Heterocyclic Compounds

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Document	Document Title
WO/2020/063696A8	PREPARATION OF SEMICARBAZIDE-SENSITIVE AMINE OXIDASE INHIBITOR AND USE THEREOF Provided are a preparation of a semicarbazide-sensitive amine oxidase inhibitor and the use thereof. In particular, dislosed are a compound as shown in formula I, or a stereoisomer or racemate or pharmaceutically acceptable salt thereof....
WO/2021/068866A1	HETEROCYCLIC COMPOUNDS AS STING MODULATORS Disclosed herein are heterocyclic compounds that may be used as STING modulators, process for synthesis and to uses of such compounds in treatment of various diseases including cancers.
WO/2021/072232A1	BICYCLIC AMINES AS CDK2 INHIBITORS The present application provides bicyclic amines that are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
WO/2021/068755A1	COMPOUND HAVING BRD4 INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF Disclosed in the present invention are a compound having a BRD4 inhibitory activity, a preparation method therefor and the use thereof. The structure of the compound having the BRD4 inhibitory activity of the present invention is as show...
WO/2021/068380A1	PREPARATION OF DEGRADATION COMPOUND TARGETING BTK PROTEIN, AND APPLICATION THEREOF IN TREATING AUTOIMMUNE DISEASES AND TUMORS A compound, the compound being a compound represented by formula I, or a stereoisomer, geometric isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof. The compound has a stro...
WO/2021/071919A1	HCK AS A THERAPEUTIC TARGET IN MYD88 MUTATED DISEASES The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided ...
WO/2021/072140A1	PRODRUGS OF MYELOPEROXIDASE INHIBITORS Disclosed are prodrugs of myeloperoxidase (MPO) inhibitors, methods of treating MPO related disorders, e.g., multiple system atrophy, amyotrophic lateral sclerosis, and Huntingtons disease, and methods of neuroprotection, which include a...
WO/2021/066088A1	NOVEL TRIAZINE DERIVATIVE Provided is a compound represented by the following formula (1) and a pharmacologically acceptable salt, which have a regulatory activity for a histamine H4 receptor and are useful for the treatment and/or prevention of diseases or condi...
WO/2021/022220A3	ANTICANCER AGENTS In an embodiment, the present disclosure pertains to a method of treating a disease by induction of activity in cells. Generally, the method includes administering a bis-indole- derived compound to a subject in need thereof. In some embo...
WO/2021/066958A1	INHIBITOR OF BTK AND MUTANTS THEREOF The disclosure includes compounds of Formula (I) wherein Q0, Q1, Q2, Q3, Q4, Z, W, i, j, m, n, Warhead, R0, R1, R3, R4, R5, R6, and R7, are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease,...
WO/2021/065980A1	BET DEGRADER Provided is a BET degrader. A BET degrader including a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is used. (In the formula, L1 and L2 are the same or different and represent a low molecular ligand f...
WO/2021/066873A1	CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS The disclosure includes compounds of Formula (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1 Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a ...
WO/2021/067215A1	PIPERIDINE COMPOUNDS AS MENIN INHIBITORS The present disclosure provides compounds represented by Formula (la): and the pharmaceutically acceptable salts thereof, wherein R1a, R1b, R1c, R2, R3, L, M and G are as defined as set forth in the specification. The present disclosure ...
WO/2021/063335A1	ERK1/2 PROTEIN KINASE INHIBITOR AND USE THEREOF The present application provides a compound represented by formula (I), or isomer or pharmaceutically acceptable salt thereof, and use thereof in the preparation of an ERK1/2-mediated disease drug.
WO/2021/067521A1	COMPOUNDS USEFUL AS IMMUNOMODULATORS The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical composit...
WO/2021/067326A1	SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X, Y, A, G, R1, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9,...
WO/2021/030238A3	METHOD OF SYNTHESIS OF COMPOUND FOR DUAL INHIBITION OF JAK2 AND BET Embodiments of the invention include quinoline compounds and methods of synthesis. Ohm-581 has demonstrated dual inhibition of JAK2 and BET and acts as a therapeutic agent for micosis fungoides (MF) and other hematologic malignancies. Em...
WO/2021/066043A1	METHOD FOR PRODUCING TRIONE COMPOUND The present invention provides a method for producing a trione compound, said method being characterized by producing a trione compound represented by formula (IV) (wherein R1 and R2 are as defined in formula (I); and R3 and Ar are as de...
