Heterocyclic Compounds

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Document	Document Title
WO/2024/084496A1	PHARMACEUTICAL COMPOSITIONS COMPRISING ACALABRUTINIB MALEATE The present invention relates to pharmaceutical compositions comprising a Bruton tyrosine kinase (BTK) inhibitor. More particularly, the present invention relates to a composition comprising Acalabrutinib maleate and one or more pharmace...
WO/2024/083024A1	PREPARATION AND USE OF RET INHIBITOR Disclosed in the present invention are preparation and a use of a c-RET inhibitor. Specifically, the present invention provides a compound as represented by formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical com...
WO/2024/084217A1	3A,4,5,6-TETRAHYDRO-1 H-PYRAZOLO[3,4-C]PYRIDIN-7(7AH)-ONE DERIVATIVES AS FACTOR XIIA INHIBITORS The present invention provides compounds of formula (I): Formula (I) compositions comprising such compounds; the use of such compounds in medicine; and methods of treating patients with such compounds; wherein R1, B1, B2, B3, B4, B5, and...
WO/2024/086296A1	COMPOUNDS USEFUL IN MODULATING EGFR AND PI3K The present disclosure relates to the field of medicinal chemistry. In particular, the disclosure relates to a new class of small-molecules having a quinazoline structure or a quinoline structure according to Formula (I), wherein Ring A,...
WO/2024/084450A1	BICYCLIC HETEROARYL COMPOUNDS AND THEIR DERIVATIVES AS PKMYT1 INHIBITORS The present disclosure provides bicyclic heteroaryl compounds and their derivatives of formula (I), which are therapeutically useful as PKMYT1 inhibitors. (I) These compounds are useful in the treatment and/or prevention of diseases or c...
WO/2024/083773A1	TRIAZOLE-SUBSTITUTED IMIDAZO[1,2-A]PYRIMIDINES AS CGAS INHIBITORS The present invention relates to compounds, compositions containing them, and to their use in the treatment of various disorders, in particular autoimmune, autoinflammatory or immune-mediated conditions, such as systemic lupus erythemato...
WO/2024/084448A2	FUSED BICYCLIC COMPOUNDS AND THEIR USE AS MER AND AXL INHIBITORS Compounds of formula (I) and a pharmaceutically acceptable salt thereof, wherein ring A, W, X, Y, L1, R1, R3, and R4, are as defined in the specification, are useful for treating or preventing cancer or an immune-related disease or condi...
WO/2024/086179A1	PYRIMIDINE SGC STIMULATORS The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutically acceptable salts thereof and pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more ...
WO/2024/083150A1	CRYSTAL FORM OF NK3R ANTAGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF Disclosed in the present invention are a crystal form A of the NK3R antagonist represented by formula (I), and a preparation method therefor and the use thereof. The X-ray powder diffraction pattern of the crystal form A comprises charac...
WO/2024/086837A1	METHODS OF SYNTHESIS FOR CUCURBITURIL COMPOUNDS Disclosure herein relates to, inter alia, inventive cucurbituril compounds and novel methods of preparing thereof using a glycoluril compound having the formula (II), a glycoluril compound having the formula (II'), a glycoluril bis-ether...
WO/2024/037667A3	FUSED RING HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF Disclosed are a fused ring heterocyclic compound represented by the following formula I, an optical isomer, a deuterated substance, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the subs...
WO/2024/086361A1	MOLECULAR GLUE DEGRADER COMPOUNDS AND USES THEREOF Described herein are molecular glue degrader compounds that bind to both a target protein and a RING E3 Ubiquitin Ligase, as well as related compositions and methods of use, e.g., for degradation of the target protein and/or the treatmen...
WO/2024/083223A1	MACROCYCLIC COMPOUNDS AND MEDICAL USE THEREOF The present disclosure relates to macrocyclic compounds and the medical use thereof, the structures of the macrocyclic compounds being represented as formula (I). The present disclosure also relates to a method for preparing the compound...
WO/2024/083246A1	KRAS INHIBITORS The present disclosure relates to compounds that inhibit KRAS. In particular, the present disclosure relates to compounds that inhibit the activity of KRAS G12D or KRAS G12V, pharmaceutical compositions comprising the compounds and metho...
WO/2024/078436A1	HETEROCYCLIC PYRIMIDINE COMPOUND, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF The present disclosure discloses a compound having formula (I) or a pharmaceutically acceptable salt thereof which acts as a USP1 inhibitor, a pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt the...
WO/2024/079351A1	NOVEL PIPERAZINE-BASED SULFONAMIDES AND THEIR USE AS NEUROPROTECTIVE AND/OR NEURORESTORATIVE AGENTS The present invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt and/or solvate thereof. The invention further relates to the use of the compounds of the invention as neuroprotective and/or neurore...
WO/2024/078263A1	PREPARATION AND USE OF MACROCYCLIC HETEROCYCLIC COMPOUND AS EGFR INHIBITOR The present invention relates to a macrocyclic heterocyclic compound as a selective inhibitor of a clinical mutant of EGFR kinase, and specifically relates to a compound represented by formula I or a pharmaceutically acceptable salt ther...
