Heterocyclic Compounds

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Document	Document Title
WO/2024/155112A1	2,4-DIANILINOPYRIMIDINE-BASED AURORA-A KINASE SELECTIVE DEGRADATION INDUCING COMPOUNDS Novel 2,4-Dianilinopyrimidine-based Aurora-A kinase (AURKA) degraders are disclosed. The present AURKA degraders are proteolysis targeting chimeras (PROTACs) that recruit AURKA protein into optimized CRBN E3 ubiquitin ligase via linkers....
WO/2024/153246A1	SUBSTITUTED TRICYCLIC COMPOUND AND USE THEREOF Provided are a compound of formula (I) which acts as a Cbl-b inhibitor, or a stereoisomer thereof or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition comprising the compound of formu...
WO/2024/153775A1	PIPERIDINE DERIVATIVES AS METTL3 INHIBITORS The present invention relates to compounds of formula (I), (I) or pharmaceutically acceptable salts and/or solvates thereof, wherein m, n, R1, R2, R3, R4, R5, L, Ar1 and Ar2 are as defined in the claims, which are useful as inhibitors of...
WO/2024/153238A1	TETRACYCLIC COMPOUND AND USE THEREOF The present disclosure relates to a tetracyclic compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof in the prevention or treatment of PI3Kα-rel...
WO/2024/155864A1	SPRK1 INHIBITORS AND METHODS OF USE Provided herein are compounds having a structure of Formula (I) and pharmaceutically acceptable salts thereof which can act as modulators of serine/arginine-rich splicing factor protein kinase- 1 (SRPK1). Further disclosed herein are met...
WO/2024/153070A1	GLP-1R AGONISTS AND USES THEREOF Provided are certain GLP-1R agonists of formula (I), pharmaceutical compositions thereof, and methods of use thereof.
WO/2024/152986A1	HETEROARYL AMINO COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF The present invention relates to a heteroaryl amino compound, a preparation method therefor, and use thereof, as well as a compound represented by formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a deuterate...
WO/2024/152973A1	PRMT5-MTA INHIBITOR Provided in the present invention is a compound as a PRMT5-MTA inhibitor, which is a compound as represented by formula (I) or a pharmaceutically acceptable salt, an isotopic variant, a tautomer or a stereoisomer thereof. Further provide...
WO/2024/155680A1	TOTAL SYNTHESES OF PORTIMINE A AND ANALOGUES THEREOF AS SMALL MOLECULE MODULATORS OF NMD3 Disclosed herein are enantioselective synthetic methods of making known cyclic imine (CI) toxins and analogues thereof as small molecule inhibitors of NMD3 with selective and potent anti -cancer activity.
WO/2024/153230A1	5-AMINO-1H-PYRROLO [3, 2-b] PYRIDINE-2-CARBOXAMIDE DERIVATIVES AS MTA-COOPERATIVE INHIBITORS OF PRMT5 Provided herein are compounds containing 5-AMINO-1H-PYRROLO [3, 2-b] PYRIDINE-2- CARBOXAMIDE derivatives as MTA-cooperative inhibitors of PRMT5, the use thereof for selectively inhibiting the activity of PRMT5 in cooperative with MTA in ...
WO/2024/150029A1	COMPOUNDS DERIVED FROM DIHYDROPIRIDINES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAID COMPOUNDS AND METHOD OF TREATMENT OF MUSCLE DISORDERS COMPRISING ADMINISTRATION OF SAID COMPOSITIONS The invention of the present application relates to compounds derived from tetrahydrofuran [3,4-b]pyridine-3-carboxylate, pharmaceutical compositions comprising said compounds and a method of prevention and treatment of muscle disorders ...
WO/2024/151833A1	SPIRO DERIVATIVES AS M4 ACTIVATORS/MODULATORS AND USES THEREOF The present disclosure provides compounds of Formula I: (l) (I), or an N- oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: A, Y, m, n,p, R1, R2, R3, R3a, R4, R5, R6, R7, and Z are as described...
