Pyrimidine or pyridine derivatives and their medical uses

Abstract

A focal adhesion kinase (FAK) inhibitor compound, a composition containing such a compound, and a use of such a compound. The compound has good therapeutic effects on cancer, pulmonary arterial hypertension, and pathological angiogenesis, and has good prospects for clinical application.

Description

[Technical Field]

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS This application claims priority from a Chinese patent application with application number 202111522765.8 filed on December 13, 2021, the entire contents of which are incorporated herein by reference. The present invention relates to the field of medicine, specifically to pyrimidine or pyridine derivatives and their pharmaceutical uses, especially to their use in preparing drugs for treating or preventing cancer, pulmonary arterial hypertension, and pathological angiogenesis. [Background technology]

[0002] Focal adhesion kinase (FAK), also known as PTK2 (protein tyrosine kinase 2), is a non-receptor tyrosine kinase located at the intersection of multiple signaling pathways and can be activated by integrins, growth factor receptors, G protein-coupled receptors, and cytokines. In addition to its role in signal transduction as a cytoplasmic kinase, related studies have shown that FAK also plays an important role in the cell nucleus. FAK promotes p53 degradation through ubiquitination, thereby causing cancer cell growth and proliferation. Tang et al. reported that FAK further regulates the expression of GATA4 and IL-33, thereby reducing inflammatory responses and immune evasion. In the tumor microenvironment, nuclear FAK can regulate the formation of new blood vessels and affect the tumor's blood supply.

[0003] FAK is widely expressed in the body and plays an important role in cell growth, proliferation, migration, and adhesion, and is involved in embryonic development and the occurrence and development of diseases (such as cancer and cardiovascular disease). Overexpression of FAK is observed in many types of cancer, including colon cancer, breast cancer, prostate cancer, thyroid cancer, neuroblastoma, ovarian cancer, cervical cancer, brain cancer, head and neck cancer, liver cancer, esophageal cancer, pancreatic cancer, lung cancer, gastric cancer, and acute leukemia. High expression of FAK often indicates a poor prognosis. For example, studies have shown that the GTPase RHOAY 42CMutations are among the most common gain-of-function mutations in diffuse gastric cancer, and RHOAY 42C Mice carrying the mutation were found to be sensitive to FAK inhibitors, suggesting that inhibiting FAK activity may be a new strategy for treating diffuse gastric cancer.

[0004] FAK functions by binding transmembrane integrin receptors to the extracellular matrix (ECM), recruiting FAK to sites of integrin accumulation. FAK does not directly interact with integrins but binds to the cell membrane and other adhesion proteins via its carboxyl-terminal FAT domain. Once recruited, the inactive FAK activates its catalytic activity through autophosphorylation at Y397. After phosphorylation, FAK functions as a molecular scaffold to recruit Src family kinases, which then phosphorylate FAK at Y576 and Y577, further enhancing FAK activity and simultaneously promoting the recruitment of downstream SH2 domain-containing proteins such as Grb2 and PI3K. When Grb2 binds to FAK, it further recruits SOS to form a complex, thereby further activating the downstream Ras-MAPK signaling pathway.

[0005] Based on the above, FAK and its signaling pathway-related targets are considered potential targets for anti-cancer drug development. FAK inhibitors are not commercially available, and only a few drugs, such as defactinib, IN10018, and GSK-2256098, have entered clinical trials. Therefore, it is crucial to develop new compounds that modulate the FAK signaling pathway.

[0006] YAP (Yes-associated protein), a transcriptional coactivator of the Hippo pathway downstream of FAK, is located on human chromosome 11q22 and promotes gene expression by enhancing the activity of transcription factors. External signals activate MST1 / 2, which then bind to the regulatory protein SAV1, phosphorylating LATS1 / 2 and MOB, which then directly phosphorylates YAP / TAZ. The phosphorylated YAP / TAZ then terminates in the cytoplasm and inhibits transcription. When this signaling pathway is blocked or inactivated, unphosphorylated YAP / TAZ translocates from the cytoplasm to the nucleus, where it binds to transcription factors such as TEADs, Smads, Runx1 / 2, p63 / p73, and ErbB4, promoting gene transcription.

[0007] The Hippo-YAP pathway, a recently discovered signaling pathway that regulates organ volume and maintains the balance between cell proliferation and apoptosis, is closely associated with uncontrolled tumor cell proliferation. Its primary function in mammals is to negatively regulate tumor progression by inhibiting the activity of the transcriptional regulators YAP and TAZ. Therefore, the Hippo pathway is considered a tumor-suppressing pathway. Specifically, core members of the pathway include the serine / threonine kinases MST1, MST2, LATS1, and LATS2, the scaffolding proteins SAV1 (which binds to MST1 and MST2) and MOB1 (which binds to LATS1 and LATS2), the transcriptional coactivator YAP, and the TEA-binding domain-containing transcription factor TEAD. Briefly, when the Hippo pathway is activated, LATS1 / 2 is activated by phosphorylation of MST1 / 2 kinases, which then phosphorylates YAP. The phosphorylated YAP is then inactivated and exported to the nucleus, while the cytoplasmic YAP is degraded by the proteasome.

[0008] Studies have confirmed that the Hippo pathway is involved in the progression of various tumors, including lung cancer, colon cancer, ovarian cancer, prostate cancer, and liver cancer. However, genetic mutations in the Hippo pathway do not occur frequently in human tumors. Based on this, dysregulation of the Hippo pathway in human tumors is caused not only by mutations in key proteins in the Hippo pathway itself, but also by crosstalk between the Hippo pathway and other abnormally expressed proteins or signaling pathways in tumor cells. Furthermore, the role of the Hippo signaling pathway in tumors is closely related to the nuclear translocation of YAP / TAZ. Recently, YAP has been found to be highly expressed in various tumors, which is associated with high pathological grade, advanced TNM stage, lymph node metastasis, etc., and exhibits nuclear localization.

[0009] On this basis, inhibiting active YAP may block relevant signaling pathways and potentially inhibit tumors, providing guidance for drug development. Summary of the Invention

[0010] The present invention provides compounds that can be used as focal adhesion kinase (FAK) inhibitors, compositions containing such compounds, and uses of such compounds. In addition to having a good inhibitory effect on FAK, the compounds of the present invention unexpectedly have a good inhibitory effect on YAP. The compounds provided by the present invention have good therapeutic effects and good prospects for clinical application in cancer, pulmonary arterial hypertension, and pathological angiogenesis.

[0011] In one aspect, the present invention provides a compound, wherein the compound is a compound of Formula I or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula I: JPEG2025500871000001.jpg33126 where, M is a covalent warhead; A is an aryl or heteroaryl group; L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, or a nitrogen protecting group, where R L1a wherein the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups are each optionally substituted with one or more substituents independently selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; L 2 is a bond, an alkyl group, a heteroalkyl group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where L 2 wherein the alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl group is optionally substituted by one or more substituents each independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, alkyl, alkenyl, alkynyl, heteroalkyl, or haloheteroalkyl groups; L 3 is a bond, an aryl group, or a heteroaryl group, where L 3 wherein the aryl or heteroaryl groups are each optionally substituted by one or more substituents independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, or haloheteroalkyl groups; L 4is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 wherein the carbon or hetero chain is optionally substituted with one or more substituents each independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, alkenyl, alkynyl, alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, hydroxyalkoxy, aminoalkoxy, alkylamino, and nitrogen protecting groups; L 5 is -NR L5a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 5 The alkyl and heteroalkyl groups for each R are optionally substituted with one or more substituents each independently selected from hydrogen (e.g., deuterium), amino, hydroxyl, oxo, cyano, halogen, alkenyl, or alkynyl; L5a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; L 6 is -NR L6a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 6 The alkyl and heteroalkyl groups in L6a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y 5 are each independently CH or N, Each R 1are independently hydrogen, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 1 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, alkoxy group, haloalkoxy group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, heteroarylalkyl group are optionally substituted by one or more substituents each independently selected from hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, Each R 2 are independently hydrogen, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 2 If there are two adjacent R 2together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 2 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, alkoxy group, haloalkoxy group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group or heteroarylalkyl group is optionally substituted by one or more substituents each independently selected from hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, Each R 3 are independently hydrogen, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 3wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, alkoxy group, haloalkoxy group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group or heteroarylalkyl group is optionally substituted by one or more substituents each independently selected from hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, and m and p are each independently 0, 1, 2, 3, or 4.

[0012] In some embodiments, the compounds provided by the present invention are compounds of Formula I, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula I: JPEG2025500871000002.jpg33126where, M is a covalent warhead, A is an aryl or heteroaryl group; L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, or a nitrogen protecting group, where R L1a wherein the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups are each optionally substituted with one or more substituents independently selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; L 2is a bond, an alkyl group, a heteroalkyl group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where L 2 wherein the alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl group is optionally substituted by one or more substituents each independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, alkyl, alkenyl, alkynyl, heteroalkyl, or haloheteroalkyl groups; L 3 is a bond, an aryl group, or a heteroaryl group, where L 3 wherein the aryl or heteroaryl groups are each optionally substituted by one or more substituents independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, or haloheteroalkyl groups; L 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 wherein the carbon or hetero chain is optionally substituted with one or more substituents each independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, alkenyl, alkynyl, alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, hydroxyalkoxy, aminoalkoxy, alkylamino, and nitrogen protecting groups; L 5 is -NR L5a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 5 The alkyl and heteroalkyl groups in L5aare independently hydrogen (e.g., deuterium), an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; L 6 is -NR L6a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 6 The alkyl and heteroalkyl groups for each R are optionally substituted with one or more substituents each independently selected from hydrogen (e.g., deuterium), amino, hydroxyl, oxo, cyano, halogen, alkenyl, or alkynyl; L6a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y 5 are each independently CH or N, Each R 1 are independently hydrogen, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 1wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, heteroarylalkyl group are optionally substituted by one or more substituents each independently selected from hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group; Each R 2 are independently hydrogen, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 2 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group or heteroarylalkyl group is optionally substituted by one or more substituents each independently selected from hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, Each R 3are independently hydrogen, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 3 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group or heteroarylalkyl group is optionally substituted by one or more substituents each independently selected from hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, and m and p are each independently 0, 1, 2, 3, or 4.

[0013] In some embodiments, X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y 5 At least one of X is a N atom. 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y5 At least two of the are N atoms.

[0014] In some embodiments, X 1 , X 2 , X 3 , X 4 At least one of X is a N atom. 1 , X 2 , X 3 , X 4 At least two of X are N atoms. 1 , X 2 , X 3 , X 4 At least one of X is a N atom. 1 , X 2 , X 3 , X 4 At least two of the are N atoms.

