, chronic granulocytic leukemia and acute granulocytic leukemia. | 2021-06-17 |
20210179586 | SOLID STATE FORMS OF BRANAPLAM AND THEIR PREPARATION - The present disclosure relates to Branaplam solid state forms, Branaplam salts and solid states thereof, processes for preparation thereof, pharmaceutical compositions and methods of use thereof. | 2021-06-17 |
20210179587 | MODULATORS OF ALPHA-1 ANTITRYPSIN - Novel compounds, compositions, and methods of using and preparing the same, which may be useful for treating alpha-1 antitrypsin deficiency (AATD). | 2021-06-17 |
20210179588 | UNSYMMETRICAL SALTS, CCC-NHC PINCER METAL COMPLEXES, AND METHODS OF MAKING THE SAME - Provided herein are unsymmetrical bis(azolium) salts, unsymmetrical CCC—NHC metal complexes, and methods of forming the same. The unsymmetrical bis(azolium) salts include a central aryl ring that is substituted with two heterocyclic rings in an ortho, meta, or para fashion. The unsymmetrical CCC—NHC metal complexes include metalated unsymmetrical bis(azolium) salts. The method of forming the unsymmetrical CCC—NHC metal complexes includes reacting a dihalogenated benzene with a first azole to form a mono(azole)benzene, reacting the mono(azole)benzene with a second azole to form an unsymmetrical bis(azole)benzene, alkylating the unsymmetrical bis(azole)benzene to form an unsymmetrical bis(azolium) salt, and metalating the unsymmetrical bis(azolium) salt to form the unsymmetrical CCC—NHC metal complex. Also provided are a bis-ligated CCC—NHC metal complex and an unsymmetrical bimetallic complex. | 2021-06-17 |
20210179589 | TETRAZOLINONE COMPOUNDS AND ITS USE - The present invention provides a compound having excellent control efficacies against plant diseases. The compound is represented by formula (I): wherein, R | 2021-06-17 |
20210179590 | SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF - The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases. | 2021-06-17 |
20210179591 | NEW COMPOUNDS FOR USE AS A THERAPEUTICALLY ACTIVE SUBSTANCE AND IN PARTICULAR FOR USE IN THE TREATMENT OF TUMORS - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 2021-06-17 |
20210179592 | 3-((HETERO-)ARYL)-ALKYL-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES - The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain. | 2021-06-17 |
20210179593 | METHOD FOR ISOLATION OF AN AROMATIC DIANHYDRIDE AND AROMATIC DIANHYDRIDES PREPARED BY THE METHOD - A method for producing an aromatic dianhydride includes reacting an aromatic diimide with a substituted or unsubstituted phthalic anhydride in an aqueous medium in the presence of an amine exchange catalyst to provide an aqueous reaction mixture including an N-substituted phthalimide, an aromatic tetraacid salt, and at least one of an aromatic triacid salt and an aromatic imide diacid salt. The method further includes removing the phthalimide from the aqueous reaction mixture by extracting the aqueous reaction mixture with an organic solvent using a single packed extraction column. The aromatic tetraacid salt is converted to the corresponding aromatic dianhydride. Aromatic dianhydrides prepared according to the method are also described. | 2021-06-17 |
20210179594 | GLP-1R AGONISTS AND USES THEREOF - The present disclosure provides compounds of Formula (I) | 2021-06-17 |
20210179595 | 8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives - The invention relates to 8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain. | 2021-06-17 |
20210179596 | HETEROCYCLIC COMPOUND, ORGANIC LIGHT EMITTING DIODE COMPRISING SAME, COMPOSITION FOR ORGANIC LAYER OF ORGANIC LIGHT EMITTING DIODE, AND METHOD FOR MANUFACTURING ORGANIC LIGHT EMITTING DIODE - The present specification relates to a heterocyclic compound represented by Chemical Formula 1, an organic light emitting device comprising the same, a composition for an organic material layer of an organic light emitting device, and a method for manufacturing an organic light emitting device. | 2021-06-17 |
20210179597 | WATER SOLUBLE NOVEL CYANINE FLUOROPHORE WITH TUNABLE PROPERTIES BETWEEN NEAR IR AND SWIR REGION FOR IN VIVO IMAGING - Cyanine fluorophores including a nine-carbon polymethine bridge are disclosed. The cyanine fluorophores have absorbance and/or emission maxima in the near-infrared (NIR) and short-wave infrared (SWIR) wavelength ranges. Methods of making and using the cyanine fluorophores are also disclosed. The compounds are useful in fluorescence imaging, more particularly in cancer treatment. The compounds have generic formula (I): | 2021-06-17 |
