Heterocyclic Compounds

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Document	Document Title
WO/2021/070150A1	AN INHALABLE DRY POWDER COMPOSITION FOR PULMONARY DISEASES The present invention relates to an inhalable composition comprising a therapeutically effective dosage amount of compound (I), 2-{4-[(2S)-1,1-difluoro-2-hydroxypropyl]phenyl}-N-{4-[3-(2-e thylphenyl) pyrazine-2-yl]phenyl}acetamide or a ...
WO/2021/068943A1	SUBSTITUTED NITROGEN HETEROCYCLIC COMPOUND AND ANESTHETIC EFFECT THEREOF Disclosed in the present invention are a substituted nitrogen heterocyclic compound and anesthetic action thereof. Specifically provided are a chemical compound as shown in formula I, a stereoisomer thereof, a pharmaceutically acceptable...
WO/2021/068820A1	ALKENE-CONTAINING CARBOXYLATE COMPOUND AND USE THEREOF Disclosed in the present invention are an alkene-containing carboxylate compound and use of an agriculturally acceptable salt thereof as a herbicide. Said compound is as represented by general formula (I). The definition of the substitue...
WO/2021/068815A1	CARBOXYLIC ACID ESTER COMPOUND AND APPLICATION THEREOF Disclosed in the present invention are a carboxylic acid ester compound and an application thereof, the structure of the compound being shown in general formula I, and the definition of each substituent in general formula I being provide...
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/2021/070132A1	BI-ARYL DIHYDROOROTATE DEHYDROGENASE INHIBITORS Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula I as follows: Formula I wherein R1, R2, R3,...
WO/2021/067460A1	BIOCATALYTIC SYNTHESIS OF CRYPTOPHYCIN ANTICANCER AGENTS The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.
WO/2021/067374A1	BICYCLIC HETEROCYCLES AS FGFR INHIBITORS The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 enzyme and are useful in the treatment of F GFR3-associated diseases such as cancer.
WO/2021/058754A1	PHARMACEUTICAL COMPOUNDS The invention provides a composition of matter which: • (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or • (ii) consists of at least 90 % by weight of an atropi...
WO/2021/060888A2	COMPOSITION FOR PREVENTING OR TREATING CANCER, CONTAINING NOVEL TRIFLUOROMETHYL PHENYL PYRAZOLE DERIVATIVE AS ACTIVE INGREDIENT The present invention relates to a composition for preventing or treating cancer, containing a novel trifluoromethyl phenyl pyrazole derivative as an active ingredient, and, more specifically, to a composition for preventing, alleviating...
WO/2021/055849A1	HEADGROUP LIPID COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS The application relates to lipids of Formula (A-1) and compositions involving the same. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) include such a lipid as well as additional lipids such as phospholipids, structural lipids, and...
WO/2021/047581A1	HEXAHYDROBENZOPYRAZOLE DERIVATIVE AND PREPARATION THEREFOF Disclosed is a hexahydrobenzopyrazole compound shown in formula (I), and a stereoisomer, a pharmaceutically acceptable salt, a solvate, a hydrate, an N-oxide, a prodrug, and a pharmaceutical composition thereof, a preparation method ther...
WO/2021/047407A1	BIARYL COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF A biaryl compound, a pharmaceutical composition thereof, a preparation method therefor, and a use thereof. The compound has the structure shown in formula I, has a significant regulatory effect on RORγ, can be used as a highly effective...
WO/2021/047583A1	TRICYCLIC PYRAZOLE DERIVATIVE AND PREPARATION THEREOF Disclosed is a tricyclic pyrazole compound shown in formula (I), and a stereoisomer, a pharmaceutically acceptable salt, a solvate, a hydrate, an N-oxide, a prodrug, and a pharmaceutical composition thereof, a preparation method therefor...
WO/2021/047677A1	IRAK4 KINASE INHIBITOR AND PREPARATION THEREOF AND USE THEREOF Provided are an IRAK4 kinase inhibitor, and preparation thereof and use thereof, specifically provided are a compound represented by formula (I), a stereoisomer thereof, a geometric isomer thereof, a tautomer thereof, a pharmaceutically ...
WO/2021/038419A1	KINASE INHIBITORS AND METHODS OF SYNTHESIS AND TREATMENT Compounds that function as kinase inhibitors are provided. The kinase inhibitors can have any structure of the formulae provided herein, such as shown for Compounds 1-4. A pharmaceutical composition can include: the compound of one of th...
WO/2021/038490A1	SUBSTITUTED UREA DIHYDROOROTATE DEHYDROGENASE INHIBITORS Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula I as follows: Formula I wherein R1, R2, R3 ...