WO/2024/078370A1	SMALL MOLECULAR COMPOUND HAVING SUBSTITUTED PHENYLSPIRO[INDOLINE-3,3'-PYRROLIDINE] STRUCTURE Disclosed in the present invention is a small molecular compound having a substituted phenylspiro[indoline-3,3'-pyrrolidine] structure. The structure thereof is as shown in general formula I, and the definition of each substituent is as ...
WO/2024/078372A1	HETEROCYCLIC SUBSTITUTED PHENOL DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF Provided are a heterocyclic substituted phenol derivative, a preparation method therefor, and a use thereof. Specifically, provided are compounds of formulas (I-1), (II-1B), (III), and (IV), stereoisomers thereof, pharmaceutically accept...
WO/2024/081914A1	COELENTERAZINE ANALOGUES Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays. For example, the compounds may be u...
WO/2024/079682A1	SULFOXIMINE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME The present invention relates to a sulfoximine compound having a novel structure, stereoisomers thereof or pharmaceutically acceptable salts thereof, and a use thereof for preventing or treating histone deacetylase-mediated diseases The ...
WO/2024/079342A1	COMPOUND ACTIVE AS INHIBITOR OF COLONY STIMULATION FACTOR-1 RECEPTOR (CSF-1R) The present invention relates to new pyrrolopyrimidines and purines which surprisingly act as CSF-1R inhibitors, to processes for making these compounds, and to uses thereof.
WO/2024/078448A1	HPK1 KINASE INHIBITOR AS WELL AS PREPARATION METHOD THEREFOR AND USE THEREOF Provided are an HPK1 kinase inhibitor, a preparation method therefor and the use thereof. The kinase inhibitor can adjust (for example, inhibit) HPK1 kinase activity, and thus can be used for treating various HPK1-related diseases includ...
WO/2024/078004A1	USE OF PEMETREXED NEAR-INFRARED FLUORESCENT MOLECULE TARGETING α-TYPE FOLATE RECEPTOR AS FLUORESCENT TRACER Disclosed is a use of a pemetrexed near-infrared fluorescent molecule targeting an α-type folate receptor as a fluorescent tracer, the structural formula of the pemetrexed near-infrared fluorescent molecule being: formula (I). The foreg...
WO/2024/081927A1	COMPOUNDS FOR IMPROVEMENT OF VIRAL PRODUCTION Provided herein are methods of improving (e.g., increasing) the production of viral particles (e.g., AAV) in mammalian cells (e.g., HEK293 or HEK293T cells) using selective HDAC6 inhibitors (e.g., compounds of Formula I, Formula II, or F...
WO/2024/078137A1	ORGANIC ELECTROLUMINESCENT DEVICE AND ELECTRONIC APPARATUS An organic electroluminescent device and an electronic apparatus. The organic electroluminescent device comprises a cathode, an anode, and an organic layer, the organic layer comprises an organic light-emitting layer, and the organic lig...
WO/2024/079345A1	COMPOUND ACTIVE AS INHIBITOR OF COLONY STIMULATION FACTOR-1 RECEPTOR (CSF-1 R) The present invention relates to new pyrrolopyrimidines and purines which surprisingly act as CSF-1R inhibitors, to processes for making these compounds, and to uses thereof.
WO/2024/079623A1	TRICYCLIC COMPOUNDS AND THEIR USES The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I): wherein R1, R2, R3, x, R4, R5, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses...
WO/2024/077273A2	COMPOUNDS, COMPOSITIONS, AND METHODS The present disclosure relates generally to small molecule inhibitors of Sterile Alpha and TIR Motif containing 1 (SARM1) protein, or a pharmaceutically acceptable salt, isotopically enriched analog, stereoisomer, mixture of stereoisomer...
WO/2024/077235A2	DIHYDROFOLATE REDUCTASE INHIBITORS FOR ANTI-BIOTIC RESISTANT INFECTIONS In one aspect, compounds and associated compositions are described herein for the treatment of various bacterial infections, including antibiotic resistant infections. In some embodiments, an antibacterial composition described herein co...
WO/2024/077061A2	GABA(A) RECEPTOR MODULATORS AND METHODS TO CONTROL SMOOTH MUSCLE CONTRACTION AND INFLAMMATION Substituted [benzo[f]imidazo[1,5-a][1,4]diazepine]-3-carboxylic acid compounds are GABA(A) receptor modulators and have utility to treat inflammation and/or inhibit smooth muscle contraction.
WO/2024/077024A2	INDAZOLE PYRIDONE COMPOUNDS AND USES THEREOF Novel tetracyclic pyridone compounds according to Formula I are provided, (I) where R and X are defined herein. Pharmaceutical compositions containing such compounds, methods of using these compounds and compositions in the treatment and...
WO/2024/076692A1	HETEROBIFUNCTIONAL COMPOUNDS AS P53 ACETYLATORS Disclosed are novel heterobifunctional compounds that induce p53Y220C acetylation, and methods for use of such compounds in the treatment of p53Y220C-mediated diseases.