20210179598 | SELECTIVE JAK2 INHIBITOR AND APPLICATION THEREOF - Provided is a selective JAK2 inhibitor and application thereof. In particular, it relates to the compound of the following Formula (I), and the use of the compound in the treatment of JAK2-mediated related diseases and in the preparation of the medicament for treating JAK2-mediated related diseases. | 2021-06-17 |
20210179599 | ALKENE SPIROCYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS - The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions. | 2021-06-17 |
20210179600 | OXAZOLE AND THIAZOLE DERIVATIVES AS INHIBITORS OF ASK1 - The present technology is directed to compounds of formula (I), compositions thereof, and methods related to inhibition of ASKI. In particular, the present compounds and compositions may be used to treat ASK1-mediated disorders and conditions, including, e.g., fibrotic diseases and acute and chronic liver diseases, among others. | 2021-06-17 |
20210179601 | IRAK INHIBITORS AND METHOD FOR MAKING AND USING - Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition. | 2021-06-17 |
20210179602 | A 5-THIAZOLECARBOXAMIDE KINASE INHIBITOR AND USES THEREOF - The invention relates to a kinase inhibitor, in particular an inhibitor of protein kinases including the protein-tyrosine kinases LCK, ABL, SRC, KIT, SIK-family and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitor of the invention displays, eg functional and ADMET properties distinct to dasatinib. Also, the invention relates to pharmaceutical compositions that comprise the kinase inhibitor, including those formulated for oral administration, such as in unit dose form that comprise particular ranges or amounts of the kinase inhibitor. The kinase inhibitor or pharmaceutical composition may be used in the treatment of a proliferative disorder, such as a leukaemia or solid tumour. The kinase inhibitor or pharmaceutical composition may be used in a treatment regimen that corresponds to, is similar to or is distinct from that used with dasatinib for a corresponding disorder, and in particular may be used in a combination treatment regimen together with one or more additional therapeutic agents, such as immune-checkpoint inhibitors. | 2021-06-17 |
20210179603 | CYCLOPROPANAMINE COMPOUND AND USE THEREOF - The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula | 2021-06-17 |
20210179604 | Indole Compounds and Their Use - The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer. | 2021-06-17 |
20210179605 | Discovery of Novel First in Class Nature-Inspired Compounds Targeting the Mitochondrial Function and Pharmaceutical Composition Thereof - The present invention relates to novel antitumor agents and pharmaceutically acceptable salts thereof, processes and intermediates for the manufacture of these novel constrained cyclic frameworks of general formula I and II, and medicaments containing such compounds. | 2021-06-17 |
20210179606 | COMPOSITIONS COMPRISING MACROCYCLE DERIVATIVES INCORPORATING BRIDGED MACROCYCLES AND METHODS OF PRODUCING AND USING SAME - Compositions are disclosed herein that include macrocycle derivatives incorporating bridged macrocycles. Also disclosed are methods of producing and using the compositions. | 2021-06-17 |
20210179607 | NOVEL SUBSTITUTED TETRAHYDROQUINOLIN COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS - Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. | 2021-06-17 |
20210179608 | NOVEL, HIGHLY ACTIVE PYRAZOLO-PIPERIDINE SUBSTITUTED INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV) - The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds. | 2021-06-17 |
20210179609 | HETEROCYCLIC COMPOUNDS AND THEIR APPLICATION IN MEDICINE - This invention relates to heterocyclic compounds and their use in medicine. In particular, the present invention discloses heterocyclic compound of formula I, or an isotopically labeled compound thereof, or an optical isomer thereof, a geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. The invention also relates to the use of these compounds in medicine. | 2021-06-17 |