WO/2021/062559A1	CANNABINOID DERIVATIVES This disclosure relates to carmabinoid derivatives of Formula (1) wherein R4 or R7 is a carboxamide group, pharmaceutical compositions comprising these compounds and methods of using the carmabinoid derivatives. These compounds are poten...
WO/2021/064141A1	INHIBITORS OF DUAL SPECIFICITY TYROSINE PHOSPHORYLATION REGULATED KINASE 1B The present invention relates to compounds of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof (I), in particular for use in...
WO/2021/062557A1	CANNABINOID DERIVATIVES This disclosure relates generally to cannabinoid derivatives having the formula (I), wherein R4 is hydrogen, -C(Q1)N(R4a)(R4b) or -C(R4J)(R4k)N(R4e)C(0)R4f, R6 is hydrogen, -C(Q2)N(R6a)(R6b) or -C(R6J)(R6k)N(R6e)C(0)R6f, provided that R6...
WO/2021/064077A1	SUBSTITUTED PYRAZOLOPYRIMIDINES AS IRAK4 INHIBITORS The present application relates to novel pyrazolopyrimidine derivatives for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments f or treatment and/or prophylaxis of diseases in humans and in anim...
WO/2021/067606A1	BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand...
WO/2021/063145A1	TETRACYCLIC PYRIMIDINONE COMPOUND, PREPARATION METHOD THEREFOR, AND COMPOSITION AND USE THEREOF Disclosed is a tetracyclic pyrimidinone compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, wherein same has the structure as shown in formula (I), is a completely new Lp-PLA2 inhibitor, and can be used for tr...
WO/2021/061803A1	PHOSPHODIESTERASE INHIBITORS AND USE The invention provides compounds that may inhibits to ENPP1, and are accordingly useful for treatment disorders related to ENPP1. The invention further provides pharmaceutical compositions containing these compounds and methods of using ...
WO/2021/062036A1	JAK INHIBITORS Described herein are Janus kinase (JAK) inhibitors and methods of utilizing JAK inhibitors in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
WO/2021/062327A1	FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF The present disclosure relates to a class of fused pyrimidine compounds of Formula I, their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to a...
WO/2021/058017A1	DEGRADATION OF ANDROGEN RECEPTOR (AR) BY CONJUGATION OF AR ANTAGONISTS WITH E3 LIGASE LIGAND AND METHODS OF USE Provided herein are novel bifunctional compounds formed by conjugating AR antagonist moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 Ubiquitin ligase for degradation, and methods of preparation ...
WO/2021/059136A1	POLYHETEROCYCLIC MODULATORS OF STING (STIMULATOR OF INTERFERON GENES) Compounds of the general formula (I), or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
WO/2021/060281A1	PROSTAGLANDIN E2 RECEPTOR EP2/EP4 DUAL ANTAGONIST The purpose of the present invention is to provide a novel compound which has a prostaglandin E2 (PGE2) receptor EP2/EP4 dual antagonizing effect and is useful as: a preventive or therapeutic agent for a disease selected from cancer, pai...
WO/2021/057796A1	SUBSTITUTED FUSED TRICYCLIC DERIVATIVE, AND COMPOSITION AND USE THEREOF Provided are a substituted fused tricyclic derivative, and a composition and use thereof. The substituted fused tricyclic derivative is a compound represented by formular (I) or a tautomer, stereisomer, prodrug, crystal form, pharmaceuti...
WO/2021/061749A1	COMBINATION THERAPIES The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a the...
WO/2021/057877A1	SUBSTITUTED AROMATIC FUSED RING DERIVATIVE AND COMPOSITION COMPRISING SAME, AND USE THEREOF Provided in the present invention are a substituted aromatic fused ring derivative, a composition comprising the compound, and the use thereof. The substituted aromatic fused ring derivative is a compound as shown as formula (I) or a tau...
WO/2021/058018A1	INHIBITORS OF KRAS G12C Disclosed herein are compounds that inhibit KRas G12C, pharmaceutical compositions, methods of preparation and uses thereof.
