Heterocyclic Compounds

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Document	Document Title
WO/2024/067304A1	COMPOUND WITH INHIBITORY ACTIVITY AGAINST SIGMA2 AND 5HT2A AND USE The present invention provides a compound with inhibitory activity against Sigma2 and 5HT2A. The compound can be used as a dual-target inhibitor of Sigma2 and 5HT2A for the treatment of a related disease mediated by Sigma2 receptor activ...
WO/2024/046277A1	SERIES OF NITROGEN-CONTAINING BRIDGED HETEROCYCLIC COMPOUNDS AND PREPARATION METHOD THEREFOR Disclosed in the present invention are a series of nitrogen-containing bridged heterocyclic compounds and a preparation method therefor, and particularly a compound represented by formula (I) and a pharmaceutically acceptable salt thereo...
WO/2024/048582A1	CATALYST LOADED BODY, CATALYST FOR VAPOR-PHASE OXIDATION OF ORGANIC COMPOUND USING SAME, AND VAPOR-PHASE OXIDATION METHOD [Problem] The present invention provides a means which is capable of oxidizing an organic compound in a vapor phase using a nitroxyl radical as a catalyst. [Solution] A catalyst loaded body is obtained by loading a carrier with a compoun...
WO/2024/044792A1	UNIVERSAL SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE SYNTHESIS Disclosed herein are chemical preparation of oligonucleotides, chemical entities useful in such preparation, processes for such preparation, and methods of use relating to the chemical preparation of oligonucleotides. Further disclosed h...
WO/2024/011155A1	OXAZOLE TRPML1 AGONISTS AND USES THEREOF Described herein are oxazole TRPML1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of TRPML1-mediated disorders or diseases.
WO/2024/006781A1	ESTROGEN RECEPTOR ALPHA DEGRADERS AND USE THEREOF The application relates to bifunctional compounds of the general formula I-3' which act as degraders of the estrogen receptor alpha(ERα) and are useful for treating disorders associated with ERα-mediated transcription regulation such a...
WO/2023/230190A1	PYRIMIDINE BASED MODULATORS AND USES THEREOF Provided herein are compounds, such as compounds of Formula (I), Formula (I-A), Formula (I-B), or pharmaceutically acceptable salts of any one there, useful for modulating KRAS GD12 and/or other G12 mutants.
WO/2023/219199A1	MANUFACTURING METHOD FOR FP-CIT PRECURSOR, AND MANUFACTURING METHOD FOR [18F]FP-CIT USING FP-CIT PRECURSOR MANUFACTURED THEREBY Disclosed are a manufacturing method for a FP-CIT precursor, and a manufacturing method for [18F]FP-CIT using a FP-CIT precursor manufactured thereby. The manufacturing method for a FP-CIT precursor, according to one embodiment of the pr...
WO/2023/215482A1	TETRAHYDROISOQUINOLINE HETEROBIFUNCTIONAL BCL-XL DEGRADERS This disclosure provides compounds of Formula (I) (e.g., (I-A) (e.g., (I-A-1), (I-A-2), or (I-A-3)), (I-B) (e.g., (I-B-1), (I-B-2), or (I-B-3)), (I-C), (I-D), (I-E) (e.g., (I-E-1), (I-E-2), or (I-E-3)), (I-Ea) (e.g., (I-Ea-1), (I-Ea-2), ...
WO/2023/202706A1	SALT FORM AND CRYSTAL FORM OF SELENIUM HETEROCYCLIC COMPOUND AND APPLICATION THEREOF The present invention relates to a salt form and a crystal form of a selenium heterocyclic compound and to an application thereof. Specifically, the present invention relates to a crystal form, each salt form and the crystal forms of the...
WO/2023/163140A1	INDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF The purpose of the present invention is to provide a compound that exhibits an H-PGDS inhibitory activity. The present invention relates to a compound expressed by formula [I] or a pharmaceutically acceptable salt thereof (in the formula...
WO/2023/141721A1	ANTICHOLINERGIC COMPOUNDS FOR USE IN TREATING NEUROMUSCULAR DISORDERS The present invention relates to an anticholinergic compound such as Darifenicin for use in the treatment of a neuromuscular disorder (in particular amyotrophic lateral sclerosis or ALS) in a human subject, wherein the neuromuscular diso...
WO/2023/142985A1	PREPARATION METHOD FOR TGF-β-INHIBITING ANTI-TUMOR DRUG The present invention belongs to the technical field of drug synthesis. Disclosed is a preparation method for a TGF-β-inhibiting anti-tumor drug. Compared with preparation methods in the existing technology, the number of reaction steps...