[0015] In some embodiments, Y 1 , Y 2 , Y 3 , Y 4 and Y 5 At least one of Y is a N atom. 1 , Y 2 , Y 3 , Y 4 and Y 5 At least two of the are N atoms.

[0016] In some embodiments, M is JPEG2025500871000003.jpg34118 JPEG2025500871000004.jpg35133 JPEG2025500871000005.jpg36138 JPEG2025500871000006.jpg35132, where: L 7 is one bond, -O-, -S-, -NR L7a - or C1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7a S(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a S(=O)2-, where each R L7a are independently hydrogen, C 1-4 is an alkyl group or a nitrogen protecting group, and each R L7b are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b groups, combined with the atoms to which they are attached, form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, wherein each L 7 , R L7a , R L7b The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4substituted by one or more substituents selected from alkyl groups; L 8 is one bond or C 1-4 is an alkyl group, where L 8 wherein the alkyl group is optionally substituted with one or more substituents selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a , -CHN(R M1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M2are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a , -N(R M3a)2 or -SR M3a where each R M3a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Optionally, R M1 and R M3 , or R M2 and R M3 , or R M1 and R M2 are optionally joined to form a saturated or partially unsaturated carbocyclyl group or a saturated or partially unsaturated heterocyclyl group, wherein the saturated or partially unsaturated carbocyclyl group or the saturated or partially unsaturated heterocyclyl group are each optionally independently selected from hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; R M4 is a leaving group and R M5 is a halogen and Z is O, S or NR Z where R Z are hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and R Zwherein the alkyl group is optionally substituted with one or more substituents selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; q is 0, 1, 2, 3, 4, 5, or 6; and r is 1 or 2.

[0017] In some embodiments, M is JPEG2025500871000007.jpg3621, JPEG2025500871000008.jpg3614, JPEG2025500871000009.jpg2924 or JPEG2025500871000010.jpg2911, where: L 7 is one bond, -O-, -S-, -NR L7a - or C 1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7a S(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a S(=O)2-, where each R L7a are independently hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and each R L7b are independently hydrogen, halogen, C 1-4 Alkyl group, C2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each L 7 , R L7a , R L7b The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Z is O, S or NR Z where R Z is hydrogen, C 1-4 is an alkyl group or a nitrogen protecting group, and R Z wherein the alkyl group is optionally substituted with one or more substituents selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a , -CHN(R M1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, C 1-4Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a Groups are optionally joined to the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R M1 , R M1a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M2 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2aThe alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a , -N(R M3a )2 or -SR M3a where each R M3a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; In some embodiments, M is JPEG2025500871000011.jpg712, JPEG2025500871000012.jpg1112, JPEG2025500871000013.jpg1120, JPEG2025500871000014.jpg1523, JPEG2025500871000015.jpg207, JPEG2025500871000016.jpg1313, JPEG2025500871000017.jpg1413, JPEG2025500871000018.jpg1624, JPEG2025500871000019.jpg1728 or JPEG2025500871000020.jpg1619. In some embodiments, A is a 6- to 10-membered aryl group or a 5- to 10-membered heteroaryl group. In some embodiments, A is a 6- to 10-membered aryl group or a 5- to 10-membered azaaryl group. In some embodiments, A is a phenyl group or a 6-membered azaaryl group. In some embodiments, A is a phenyl group, an imidazolyl group, a pyrazolyl group, a triazolyl group, a tetrazolyl group, an oxazolyl group, a thiazolyl group, a furyl group, a thienyl group, a pyrrolyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, a pyridazinyl group, or JPEG2025500871000021.jpg1523, JPEG2025500871000022.jpg1623, JPEG2025500871000023.jpg1524, JPEG2025500871000024.jpg1523, JPEG2025500871000025.jpg1523, JPEG2025500871000026.jpg1523, JPEG2025500871000027.jpg1723, JPEG2025500871000028.jpg1324, JPEG2025500871000029.jpg1723, JPEG2025500871000030.jpg1523, JPEG2025500871000031.jpg1723, JPEG2025500871000032.jpg1324, JPEG2025500871000033.jpg1723, JPEG2025500871000034.jpg1723, JPEG2025500871000035.jpg1224, JPEG2025500871000036.jpg1226, JPEG2025500871000037.jpg1326 or JPEG2025500871000038.jpg1525, JPEG2025500871000039.jpg73 is A is L 6 One end is connected to

[0018] In some embodiments, A is a phenyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, or a pyridazinyl group. In some embodiments, A is a phenyl group or a pyrazinyl group.

[0019] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 Haloalkyl group, C 1-4 a haloheteroalkyl group or a nitrogen protecting group, where R L1aThe alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl group, heteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may each independently optionally be hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4The carbon or hetero chains for each of the groups may optionally each independently be hydrogen (e.g., deuterium), a hydroxyl group, an amino group, a cyano group, a halogen, an oxo, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Alkyl group, C 1-4 Haloalkyl group, C 1-4 Hydroxyalkyl group, C 1-4 Aminoalkyl group, C 1-4 Alkoxy group, C 1-4 Haloalkoxy group, C 1-4 Hydroxyalkoxy group, C 1-4 Aminoalkoxy group, C 1-4 It is substituted with one or more substituents selected from alkylamino groups, nitrogen protecting groups.

[0020] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)2NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, methyl, ethyl, vinyl, ethynyl, or trifluoromethyl; L 2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 3is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 4 is a carbon chain or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains in are optionally substituted with one or more substituents, each independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, and nitrogen protecting groups.

[0021] In some embodiments, L 1 is one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NH-, -NHC(=O)-, -S(=O)2NH- or -NHS(=O)2-, and L 2 is a bond, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where L 2 The saturated or partially unsaturated carbocyclyl group and the saturated or partially unsaturated heterocyclyl group in the formula (I) are each optionally substituted by one or more substituents independently selected from hydroxyl, amino, cyano, fluorine, chlorine, oxo, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy, and methylamino groups; and L 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3The aryl or heteroaryl groups in 4 is a carbon chain or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains in are optionally substituted with one or more substituents, each independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, and nitrogen protecting groups.

[0022] In some embodiments, L 1 is one bond, —C(═O)— or —C(═O)NH—, and L 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group, and L 3 is a bond, a phenyl group, or a pyridyl group, and L 4 are -NHCH2-, -CH2NH-, -OCH2-, -CH2O-, -SCH2-, -CH2S-, -NHCH2CH2-, -CH2NHCH2-, -CH2CH2NH-, -OCH2CH2-, -CH2OCH2-, -CH2CH2O-, -SCH2CH2-, -CH2SCH2-, -CH2CH2S-, -NHCH2CH2CH2-, -CH2NHCH2CH2-, -CH2CH2NHCH2-, -CH2CH2 CH2NH-, -OCH2CH2CH2-, -CH2OCH2CH2-, -CH2CH2OCH2-, -CH2CH2CH2O-, -SCH2CH2CH2-, -CH2SCH2CH2-, -CH2CH2SCH2-, -CH2CH2CH2S-, -CH2OCH2O-, -OCH2OCH2-, -NHCH2CH2O-, -CH2NHCH2O- or -NHCH2OCH2-, wherein L 4wherein the hydrogens of CH2 are each optionally replaced by a substituent independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, and methylamino; and L 4 wherein the hydrogen of NH is optionally replaced by a substituent independently selected from deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, and a nitrogen protecting group.

[0023] In some embodiments, L 1 is one bond, —C(═O)— or —C(═O)NH—, and L 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group, L 3 is a bond, a phenyl group, or a pyridyl group, and L 4 is -NHCH2-, -CH2NHCH2-, -NHC(=O)-, -CH2NHC(=O)-, -C(=O)NHCH2- or -NHCH(CH3)-.

[0024] In some embodiments, L 5 is -NR L5a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 heteroalkyl group, where L 5 The alkyl and heteroalkyl groups in the formula (I) are optionally each independently selected from hydrogen (e.g., deuterium), amino, hydroxyl, oxo, cyano, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, and each R L5aare independently hydrogen, deuterium, and C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 is a haloalkyl group or a nitrogen protecting group, and L 6 is -NR L6a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 heteroalkyl group, where L 6 The alkyl and heteroalkyl groups in the formula (I) are optionally each independently selected from hydrogen (e.g., deuterium), amino, hydroxyl, oxo, cyano, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, and each R L6a are independently hydrogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 It is a haloalkyl group or a nitrogen protecting group.

[0025] In some embodiments, L 5 is -NR L5a , -CR L5b R L5c -, -O-, -S-, -CR L5b R L5c NR L5a -, -NR L5a CR L5b R L5c -, -CR L5b R L5c O-, -OCR L5b R L5c -, -CR L5b R L5c S- or -SCR L5b R L5c -, where each R L5b and R L5care each independently hydrogen, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen atom, or C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L5a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 is a haloalkyl group or a nitrogen protecting group, and L 6 is -NR L6a , -CR L6b R L6c -, -O-, -S-, -CR L6b R L6c NR L6a -, -NR L6a CR L6b R L6c -, -CR L6b R L6c O-, -OCR L6b R L6c -, -CR L6b R L6c S- or -SCR L6b R L6c -, where each R L6b and R L6c are each independently hydrogen, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen atom, or C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L6a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 It is a haloalkyl group or a nitrogen protecting group.

[0026] In some embodiments, L 5 is -NH-, -O-, -S-, -NHCH2-, -OCH2-, -SCH2-, -CH2NH-, -CH2O- or -CH2S-, and L 6 is -NH-, -O-, -S-, -NHCH2-, -OCH2-, -SCH2-, -CH2NH-, -CH2O-, or -CH2S-. In some embodiments, L 5 is -NH-, and L 6 is —NH— or —NHCH2—.

[0027] In some embodiments, each R 1 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Alkoxy group, C 1-6 Haloalkoxy group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group in the above may each optionally independently be hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R 2 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl groups, C 1-6 Alkoxy group, C 1-6 Haloalkoxy group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group in the above may each optionally independently be hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups, and Each R 3 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl groups, C 1-6 Alkoxy group, C 1-6 Haloalkoxy group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group in the above may each optionally independently be hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0028] In some embodiments, each R 1 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl, or heteroaryl groups in 1-4 alkyl groups, and each R 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl, or heteroaryl groups in 1-4 alkyl group, and each R 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl, or heteroaryl groups in 1-4It is substituted by one or more substituents selected from alkyl groups.

[0029] In some embodiments, each R 1 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 a haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 a haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 3 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3The alkyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, and 3- to 6-membered saturated or partially unsaturated heterocyclyl group in the above-mentioned formula (I) are optionally each independently selected from hydrogen (e.g., deuterium), hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0030] In some embodiments, each R 1 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 a haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 a haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 3 are independently hydrogen, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl, heteroalkyl, haloalkyl, haloheteroalkyl, 3- to 6-membered saturated or partially unsaturated carbocyclyl, and 3- to 6-membered saturated or partially unsaturated heterocyclyl groups in the above are optionally substituted with one or more substituents independently selected from hydrogen (e.g., deuterium), hydroxyl, amino, cyano, halogen, oxo, methyl, ethyl, and isopropyl.

