Heterocyclic Compounds

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Document	Document Title
WO/2024/067819A1	PIPERIDINE-CONTAINING POLYCYCLIC DERIVATIVE MODULATOR, PREPARATION METHOD THEREFOR, AND USE THEREOF A piperidine-containing polycyclic derivative modulator, a preparation method therefor, and use thereof. In particular, the present invention relates to a compound represented by general formula (II-a), a preparation method therefor, a p...
WO/2024/067463A1	BENZO[7]ANNULENE DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND MEDICAL USES THEREOF Provided are a compound of formula (I) or a pharmaceutically acceptable salt, ester, optical isomer, tautomer, stereoisomer, polymorph, solvate, N-oxide, isotope-labeled compound, metabolite, chelate, complex, inclusion compound or prodr...
WO/2024/046361A1	AZEPINE FUSED RING COMPOUND AS RIPK1 INHIBITOR AND USE THEREOF The present disclosure provides a compound of formula (I), a pharmaceutical composition thereof, and a use thereof in treating and/or preventing diseases or conditions related to the activity of RIPK1 kinase.
WO/2023/199091A1	HETEROCYCLIC COMPOUND The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. [Solving Means] A compound represented by the formula (I) is useful as an agent for the prophylaxis or treatment of narcolepsy.
WO/2023/160579A1	DIPEPTIDYL PEPTIDASE 1 INHIBITOR POLYMORPH, PREPARATION METHOD AND USE THEREFOR Disclosed in the present invention are a polymorph of a compound as shown in formula I, and a preparation method and use therefor. The polymorph of the present invention comprises a crystal form B, a crystal form C, and a crystal form D....
WO/2023/160541A1	PREPARATION METHOD OF NITROGEN-CONTAINING HETEROCYCLIC COMPOUND Disclosed is a preparation method of a nitrogen-containing heterocyclic compound represented by formula (I). The method comprises: carrying out a coupling reaction on a compound 1A and a compound 2a, and sequentially carrying out deprote...
WO/2023/160542A1	SALT AND CRYSTAL FORM OF DIPEPTIDYL PEPTIDASE INHIBITOR COMPOUND Disclosed are a crystal of the compound (S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydro benzo[d]oxazole-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-c arboxamide salt or a salt thereof, a preparation method therefor, and the u...
WO/2023/143386A1	AROMATIC RING-FUSED HETEROCYCLIC RING COMPOUND AS POTASSIUM CHANNEL REGULATOR, AND PREPARATION THEREFOR AND USE THEREOF The present invention relates to an aromatic ring-fused heterocyclic ring compound as a potassium channel regulator, and the preparation therefor and the use thereof. Specifically, the compound of the present invention has a structure as...
WO/2023/143389A1	FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND MEDICAL APPLICATION THEREOF The present disclosure relates to a fused heterocyclic compound, a preparation method therefor, and a medical application thereof. Specifically, the present disclosure relates to a fused heterocyclic compound represented by general formu...
WO/2023/093398A1	SYNTHESIS METHOD OF OXAZEPINE DERIVATIVE Disclosed is a synthesis method of an oxazepine derivative. Dibenzo[b,f][1,4] oxazepine and a derivative thereof, and β-keto acid and a derivative thereof are used as raw materials, and under the condition of no photooxidation reduction...
WO/2023/076615A1	CERTAIN N-(1-CYANO-2-PHENYLETHYL)-1,4-OXAZEPANE-2-CARBOXAMIDES FOR TREATING CHRONIC RHINOSINUSITIS The present disclosure relates to methods for treating chronic rhinosinusitis with a composition comprising an effective amount of a N-(1-cyano-2-phenylethyl)-1,4-oxazepane-2-carboxamide DPP1 inhibitor compound of Formula (I) or a pharma...
WO/2023/051681A1	FOUR-MEMBERED FUSED RING COMPOUND AND PREPARATION METHOD AND USE THEREOF The present invention relates to a four-membered fused ring compound, a preparation method and use thereof, and specifically relates to a four-membered fused ring compound, a preparation method, a pharmaceutical composition containing a ...
WO/2023/016528A1	CLASS OF BENZOMORPHOLINE COMPOUNDS, AND PREPARATION METHOD THEREFOR AND USE THEREOF Disclosed are a class of benzomorpholine compounds, and a preparation method therefor and the use thereof. Specifically disclosed are a compound as represented by formula (I) and a pharmaceutically acceptable salt thereof. The compound h...