WO/2024/151172A1	CYANODIPHENYL SULFONE DERIVATIVES, A PROCESS FOR THEIR PREPARATION, AN EMISSIVE LAYER CONTAINING THEM, AN ELECTROLUMINESCENT DEVICE, AND THEIR USE The subject of the invention is new cyanodiphenyl sulfone derivatives of Formula 1 and a process for their preparation, an emissive layer containing them, an electroluminescent device, and their use. The invention belongs to the field of...
WO/2024/151672A1	DIRECTED BIOSYNTHESIS OF MODIFIED ANTHRAQUINONE-FUSED ENEDIYNES AS POTENTIAL CANCER THERAPEUTICS Analogues of dynemicin, methods of their preparation, and their use for treating cancer are disclosed.
WO/2024/149193A1	PREPARATION METHOD FOR NITROGEN-CONTAINING FUSED RING COMPOUND The present application provides a preparation method for a nitrogen-containing fused ring compound having anti-tumor activity. According to the method, a target product can be efficiently obtained under relatively mild reaction conditio...
WO/2024/148088A1	SPIROCYCLOALKYL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THAT MODULATE IKZF2 Disclosed are compounds and salts thereof that bind to and modulate cereblon activity. In some embodiments, the binding and modulation of cereblon results in the degradation of IKAROS family zinc finger proteins (e.g., IKZF2). The compou...
WO/2024/140443A1	ANTIBODY-DRUG CONJUGATE OF N-AZIDOALKYL SUBSTITUTED CAMPTOTHECIN DERIVATIVE An antibody-drug conjugate as represented by formula (I) with an azidoalkyl substituted camptothecin derivative as the toxic part of a drug. The antibody-drug conjugate has a significant anti-tumor effect.
WO/2024/140637A1	OXOISOINDOLINYL SUBSTITUTED PIPERIDINEDIONE DERIVATIVE AND USE THEREOF The present disclosure relates to a compound of formula (I) or a salt, enantiomer, stereoisomer, solvate or polymorph thereof, and a use thereof. The present disclosure further relates to a pharmaceutical composition comprising the compo...
WO/2024/140447A1	ANTIBODY-DRUG CONJUGATE FROM N-HALOALKYL SUBSTITUTED CAMPTOTHECIN DERIVATIVE An oxycycloalkyl-substituted camptothecin derivative used as an antibody-drug conjugate represented by formula (I) in the drug toxicity portion. The antibody-drug conjugate has a significant antitumor effect.
WO/2024/140671A1	FUSED TRICYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND USE THEREOF The present invention relates to a fused tricyclic derivative, a pharmaceutical composition comprising same, and an application thereof. Specifically, the present invention provides a compound shown in formula (I) or a pharmaceutically a...
WO/2024/141535A1	NLRP3 INFLAMMASOME INHIBITORS The specification generally relates to compounds of Formula (I), Formula (II) and Formula (VI), and pharmaceutically acceptable salts thereof. Such compounds are useful in inhibiting NLRP3 inflammasome activity and may be useful as thera...
WO/2024/140449A1	ANTIBODY-DRUG CONJUGATE FROM N-OXYCYCLOALKYL SUBSTITUTED CAMPTOTHECIN DERIVATIVE An oxycycloalkyl-substituted camptothecin derivative used as an antibody-drug conjugate represented by formula (I) in the drug toxicity portion. The antibody-drug conjugate has a significant antitumor effect.
WO/2024/140969A1	TRICYCLIC COMPOUND, AND PREPARATION METHOD AND USE THEREFOR Disclosed in the present invention are a tricyclic compound and a use thereof in drugs, particularly relating to a novel tricyclic compound and a pharmaceutical composition containing the compound. The invention also relates to a prepara...
WO/2024/144246A1	ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE USING SAME The present invention relates to a novel organic compound and an organic electroluminescent device using same, and, more specifically, to an organic compound having excellent electron transport ability, heat resistance, carrier transport...