WO/2021/036845A1	SUBSTITUTED BENZOYL COMPOUND AND APPLICATION THEREOF Provided is a substituted benzoyl compound and an application thereof; specifically, provided is a compound represented by formula (I), a preparation method therefor and a use thereof as an herbicide. Q is optionally substituted oxocyclo...
WO/2021/035788A1	PYRAZOLE DERIVATIVE AND USE THEREOF A PDGFR kinase inhibitor represented by structural formula (I) as well as use thereof and a method using same for preventing or treating PDGFR kinase activity related diseases.
WO/2021/037219A1	PYRAZOLE DERIVATIVE FOR FGFR INHIBITOR AND PREPARATION METHOD THEREFOR The present invention provides an amide pyrazole compound used as an FGFR irreversible inhibitor, a preparation method therefor, and use thereof. Specifically, the present invention provides a compound of formula I, or a pharmaceutically...
WO/2021/039824A1	RNA METHYLTRANSFERASE INHIBITOR, SCREENING METHOD THEREFOR, ANTI-CANCER AGENT EFFICACY ASSESSMENT MARKER, AND KIT FOR EFFECTIVELY PREDICTING FTSJ1 INHIBITOR An RNA methyltransferase inhibitor containing at least one type of compound selected from the group consisting of sulfonamide-based compounds represented by general formula (1) and pyrazoline-based compounds represented by general formul...
WO/2021/031984A1	CARBOXYLIC ACID OXIME ESTER COMPOUND AND USE THEREOF Disclosed are a carboxylic acid oxime ester compound and the use thereof as a herbicide and for preparing a microbicide. The carboxylic acid oxime ester compound is as represented by general formula I:
WO/2021/033165A1	PROCESS FOR SYNTHESIS OF PYRAZOLIDINONE COMPOUNDS The present disclosure relates to a process for the synthesis of pyrazolidinone, particularly alkyl 2-(3-chloropyridin-2-yl)-5-oxo-pyrazolidine-3-carboxylate (pyrazolidinone) compound. The process of the present disclosure is simple, eco...
WO/2020/247819A3	METHODS OF TREATMENT WITH AMINOLEVULINIC ACID SYNTHASE 2 (ALAS2) MODULATORS Described herein is a compound of Formula I or a pharmaceutically acceptable salt thereof: wherein Ring A R1, R2, a, b, and n are as defined herein. Also described is a method of treating a subject having a disorder in need of treatment,...
WO/2021/033166A1	PROCESS FOR SYNTHESIS OF PYRAZOLIDINONE COMPOUNDS The present disclosure relates to a process for the synthesis of pyrazolidinone, particularly alkyl 2-(3-chloropyridin-2-yl)-5-oxo-pyrazolidine-3-carboxylate (pyrazolidinone) compound. The process of the present disclosure is simple, eco...
WO/2021/030554A1	PROCESS OF MAKING CFTR MODULATORS The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.
WO/2021/028512A1	ARYLSULFONAMIDE DERIVATIVES AS MGLUR4 NEGATIVE ALLOSTERIC MODULATORS The present invention provides new arylsulfonamide compounds having the general formula (I), wherein L, R1, R2, R3 and R4are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods ...
WO/2021/026182A1	PROCESS-SCALE SYNTHESIS OF A PLASMA KALLIKREIN INHIBITOR Disclosed are methods of preparing Compound (I), and salts thereof. The methods of preparing Compound (I) are suitable for use on process scale.
WO/2021/023213A1	SALT AND CRYSTAL FORM OF STEROID DERIVATIVE REGULATOR The present invention relates to a steroid derivative regulator, in particular to a compound of formula (I), a salt and crystal form thereof, a preparation method therefor, a pharmaceutical composition containing a therapeutically effect...
WO/2021/023993A1	MOLECULAR COMPLEXES The present invention relates to a crystalline molecular complex comprising metazachlor and a carboxylic acid. The invention also relates to a process for the preparation of the crystalline molecular complex, a herbicidal composition com...
WO/2021/026179A1	AGONISTS OF ROR GAMMAt The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositio...
WO/2021/025969A1	SOLID STATE FORMS OF BEROTRALSTAT The present disclosure relates to solid state forms of Berotralstat, pharmaceutically acceptable salts thereof, particularly Berotralstat dihydrochloride, processes for preparation thereof and pharmaceutical compositions thereof.
WO/2021/022761A1	HALOGEN SUBSTITUTED COMPOUND, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF The present invention relates to a preparation method for a halogen substituted compound. A piperazine derivative represented as formula I reacts with a halogenated acetyl halide derivative represented as formula VI to generate the halog...