WO/2023/287793A1	THERAPEUTIC COMPOUNDS AND METHODS The invention provides a compound of formula (I): or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 have any of the values described in the specification, as well as compositions comprising a compound...
WO/2023/285787A1	SULFUR COMPOUNDS AND PROCESSES AND INTERMEDIATES USEFUL IN THE PREPARATION THEREOF A process for preparing a compound of formula I, or a salt thereof, as defined herein. Also, compounds of formula I and intermediate compounds useful in the preparation of a compound of formula I.
WO/2023/285788A1	SULFUR COMPOUNDS AND PROCESSES AND INTERMEDIATES USEFUL IN THE PREPARATION THEREOF A process for preparing a compound of formula (I), or a salt thereof, as defined herein. Also, compounds of formula I and intermediate compounds useful in the preparation of a compound of formula (I).
WO/2022/272060A1	EP2 ANTAGONIST COMPOUNDS Described herein are compounds that are EP2 antagonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of diseases or conditi...
WO/2022/237849A1	NMDA RECEPTOR ANTAGONIST AND USE THEREOF The present invention relates to a NMDA receptor antagonist and use thereof. The NMDA receptor antagonist of the present invention is a compound of formula I below, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a ...
WO/2022/232420A1	CERTAIN N-(1-CYANO-2-PHENYLETHYL)-1,4-OXAZEPANE-2-CARBOXAMIDES FOR TREATING CANCER The present disclosure relates to methods for treating cancer or cancer-induced bone pain, with a composition comprising an effective amount of a N-(1-cyano-2-phenylethyl)-1,4-oxazepane-2-carboxamide DPP1 inhibitor compound of Formula (I...
WO/2022/231928A1	RIPK1 INHIBITORS AND METHODS OF USE Described herein are compounds of Formula I I, or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related di...
WO/2022/231927A1	PHENYL AZEPINES AS RIPK1 INHIBITORS AND METHODS OF USE THEREOF Described herein are compounds of Formula I: (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related...
WO/2022/228413A1	COMPOUND FOR INHIBITING PROGRAMMED CELL DEATH AND PREPARATION METHOD THEREFOR Disclosed in the present invention are an RIPK1 inhibitor for inhibiting programmed cell death and a preparation method therefor. The RIPK1 inhibitor of the present invention is as represented by general formula I, wherein X, Y, Z, L, R1...
WO/2022/166721A1	FUSED RING DERIVATIVES CONTAINING 1,4-OXAZEPANE The present invention relates to a series of fused ring derivatives containing 1,4-oxazepane and a preparation method therefor, and in particular relates to a compound as shown in formula (II) and a pharmaceutically acceptable salt thereof.
WO/2022/159445A1	COMPOUNDS AND METHODS OF ACTIVATING LIPOPROTEIN LIPASE The present disclosure is generally directed to activators of lipoprotein lipase useful in the treatment of diseases and disorders modulated by said enzyme and having the Formula (I), or a pharmaceutically acceptable salt, isomer, solvat...
WO/2022/140516A1	CERTAIN (25)-IV-[(LS')~ I-C YAN0-2-PHENYLETHYL·]- 1,4-OXAZEPANE-2- CARBOXAMIDES FOR TREATING BEHCET'S DISEASE The present disclosure relates to methods for treating Behçet's Disease with compositions comprising an effective amount of certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxam ide compounds of Formula (I), including pha...
WO/2022/108984A1	PROCESSES AND INTERMEDIATES FOR PREPARING MACROCYCLIC MCL1 INHIBITORS The invention relates in particular to methods and intermediates for the synthesis of Compound 1 that inhibits MCL1 and is useful in the treatment of cancers.
WO/2022/051317A1	DIOL DESYMMETRIZATION BY NUCLEOPHILIC AROMATIC SUBSTITUTION Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound Y that can be used to prepare them where the variable R1 is as defined herein. In particular, provided herein are processes for synthesizi...
WO/2022/042591A1	NITRILE DERIVATIVE THAT ACTS AS INHIBITOR OF DIPEPTIDYL PEPTIDASE 1 AND USE THEREOF Provided is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The c...
WO/2022/022612A1	NOVEL GLUTAMINE ANALOGS The invention relates to novel glutamine analogs shown as the formula I, a composition containing the glutamine analogs and the use thereof.