[0031] In some embodiments, each R 1are independently hydrogen, amino group, hydroxyl group, cyano group, fluorine, chlorine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC(=O )-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2-, C H3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3)2 CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)-, CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(CH 3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH2 CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and each R 2are independently hydrogen, amino group, hydroxyl group, cyano group, fluorine, chlorine, bromine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC( =O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2-, CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3) 2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)-, CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(CH 3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH2 CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and each R 3are independently hydrogen, amino group, hydroxyl group, cyano group, fluorine, chlorine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC(=O )-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2-, C H3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3)2 CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)-, CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(CH 3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH2 CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3) S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and two adjacent R, 3 If there are two adjacent R 3 together with the atoms to which they are attached, and optionally JPEG2025500871000040.jpg1918, JPEG2025500871000041.jpg1919, JPEG2025500871000042.jpg1921, JPEG2025500871000043.jpg1921, JPEG2025500871000044.jpg2019, JPEG2025500871000045.jpg2019, JPEG2025500871000046.jpg2023, JPEG2025500871000047.jpg2023, JPEG2025500871000048.jpg1921 or Form JPEG2025500871000049.jpg1919. In some embodiments, the saturated or partially unsaturated carbocyclyl group is selected from formulas ii-1 to ii-6, wherein when formulas ii-1 to ii-6 are linked to the rest of the molecule by one bond, formulas ii-1 to ii-6 are monovalent, and when formulas ii-1 to ii-6 are linked to the rest of the molecule by two bonds, formulas ii-1 to ii-6 are divalent; and the saturated or partially unsaturated carbocyclyl groups represented by formulas ii-1 to ii-6 are optionally substituted with one or more substituents, each independently defined by the corresponding group of the present invention as defined above; JPEG2025500871000050.jpg1410, JPEG2025500871000051.jpg1810, JPEG2025500871000052.jpg2111, JPEG2025500871000053.jpg2214, JPEG2025500871000054.jpg2221 or JPEG2025500871000055.jpg2314, the saturated or partially unsaturated heterocyclyl group is selected from formulae iii-1 to iii-16, where formulae iii-1 to iii-16 are monovalent when they are linked to the rest of the molecule by one bond, and are divalent when they are linked to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl group represented by formulae iii-1 to iii-16 is optionally substituted by one or more substituents, each independently defined by the corresponding group of the present invention as defined above; JPEG2025500871000056.jpg1710, JPEG2025500871000057.jpg1711, JPEG2025500871000058.jpg1610, JPEG2025500871000059.jpg1813, JPEG2025500871000060.jpg2313, JPEG2025500871000061.jpg2013, JPEG2025500871000062.jpg2414, JPEG2025500871000063.jpg2714, JPEG2025500871000064.jpg2421, JPEG2025500871000065.jpg2321, JPEG2025500871000066.jpg2321, JPEG2025500871000067.jpg2221, JPEG2025500871000068.jpg2221, JPEG2025500871000069.jpg2521, JPEG2025500871000070.jpg2016 or JPEG2025500871000071.jpg2118, wherein each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5.

[0032] The phrase "substituted by a substituent defined by the corresponding group of the present invention" refers to a substituent substituted with a group related to the "saturated or partially unsaturated carbocyclyl group" and "saturated or partially unsaturated heterocyclyl group" described above.

[0033] In some embodiments, the saturated or partially unsaturated carbocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by one bond, and the following groups are divalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated carbocyclyl groups represented below are optionally substituted with one or more substituents, each independently defined by the corresponding group of the invention described above: JPEG2025500871000072.jpg13141, The saturated or partially unsaturated heterocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated heterocyclyl group is linked to the rest of the molecule by one bond, and the following groups are divalent when the saturated or partially unsaturated heterocyclyl group is linked to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl groups represented below are optionally substituted with one or more substituents, each independently defined by the corresponding groups of the present invention described above.

[0034] JPEG2025500871000073.jpg21141 JPEG2025500871000074.jpg21137 JPEG2025500871000075.jpg15122 JPEG2025500871000076.jpg18125 "Substituted by a substituent defined by the corresponding group described above in the present invention" refers to a substituent substituted with a group related to the "saturated or partially unsaturated carbocyclyl group" and "saturated or partially unsaturated heterocyclyl group" described above.

[0035] In some embodiments, the compound of the present invention is a compound represented by any one of Formulas II-1 to II-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof; Formula II-1: JPEG2025500871000077.jpg29113, Formula II-2: JPEG2025500871000078.jpg27113, Formula II-3: JPEG2025500871000079.jpg26109, Formula II-4: JPEG2025500871000080.jpg30113, Formula II-5: JPEG2025500871000081.jpg28114 or Formula II-6: JPEG2025500871000082.jpg28113, wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally contains hydrogen (e.g., deuterium), a hydroxyl group, an amino group, a cyano group, a halogen, an oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 and substituted by one or more substituents selected from haloheteroalkyl groups.

[0036] In some embodiments, the compound of the present invention is a compound of Formula III or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof, Formula III: JPEG2025500871000083.jpg24118 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and RL4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; and k and v are each independently 0, 1, or 2.

[0037] In some embodiments, the compound of the present invention is a compound represented by any one of formulas IV-1 to IV-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof; Formula IV-1: JPEG2025500871000084.jpg22113, Formula IV-2: JPEG2025500871000085.jpg21108, Formula IV-3: JPEG2025500871000086.jpg22107, Formula IV-4: JPEG2025500871000087.jpg22104, Formula IV-5: JPEG2025500871000088.jpg20104 or Formula IV-6: JPEG2025500871000089.jpg23114, wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally contains hydrogen (e.g., deuterium), a hydroxyl group, an amino group, a cyano group, a halogen, an oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4ais hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; and k and v are each independently 0, 1, or 2.

[0038] In some embodiments, the compound of the present invention is a compound represented by any one of Formulas V-1 to V-7, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof.

[0039] Formula V-1: JPEG2025500871000090.jpg29114, Formula V-2: JPEG2025500871000091.jpg30119, Formula V-3: JPEG2025500871000092.jpg30119, Formula V-4: JPEG2025500871000093.jpg30117, Formula V-5: JPEG2025500871000094.jpg30118, Formula V-6: JPEG2025500871000095.jpg28110 or Formula V-7: JPEG2025500871000096.jpg30115 In some embodiments, the compound of the present invention is a compound represented by any one of Formulas VI-1 to VI-5 or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof.

[0040] Formula VI-1: JPEG2025500871000097.jpg26110, Equation VI-2: JPEG2025500871000098.jpg27113, Equation VI-3: JPEG2025500871000099.jpg26109, Equation VI-4: JPEG2025500871000100.jpg25104 or Equation VI-5: In some embodiments, the compound of the present invention is a compound represented by any one of Formulas VII-1 to VII-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof, Formula VII-1: JPEG2025500871000102.jpg21110, Formula VII-2: JPEG2025500871000103.jpg19104, Formula VII-3: JPEG2025500871000104.jpg21109, Formula VII-4: JPEG2025500871000105.jpg21106, Formula VII-5: JPEG2025500871000106.jpg1899 or Formula VII-6: JPEG2025500871000107.jpg22108, wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally contains hydrogen (e.g., deuterium), a hydroxyl group, an amino group, a cyano group, a halogen, an oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2.

[0041] In some embodiments, the compound of the present invention is a compound represented by any one of Formulas VIII-1 to VIII-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystalline form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharmaceutically acceptable salt, or prodrug thereof; Formula VIII-1: JPEG2025500871000108.jpg23102, Formula VIII-2: JPEG2025500871000109.jpg23103, Formula VIII-3: JPEG2025500871000110.jpg22103, Formula VIII-4: JPEG2025500871000111.jpg24103, Formula VIII-5: JPEG2025500871000112.jpg2095 or Formula VIII-6: JPEG2025500871000113.jpg23104, wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4eare each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2.

[0042] The present invention further relates to methods for the preparation, isolation and purification of the compounds according to the invention.

[0043] The present invention further relates to a method for preparing the compounds according to the present invention, the method comprising one or more of the following steps (1) to (3): (1) reacting a compound of formula a1 with a compound of formula a2 to produce a compound of formula a3; (2) reacting a compound of formula a3 with a compound of formula a4 to produce a compound of formula a5; (3) reacting a compound of formula a5 with a compound of formula a6 to produce a compound of formula a7; JPEG2025500871000114.jpg31141 JPEG2025500871000115.jpg56114, Alternatively, the preparation method may include one or more of the following steps (4) to (9): (4) reacting a compound of formula b1 with a compound of formula b2 to produce a compound of formula b3; (5) converting the compound of formula b3 to a compound of formula b4; (6) converting the compound of formula b4 to a compound of formula b5; (7) reacting the compound of formula b5 with a compound of formula b3 to form a compound of formula b6; (8) converting the compound of formula b6 to a compound of formula b7; (9) converting the compound of formula b7 to a compound of formula b8; JPEG2025500871000116.jpg54141 JPEG2025500871000117.jpg89138 where Hal is halogen, Cy represents a variety of ring system structures (including, but not limited to, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group), Pg represents a protecting group, A, R 1 , R 2 , R 3 , R 4 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , L 1 , L 2 , L 5 , L 6 , M, n, m, p are as defined in the present invention.

[0044] In another aspect, the present invention relates to the preparation of intermediates of compounds of formula I, II-1 to II-6, III, IV-1 to IV-6, V-1 to V-6), VI-1 to VI-5, VII-1 to VII-6, VIII-1 to VIII-6.

[0045] In another aspect, the present invention provides a pharmaceutical composition, said pharmaceutical composition comprising a compound according to the present invention and a pharmaceutically acceptable excipient thereof.

[0046] In another aspect, the present invention provides the use of a compound or pharmaceutical composition according to the present invention in the preparation of a medicament for the prevention or treatment of a FAK-related disease.

[0047] In another aspect, the present invention provides the use of a compound or pharmaceutical composition according to the present invention in the prevention or treatment of a FAK-related disease.

[0048] In another aspect, the present invention provides a method for preventing or treating a FAK-related disease using a compound or pharmaceutical composition according to the present invention.

[0049] In another aspect, the present invention provides a method for preventing or treating a FAK-related disease by administering an effective amount of a compound or pharmaceutical composition according to the present invention.

[0050] In some embodiments, the FAK-associated disease comprises cancer, pulmonary arterial hypertension, and pathological angiogenesis.