WO/2021/057893A1	PYRAZOLOPYRIDINE COMPOUNDS AS SELECTIVE BTK KINASE INHIBITORS Disclosed are a class of BTK kinase inhibitor compounds with a high activity and a high selectivity and the use thereof in the preparation of a drug for treating BTK target-related diseases. Specifically, disclosed are a compound shown a...
WO/2021/058027A1	PYRROLO HETEROARYL DERIVATIVE OR CONJUGATE THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF A pyrrolo heteroaryl derivative or a conjugate thereof, a preparation method therefor and an application thereof. Specifically, a compound represented by general formula (D) or a ligand-drug conjugate thereof, a preparation method theref...
WO/2021/058021A1	DRUG COMBINATION CONTAINING TLR7 AGONIST A drug combination containing a TLR7 agonist. Specifically, a drug combination jointly using the compound of formula I acting as a TLR7 agonist and entecavir for the treatment of hepatitis B virus infection and a use thereof, the drug co...
WO/2021/053158A1	NOVEL HISTONE METHYLTRANSFERASE INHIBITORS The present invention relates to novel compounds of formula (I) as defined herein. The compounds are inhibitors of histone methyltransferases of the seven-beta-strand family, in particular of KMT9.
WO/2021/053495A1	BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE Described herein are bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target...
WO/2021/053690A1	AN IMPROVED PROCESS FOR THE PREPARATION OF BARICITINIB The present invention provides an improved process for the preparation of Baricitinib of formula (I),
WO/2021/055863A1	PYRUVATE KINASE R (PKR) ACTIVATING COMPOSITIONS The present disclosure provides crystalline solid forms, spray-dried dispersions and pharmaceutical compositions, including solid oral dosage forms, of (S)-1-(5-[2H,3H-[1,4]dioxino[2,3-b]pyridine-7-sulfonyl]-1H,2 H,3H,4H,5H,6H-pyrrolo[3,...
WO/2021/055591A1	SUBSTITUTED BENZIMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, l...
WO/2021/032004A9	AZAHETEROARYL COMPOUND AND APPLICATION THEREOF Disclosed in the present invention are an azaheteroaryl compound, a pharmaceutically acceptable salt thereof, and a solvate thereof. The present invention also provides a method for preparing said compound, a composition containing said ...
WO/2021/055627A1	SUBSTITUTED N-HETEROCYCLIC CARBOXAMIDES AS ACID CERAMIDASE INHIBITORS AND THEIR USE AS MEDICAMENTS The invention provides substituted N-heterocyclic carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, ...
WO/2021/055376A1	IL-17A MODULATORS AND USES THEREOF The disclosure herein provides compounds and pharmaceutical compositions for the modulation of IL-17A useful for the treatment of inflammatory conditions, such as psoriasis.
WO/2021/055807A1	ACTIVATING PYRUVATE KINASE R The compound (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfo nyl)-3,4,5,6- tetrahydropyrrolo[3,4-c]pyrroll-2(1H)-yl)-3-hydroxy-2-phenyl propan-1-one, or a pharmaceutically acceptable salt thereof, is useful to increase the a...
WO/2021/054365A1	LIQUID CRYSTAL ALIGNMENT AGENT, LIQUID CRYSTAL ALIGNMENT FILM, AND LIQUID CRYSTAL DISPLAY ELEMENT The purpose of the present invention is to provide a liquid crystal alignment agent which can produce a liquid crystal alignment film having the required functions, including adhesion, and having favorable workability, and to provide a l...
WO/2021/055326A1	AZOLE-FUSED PYRIDAZIN-3(2H)-ONE DERIVATIVES Disclosed are compounds of Formula (1) and pharmaceutically acceptable salts thereof, wherein α, β, n, R4, R5, R6, R8, R9, R10, R11, X1, X2, X3 and X7 are defined in the specification. This disclosure also relates to materials and meth...
WO/2021/053617A1	MLL1 INHIBITORS AND ANTI-CANCER AGENTS The present invention provides a compound of Formula (I): or an enantiomer, an enantiomeric mixture, or a pharmaceutically acceptable salt thereof; wherein the variables are as defined herein. The present invention further provides pharm...
WO/2021/055518A1	BENZIMIDAZOLES AND METHODS OF USING SAME The present disclosure is concerned with benzimidazole compounds and methods of using these compounds for the treatment of hepatitis (e.g., hepatitis C), RNA virus infections (e.g., Zika virus, dengue virus, Powassan virus, Chikungunya v...

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