WO/2024/145623A1	HETEROCYCLIC AND HETEROARYL COMPOUNDS AS INHIBITORS OF NLRP3 The present invention relates to novel compounds of Formula (I): wherein each ring A, R1, R2, X, Y, and Z are as defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to th...
WO/2024/140933A1	CAMPTOTHECIN DERIVATIVE, PHARMACEUTICAL COMPOSITION, AND PREPARATION METHOD AND USE THEREFOR The invention relates to a camptothecin derivative as shown in general formula I, a pharmaceutical composition, and a preparation method and use therefor. The camptothecin derivative has good tumor inhibitory activity, can be used for tr...
WO/2024/141757A1	LSD1 MODULATORS Disclosed are compounds, compositions and methods for treating disease, syndromes, conditions and disorders that are affected by the modulation of LSD1. Such compounds are represented by formula (I) wherein the variables are defined herein.
WO/2024/140934A1	PREPARATION METHOD FOR LINKER-DRUG CONJUGATE AND INTERMEDIATE THEREOF Provided are a preparation method for a linker-drug conjugate and an intermediate thereof. Particularly provided is a preparation method for a compound LE14, comprising subjecting an intermediate, i.e., a compound of formula II, and a co...
WO/2024/140868A1	CRYSTAL FORM OF TRICYCLIC COMPOUND AND USE THEREOF Provided are a crystal form of a tricyclic compound and a use thereof. Specifically, provided are a crystal form of a compound 2-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methox y-10,11-dihydrobenzo[6,7]oxazole [3,2-b]pyridine-...
WO/2024/133499A1	GLYCINE DERIVATIVES WITH P2X4 RECEPTOR-BLOCKING ACTIVITY AS DIAGNOSTICS AND FOR THE TREATMENT OF PAIN, INFLAMMATION, CANCER, AND OTHER P2X4 RECEPTOR-RELATED DISEASES The invention relates to glycine derivatives with P2X4 receptor-blocking activity for the treatment of pain, inflammation, cancer, and other P2X4 receptor-related diseases.
WO/2024/130526A1	A BIOORTHOGONAL CYCLOADDITION REACTION AND USE THEREOF Provided is a bioorthogonal cycloaddition reaction, as well as the use in assembly of TAC-type molecules and use in preparation of bioconjugates.
WO/2024/131166A1	NITROGEN-CONTAINING COMPOUND, AND ORGANIC ELECTROLUMINESCENT DEVICE AND ELECTRONIC APPARATUS The present application relates to the technical field of organic electroluminescent materials, and provides a nitrogen-containing compound, and an organic electroluminescent device and an electronic apparatus comprising same. In the com...
WO/2024/131777A1	KRAS-PROTAC CHIMERIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF The present invention relates to a compound as represented by formula (I) or a pharmaceutically acceptable salt and a stereoisomer thereof, and the use thereof in the treatment of tumors, immunological diseases, inflammation and other di...
WO/2024/138045A1	MODULATORS OF NLRP3 INFLAMMASOME AND RELATED PRODUCTS AND METHODS Compounds are provided for inhibiting NLRP3 inflammasome generally, or for treating a NLRP3 inflammasome dependent condition more specifically, by contacting the NLRP3 inflammasome or administering to a subject in need thereof, respectiv...
WO/2024/134466A1	SUBSTITUTED ARYLAMINE COMPOUNDS, SUBSTITUTED HETEROARYLAMINE COMPOUNDS, AND METHODS USING SAME The present disclosure relates to substituted arylamine and substituted heteroarylamine compounds, analogues thereof, and compositions comprising the same. In one aspect, the compounds contemplated in the disclosure can be used to treat,...
WO/2024/133014A1	PHENYLPIPERIDINE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN The present disclosure provides certain phenylpiperidine derivatives of formula (I), and pharmaceutically acceptable salts thereof, that are inhibitors of Glutaminyl -peptide cyclotransferase (QPCT) and glutaminyl-peptide cyclotransferas...
WO/2024/136503A1	ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE USING SAME The present invention relates to: a novel compound having excellent carrier transport capacity, luminescence capacity, and thermal stability; and an organic electroluminescent device of which characteristics such as luminescence efficien...