[0051] In some embodiments, the FAK-related disease comprises lung cancer, bone cancer, pancreatic cancer, skin cancer, head and neck cancer, cutaneous or intraocular melanoma, uterine cancer, ovarian cancer, rectal cancer, cancer of the anal region, stomach cancer, colon cancer, breast cancer, uterine cancer, fallopian tube cancer, endometrial cancer, cervical cancer, trichilemmal carcinoma, vulvar cancer, Hodgkin's disease, esophageal cancer, small intestine cancer, endocrine system cancer, thyroid cancer, parathyroid cancer, adrenal gland cancer, soft tissue sarcoma, urethral cancer, penile cancer, prostate cancer, chronic or acute leukemia, lymphocytic lymphoma, bladder cancer, kidney or ureter cancer, renal cell carcinoma, renal pelvis cancer, central nervous system (CNS) tumors, primary CNS lymphoma, spinal axis cancer, brain stem glioma, pituitary adenoma, or a combination of one or more of the foregoing cancers.

[0052] In another aspect, the present invention provides a method for modulating the Hippo-YAP signaling pathway, comprising administering a compound or pharmaceutical composition according to the present invention.

[0053] In another aspect, the present invention provides the use of a compound or pharmaceutical composition according to the present invention in the preparation of an inhibitor of the Hippo-YAP signaling pathway.

[0054] In another aspect, the present invention provides the use of a compound or pharmaceutical composition according to the present invention in the preparation of a medicament for preventing or treating a YAP-associated disease.

[0055] In another aspect, the present invention provides the use of a compound or pharmaceutical composition according to the present invention in the prevention or treatment of a YAP-associated disease.

[0056] In another aspect, the present invention provides a method for preventing or treating a YAP-associated disease, comprising administering an effective amount of a compound or pharmaceutical composition according to the present invention.

[0057] In another aspect, the present invention provides a method for preventing or treating a YAP-associated disease, comprising administering an effective amount of a compound or pharmaceutical composition according to the present invention.

[0058] In some embodiments, the YAP-associated disease is selected from cancer, including one or more of skin cancer, bone cancer, glioma, breast cancer, adrenal gland cancer, bladder cancer, esophageal cancer, head and neck cancer, liver cancer, parathyroid cancer, penile cancer, small intestine cancer, thyroid cancer, urethral cancer, cervical cancer, endometrial cancer, fallopian tube cancer, renal pelvis cancer, vaginal cancer, vulvar cancer, chronic or acute leukemia, colon cancer, melanoma, hematological malignancies, Hodgkin's lymphoma, lung cancer, lymphocytic lymphoma, central nervous system tumors (CNS), ovarian cancer, pancreatic cancer, pituitary adenoma, prostate cancer, soft tissue sarcoma, gastric cancer, and uterine cancer.

[0059] In another aspect, the present invention provides a method for inhibiting FAK kinase and / or YAP protein activity in a cell or a subject, said method comprising contacting said cell or administering to said subject a compound or pharmaceutical composition described in the present invention.

[0060] In some embodiments, the cell is a mammalian cell. In some embodiments, the subject is a mammal, preferably a human. Detailed Description Specific embodiments of the present invention will now be described in detail, examples of which are illustrated by the accompanying structural or chemical formulae. The present invention is intended to cover all alternatives, modifications, and equivalent technical solutions, all of which are included within the scope of the present invention as defined by the claims. Those skilled in the art will recognize that many methods and materials similar or equivalent to those described herein can be used to practice the present invention. The present invention is in no way limited to the methods and materials described herein. In the event that one or more of the incorporated literature, patents, and similar materials differs or contradicts with this application (including, but not limited to, defined terms, term applications, described techniques, etc.), this application shall control.

[0061] It will further be appreciated that certain features of the invention may, for clarity, be described in the context of multiple separate embodiments, but may also be provided in combination in a single embodiment. Conversely, various features of the invention, which are, for brevity, described in the context of a single embodiment, may also be provided singly or in any suitable subcombination.

[0062] Definitions and General Terms Unless otherwise specified, all scientific and technical terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. All patents and published publications relating to this invention are incorporated herein by reference in their entirety.

[0063] Unless otherwise specified or clearly contradicted by context, the articles "a," "an," "one," and "said," as used herein, are intended to include "at least one" or "one or more." Thus, as used herein, these articles refer to one or more (i.e., at least one) object. For example, "a component" refers to one or more components, i.e., it is contemplated that more than one component may be employed or used in the embodiment of the embodiment.

[0064] As used herein, "one or more" means one or more than one. In some embodiments, "one or more" means 1 to 5, in some embodiments, "one or more" means 1 to 4, in some embodiments, "one or more" means 1 to 3, in some embodiments, "one or more" means 1 to 2, in some embodiments, "one or more" means 1, and in other embodiments, "one or more" means 1, 2, 3, 4, or 5.

[0065] As used herein, the term "subject" refers to an animal. Typically, the animal is a mammal. The subject also refers to, for example, primates (e.g., humans, male or female), cows, sheep, goats, horses, dogs, cats, rabbits, rats, mice, fish, birds, etc. In some embodiments, the subject is a primate. In other embodiments, the subject is a human.

[0066] As used herein, the term "patient" refers to a human (including adults and children) or other animal. In some embodiments, a "patient" is a human.

[0067] The term "comprises" as used herein is open-ended, i.e. includes the subject matter specified in the present invention, but does not exclude other aspects of the subject matter.

[0068] Unless otherwise specified, the descriptive forms "each independently", "each independently", "independently" and "each independently" used in the present invention are interchangeable and should all be understood in a broad sense, which may mean that specific options represented by the same symbol in different groups do not affect each other, or that specific options represented by the same symbol in the same group do not affect each other.

[0069] Unless otherwise specified, the descriptive forms "optionally" and "optionally" used herein mean that the following action may or may not occur. For example, "optionally substituted," "optionally substituted," and "optionally substituted..." mean that a group may or may not be substituted. Unless otherwise stated, one optional substituent may be substituted at any substitutable position of the group.

[0070] Unless otherwise specified, when "each...independently," "each...independently," "...independently," or "each...each independently" can be combined with "optionally" and "optionally," the combined words have the same meaning regardless of order, for example, "optionally, each independently" and "independently optionally" mean that specific options represented by the same symbol in different groups do not affect each other, and the subsequent action may or may not occur.

[0071] Used alone as a prefix, "C m-n The term "group" refers to any group having m to n carbon atoms, C m refers to any group having m carbon atoms. For example, C 1-20 Alkyl group refers to an alkyl group containing 1 to 20 carbon atoms, C 1-8 An alkoxy group refers to an alkoxy group containing 1 to 8 carbon atoms, C 2-6 An alkenyl group refers to an alkenyl group containing 2 to 6 carbon atoms, and a C6 haloalkyl group refers to a haloalkyl group containing 6 carbon atoms.

[0072] The term "m-membered" group used alone as a prefix refers to a ring having m to n ring atoms, for example, a "3- to 6-membered saturated or partially unsaturated carbocyclyl group" means that the carbocyclyl group has 3 to 6 ring atoms, a "3- to 6-membered saturated or partially unsaturated heterocyclyl group" means that the heterocyclyl group has 3 to 6 ring atoms, a "6- to 10-membered aryl group" means that the aryl group has 6 to 10 ring atoms, and a "5- to 10-membered heteroaryl group" means that the heteroaryl group has 5 to 10 ring atoms.

[0073] The term "replace" as used in the present invention means that one or more carbon units in a given structure are replaced by a specific substituent. When two or more carbon units in a given structural formula can be replaced by one or more substituents selected from a specific group, the substituents may be the same or different at various positions. Here, the substituents are selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7a S(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a can be, but is not limited to, S(=O)-, where R L7a are hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and R L7b are hydrogen, deuterium, halogens, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R L7b groups are optionally joined to form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where L 7 , R L7a , R L7b The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may optionally each independently be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; The term "substituted" or "substituted" as used herein means that one or more hydrogen atoms in a given structure are replaced by a specific substituent. When one or more positions in a given structural formula can be substituted by one or more substituents selected from a specific group, the substituents may be the same or different at various positions. Here, the substituents may be deuterium, fluorine, chlorine, bromine, iodine, amino, hydroxyl, carboxyl, amide, aminoacyl, sulfonyl, cyano, oxo (=O), nitro, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 2-6 Alkenyloxy group, C 1-6 Alkoxy group, C 1-6 Alkylamino group, bis(C 1-6 alkyl)amino group, C 1-6 Haloalkyl groups, 3- to 12-membered heterocyclyl groups, 3- to 10-membered carbocyclyl groups, C 6-10 Aryl group, C 1-9 Heteroaryl groups, 3- to 12-membered heterocyclylC 1-6 Alkyl group, C 6-10 Aryl C 1-6 Alkyl group, C 1-9 Heteroaryl C 1-6Alkyl group, C 1-6 Hydroxyalkyl group, C 1-6 Alkoxy C 1-6 The alkyl group may be, but is not limited to, an alkyl group, and the like.

[0074] The term "a group associated with a Markush variable" used in the description of some groups is intended to distinguish the same group in different Markush variables, e.g., "R L1a The alkyl group with respect to R L1a For simplicity, the prefix "C" used in the alkyl group is m-n ", i.e. C m-n The alkyl group is represented by "R L1a Regarding C m-n alkyl group” to “R L1a "Alkyl group related to" and "R L1a The alkyl group with respect to R L1a Defined in C m-n Refers to an alkyl group.

[0075] As used herein, the term "stereoisomer" refers to compounds that have the same chemical structure but differ in the way atoms or groups are arranged in space. Stereoisomers include enantiomers, diastereomers, conformational isomers (rotational isomers), geometric isomers (cis / trans isomers), atropisomers, etc. Unless otherwise stated, all stereoisomers or mixtures of stereoisomers of the structural formulas described herein are within the scope of the present invention. As used herein, the term "enantiomer" refers to stereoisomers that are real and mirror images that are not superimposable with each other. "Diastereomer" refers to stereoisomers whose molecules have two or more chiral centers and are non-mirror-image related to each other.

[0076] As used herein, the term "geometric isomer" includes cis-trans isomers, isotactic and syndiotactic polymers, rotational isomers caused by steric hindrance, and the like.

[0077] The stereochemical definitions and rules used in the present invention generally follow those in S.P. Parker, Ed., McGraw-Hill Dictionary of Chemical Terms (1984) McGraw-Hill Book Company, New York, and Eliel, E. and Wilen, S., "Stereochemistry of Organic Compounds", John Wiley & Sons, Inc., New York, 1994.

[0078] Any resulting mixture of stereoisomers can be separated into pure or substantially pure geometric isomers, enantiomers, or diastereomers based on the differences in the physicochemical properties of the components, for example, by chromatography and / or fractional crystallization.