WO/2022/026500A1	SUBSTITUTED HALOALKYL SULFONANILIDE HERBICIDES Disclosed are compounds of Formula 1, all stereoisomers, N-oxides and salts thereof, wherein G is CONR5R6 or selected from and R1 through R18 Rf and G are as defined in the Disclosure. Also disclosed are compositions containing the compo...
WO/2022/022664A1	INDOLO HEPTAMYL OXIME ANALOG CRYSTAL AS PARP INHIBITOR AND METHOD FOR PREPARING SAME Disclosed is a type of indolo heptamyl oxime analog crystal as a PARP inhibitor and a method for preparing the same, specifically relating to a crystal of a compound as represented by formula (I) and a method for preparing the same.
WO/2021/259331A1	EIGHT-MEMBERED N-CONTAINING HETEROCYCLIC COMPOUND Disclosed is an eight-membered N-containing heterocyclic compound as shown in formula (P) and the use thereof in the preparation of a KRAS G12C mutant protein inhibitor.
WO/2021/236449A1	P38ALPHA MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS Disclosed herein are p38a mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38a mitogen-activated protein kinase inhibitors.
WO/2021/225835A1	SYNTHESIS OF VINYLIC ALCOHOL INTERMEDIATES Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound (E), wherein R1 is described herein. Compound (E) can be useful in ...
WO/2021/226168A1	RING CLOSING SYNTHESIS OF MACROCYCLIC MCL-1 INHIBITOR INTERMEDIATES Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizi...
WO/2021/225823A1	SYNTHESIS OF VINYLIC PROTECTED ALCOHOL INTERMEDIATES Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound D, wherein OPG and R1 are described herein. Compound D can be usefu...
WO/2021/222858A1	ANTAGONISTS OF GPR39 PROTEIN Novel compounds that act as antagonists to human GPR39 protein are disclosed. Pharmaceutical compositions and methods of use for antagonists to human GPR39 protein are disclosed. In particular, methods of using the antagonists in the tre...
WO/2021/208945A1	BENZONITRIC HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF Disclosed are a benzonitric heterocyclic compound, a preparation method therefor and the use thereof. Provided in the present invention is a benzonitric heterocyclic compound represented by formula I, or a pharmaceutically acceptable sal...
WO/2021/188620A1	PEPTIDOMIMETIC N5-METHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE DERIVATIVES, TRIAZASPIRO[4.14]NONADECANE DERIVATIVES AND SIMILAR COMPOUNDS AS INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sa...
WO/2021/170913A1	TRICYCLIC MODULATORS OF PP2A Chemical modulators of PP2A, comprising tricyclic sulfonimidamides are disclosed. The compounds are useful in preventing or treating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic o...
WO/2021/130451A1	CHEMICAL COMPOUNDS TARGETING THE EYE AND USE THEREOF IN THE TREATMENT OF EYE DISEASES The invention relates to chemical compounds C that are derivatives of norbixine and have tropism for the eye, and are intended to be used in the treatment of eye diseases in mammals, in particular in the context of altering the retinal p...
WO/2021/108198A1	INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASE Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
WO/2021/108254A1	PROCESSES AND INTERMEDIATES FOR PREPARING MCL1 INHIBITORS The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
WO/2021/062199A1	INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASE Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
WO/2021/050672A1	KINASE INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES Described herein are compounds that are kinase inhibitors. The disclosed compounds have improved properties that lead to specific targeting of kinases without inhibiting the activity of related enzymes including, making them useful for t...
WO/2021/050555A1	COMPOSITIONS AND USES THEREOF The present invention relates to compositions and methods for the treatment of disorders that lead to accumulation of oxalate, such as primary hyperoxaluria 1.
WO/2020/245213A1	HECT E3 LIGASE INHIBITORS AND USES THEREOF The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising ...
WO/2020/145250A1	15-PGDH INHIBITOR [Problem] To provide a compound having a 15-PGDH inhibitory effect. [Solution] A compound represented by general formula (1) or a pharmacologically acceptable salt thereof.
WO/2020/127390A1	METHODS FOR PREPARING COMPOUNDS A method is provided for preparing a compound d having the formula (D) The method comprises carrying out the following reaction (c) → (d), where the reaction is carried out at a temperature of at least 100 °C and in the presence of a ...
WO/2020/127385A1	METHODS FOR PREPARING COMPOUNDS A method is provided for preparing a compound d having the formula: Formula (I). The method comprises carrying out the following reaction: Formula (i), (ii), (d) where: step (i) is carried out in the presence of a metal catalyst and a hy...

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