Heterocyclic Compounds

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Document	Document Title
WO/2022/169834A2	SMALL MOLECULE INHIBITORS OF GRP78 AND USES THEREOF This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules as defined within Formula I (as defined herein) which function as inhibitors of glucose-regulated protein 78 (G...
WO/2022/168808A1	PYRIMIDINE DERIVATIVE The present invention pertains to: a compound that is represented by formula (I), that has a mPGES-1 inhibitory effect, and that is useful as an active ingredient of a medicine for treating and/or preventing diseases such as inflammation...
WO/2022/166890A1	SUBSTITUTED PYRIDAZINE PHENOL DERIVATIVES Substituted pyridazine phenol derivatives and a preparation method therefor, specifically relating to a compound as shown in formula (VI) and a pharmaceutically acceptable salt thereof, which can be used as an NLRP3 inhibitor.
WO/2022/166747A1	AMINO LIPID COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF The present invention relates to an amino lipid compound, namely a compound represented by chemical formula I, or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof. Moreover, also disclosed are a preparation m...
WO/2022/166468A1	BRUTON'S TYROSINE KINASE INHIBITOR AND APPLICATION THEREOF A heterocyclic compound that acts as a BTK inhibitor, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to a compound represented by general formula (I) and a pharmaceutica...
WO/2022/166916A1	SUBSTITUTED HETEROARYL DERIVATIVE, AND COMPOSITION AND USE THEREOF Provided are a substituted heteroaryl derivative, and a composition containing same and the use thereof, wherein the substituted heteroaryl derivative is a compound as represented by formula (I) or a tautomer, a stereoisomer, a prodrug, ...
WO/2022/166970A1	BIFUNCTIONAL MDM2 PROTEIN DEGRADER, AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITION AND USE THEREOF Provided in the present invention are a proteolysis targeting chimera, and a preparation method therefor and a pharmaceutical composition and the use thereof. Specifically, the proteolysis targeting chimera comprises the following struct...
WO/2022/166799A1	FUSED TRICYCLIC CYCLIN-DEPENDENT KINASE INHIBITOR, AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF Provided are a fused tricyclic cyclin-dependent kinase inhibitor, and a preparation method therefor and a pharmaceutical use thereof. In particular, the structure of the fused tricyclic cyclin-dependent kinase inhibitor is shown in formu...
WO/2022/169998A1	AMIDES AS CBL-B INHIBITORS Various amide compounds that bind Cbl-B, including those that are selective for C-Cbl, and methods of making and using the same. Representative amide compounds include molecules falling within the following formulae:
WO/2022/166844A1	TRICYCLIC COMPOUNDS AND USES THEREOF Tricyclic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein each variable is as defined in the description.
WO/2022/170043A1	QUINAZOLINE DERIVED COMPOUNDS AS EGFR INHIBITORS AND THEIR USES THEREOF The invention provides compounds and pharmaceutical compositions thereof, which are useful for inhibiting EGFR, as well as methods for using such compounds to treat cancer associated with an EGFR or HER2 exon 20 insertion mutation.
WO/2022/167445A1	GPR84 ANTAGONISTS AND USES THEREOF The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of GPR84, and the treatment of GPR84-mediated disorders.
WO/2022/166917A1	TYK2 INHIBITOR COMPOUND CONTAINING BICYCLIC RING A TYK2 inhibitor compound containing a bicyclic ring and the use thereof in the preparation of a drug for treating or preventing TYK2-related diseases.
WO/2022/166768A1	TETRAHYDROPYRROLOCYCLIC COMPOUND AND APPLICATION THEREOF A tetrahydropyrrolocyclic compound as represented by formula (I), a pharmaceutically acceptable salt thereof, and an application thereof in preparation of a drug for treating a disease related to a selective orexin-2 (OX-2) receptor anta...
WO/2022/167866A1	MODULATORS OF PROTEIN PHOSPHATASE 2A (PP2A) AND METHODS USING SAME The present disclosure relates in part to chemical modulators of protein phosphatase 2A (PP2A), comprising formula (I). The compounds of the present disclosure are useful in treating, preventing, and/or ameliorating cancer, diabetes, aut...
WO/2022/167819A1	NOVEL COMPOUNDS The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, N-oxides, solvates and prodrugs thereof Formula (I) wherein R2, R3, R4, X1, X2, X3 and X4 are as defined in the specification, processes for t...
WO/2022/166469A1	FGFR KINASE INHIBITOR AND USE THEREOF A heterocyclic compound as a fibroblast growth factor receptor (FGFR) inhibitor, a preparation method therefor, and the pharmaceutical use thereof. In particular, the present invention relates to a compound represented by general formula...