[0079] The term "tautomer" or "tautomeric form" as used herein refers to structural isomers with different energies that are interconvertible via a low energy barrier. When tautomerism is possible (e.g., in solution), a chemical balance of tautomers can be achieved. For example, proton tautomers (called prototropic tautomers) include interconversions via proton migration, such as keto-enol isomerization and imine-enamine isomerization. Valence tautomers include interconversions via rearrangement of some of the bonding electrons. A specific example of keto-enol tautomerism is the tautomerism of pentane-2,4-dione and 4-hydroxypent-3-en-2-one. Another example of tautomerism is phenol-ketone tautomerism. A specific example of phenol-ketone tautomerism is that of pyridin-4-ol and pyridin-4(1H)-one tautomers. Unless otherwise stated, all tautomeric forms of the compounds of the present invention are within the scope of the present invention.

[0080] The term "nitrogen oxide" as used herein refers to a compound that can oxidize one or more nitrogen atoms to form an N-oxide when the compound contains several amine functional groups. Specific examples of N-oxides are the N-oxides of tertiary amines or the N-oxides of nitrogen atoms in nitrogen-containing heterocycles. The corresponding amines can be N-oxides formed with oxidizing agents such as hydrogen peroxide or peracids (e.g., peroxycarboxylic acids) (see Advanced Organic Chemistry, Wiley Interscience, 4th Edition, Jerry March, pages 1977). In particular, N-oxides can be prepared by the method of L.W. Deady (Syn. Comm. 1977, 7, 509-514), which involves reacting an amine compound with m-chloroperoxybenzoic acid (MCPBA) in an inert solvent such as dichloromethane.

[0081] The term "solvate" as used herein refers to a complex formed between one or more solvent molecules and a compound of the present invention. Solvents that form solvates include, but are not limited to, water, isopropanol, ethanol, methanol, dimethyl sulfoxide, ethyl acetate, acetic acid, and aminoethanol. The term "hydrate" refers to a complex formed with water as the solvent molecule.

[0082] The term "metabolite" as used herein refers to a product obtained by metabolic action of a specific compound or its salt in the body. Metabolic products of a compound can be identified by techniques well known in the art, and their activity can be characterized by such tests described in this invention. Such products can be obtained by administering a compound through oxidation, reduction, hydrolysis, amidation, deamidation, esterification, delipidation, enzymatic cleavage, etc. Correspondingly, the present invention includes metabolic products of a compound, including metabolic products produced by contacting a compound of the present invention with a mammal for a sufficient period of time.

[0083] The term "ester" includes compounds or fragments that contain a carbon or heteroatom bound to an oxygen atom that is bonded to a carbon on a carbonyl group. The term "ester" includes alkoxycarbonyl groups, such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, pentoxycarbonyl, and the like.

[0084] It is understood that the compounds of the present invention can be described as different tautomers. If a compound has tautomeric forms, it is intended that all tautomeric forms are included within the scope of the present invention, and it is also understood that the naming of the compound does not exclude any tautomeric form. It is understood that certain tautomers may have a higher level of activity than other tautomers.

[0085] The term "crystalline form" refers to a crystalline structure in which a compound (or its salt or solvate) can crystallize in different crystal packing forms, all of which have the same elemental composition. Different crystalline forms generally have different X-ray diffraction patterns, infrared spectra, melting points, densities, hardness, crystal shape, optical and electrical properties, stability, and solubility. Depending on the recrystallization solvent, crystallization rate, storage temperature, and other factors, one crystalline form may predominate. Crystalline forms of a compound can be prepared by crystallization under various conditions.

[0086] The term "isotopic labeling" refers to the process of substituting an isotope for a corresponding element in a particular compound molecule. "Isotopes" are identical elements with different masses but the same chemical properties. The process of substituting a specific atom in a molecule with its isotope is called isotopic labeling.

[0087] As used herein, the term "pharmaceutically acceptable" refers to such compounds, ingredients, compositions and / or dosage forms which are, within the scope of reasonable medical judgment, suitable for contact with patient tissues effective for their intended use without undue toxicity, irritation, allergic response, or other problem and complication commensurate with a reasonable benefit / risk ratio.

[0088] The term "pharmaceutically acceptable salts" as used herein refers to organic and inorganic salts of the compounds of the present invention. Pharmaceutically acceptable salts are well known in the art and are described, for example, in S. M. Berge et al., "Describe pharmaceutically acceptable salts in detail in J. Pharmaceutical Sciences, 1977, 66:1-19." Pharmaceutically acceptable non-toxic acid-formed salts include, but are not limited to, inorganic acid salts such as hydrochloride, hydrobromide, phosphate, sulfate, perchlorate, and organic acid salts such as acetate, oxalate, maleate, tartrate, citrate, succinate, malonate, or salts thereof obtained by methods described in the literature, such as ion exchange methods. Other pharmaceutically acceptable salts include adipate, alginate, ascorbate, aspartate, benzenesulfonate, benzoate, bisulfate, borate, butyrate, camphorate, camphorsulfonate, cyclopentylpropionate, digluconate, dodecyl sulfate, ethanesulfonate, formate, fumarate, glucoheptonate, glycerophosphate, gluconate, hemisulfate, enanthate, hexanoate, hydroiodide, 2-hydrogen phosphate, and the like. Salts obtained with suitable bases include alkali metal, alkaline earth metal, ammonium salts, e.g., where R is H, C, D, E, E, F, H, G, H, H, H, H, G ... 1-4 Alkyl group, C 6-10Salts of N+(R)4, such as aryl groups, and cyclic ammonium salts, such as piperidine, morpholine, and piperazine, are included. The present invention also contemplates quaternary ammonium salts formed with any compound containing an N group. Water- or oil-soluble or dispersible products can be obtained by quaternization. Alkali metals or alkaline earth metals include sodium, lithium, potassium, calcium, magnesium, and the like. Pharmaceutically acceptable salts include halides, hydroxides, carboxylates, sulfates, phosphates, nitrates, C 1-8 Suitable non-toxic ammonium salts, such as sulfonates and aromatic sulfonates, include quaternary ammonium salts, and amine ions that resist counterion formation.

[0089] The term "prodrug" as used herein refers to a compound that converts in the body to a compound of Formula I, II-1 to II-6, III, IV-1 to IV-6, V-1 to V-6, VI-1 to VI-5, VII-1 to VII-6, or VIII-1 to VIII-6. Such conversion is subject to hydrolysis of the prodrug in the blood or enzymatic conversion to the parent structure in the blood or tissue. The prodrug compounds of the present invention may be esters, and among the esters that can be used as prodrugs in existing inventions are phenyl esters, aliphatic (C 1-24) esters, acyloxymethyl esters, carbonates, carbamates, and amino acid esters. For example, if a compound of the present invention contains a hydroxyl group, it can be acylated to obtain a prodrug form of the compound. Other prodrug forms include phosphate esters; for example, these phosphate ester compounds can be obtained by phosphorylating the hydroxyl group of the parent group. For a complete discussion of prodrugs, see the following references: T. Higuchi and V. Stella, Prodrugs as Novel Delivery Systems, Vol. 14 of the ACS Symposium Series, Edward B. Roche, ed., Bioreversible Carriers in Drug Design, American Pharmaceutical Association and Pergamon Press, 1987; J. Rautio et al., Prodrugs: Design and Clinical Applications, Nature Review Drug Discovery, 2008, 7, 255-270; and S.J. Hecker et al., Prodrugs of Phosphates and Phosphonates, Journal of Medicinal Chemistry, 2008, 51, 2328-2345.

[0090] As used herein, the term "treating" any disease or condition refers, in some embodiments, to ameliorating the disease or condition (i.e., alleviating, arresting, or alleviating the onset of the disease or at least one of its clinical symptoms). In other embodiments, "treatment" refers to alleviating or improving at least one physical parameter, including physical parameters that may not be noticeable to the patient. In other embodiments, "treatment" refers to modulating the disease or condition physically (e.g., stabilizing significant symptoms) or physiologically (e.g., stabilizing physical parameters), or both. In other embodiments, "treatment" refers to preventing or delaying the onset, development, or worsening of the disease or condition.

[0091] In various parts of this specification, substituents of the compounds disclosed in the present invention are disclosed according to radical types or ranges. In particular, the present invention includes all independent subcombinations of each member of these radical types and ranges. For example, "C 1-6 The term "alkyl group" specifically refers to methyl, ethyl, C3 alkyl groups, C4 alkyl groups, C5 alkyl groups, and C6 alkyl groups, each of which is disclosed independently.

[0092] In each section of the present invention, linking substituents are described. When the structure explicitly requires a linking group, the Markush variable listed for that group should be understood to refer to the linking group. For example, when the structure requires a linking group and the Markush group definition for that variable lists an "alkyl group" or an "aryl group," it should be understood that the "alkyl group" or "aryl group" represents a linked alkylene or arylene group, respectively.

[0093] The term "covalent warhead" refers to a group that interacts with a specific target protein to form a covalent bond.

[0094] JPEG2025500871000118.jpg41142 JPEG2025500871000119.jpg35137 JPEG2025500871000120.jpg36138 Including, but not limited to, JPEG2025500871000121.jpg35132, where: L 7 is one bond, -O-, -S-, -NR L7a - or C 1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a-, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7a S(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a S(=O)2-, where each R L7a are independently hydrogen, C 1-4 is an alkyl group or a nitrogen protecting group, and each R L7b are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b groups, combined with the atoms to which they are attached, form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each L 7 , R L7a , R L7b The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; L 8 is one bond or C 1-4 is an alkyl group, where L 8wherein the alkyl group is optionally substituted with one or more substituents selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a , -CHN(R M1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M2 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a , -N(R M3a )2 or -SR M3a where each R M3a are independently hydrogen, C 1-4Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group in the above may optionally each independently be hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Optionally, R M1 and R M3 , or R M2 and R M3 , or R M1 and R M2 are optionally joined to form a saturated or partially unsaturated carbocyclyl group or a saturated or partially unsaturated heterocyclyl group, wherein the saturated or partially unsaturated carbocyclyl group or the saturated or partially unsaturated heterocyclyl group are each optionally independently selected from hydrogen (e.g., deuterium), halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; R M4 is a leaving group and R M5 is a halogen and Z is O, S or NR Z where R Z is hydrogen, C 1-4 is an alkyl group or a nitrogen protecting group, and R Z wherein the alkyl group is optionally substituted with one or more substituents selected from hydrogen (e.g., deuterium), halogen, hydroxyl, amino, cyano, and oxo; q is 0, 1, 2, 3, 4, 5, or 6; and r is 1 or 2.

