Heterocyclic Compounds

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Document	Document Title
WO/2022/169780A1	SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling...
WO/2022/166879A1	BENZO SEVEN-MEMBERED RING BIFUNCTIONAL COMPOUND AND APPLICATION THEREOF The present invention relates to a benzo seven-membered ring bifunctional compound and an application thereof, and in particular to a compound represented by formula (IV) and a pharmaceutically acceptable salt thereof. The compound can b...
WO/2022/166721A1	FUSED RING DERIVATIVES CONTAINING 1,4-OXAZEPANE The present invention relates to a series of fused ring derivatives containing 1,4-oxazepane and a preparation method therefor, and in particular relates to a compound as shown in formula (II) and a pharmaceutically acceptable salt thereof.
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/2022/167819A1	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/2022/166923A1	PHENYLDIHYDROPYRIMIDINE COMPOUND AND USE THEREOF A phenyldihydropyrimidine compound as represented by formula I, a tautomer or a pharmaceutically acceptable salt thereof. The phenyldihydropyrimidine compound has a good anti-HBV activity and can be used for preparing drugs for treating ...
WO/2022/166938A1	URACIL COMPOUND CONTAINING CARBOXYLATE FRAGMENT AND PREPARATION METHOD THEREFOR, HERBICIDAL COMPOSITION, AND USE The present invention relates to the field of herbicides, and in particular, to a uracil compound containing a carboxylate fragment and a preparation method therefor, a herbicidal composition, and a use. The uracil compound containing a ...
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/2022/167682A1	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/2022/169239A1	NLRP3 INFLAMMASOME SMALL-MOLECULE INHIBITOR FOR TREATMENT OF ALZHEIMER'S DISEASE In the present invention, a NLRP3-inhibitory compound 7 (NIC7) and a potent derivative NIC7w which are a novel small-molecule inhibitor for inhibiting NLRP3 inflammasomes are identified. Specifically, the compound and the derivative inhi...
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/2022/162017A1	CRYSTALLINE FORM OF A PIPERAZINYL-THIAZOLE DERIVATIVE The invention relates to a crystalline form of 1-{(R)-2-(2-Hydroxy-ethyl)-4-[2-trifluoromethyl-4-(2-trifluo romethyl-pyrimidin-5-yl)-thiazol-5-yl]-piperazin-1-yl}-2-(3- methyl-[1,2,4]triazol-1-yl)-ethanone, processes for the preparation ...
WO/2022/164135A1	BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT The present invention relates to a benzothiazole or benzimidazole derivative, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same as an active ingredient for prevention or treatment of SIRTUIN 7 p...
WO/2022/160928A1	NITROGEN-CONTAINING COMPOUND, AND ELECTRONIC COMPONENT AND ELECTRONIC DEVICE CONTAINING SAME The present application belongs to the technical field of organic materials. Provided are a nitrogen-containing compound, and an electronic component and an electronic device containing same. The structural formula of the nitrogen-contai...
WO/2022/161166A1	TARGETING CHIMERIC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR AND USE THEREOF A targeting chimeric compound, a pharmaceutical composition comprising same, a preparation method therefor and use thereof. The targeting chimeric compound is as represented by general formula (I), and each substituent in the general for...
WO/2022/157324A1	METHOD FOR PREPARING 2-[2-(2-CHLOROTHIAZOL-5-YL)-2-OXO-ETHYL]SULFANYL-6-HYDROXY-3-METHYL-5-PHENYL-PYR IMIDIN-4-ONE The present invention relates to a method for preparing 2-[2-(2-chlorothiazol-5-yl)-2- oxo-ethyl]sulfanyl-6-hydroxy-3-methyl-5-phenyl-pyrimidin-4-o ne or a tautomer thereof, to 2-[2-(2-chlorothiazol-5-yl)-2-oxo-ethyl]sulfanyl-6-hydroxy-3...
WO/2022/156059A1	CDK6/DYRK2 DUAL-TARGET INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF Disclosed are a compound as represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. Further disclosed are a method for preparing the above-mentioned compound and the use thereof in preventing and/o...