WO/2024/076929A2	IRREVERSIBLE INACTIVATORS TARGETING ARAF/MEK COMPLEXES The disclosure relates to compounds that act as irreversible inactivators that target ARAF/MEK complexes; pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including ca...
WO/2024/077277A1	DRUG LINKERS AND ANTIBODY CONJUGATES THEREOF Disclosed herein are antibody drug conjugates (ADCs), drug-linkers for ADCs, and tunable phosphate-based linkers. ADCs of the present disclosure include antibodies such as anti-CD70 antibodies conjugated to duocarmycin analogs via phosph...
WO/2024/074977A1	SUBSTITUTED 1 H-PYRAZOLO-PYRIDINE AND-PYRIMIDINE COMPOUNDS This disclosure relates to compounds of Formula (I) (I), or a pharmaceutically acceptable salt thereof, in which R3, R4, L2, W, X, Y, and Z are as 5 defined herein, to pharmaceutical compositions comprising such compounds and salts; to p...
WO/2024/077057A1	PHENYL OXY AMIDE KINASE INHIBITORS Compounds having activity as kinase inhibitors are provided. The compounds have Structure (I), or a stereoisomer, tautomer, or salt thereof, wherein, R1, R3, and m are as defined herein. Methods associated with preparation and use of suc...
WO/2024/076614A2	MULTI-CYCLIC IRAK AND FLT3 INHIBITING COMPOUNDS AND USES THEREOF The present disclosure provides pyrazolo[1,5-a]pyrimidine compounds and compositions comprising the same which inhibit IRAK and/or FLT3. The present disclosure further provides methods of using the pyrazolo[1,5-a]pyrimidine compounds to ...
WO/2024/075131A1	CO-CRYSTAL OF UPADACITINIB AND DIACETYL-D-TARTARIC ACID AND PROCESS FOR THE PREPARATION THEREOF 5 The present invention relates to a Co-crystal of Upadacitinib. More particularly, the present invention relates to a compound of Formula-I, which is a Co-crystal of Upadacitinib and Diacetyl-D-tartaric acid (DATA), characterized by pow...
WO/2024/076680A1	CRYSTAL FORMS OF AN ANTI-SARS COV-2 AGENT The present invention features crystalline forms of Compound I, including polymorphs and pseudopolymorphs, which are useful in the preparation of pharmaceutical compositions.
WO/2024/075051A1	HSD17B13 INHIBITORS AND/OR DEGRADERS Described herein are compounds of Formula I, wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD an...
WO/2024/076999A2	GABAA RECEPTOR MODULATORS AND USES THEREOF Described herein are uses of 2',6-difluoro-5'-(3-(2-hydroxypropan-2-yl)imidazo[1,2-b][1,2 ,4]triazin-7-yl)-[1,1'-biphenyl]-2-carbonitrile or a salt thereof. Also described herein are compositions, such as dosage forms, of 2',6-difluoro-5...
WO/2024/077216A1	CDK INHIBITORS AND THEIR USE AS PHARMACEUTICALS The disclosure is directed to compounds of Formula I (I). Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
WO/2024/066548A1	β-ELEMENE DERIVATIVE CONTAINING PHOTOAFFINITY GROUP DIAZIRINE, PREPARATION METHOD THEREFOR, AND USE THEREOF AS PHOTOAFFINITY MOLECULAR PROBE The present invention provides a β-elemene derivative containing the photoaffinity group diazirine, a preparation method therefor, and use thereof as a photoaffinity molecular probe. The present invention provides a compound of a struct...
WO/2024/069646A1	IMPROVED PROCESS FOR THE PREPARATION OF RISDIPLAM AND ITS INTERMEDIATES The present invention relates to an improved process for the preparation of Risdiplam compound of Formula-I. The present invention also relates to novel intermediates of Risdiplam compound of Formula-I and process for the preparation of ...
WO/2024/068740A1	NOVEL CDK9 INHIBITORS The present invention relates to novel compounds of formula (I). These compounds are inhibitors of CDK9 and are useful in the treatment of a variety of diseases including hyperproliferative diseases, virally induced infectious diseases, ...
WO/2024/067465A1	KIF18A INHIBITOR Provided are a compound useful as a KIF18A inhibitor, a pharmaceutically acceptable salt, an ester or a stereoisomer thereof, a pharmaceutical composition and a preparation comprising the compound or the pharmaceutically acceptable salt,...
WO/2024/067773A1	TEAD INHIBITORS AND METHODS OF USES THEREOF Provided herein are compounds and methods for modulating or inhibiting TEAD. Further provided herein are pharmaceutical compositions comprising the TEAD inhibitors and methods of treatment using the TEAD inhibitors or the pharmaceutical ...
WO/2024/073658A1	HYDANTOIN MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION The subject matter described herein is directed to myelin-promoting compounds of Formula (I) and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of admin...
WO/2024/066984A1	TRICYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE Provided in the present invention is a tricyclic derivative, and the structure thereof is as shown in formula (I). In addition, further disclosed in the present invention are a pharmaceutically acceptable salt of the derivative, a stereo...

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