[0095] The term "alkyl" or "alkyl group" refers to a saturated straight or branched chain hydrocarbon group, wherein the alkyl group can be optionally substituted with one or more substituents described herein. In some embodiments, the alkyl group is a C 1-20 In some embodiments, the alkyl group is C 1-10 In another embodiment, the alkyl group is C 1-6 In another embodiment, the alkyl group is C 1-4 In another embodiment, the alkyl group is C 1-3 In some specific structures, when an alkyl group is explicitly depicted as a linking group, the alkyl group represents a linked alkylene group, for example, as shown in the structural formula (C 6-10 Aryl)-(C 1-6 C in alkyl)- 1-6 The alkyl group is C 1-6It should be understood as an alkylene group. Examples of alkyl groups include methyl (Me, -CH), ethyl (Et, -CHCH), n-propyl (n-Pr, -CHCHCH), isopropyl (i-Pr, -CH(CH)), n-butyl (n-Bu, -CHCHCHCH), 2-methylpropyl or isobutyl (i-Bu, -CHCH(CH)), 1-methylpropyl or s-butyl (s-Bu, -CH(CH)CHCH). 3), t-butyl group (t-Bu, -C(CH3)3), n-pentyl group (-CH2CH2CH2CH2CH3), 2-pentyl group (-CH(CH3)CH2CH2CH3), 3-pentyl group (-CH(CH2CH3)2), 2-methyl-2-butyl group (-C(CH3)2CH2CH3), 3-methyl-2-butyl group (-CH(CH3)CH(CH3)2), 3-methyl-1-butyl group (-CH2CH2CH(CH3)2), 2-methyl -1-butyl group (-CH2CH(CH3)CH2CH3), n-hexyl group (-CH2CH2CH2CH2CH2CH2CH3), 2-hexyl group (-CH(CH3)CH2CH2CH2CH2CH3), 3-hexyl group (-CH(CH2CH3)(CH2CH2CH3)), 2-methyl-2-pentyl group (-C(CH3)2CH2CH2CH3), 3-methyl-2-pentyl group (-CH(CH3)CH(CH3)CH2CH3), 4-methyl- These include, but are not limited to, 2-pentyl (-CH(CH3)CH2CH(CH3)2), 3-methyl-3-pentyl (-C(CH3)(CH2CH3)2), 2-methyl-3-pentyl (-CH(CH2CH3)CH(CH3)2), 2,3-dimethyl-2-butyl (-C(CH3)2CH(CH3)2), 3,3-dimethyl-2-butyl (-CH(CH3)C(CH3)3), n-heptyl, n-octyl, and the like.

[0096] The term "heteroalkyl group" refers to a group obtained by inserting one or more heteroatoms into an alkyl group, wherein the alkyl group and heteroatoms have the meanings described herein. The heteroalkyl group can be optionally substituted with one or more substituents described herein. A heteroalkyl group can be bonded to the remainder of the molecule through a carbon atom or a heteroatom. In some embodiments, a heteroalkyl group is a C 1-20 In some embodiments, the heteroalkyl group is C 1-10 In another embodiment, the heteroalkyl group is C 1-6 In another embodiment, the heteroalkyl group is C 1-4 In another embodiment, the heteroalkyl group is C 1-3It is a heteroalkyl group. Examples of heteroalkyl groups include methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethoxy group, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC(=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2-, CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3)2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)-, CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(CH3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-, CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-Examples include, but are not limited to, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)-, or (CH3)2CH(CH3CH2)P(=O)-. Where a heteroalkyl group is a linking group and the Markush group defines a "heteroalkyl group," a "heteroalkyl group" refers to the linked heteroalkylene groups. Examples of heteroalkylene groups include -NHCH2-, -CH2NH-, -OCH2-, -CH2O-, -SCH2-, -CH2S-, -NHCH2CH2-, -CH2NHCH2-, -CH2CH2NH-, -OCH2CH2-, -CH2OCH2-, -CH2CH2O-, -SCH2CH2-, -CH2SCH2-, -CH2CH2S-, -NHCH2CH2CH2-, -CH2NHCH2CH2-, -CH2CH2NHCH2-, -CH Examples include, but are not limited to, 2CH2CH2NH-, -OCH2CH2CH2-, -CH2OCH2CH2-, -CH2CH2OCH2-, -CH2CH2CH2O-, -SCH2CH2CH2-, -CH2SCH2CH2-, -CH2CH2SCH2-, -CH2CH2CH2S-, -CH2OCH2O-, -OCH2OCH2-, -NHCH2CH2O-, -CH2NHCH2O-, or -NHCH2OCH2-.

[0097] The term "alkenyl group" refers to a straight or branched chain hydrocarbon group, which has at least one site of unsaturation, i.e., one carbon-carbon sp2 double bond, and which may be optionally substituted with one or more substituents described herein, including "cis" and "tans" positions, or "E" and "Z" positions, and which can be bonded to the rest of the molecule through an atom that forms a double bond or through an atom that does not form a double bond. In some embodiments, an alkenyl group is a C 2-12 alkenyl group, and in one embodiment the alkenyl group is C 2-8In another embodiment, the alkenyl group is C 2-6 In another embodiment, the alkenyl group is C 2-4 It is an alkenyl group. Examples of alkenyl groups include, but are not limited to, vinyl (-CH=CH2), allyl (-CH2CH=CH2), etc. When an alkenyl group is a linking group and the Markush group defines an "alkenyl group," the "alkenyl group" represents a linked alkenylene group. Examples of alkenyl groups represented as linked alkenylene groups include, but are not limited to, -CH=CH-, -CH2CH=CH-, and -CH2CH=CHCH2-.

[0098] The term "alkynyl group" refers to a straight or branched chain hydrocarbon group, which has at least one site of unsaturation, i.e., one carbon-carbon sp triple bond, and wherein said alkynyl group can be optionally substituted with one or more substituents described herein, and wherein the alkynyl group can be attached to the rest of the molecule through an atom that forms a triple bond or through an atom that does not form a triple bond. In some embodiments, an alkynyl group is a C 2-12 is an alkynyl group, and in one embodiment, the alkynyl group is C 2-8 In another embodiment, the alkynyl group is C 2-6 In another embodiment, the alkynyl group is C 2-4 It is an alkynyl group. Examples of alkynyl groups include, but are not limited to, ethynyl (-C≡CH), propargyl (-CHC≡CH), 1-propynyl (-C≡C-CH), and the like. When an alkynyl group is the linking group and the Markush group defines the "alkynyl group," the "alkynyl group" represents a linked alkynylene group. Examples of alkynyl groups represented as linked alkynylene groups include, but are not limited to, -C≡C-, -CHC≡C-, -CHC≡CCH-, and the like.

[0099] The term "alkoxy group" refers to an alkyl group attached to the remainder of the molecule via an oxygen atom, wherein alkyl group has the meaning described herein. The alkoxy group can be optionally substituted with one or more substituents described herein. Unless otherwise specified in detail, in some embodiments, the alkoxy group is selected from the group consisting of C 1-20 In some embodiments, the alkoxy group is C 1-10 In another embodiment, the alkoxy group is C 1-6 In another embodiment, the alkoxy group is C 1-4 In another embodiment, the alkoxy group is C 1-3 When an alkoxy group is the linking group and the Markush group defines an "alkoxy group," the "alkoxy group" refers to the linked alkyleneoxy group. Examples of alkoxy groups include methoxy (MeO, -OCH3), ethoxy (EtO, -OCH2CH3), 1-propoxy (n-PrO, -OCH2CH2CH3), 2-propoxy (i-PrO, -OCH(CH3)2), 1-butoxy (n-BuO, -OCH2CH2CH2CH3), 2-methyl-l-propoxy (i-BuO, -OCH2CH(CH3)2), 2-butoxy (s-BuO, -OCH(CH3)CH2CH3), 2-methyl-2-propoxy (t-BuO , t-butoxy group, -OC(CH3)3), 1-pentyloxy group (n-pentyloxy group, -OCH2CH2CH2CH2CH3), 2-pentyloxy group (-OCH(CH3)CH2CH2CH3), 3-pentyloxy group (-OCH(CH2CH3)2), 2-methyl-2-butoxy group (-OC(CH3)2CH2CH3), 3-methyl-2-butoxy group (-OCH(CH3)CH(CH3)2), 3-methyl-l-butoxy group (-OCH2CH2CH(CH3)2), 2-methyl-l-butoxy group (-OCH2CH(CH3)CH2CH3), and the like.

[0100] The term "alkylamino group" refers to an alkyl group attached to the remainder of the molecule via nitrogen, where alkyl group has the meaning described herein. The alkylamino group can be optionally substituted with one or more substituents described herein. In some embodiments, the alkylamino group is a C 1-20 In some embodiments, the alkylamino group is C 1-10 In another embodiment, the alkylamino group is C 1-6 In another embodiment, the alkylamino group is C 1-4 In another embodiment, the alkylamino group is C 1-3 An alkylamino group. When an alkylamino group is the linking group and the Markush group defines an "alkylamino group," the "alkylamino group" refers to the linked alkyleneamino group. Examples of alkylamino groups include, but are not limited to, methylamino, ethylamino, n-propylamino, and isopropylamino groups.

[0101] The term "haloalkyl group" refers to an alkyl group substituted with one or more halogen atoms, wherein the alkyl group has the meaning described herein. In some embodiments, the haloalkyl group is C 1-20 In some embodiments, the haloalkyl group is C 1-10 In another embodiment, the haloalkyl group is C 1-6 In another embodiment, the haloalkyl group is C 1-4 In another embodiment, the haloalkyl group is C 1-3It is a haloalkyl group. When a haloalkyl group is a linking group and the Markush group defines a "haloalkyl group," the "haloalkyl group" refers to the linked haloalkylene group. Examples of haloalkyl groups include, but are not limited to, monofluoromethyl, difluoromethyl, trifluoromethyl, 1-fluoroethyl, 2-fluoroethyl, 1,2-difluoroethyl, 1,1-difluoroethyl, 2,2-difluoroethyl, monochloromethyl, dichloromethyl, trichloromethyl, 2-chloroethyl, 1-chloroethyl, 1,2-dichloroethyl, 1,1-dichloroethyl, 2,2-dichloroethyl, 1,1-dibromoethyl, and the like.

[0102] The term "haloalkoxy group" refers to an alkoxy group substituted with one or more halogen atoms, wherein the alkoxy group has the meaning described herein. In some embodiments, the haloalkoxy group is C 1-20 In some embodiments, the haloalkoxy group is a C 1-10 In another embodiment, the haloalkoxy group is C 1-6 In another embodiment, the haloalkoxy group is C 1-4 In another embodiment, the haloalkoxy group is C 1-3 A haloalkoxy group. When a haloalkoxy group is the linking group and the Markush group defines a "haloalkoxy group," the "haloalkoxy group" refers to the linked haloalkyleneoxy group. Examples of haloalkoxy groups include, but are not limited to, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, 1-fluoroethoxy, 2-fluoroethoxy, 1,2-difluoroethoxy, 1,1-difluoroethoxy, 2,2-difluoroethoxy, monochloromethoxy, dichloromethoxy, trichloromethoxy, 2-chloroethoxy, 1,2-dichloroethoxy, 1,1-dichloroethoxy, 2,2-dichloroethoxy, 1,1-dibromoethoxy, and the like.