WO/2022/156764A1	COMPOUND FOR DEGRADING DEOXYRIBONUCLEIC ACID (DNA) POLYMERASE, AND USE THEREOF The present invention relates to the field of biomedicine, and specifically relates to a proteolysis-targeting chimera (PROTAC) compound. The structure of the PROTAC compound can be represented by general formula LGP-LK-LGE, wherein LGP ...
WO/2022/157499A1	PROTECTED HDAC (HISTONE DEACETYLASE) INHIBITORS The invention relates to protected HDAC inhibitor compounds of formula I, in which Y, Ar1, Ar2, X, R1 and R2 are as defined herein. In aspects, the inventions relates to use of the compounds, and to methods of deprotecting the compounds.
WO/2022/157316A1	METHOD FOR PREPARING AN ENANTIOMERICALLY ENRICHED FORM OF 2-[2-(2-CHLOROTHIAZOL-5-YL)-2-HYDROXY-ETHYL]SULFANYL-6-HYDROXY-3-METHYL-5-PHENYL -PYRIMIDIN-4-ONE The present invention relates to a method for preparing 2-[2-(2-chlorothiazol-5-yl)-2- hydroxy-ethyl]sulfanyl-6-hydroxy-3-methyl-5-phenyl-pyrimidin -4-one or a tautomer thereof or enantiomerically enriched forms thereof, to 2-[2-(2-chlor...
WO/2022/155941A1	CDK2 INHIBITORS The invention provides a compound represented by structural formula (I), or a pharmaceutically acceptable salt, or a stereoisomer thereof useful for treating a disease or disorder associated with CDK2.
WO/2022/156708A1	PARP7 ENZYME INHIBITOR Provided are a PARP7 enzyme inhibitor, a composition containing the inhibitor and the use thereof, synthetic methods for the preparation of PARP7 enzyme inhibitor and useful intermediates thereof.
WO/2022/159445A1	COMPOUNDS AND METHODS OF ACTIVATING LIPOPROTEIN LIPASE The present disclosure is generally directed to activators of lipoprotein lipase useful in the treatment of diseases and disorders modulated by said enzyme and having the Formula (I), or a pharmaceutically acceptable salt, isomer, solvat...
WO/2022/152821A1	ISOINDOLINONE COMPOUNDS Disclosed herein are compound or pharmaceutically acceptable salts or stereoisomers thereof of formula (I). These compounds find use as modulators of cereblon, in particular in the treatment of abnormal cell growth in mammals, especially...
WO/2022/152852A1	ANTAGONISTS OF MRGX2 This application relates to compounds of Formula (I), which are antagonists of MrgX2 (Mas-related Gene X2) and thus are useful as therapeutic agents, specifically therapeutic agents for use in the treatment of chronic spontaneous urticar...
WO/2022/152853A1	ANTAGONISTS OF MRGX2 This application relates to compounds of Formula I which are antagonists of MrgX2 (Mas-related Gene X2) and thus are useful as therapeutic agents, specifically therapeutic agents for use in the treatment of chronic spontaneous urticaria,...
WO/2022/147694A1	AMINOHETEROARYL COMPOUNDS AND USES THEREOF Provided herein are novel compounds (e.g., Formula I, II, III, or IV), pharmaceutical compositions, and methods of using the same. The compounds herein can typically induce UCP-1 expression and/or browning of white adipose tissues. The c...
WO/2022/150574A1	INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS LIPOAMIDE DEHYDROGENASE Disclosed are compounds for inhibiting lipoamide dehydrogenase (Lpd), and methods of treating tuberculosis.
WO/2022/147993A1	DIPHENYLPYRAZOLE COMPOUND, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF Provided are a diphenylpyrazole compound as represented by formula (I) below or an agrochemically acceptable salt thereof, which is a novel inhibitor targeting pest GSTs, has a wide range of inhibitory activity on GSTs in various pests, ...
WO/2022/150384A1	AMINOTHIAZOLE COMPOUNDS AS C-KIT INHIBITORS The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having a structure according to Formula (I): wherein X1, R1, R2, m, and n are described herein.
WO/2022/148331A1	AMINOHETEROARYL COMPOUNDS AND USES THEREOF Provided herein are novel compounds (e.g., Formula I, II, III, or IV), pharmaceutical compositions, and methods of using the same. The compounds herein can typically induce UCP-1 expression and/or browning of white adipose tissues. The c...