WO/2022/170052A1	QUINAZOLINE DERIVATIVES, PYRIDOPYRIMIDINE DERIVATIVES, PYRIMIDOPYRIMIDINE DERIVATIVES, AND USES THEREOF The present disclosure relates to compounds of Formula (I) or a stereoisomer, polymorph, hydrate, solvate, or pharmaceutically acceptable salt thereof. The present disclosure also relates to uses of the compounds, e.g., in treating or pr...
WO/2022/169997A1	LACTAMS AS CBL-B INHIBITORS Various lactam compound that binds Cbl-B, many of which are selective for Cbl-B over C-Cbl, and methods of making and using the same. Representative lactam compounds include molecules falling within the following formulae:
WO/2022/166638A1	SALT OF INDOLE DERIVATIVE AND USE THEREOF A salt of a compound, as represented by formula I, a crystal form thereof, a pharmaceutical composition containing the salt and/or the crystal form thereof, and the use of the salt, the crystal form thereof and/or the pharmaceutical comp...
WO/2022/166570A1	COMPOUNDS FOR SIMULTANEOUSLY INDUCING DEGRADATION OF EGFR AND PARP PROTEINS, PREPARATION METHOD THEREFOR AND USE THEREOF A series of new-type dual-targeting degradation compounds, which have two independent inhibitor units and an E3 ligase ligand, or a pharmaceutically acceptable salt, hydrate, stereoisomer or prodrug thereof, a preparation method therefor...
WO/2022/169755A1	SULFONAMIDE SUBSTITUTED N-(1H-INDOL-7-YL) BENZENESULFONAMIDES AND USES THEREOF The present application discloses novel compounds of formula (I), pharmaceutical compositions containing these compounds and methods of inducing degradation of a protein, comprising contacting the protein with an effective amount of a co...
WO/2022/169840A1	COMBINATION OF DUAL ATM AND DNA-PK INHIBITORS AND IMMUNOTHERAPEUTIC AGENTS FOR USE IN CANCER THERAPY A combined cancer therapy comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, an immune checkpoint inhibitor, and optionally a radiotherapy.
WO/2022/169248A1	NOVEL COMPOUND AS PROTEIN KINASE INHIBITOR The present invention relates to a novel compound as a protein kinase inhibitor.
WO/2022/167682A1	AZABICYCLIC SHP2 INHIBITORS The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase, having the general Formula (I).
WO/2022/167867A1	SUBSTITUTED CYCLIC MODULATORS OF PROTEIN PHOSPHATASE 2A (PP2A) AND METHODS USING SAME The present disclosure relates in part to chemical modulators of protein phosphatase 2A (PP2A). The compounds of the present disclosure are useful in treating, preventing, and/or ameliorating cancer, diabetes, autoimmune disease, solid o...
WO/2022/166793A1	CDK INHIBITOR A compound serving as a selective CDK inhibitor, a pharmaceutical composition containing same, a useful intermediate for preparing the compound, and a use of the compound for preparing a drug for the treatment of cell proliferative disea...
WO/2022/166792A1	SALT, SOLVATE, POLYMORPH, PREPARATION METHOD AND USE OF BENZAZEPINE DERIVATIVE A salt, a solvate, a polymorph, a preparation method and the use of a benzazepine derivative. Specifically disclosed is a compound as shown in formula (I). The crystal form of the compound as shown in formula (I) has better solubility an...
WO/2022/167817A1	NOVEL PROCESS The invention relates to a process for preparing heterocyclic amide derivatives, to novel polymorphic forms obtained from said process and the use of said polymorphic forms for use in the treatment and prophylaxis of cancer.
WO/2022/166748A1	COMPOUND FOR TREATING OR PREVENTING VIMENTIN-MEDIATED DISEASES Provided in the present invention is a compound for treating or preventing vimentin-mediated diseases. The compound of the present invention is a s-triazine derivative, as shown in the following formula A, or a pharmaceutically acceptabl...
WO/2022/169696A1	METHODS OF MAKING TRANS ISOMERIC FORMS OF G PROTEIN-COUPLED RECEPTOR Disclosed herein, inter alia, methods of synthesis of trans isomeric forms of G protein- coupled receptor modulators of high trans isomeric purity.
WO/2022/167631A1	NOVEL HETEROARYL-SUBSTITUTED IMIDAZOLE DERIVATIVES The invention provides novel heteroaryl-substituted imidazole derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein A and R1 to R6 are as described herein. Further provided are pharmaceutical ...