WO/2024/137852A1	PRMT5 INHIBITORS AND USES THEREOF The present disclosure relates generally to compounds that inhibit PRMT5. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through inhibiting P...
WO/2024/138206A1	FLUOROPYRIDOPYRIMIDINE AND FLUOROQUINAZOLINE DERIVATIES AND METHODS OF USE THEREOF The present disclosure provides compounds and methods useful in the treatment and suppression of cancer, for example, useful for treating or suppressing cancers characterized by KRAS G12C. Also provided are pharmaceutical compositions co...
WO/2024/129601A1	COMPOUND EMBODIMENTS FOR MUSCLE MYOSIN INHIBITION AND METHODS OF MAKING AND USING THE SAME Disclosed herein are compounds for use as muscle myosin inhibitors, along with methods for making and using the same. Compounds of the present disclosure can exhibit a selectivity for cardiac vs. skeletal myosin and do not inhibit non-mu...
WO/2024/125488A1	AROMATIC AMIDE DERIVATIVE, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF Provided are an aromatic amide derivative, a preparation method therefor, and the pharmaceutical use of a pharmaceutical composition containing the derivative. Specifically, provided are an aromatic amide derivative as shown in general f...
WO/2024/129614A1	SOMATOSTATIN SUBTYPE-2 RECEPTOR (SST2R) TARGETED THERAPEUTICS AND USES THEREOF Described herein are somatostatin subtype-2 receptor (SST2R) targeted thereapeutics that target tumor cells expressing SST2R and their use in the treatment of cancer.
WO/2024/130095A1	COMPOUNDS AND COMPOSITIONS AS CBP/P300 DEGRADERS AND USES THEREOF Described herein are compounds of Formula I and their pharmaceutically acceptable salts, solvates, or stereoisomers thereof, as well as their uses (e.g., for degrading certain proteins such as p300/CBP proteins).
WO/2024/125603A1	SHP2 INHIBITOR AND USE THEREOF The present invention pertains to the technical field of pharmaceuticals, and relates to an SHP2 inhibitor and use thereof. In particular, the present invention relates to a compound represented by formula (I), an isomer thereof, a deute...
WO/2024/130161A2	NOVEL CAMPTOTHECIN DERIVATIVES AND CONJUGATES THEREOF The present disclosure provides novel camptothecin derivatives and their conjugates thereof. The present disclosure further provides to pharmaceutical composition comprising the novel camptothecin derivatives or their conjugates thereof,...
WO/2024/125627A1	CAMPTOTHECIN COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF The present disclosure belongs to the technical field of pharmaceutical chemistry, and particularly relates to a class of camptothecin compounds and a preparation method therefor. The class of compounds exhibits good tumor inhibitory act...
WO/2024/124357A1	DIAGNOSIS AND TREATMENT OF LONG-COVID A method of determining a risk of developing a neurological disorder in a Long-COVID patient comprising: (a) testing levels of at least one marker associated with a neurologic disorder in a sample taken from the Long-COVID patient, and (...
WO/2024/125482A1	COMPOUND USED AS KETOHEXOKINASE INHIBITOR, USE THEREOF, AND COMPOSITION CONTAINING SAME Provided are a compound of formula (I), a pharmaceutically acceptable salt thereof, a stereoisomer thereof, or an isotope marker thereof, and a pharmaceutical composition containing the compound of formula (I), as well as a use of the co...
WO/2024/120419A1	FUSED TETRACYCLIC COMPOUNDS AS KRAS G12D MODULATORS AND USES THEREOF This application discloses compounds of formula (I), which can be inhibitors of KRAS G12D, and their uses.
WO/2024/119277A1	KRAS INHIBITORS AND PHARMACEUTICAL USES THEREOF The disclosure relates to KRAS inhibitor compounds having the structure of Formula (I), pharmaceutical compositions thereof, and methods of use thereof for inhibiting, treating, and/or preventing KRAS-associated diseases, disorders and c...

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