20210179610 | PARP/PI3K DOUBLE-TARGET INHIBITOR CONTAINING PYRIDOPYRIMIDINE STRUCTURE - The present disclosure relates to the field of pharmaceutical chemistry, in particular to a class of PARP/PI3K double-target inhibitors (I) containing structures of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine and phthalazin-1(2H)-one and a preparation method thereof. As proved by pharmacodynamic tests, the compounds of the present disclosure have PARP/PI3K double-target inhibitory activity and can be used for anti-tumor. | 2021-06-17 |
20210179611 | INHIBITORS OF THE MENIN-MLL INTERACTION - The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction. | 2021-06-17 |
20210179612 | MASP-2 INHIBITORS AND METHODS OF USE - The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds. | 2021-06-17 |
20210179613 | GHRELIN RECEPTOR AGONIST FOR TREATMENT OF CACHEXIA - The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease. | 2021-06-17 |
20210179614 | HETEROCYCLIC COMPOUND - One of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity. Another of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity and exhibits a protein degradation induction activity. The present invention provides a compound represented by formula (I) (the symbols in the formula are as defined in the present Description) and salts thereof. | 2021-06-17 |
20210179615 | NICLOSAMIDE ANALOGUES AND THERAPEUTIC USE THEREOF - Described are niclosamide analogue compounds, pharmaceutical compositions thereof, and method of using the corner pounds and compositions for treating a disease associated with dysregulation of the Wnt/Frizzled signaling pathway, such as cancer, fatty liver, antibiotic resistance, and viral infection. The disclosed compounds and compositions may also be used for modulating mitochondrial function and for treating certain non-cancer diseases and/or diorders, such as diabetes, fibrotic disease, primary sclerosing cholangitis. | 2021-06-17 |
20210179616 | 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. | 2021-06-17 |
20210179617 | TRICYCLIC COMPOUNDS - Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit. | 2021-06-17 |
20210179619 | MITRAGYNINE ANALOGS FOR THE TREATMENT OF PAIN, MOOD DISORDERS AND SUBSTANCE USE DISORDERS - The present invention provides a compound having the structure: | 2021-06-17 |
20210179620 | MESOIONIC IMIDAZOLIUM COMPOUNDS AND DERIVATIVES FOR COMBATING ANIMAL PESTS - The present invention relates to compounds of formula (I), | 2021-06-17 |
20210179621 | Toll-Like Receptor 8 (TLR8) Specific Antagonists and Methods of Making and Uses Thereof - Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder. | 2021-06-17 |
20210179622 | NOVEL COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME - Provided is a compound of Chemical Formula 1: | 2021-06-17 |
20210179623 | NEW CHEMICAL COMPOUND CONTAINING ACTIVE ENANTIOMETER S-(-) KETOROLAC TROMETHAMINE FOR THE TREATMENT OF PAIN - The invention relates to a novel chemical compound characterized in that it contains the active enantiomer S-(−) ketorolac tromethamine combined with other pharmaceutically acceptable adjuvants or excipients, said compound being advantageous over other NSAIDs and, in particular, the known active principle ketorolac tromethamine, comprising a single isomer that is pure and has a better therapeutic index, retaining its therapeutic activity by improving its physicochemical properties, such as solubility or stability, which translates into a decrease in the dose administered, reducing direct gastrointestinal side effects and the time required for the development of the desired therapeutic action. The invention is suitable for use as a medication for the treatment of pain of moderate to high intensity and can be administered in any form in the dose range from 0.5 milligrams to 30 milligrams. | 2021-06-17 |
20210179624 | SECONDARY BATTERY - A secondary battery includes a protection module package including a tab bridge, an input/output terminal, and an insulating body that includes a middle block and side block, the middle block having the input/output terminal therein, the side block being spaced apart from the middle block, and the tab bridge connecting the middle block to the side block; and a bare cell including an electrode that is electrically connected to the tab bridge. | 2021-06-17 |
20210179625 | ARYL HYDROCARBON RECEPTOR ANTAGONISTS AND USES THEREOF - The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells. | 2021-06-17 |
20210179626 | PYRAZOLOCHLOROPHENYL COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - Compounds of Formula I and methods of use as Janus kinase inhibitors are described herein. | 2021-06-17 |