[0103] The term "haloheteroalkyl group" denotes a heteroalkyl group substituted with one or more halogen atoms, wherein the heteroalkyl group has the meaning described herein. In some embodiments, the haloheteroalkyl group is 1-20 In some embodiments, the haloheteroalkyl group is C 1-10 In another embodiment, the haloheteroalkyl group is C 1-6 In another embodiment, the haloheteroalkyl group is C 1-4 In another embodiment, the haloheteroalkyl group is C 1-3 When a haloheteroalkyl group is a linking group and the Markush group defines a "haloheteroalkyl group," the "haloheteroalkyl group" represents the linked haloheteroalkylene group.

[0104] The term "halogen" refers to fluorine (F), chlorine (Cl), bromine (Br), or iodine (I). The term "hydroxyl group" refers to "-OH". The term "amino group" refers to "-NH2". The term "cyano group" refers to "-CN" or "-C≡N". The term "hydrogen" refers to H, including 1H, 2H, and 3H. In some embodiments, hydrogen refers to 1H. In some embodiments, hydrogen refers to 2H (i.e., deuterium). The term "oxo" refers to "=O". The term "heteroatom" refers to N, O, S, or P. In some embodiments, heteroatom refers to N, O, or S. In some embodiments, heteroatom refers to N.

[0105] The terms "saturated or partially unsaturated carbocyclyl group" and "saturated or partially unsaturated carbocycle" are used interchangeably and refer to a non-aromatic saturated or partially unsaturated monocyclic or polycyclic ring system composed of carbon atoms as ring atoms. In some embodiments, the polycyclic ring system is bicyclic or tricyclic. Saturated or partially unsaturated carbocyclyl groups include saturated or partially unsaturated monocarbocyclyl groups, saturated or partially unsaturated spirocarbocyclyl groups, saturated or partially unsaturated fused carbocyclyl groups, and saturated or partially unsaturated bridged carbocyclyl groups. In some embodiments, the saturated or partially unsaturated carbocyclyl group refers to a 3- to 12-membered saturated or partially unsaturated carbocyclyl group; in other embodiments, the saturated or partially unsaturated carbocyclyl group refers to a 3- to 10-membered saturated or partially unsaturated carbocyclyl group; and in other embodiments, the saturated or partially unsaturated carbocyclyl group refers to a 3- to 7-membered saturated or partially unsaturated carbocyclyl group. The saturated or partially unsaturated carbocyclyl group can independently be optionally substituted with one or more substituents described herein. When the saturated or partially unsaturated carbocyclyl group is a linking group, the term "saturated or partially unsaturated carbocyclyl group" refers to a "saturated or partially unsaturated carbocyclylene group."

[0106] In some other embodiments, the saturated or partially unsaturated carbocyclyl group refers to a 3- to 6-membered saturated or partially unsaturated carbocyclyl group. In some other embodiments, the "saturated or partially unsaturated carbocyclyl group" is selected from formulae ii-1 to ii-6, and when formulae ii-1 to ii-6 are bonded to the rest of the molecule by one bond, formulae ii-1 to ii-6 are monovalent, and when formulae ii-1 to ii-6 are bonded to the rest of the molecule by two bonds, formulae ii-1 to ii-6 are divalent, and the saturated or partially unsaturated carbocyclyl groups represented by formulae ii-1 to ii-6 are each optionally and independently substituted with one or more substituents described in the present invention, JPEG2025500871000122.jpg1410, JPEG2025500871000123.jpg1810, JPEG2025500871000124.jpg2111, JPEG2025500871000125.jpg2214, JPEG2025500871000126.jpg2221 or JPEG2025500871000127.jpg2314 where each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5.

[0107] In some other embodiments, the saturated or partially unsaturated carbocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by one bond, and the following groups are divalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated carbocyclyl groups represented below are optionally substituted, each independently, with one or more substituents described herein: JPEG2025500871000128.jpg13141.

[0108] A "saturated or partially unsaturated monocarbocyclyl group" is a monocyclic system and is used interchangeably with "saturated or partially unsaturated monocarbocyclyl group." In some embodiments, the saturated or partially unsaturated monocarbocyclyl group is a 3- to 8-membered saturated or partially unsaturated monocarbocyclyl group, in some other embodiments, the saturated or partially unsaturated monocarbocyclyl group is a 3- to 7-membered saturated or partially unsaturated monocarbocyclyl group, in some other embodiments, the saturated or partially unsaturated monocarbocyclyl group is a 3- to 6-membered saturated or partially unsaturated monocarbocyclyl group, and in some other embodiments, the saturated or partially unsaturated monocarbocyclyl group is a 5- to 6-membered saturated or partially unsaturated monocarbocyclyl group. Examples of saturated or partially unsaturated monocarbocyclyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentadienyl, cyclohexenyl, etc. When the saturated or partially unsaturated monocarbocyclyl group is the linking group, the saturated or partially unsaturated monocarbocyclyl group represents the linked saturated or partially unsaturated monocarbocyclylene group. The saturated or partially unsaturated monocarbocyclyl groups can be independently and optionally substituted with one or more substituents described herein.

[0109] A "saturated or partially unsaturated spirocarbocyclyl group" is a polycyclic ring system, and is used interchangeably with "saturated or partially unsaturated spirocarbocycle," where the saturated or partially unsaturated non-aromatic ring system contains at least one such ring system and is formed by two carbocycles shared by a carbon atom. In some embodiments, the saturated or partially unsaturated spirocarbocyclyl group is a 7- to 12-membered saturated or partially unsaturated spirocarbocyclyl group, and in other embodiments, the saturated or partially unsaturated spirocarbocyclyl group is a 7- to 10-membered saturated or partially unsaturated spirocarbocyclyl group. Examples of saturated or partially unsaturated spirocarbocyclyl groups include, but are not limited to, spiro[4.4]nonanyl, spiro[3.4]octyl, spiro[4.5]decanyl, and the like. When the saturated or partially unsaturated spirocarbocyclyl group is the linking group, it represents the linked saturated or partially unsaturated spirocarbocyclylene group, which can independently be optionally substituted with one or more substituents described herein.

[0110] A "saturated or partially unsaturated fused carbocyclyl group" is a polycyclic ring system, and is used interchangeably with "saturated or partially unsaturated fused carbocyclic ring," where the non-aromatic saturated or partially unsaturated ring system contains at least one such ring system and two carbocyclic rings share two carbon atoms. In some embodiments, the saturated or partially unsaturated fused carbocyclyl group is a 6- to 12-membered saturated or partially unsaturated fused carbocyclyl group; in other embodiments, the saturated or partially unsaturated fused carbocyclyl group is a 6- to 10-membered saturated or partially unsaturated fused carbocyclyl group; and in other embodiments, the saturated or partially unsaturated fused carbocyclyl group is an 8- to 10-membered saturated or partially unsaturated fused carbocyclyl group. Examples of saturated or partially unsaturated fused carbocyclyl groups include, but are not limited to, bicyclo[3.1.0]hexyl, bicyclo[3.2.0]heptyl, bicyclo[3.3.0]octyl, bicyclo[4.3.0]nonyl, etc. When the saturated or partially unsaturated fused carbocyclyl group is a linking group, the saturated or partially unsaturated fused carbocyclyl group represents the linked saturated or partially unsaturated fused carbocyclylene group. The saturated or partially unsaturated fused carbocyclyl groups can be independently and optionally substituted with one or more substituents described herein.

[0111] A "saturated or partially unsaturated bridged carbocyclyl group" is a polycyclic ring system, and is used interchangeably with "saturated or partially unsaturated bridged carbocyclic ring," where the non-aromatic saturated or partially unsaturated ring system contains at least one such ring system and where two carbocyclic rings share three or more carbon atoms. In some embodiments, the saturated or partially unsaturated bridged carbocyclyl group is a 5- to 12-membered saturated or partially unsaturated bridged carbocyclyl group; in some other embodiments, the saturated or partially unsaturated bridged carbocyclyl group is a 5- to 10-membered saturated or partially unsaturated bridged carbocyclyl group; and in some other embodiments, the saturated or partially unsaturated bridged carbocyclyl group is a 5- to 8-membered saturated or partially unsaturated bridged carbocyclyl group. Examples of saturated or partially unsaturated bridged carbocyclyl groups include, but are not limited to, bicyclo[3.1.1]heptyl, bicyclo[3.2.1]octyl, bicyclo[2.2.2]octyl, etc. When the saturated or partially unsaturated bridged carbocyclyl group is the linking group, the saturated or partially unsaturated bridged carbocyclyl group represents the linked saturated or partially unsaturated bridged carbocyclylene group. The saturated or partially unsaturated bridged carbocyclyl groups can be independently and optionally substituted with one or more substituents described herein.

[0112] The terms "saturated or partially unsaturated heterocyclyl group" and "saturated or partially unsaturated heterocycle" are used interchangeably and refer to a non-aromatic saturated or partially unsaturated monocyclic or polycyclic ring system, the ring atoms of which contain at least one carbon atom and one or more heteroatoms, said heteroatoms having the meanings described herein. Unless otherwise specified, a saturated or partially unsaturated heterocyclyl group can be bonded to the remainder of the molecule through its carbon atom or through a heteroatom. In some embodiments, the polycyclic system is bicyclic or tricyclic. Saturated or partially unsaturated heterocyclyl groups include saturated or partially unsaturated monoheterocyclyl groups, saturated or partially unsaturated spiroheterocyclyl groups, saturated or partially unsaturated fused heterocyclyl groups, and saturated or partially unsaturated bridged heterocyclyl groups. In some embodiments, the saturated or partially unsaturated heterocyclyl group refers to a 3- to 12-membered saturated or partially unsaturated heterocyclyl group; in other embodiments, the saturated or partially unsaturated heterocyclyl group refers to a 3- to 10-membered saturated or partially unsaturated heterocyclyl group; in other embodiments, the saturated or partially unsaturated heterocyclyl group refers to a 3- to 7-membered saturated or partially unsaturated heterocyclyl group; and in other embodiments, the saturated or partially unsaturated heterocyclyl group refers to a 3- to 6-membered saturated or partially unsaturated heterocyclyl group. The saturated or partially unsaturated heterocyclyl groups can be independently and optionally substituted with one or more substituents described herein. When the saturated or partially unsaturated heterocyclyl group is a linking group, the term "saturated or partially unsaturated heterocyclyl group" is expressed as a "saturated or partially unsaturated heterocyclylene group."