WO/2023/141323A1	EMOPAMIL-BINDING PROTEIN INHIBITORS AND USES THEREOF Provided are compounds of the Formula (I): (I), or pharmaceutically acceptable salts thereof, which are useful for the inhibition of EBP and in the treatment of a variety of EBP mediated conditions or diseases, such as multiple sclerosis.
WO/2023/136279A1	CRYSTAL OF SUBSTITUTED PIPERIDINE COMPOUND, SALTS OF SUBSTITUTED PIPERIDINE COMPOUND, AND CRYSTALS THEREOF Provided are a crystal of a compound represented by formula (I) that can be used as an active pharmaceutical ingredient of a drug, salts of the compound represented by formula (I), and crystals thereof.
WO/2023/133229A2	COMPOUNDS AND METHODS FOR MODULATING SPLICING The present disclosure features compounds and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof.
WO/2023/129963A1	ANTIMICROBIAL COMPOUNDS AND METHODS The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-nega...
WO/2023/094911A1	METHOD FOR SYNTHESIZING (RS)-WARFARIN A method for synthesizing (RS)-Warfarin comprising preparing a liquid mixture, wherein the liquid mixture comprises trihexyltetradecylphosphonium bromide, methyl salicylate, acetyl chloride, benzaldehyde, and acetone. The method may furt...
WO/2023/067628A1	A METHOD FOR THE PREPARATION OF INDOLE-3-CARBOXYLIC ACID DERIVATIVES The present invention provides a new synthetic method for the preparation of building block indole-3-carboxylic acid (ICA) derivatives used as a key starting material to produce several artificial drugs. An efficient, safe, operationally...
WO/2023/061999A1	PROCESS FOR PREPARING A PHENOLIC HYDROCARBON The present invention discloses a distinct mode of action of a nickel catalyst to forge C-0 bonds to unlock the mild utilization of N2O as O-atom transfer reagent in the synthesis of complex phenols from the corresponding aryl halides.
WO/2023/043938A1	SULFAMIDE RIBONUCLEOTIDE REDUCTASE (RNR) INHIBITORS AND USES THEREOF Provided herein are compounds and methods for the treatment of cancer. The methods include administering to a subject in need a therapeutically effective amount of a sulfamide RNR inhibitor disclosed herein.
WO/2023/042879A1	BICYCLIC HETEROCYCLIC DERIVATIVE HAVING VIRAL GROWTH INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME The present invention provides: a compound having coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing same. Provided is a compound represented by formula...
WO/2023/034833A1	COMPOUNDS AND METHODS FOR MODULATING SPLICING The present disclosure features compounds (I) and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof.
WO/2023/028054A1	QUINAZOLINE COMPOUNDS FOR TREATMENT OF DISEASE Described herein are inhibitors of EGFR exon 20 insertion mutants and methods of treating cancer comprising the administration of said inhibitors.
WO/2023/018781A1	COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes...
WO/2023/011359A1	BRIDGED RING COMPOUND AND USE THEREOF A bridged ring compound and the use thereof in the preparation of a drug for treating related diseases. Specifically disclosed are a compound as represented by formula (I) and a pharmaceutically acceptable salt thereof.
WO/2023/009330A1	SEROTONIN 5-HT2B INHIBITORY COMPOUNDS The invention describes novel serotonin c5-HT2B receptor antagonists of Formula (1), and pharmaceutically acceptable salts thereof; wherein Ring A, L, X, X', R3, (1) R4, m and n are as defined herein. Also described are compositions comp...
WO/2022/250108A1	PHENYL UREA DERIVATIVE The present invention pertains to a therapeutic agent or preventative agent against diseases involving an orexin receptor, particularly an orexin type-2 receptor, the agent containing a novel compound having a urea skeleton, or a pharmac...
WO/2022/241188A1	ENANTIOSELECTIVE SYNTHESIS OF AMINOTROPANE COMPOUND The present disclosure provides processes for preparing fert-butyl (1 R,3s,5S)-3- amino-8-azabicyclo[3.2.1]octane-8-carboxylate or a salt thereof. The present disclosure also provides enantioselective processes for preparing exo-aminotro...
WO/2022/204299A1	PYRIMIDINE DERIVATIVES USEFUL AS LRRK2 KINASE INHIBITORS Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R1a, R1b, R2, and L are as defined herein. Meth...
WO/2022/204140A1	ALGOSTATIC AGENTS FOR PREVENTING TRANSITION FROM ACUTE TO CHRONIC PAIN Disclosed herein, inter alia, are methods of stimulating mitochondrial respiration and methods of treating pain.
WO/2021/174176A9	PYRIDAZINE DERIVATIVES FOR MODULATING NUCLEIC ACID SPLICING The present disclosure features compounds and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof.