WO/2022/145408A1	CYCLIC AMINE DERIVATIVES HAVING SEROTONIN RECEPTOR BINDING ACTIVITY The present invention provides compounds that have a serotonin 5-HT2A receptor antagonist and/or inverse agonist activity, and pharmaceutically acceptable salts thereof, and also provides a serotonin 5-HT2A receptor antagonist and/or inv...
WO/2022/141977A1	ORAL GSNOR INHIBITORS AND PHARMACEUTICAL USE THEREOF Provided are a class of oral GSNOR inhibitors and a pharmaceutical use thereof, the structural features thereof being shown in formula I. Compared to N6022, the compound has good oral bioavailability and a longer half-life. In in vitro e...
WO/2022/144002A1	DERIVATIVE OF 2,5-DIKETOPIPERAZINE COMPOUND, AND PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF Disclosed are a derivative of a 2,5-diketopiperazine compound, and a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically, disclosed are a compound as represented by formula (I), a stereoiso...
WO/2022/147210A1	ANTI-TUMOR COMPOSITIONS AND METHODS Novel thiazole- and/or isoquinoline- containing compounds are presented that are useful for treating cancers as well as treating and/or preventing viral infections. Methods of treating and/or preventing broad-spectrum viral infections ar...
WO/2022/143773A1	BENZIMIDAZOLE COMPOUND AND APPLICATION THEREOF Provided are a class of benzimidazole compounds and an application thereof as a 300/CBP inhibitor. Specifically, provided are a compound represented by formula (P) and a pharmaceutically acceptable salt thereof.
WO/2022/147246A1	INDAZOLE COMPOUNDS AS KINASE INHIBITORS Disclosed herein are compounds and methods of treating diseases and/or conditions associated with FGFR inhibition.
WO/2022/143771A1	RORγT MODULATOR, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF Provided are an RORγt modulator, and a preparation method therefor and an application thereof. The RORγt modulator is selected from a compound represented by formula I, and a pharmaceutically acceptable salt, solvate, solvate of the ph...
WO/2022/135514A1	MULTI-SUBSTITUTED URACIL DERIVATIVES AND USE THEREOF Provided are a class of multi-substituted uracil derivatives and a pharmaceutical composition containing such compounds, which compounds can be used as chymase inhibitors. Also provided are a method for preparing such compounds and the p...
WO/2022/140325A1	6-SUBSTITUTED INDOLE COMPOUNDS The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided...
WO/2022/133529A1	HETEROCYCLIC INHIBITORS OF PCSK9 This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and ...
WO/2022/138944A1	THERAPY BASED ON SYNTHETIC LETHALITY IN SWI/SNF COMPLEX-DYSFUNCTION CANCER The present disclosure provides a pharmaceutical composition for treating and/or preventing SWI/SNF complex-dysfunction cancer. More specifically, according to the present disclosure, a compound represented by formulae (1) to (23) (the f...
WO/2022/138987A1	TRIAZINE DERIVATIVE HAVING VIRUS PROPAGATION INHIBITORY EFFECT, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME The present invention provides a compound exhibiting a coronavirus 3CL protease inhibitory effect and pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing the same. Further provided are crystals that are...
WO/2022/134641A1	AROMATIC HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION AND USE THEREOF An aromatic heterocyclic compound, a pharmaceutical composition and use thereof. Specifically disclosed are a compound as shown in formula I, a stereoisomer thereof, a diastereomer thereof, or a pharmaceutically acceptable salt of any on...
WO/2022/136365A1	NOVEL GALACTOSIDE INHIBITOR OF GALECTINS The present invention relates to a D-galactopyranose compound of formula (1) wherein the pyranose ring is β-D-galactopyranose. A1 is (II) wherein the asterix * indicates the nitrogen atom of the triazole ring that is covalently attached...
WO/2022/138888A1	TETRAHYDROQUINOLINE DERIVATIVE AND MEDICINAL USE THEREOF The purpose of the present invention is to provide a compound having a tetrahydroquinoline skeleton, said compound having ferroptosis inhibitory action and exhibiting a treatment effect or a prevention effect for a disease, disorder, or ...
WO/2022/135580A1	CRYSTAL FORM OF PYRIDOPYRROLE COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF A crystal form of a pyridopyrrole compound, and a preparation method therefor and the use thereof.

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