WO/2022/167457A1	GPR84 ANTAGONISTS AND USES THEREOF The present invention provides compounds of formula (I), compositions thereof, and methods of using the same for the inhibition of GPR84, and the treatment of GPR84-mediated disorders.
WO/2022/169184A1	NOVEL COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT COMPRISING SAME The present invention relates to a novel compound and an organic light-emitting element comprising the novel compound in one or more organic layers to thus be highly efficient.
WO/2022/165114A1	QUINOLINES AND AZAQUINOLINES AS INHIBITORS OF CD38 The present invention relates to compounds which are inhibitors of CD38 and are useful in the treatment of cancer.
WO/2022/164735A1	FACTOR XIA INHIBITORS The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fi...
WO/2022/162447A1	PROCESSES FOR PREPARATION OF CHLORANTRANILIPROLE OR A SALT OR ITS INTERMEDIATES THEREOF The present invention generally relates to a process for preparation of chlorantraniliprole or a salt thereof. Further, the present invention relates to an improved process for preparation of intermediate of chlorantraniliprole.
WO/2022/165494A1	SALT CRYSTALS The present disclosure relates to free base and salt crystals of 2-(4-acetylbenzyl)-3-((4-fluorophenyl)amino)-5,7,7-trimethyl -7,8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H) -one, composition comprising the same and the meth...
WO/2022/164239A1	PYRAZOLE-CARBOXAMIDE DERIVATIVE COMPOUND AND USE THEREOF A novel pyrazole-carboxamide derivative compound provided as one example of the present invention exhibits an antagonist activity specific to cannabinoid receptor 1, and thus has a technical effect of effectively preventing or treating d...
WO/2022/160338A1	RADIOACTIVELY LABELED LIGAND FOR FIBROBLAST ACTIVATION PROTEIN-ALPHA IMAGING AGENT AND PREPARATION METHOD THEREFOR The present invention relates to a radioactively labeled ligand for a fibroblast activation protein-alpha imaging agent and a preparation method therefor, and belongs to the field of radiopharmaceutical chemistry. The radioactively label...
WO/2022/161274A1	PYRIMIDINE-2,4-DIAMINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF Disclosed in the present invention are a pyrimidine-2,4-diamine compound, a preparation method therefor and the use thereof, relating to the technical field of pharmaceutical chemistry. The pyrimidine-2,4-diamine compound of the present ...
WO/2022/164871A1	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.
WO/2022/165189A1	METHODS AND AGENTS THAT STIMULATE MITOCHONDRIAL TURNOVER FOR TREATING DISEASE Provided herein are methods of stimulating mitophagy in a subject in need thereof administering to the subject a mitophagy-stimulating amount of a MAS receptoragonist or substance that triggers endogenous production of a MAS receptor ago...
WO/2022/160037A1	IMPROVED T-CELLS FOR CANCER THERAPY USING AMINO ACID STARVATION PATHWAYS There is described herein a method for improving the anti-cancer properties of T-cells, the method comprising: providing a population of T-cells; and culturing the T-cells in an environment that activates the GCN2 pathway.
WO/2022/165185A1	CANCER-SELECTIVE TARGET DEGRADATION BY TARGETING GROUP CAGED PROTACS PROTACs (PROteolysis TArgeting Chimeras) are an emerging class of promising therapeutic modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin-proteasome system. However, potential toxicity of PROTACs i...
WO/2022/164249A1	NOVEL BENZOTRIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY AGAINST ECTONUCLEOTIDE PYROPHOSPHATASE-PHOSPHODIESTERASE, AND USE THEREOF The present invention relates to a novel benzotriazole derivative compound, a tautomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, which are related to a compound for inhibiting ENPP...
WO/2022/161447A1	DICARBOXAMIDE COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL USE THEREOF The present invention relates to a dicarboxamide compound, a preparation method therefor, and a pharmaceutical use thereof. Specifically, the present invention relates to a dicarboxamide compound represented by general formula (I), a pre...
WO/2022/164857A1	AZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N -oxides, and salts thereof, Wherein R1, R2, R3, A, X and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of F...
WO/2022/165076A1	GPCR RECEPTOR AGONISTS, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME, AND METHODS FOR THEIR USE Provided herein are GLP-1 receptor modulator compounds, pharmaceutical compositions, methods of their preparation, and methods of their use in treatment, and/or diagnosis.
WO/2022/165173A1	COMPOUNDS AND USE THEREOF FOR TREATMENT OF NEURODEGENERATIVE, DEGENERATIVE AND METABOLIC DISORDERS Provided are, inter alia, compounds having a structure of Formula (X), (XI), (XII), or (XIII), or a subordinate structure thereof, composition including the same and methods of use.

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