WO/2021/174170A9	PYRIDAZINE DERIVATIVES FOR MODULATING NUCLEIC ACID SPLICING The present disclosure features compounds and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof.
WO/2022/171265A1	MODULATORS OF COMPLEX I The present invention describes compounds modulating the function of mitochondrial complex I (NADH-quinone oxidoreductase) having formula (I).
WO/2022/162992A1	PHARMACEUTICAL COMPOSITION FOR TREATING ALLERGY The present invention addresses the problem of providing a new pharmaceutical composition that can treat a T cell-independent reaction or an early phase reaction (a symptom in an early phase) of an allergic disease.　Examples of the pre...
WO/2022/163041A1	INDOLE-STRUCTURE-SELECTIVE REACTION AGENT, INDOLE-STRUCTURE-SELECTIVE CROSSLINKING AGENT, AND METHOD FOR PRODUCING COMPOSITE USING THESE Provided are: an indole-structure-selective reaction agent and an indole-structure-selective crosslinking agent which are capable of selectively modifying, under mild conditions, an indole structure of a molecule (e.g., tryptophan) conta...
WO/2022/147620A1	THIENYL AND CYCLOALKYL AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF NUAK KINASES, COMPOSITIONS AND USES THEREOF The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs...
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/2022/129951A1	PHARMACEUTICAL COMPOUNDS This invention relates to compounds that are agonists of the muscarinic M1 and M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and/or M4 receptors. Also provided are pharmaceutical compositions...
WO/2022/111683A1	SUBSTITUTED AZABICYCLOOCTANE COMPOUND AND PREPARATION METHOD THEREFOR, AND INTERMEDIATE AND PREPARATION METHOD THEREFOR The present invention relates to an intermediate of a substituted azabicyclo[3.2.1]octane compound, and a preparation method therefor. Specifically, disclosed in the present invention are an intermediate (the compound of formula (I)), a ...
WO/2022/094668A1	PROCESS FOR PREPARING HETEROCYCLIC METHANONE COMPOUNDS AND AZA-BICYCLO INTERMEDIATES THEREOF The present disclosure relates to a process for synthesis of heterocyclic methanone compounds, and in particular 3'-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-y l)-thiophen-3-yl]-methanone compounds, and aza-...
WO/2022/083687A1	SELENIUM HETEROCYCLIC COMPOUNDS AND APPLICATION THEREOF A class of selenium heterocyclic compounds and an application thereof. Specifically disclosed are a compound represented by formula (II) and a pharmaceutically acceptable salt thereof.
WO/2022/076703A1	PROCESSES FOR PREPARING A PAN-JAK INHIBITOR AND RELATED INTERMEDIATE COMPOUNDS The present disclosure provides processes for preparing a crystalline form of 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-na phthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propane nitrile and related intermediate comp...
WO/2022/076717A1	SOLVATE FORMS OF A PAN-JAK INHIBITOR The present invention provides crystalline solvate and solvate/hydrate forms of 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-na phthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propane nitrile, and methods of making and ...
WO/2022/076714A1	SOLID FORMS OF A PAN-JAK INHIBITOR The present invention provides amorphous and crystalline hydrate forms of 3-((lR,3s,5S)-3-((7-((5-methyl-lH-pyrazol-3-yl)amino)-l,6-na phthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propane nitrile, and methods of making and using ...
WO/2022/063050A1	PYRAZOLE COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF The present invention relates to a pyrazole compound and a preparation method therefor and a use thereof. In particular, the present invention relates to a compound shown in formula I, a pharmaceutical composition containing same or a ph...
WO/2022/040259A1	IMIDAZO[1,2-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-A]PYRIDINE DERIVATIVES AS TLR9 INHIBITORS FOR THE TREATMENT OF FIBROSIS The present invention relates to imidazo[1,2-a]pyridine and [1,2,4]triazolo[1, 5-a]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic...
WO/2022/040260A1	1H-BENZO[D]IMIDAZOLE DERIVATIVES AS TLR9 INHIBITORS FOR THE TREATMENT OF FIBROSIS The present invention relates to lH-benzo[d]imidazole derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis...
WO/2022/040267A1	1H-PYRROLO[3,2-C]PYRIDINE AND 1H-PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS TLR9 INHIBITORS FOR THE TREATMENT OF FIBROSIS The present invention relates to 1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic di...
WO/2022/014680A1	SUBSTITUTED PIPERIDINE COMPOUND AND APPLICATION THEREOF The present invention provides: compounds that have an agonist activity against the orexin receptor type-2 and that are represented by formula (I), (II), (III), and (IV); and pharmaceutically acceptable salts thereof.

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