WO/2021/019537A1	PROCESS AND INTERMEDIATES FOR THE PREPARATION OF PYROXASULFONE The invention provides a process which comprises the step of thiomethylating a pyrazole, to create R2-C(O)-S-CH2- functionality at position 4 of the pyrazole ring. The process is useful in preparing Pyroxasulfone. The invention also prov...
WO/2021/021634A1	NANOMATERIALS CONTAINING CONSTRAINED LIPIDS AND USES THEREOF Compositions for delivering nucleic acids to cells or tissue microenvironments are provided. In one embodiment, the compositions are lipid nanoparticle compositions formulated to have reduced splenic and hepatic clearance. It has been di...
WO/2021/020429A1	UREA COMPOUND FOR ANTAGONIZING LPA1 RECEPTOR The present invention provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof which has the effect of antagonizing the LPA1 receptor.
WO/2021/018849A1	PYRAZOLE DERIVATIVES FOR CONTROLLING ARTHROPODS The present invention relates to novel halogen-substituted compounds, to processes for their preparation and to their use for controlling animal pests, in particular arthropods and especially insects and arachnids.
WO/2021/021706A1	INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR The present application provides a compound of Formula (I): [Formula 1] or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, W, L, R8, and R9 are as described herein. Pharmaceutical compositions including these ...
WO/2020/263967A8	2H-INDAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE This invention relates to 2H-indazole Derivatives of formula (I'), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, capable of modulating the activity of IRAK4. The inventio...
WO/2021/014437A1	PROCESS FOR THE PREPARATION OF BIPHENYLAMINES The invention relates to a method for the preparation of 2-aminobiphenyls, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises reacting an ortho-substituted aniline and a phen...
WO/2021/016388A1	INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 AND USES THEREOF The present disclosure provides compounds of Formula (I), (II- 1), (II-2), (II-3), or (II- 4). The compounds of the present disclosure may be inhibitors of kinases (e.g., a cyclin- dependent kinase (CDK) (e.g., CDK7)). In some embodiment...
WO/2021/012949A1	1,2-BIS(DIPHENYLPHOSPHINOALKYLAMIDO)-1,2-DISUBSTITUTED ETHANE AND SYNTHESIS AND USE THEREOF Disclosed are a chiral phosphine ligand, 1,2-bis(diphenylphosphinoalkylamido)-1,2-disubstituted ethane, a synthesis method therefor and the use thereof in an asymmetric catalytic reaction, for example, in the asymmetric catalytic synthes...
WO/2021/013712A1	POLYAROMATIC UREA DERIVATIVES AND THEIR USE IN THE TREATMENT OF MUSCLE DISEASES The current invention provides urea derivatives, in particular compounds having the core structure heteroaryl-NH-CO-NH-aryl-O- heteroaryl, for use in treating, ameliorating, delaying, curing and/ or preventing a disease or condition asso...
WO/2021/009384A1	NOVEL PYRAZOLONE DERIVATIVES AS PD-1/PD-L1 INTERACTION INHIBITORS The present invention relates to novel pyrazolone derivatives of the following formula (I): (I) or a pharmaceutically acceptable salt and/or solvate thereof and to a pharmaceutical composition comprising thereof. The present invention al...
WO/2021/010492A1	COMPOUND HAVING KDM5 INHIBITORY ACTIVITY AND PHARMACEUTICAL USE THEREOF The present invention provides KDM5 inhibitor. The compound disclosed herein represented by the general formula (Z): wherein all symbols have the same meanings as the definitions described in the specification; or a salt thereof is usefu...
WO/2021/007189A1	CRYSTALLINE FORMS OF PLASMA KALLIKREIN INHIBITORS Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.
WO/2021/007190A1	PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS A process for preparing and purifying a compound of Formula (I) is provided; or a salt thereof, wherein the subscript m is an integer of from 0 to 3; each Ra is independently selected from the group consisting of (C3-C8)cycloalkyl, (C1-C...
WO/2020/210174A4	SULFONYLDIAZOLES AND N-(FLUOROSULFONYL)AZOLES, AND METHODS OF MAKING THE SAME The present disclosure provides methods for producing N-(fluorosulfonyl)azoles, sulfonyldiazoles, or related derivatives thereof; and the related products including N- (fluorosulfonyl)azoles, sulfonyldiazoles, and related derivatives the...
WO/2021/001825A1	METHIONINE METABOLIC PATHWAY INHIBITORS The present invention provides novel inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides...
WO/2021/000736A1	SUBSTITUTED BENZOYL-PYRAZOLE COMPOUND, AND APPLICATION THEREOF IN AGRICULTURE A substituted benzoyl-pyrazole compound, and an application thereof in agriculture; specifically, compounds represented by formula (I) and a preparation method therefor; a composition and preparation containing the compounds, and use the...

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