[0113] In some other embodiments, the saturated or partially unsaturated heterocyclyl group is selected from Formulae iii-1 to iii-16, wherein Formulae iii-1 to iii-16 are monovalent when they are linked to the rest of the molecule by one bond, and wherein Formulae iii-1 to iii-16 are divalent when they are linked to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl group represented by Formulae iii-1 to iii-16 is optionally substituted with one or more substituents, each independently defined by the corresponding group of the present invention as defined above; JPEG2025500871000129.jpg1710, JPEG2025500871000130.jpg1711, JPEG2025500871000131.jpg1610, JPEG2025500871000132.jpg1813, JPEG2025500871000133.jpg2313, JPEG2025500871000134.jpg2013, JPEG2025500871000135.jpg2414, JPEG2025500871000136.jpg2614, JPEG2025500871000137.jpg2321, JPEG2025500871000138.jpg2321, JPEG2025500871000139.jpg2321, JPEG2025500871000140.jpg2321, JPEG2025500871000141.jpg2321, JPEG2025500871000142.jpg2521, JPEG2025500871000143.jpg2016 or JPEG2025500871000144.jpg2118, wherein each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5.

[0114] The phrase "substituted by a substituent defined by the corresponding group of the present invention" refers to a substituent substituted with a group related to the "saturated or partially unsaturated carbocyclyl group" and "saturated or partially unsaturated heterocyclyl group" described above.

[0115] In some other embodiments, the saturated or partially unsaturated heterocyclyl group is selected from the following groups, where the following group is monovalent when the saturated or partially unsaturated heterocyclyl group is connected to the rest of the molecule by one bond, and the following group is divalent when the saturated or partially unsaturated heterocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl group represented below is optionally substituted with one or more substituents, each independently defined by the corresponding group of the present invention described above.

[0116] JPEG2025500871000145.jpg21141 JPEG2025500871000146.jpg21137 JPEG2025500871000147.jpg15122 JPEG2025500871000148.jpg18125 A "saturated or partially unsaturated monoheterocyclyl group" is a monocyclic system and is used interchangeably with "saturated or partially unsaturated monoheterocycle." In some embodiments, the saturated or partially unsaturated monoheterocyclyl group is a 3- to 8-membered saturated or partially unsaturated monoheterocyclyl group, in some other embodiments, the saturated or partially unsaturated monoheterocyclyl group is a 3- to 7-membered saturated or partially unsaturated monoheterocyclyl group, in some other embodiments, the saturated or partially unsaturated monoheterocyclyl group is a 3- to 6-membered saturated or partially unsaturated monoheterocyclyl group, and in some other embodiments, the saturated or partially unsaturated monoheterocyclyl group is a 5- to 6-membered saturated or partially unsaturated monoheterocyclyl group. Examples of saturated or partially unsaturated monoheterocyclyl groups include, but are not limited to, oxiranyl, azetidinyl, oxetanyl, thietanyl, pyrrolidinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrazolinyl, pyrazolidinyl, imidazolinyl, imidazolidinyl, tetrahydrofuryl, dihydrofuryl, tetrahydrothienyl, dihydrothienyl, 1,3-dioxocyclopentyl, dithiocyclopentyl, tetrahydropyranyl, dihydropyranyl, 2H-pyranyl, 4H-pyranyl, tetrahydrothiapyranyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, dioxanyl, dithianyl, thioxanyl, homopiperazinyl, homopiperidinyl, 1,1-dioxo-1,3-thiomorpholine, and the like. Examples of heterocyclyl groups in which -CH-yl is replaced by -C(=O)- include, but are not limited to, 2-oxopyrrolidyl, oxo-1,3-thiazolidinyl, 2-piperidinonyl, and 3,5-dioxopiperidinyl. When a saturated or partially unsaturated monoheterocyclyl group is the linking group, the saturated or partially unsaturated monoheterocyclyl group represents the linked saturated or partially unsaturated monoheterocyclylene group. The saturated or partially unsaturated monoheterocyclyl group can be independently and optionally substituted with one or more substituents described herein.

[0117] A "saturated or partially unsaturated spiroheterocyclyl group" is a polycyclic ring system, and is used interchangeably with "saturated or partially unsaturated spiroheterocycle," where the saturated or partially unsaturated non-aromatic ring system contains at least one such ring system and is formed by two heterocycles sharing a heteroatom. In some embodiments, the saturated or partially unsaturated spiroheterocyclyl group is a 7- to 12-membered saturated or partially unsaturated spiroheterocyclyl group, and in some other embodiments, the saturated or partially unsaturated spiroheterocyclyl group is a 7- to 10-membered saturated or partially unsaturated spiroheterocyclyl group. Examples of saturated or partially unsaturated spiroheterocyclyl groups include, but are not limited to, 4,7-diazaspiro[2.5]octanyl, 2,8-diazaspiro[4.5]decanyl, 2,7-diazaspiro[4.5]decanyl, 2,7-diazaspiro[3.5]decanyl, 2,6-diazaspiro[3.3]heptanyl, 2,7-diazaspiro[4.4]nonanyl, 3-azaspiro[5.5]undecanyl, 2,7-diazaspiro[4.4]nonyl-1-one, etc. When the saturated or partially unsaturated spiroheterocyclyl group is a linking group, the saturated or partially unsaturated spiroheterocyclyl group represents the linked saturated or partially unsaturated spiroheterocyclylene groups. The saturated or partially unsaturated spiroheterocyclyl groups can be independently optionally substituted with one or more substituents described herein.

[0118] A "saturated or partially unsaturated fused heterocyclyl group" is a polycyclic ring system, and is used interchangeably with "saturated or partially unsaturated fused heterocycle," where the non-aromatic saturated or partially unsaturated ring system contains at least one such ring system, and where two heterocycles share two heteroatoms. In some embodiments, the saturated or partially unsaturated fused heterocyclyl group is a 6- to 12-membered saturated or partially unsaturated fused heterocyclyl group; in other embodiments, the saturated or partially unsaturated fused heterocyclyl group is a 6- to 10-membered saturated or partially unsaturated fused heterocyclyl group; and in other embodiments, the saturated or partially unsaturated fused heterocyclyl group is an 8- to 10-membered saturated or partially unsaturated fused heterocyclyl group. Examples of saturated or partially unsaturated fused heterocyclyl groups include, but are not limited to, octahydroimidazo[1,5-c]pyrimidine, and the like. When the saturated or partially unsaturated fused heterocyclyl group is the linking group, the saturated or partially unsaturated fused heterocyclyl group represents the linked saturated or partially unsaturated fused heterocyclylene group, which can independently be optionally substituted with one or more substituents described herein.

[0119] A "saturated or partially unsaturated bridged heterocyclyl group" is a polycyclic ring system, and is used interchangeably with "saturated or partially unsaturated bridged heterocycle," where the non-aromatic saturated or partially unsaturated ring system contains at least one such ring system and where two heterocycles share three or more heteroatoms. In some embodiments, the saturated or partially unsaturated bridged heterocyclyl group is a 5- to 12-membered saturated or partially unsaturated bridged heterocyclyl group; in some other embodiments, the saturated or partially unsaturated bridged heterocyclyl group is a 5- to 10-membered saturated or partially unsaturated bridged heterocyclyl group; and in some other embodiments, the saturated or partially unsaturated bridged heterocyclyl group is a 5- to 8-membered saturated or partially unsaturated bridged heterocyclyl group. Examples of saturated or partially unsaturated bridged heterocyclyl groups include, but are not limited to, 3,6-diazabicyclo[3.1.1]heptane, 3,8-diazabicyclo[3.2.1]octane, 2-azabicyclo[2.2.1]heptane, 6-azabicyclo[3.1.1]heptane, 3-azabicyclo[3.1.1]heptane, 8-azabicyclo[3.2.1]octane, 3-azabicyclo[3.2.1]octane, 2-diazabicyclo[2.2.2]octane, etc. When the saturated or partially unsaturated bridged heterocyclyl group is the linking group, the saturated or partially unsaturated bridged heterocyclyl group refers to the linked saturated or partially unsaturated bridged heterocyclylene groups. The saturated or partially unsaturated bridged heterocyclyl groups can be independently optionally substituted with one or more substituents described herein.

[0120] The terms "aryl group" and "aromatic ring" are used interchangeably and refer to aromatic monocyclic or polycyclic ring systems composed of carbon atoms as ring atoms. In some embodiments, polycyclic ring systems are bicyclic or tricyclic. In some embodiments, the aryl group is a 6- to 14-membered aryl group; in other embodiments, the aryl group is a 6- to 10-membered aryl group; and in other embodiments, the aryl group is a phenyl or naphthyl group. When the aryl group is a linking group, it refers to the linked arylene group. The aryl groups can be independently and optionally substituted with one or more substituents described herein.

[0121] The terms "heteroaryl group" and "heteroaryl ring" are used interchangeably and refer to an aromatic monocyclic or polycyclic ring system composed of at least one carbon atom and one or more heteroatoms as ring atoms, wherein the heteroatoms have the meanings described herein. In some embodiments, the polycyclic ring system is bicyclic or tricyclic. In some embodiments, the heteroaryl group is a 5- to 14-membered heteroaryl group; in other embodiments, the heteroaryl group is a 5- to 10-membered heteroaryl group; and in other embodiments, the heteroaryl group is a 5- to 6-membered heteroaryl group. In other embodiments, the heteroaryl group is a 5- to 10-membered azaaryl group; in other embodiments, the heteroaryl group is a 5- to 6-membered azaaryl group; and in other embodiments, the heteroaryl group is a 6-membered azaaryl group.Examples of heteroaryl groups include a 2-furyl group, a 3-furyl group, an N-imidazolyl group, a 2-imidazolyl group, a 4-imidazolyl group, a 5-imidazolyl group, a 3-isoxazolyl group, a 4-isoxazolyl group, a 5-isoxazolyl group, a 2-oxazolyl group, a 4-oxazolyl group, a 5-oxazolyl group, an N-pyrrolyl group, a 2-pyrrolyl group, a pyrazinyl group, a 3-pyrrolyl group, a 2-pyridyl group, a 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, 4-pyrimidinyl group, 5-pyrimidinyl group, pyridazinyl group (e.g., 3-pyridazinyl group), 2-thiazolyl group, 4-thiazolyl group, 5-thiazolyl group, tetrazolyl group (e.g., 5-tetrazolyl group), triazolyl group (e.g., 2-triazolyl group and 5-triazolyl group), 2-thienyl group, 3-thienyl group, pyrazolyl group (e.g., 2-pyrazolyl group), isothiazolyl group, 1,2,3-oxadiazolyl group, 1,2,5-oxadiazolyl group a aryl group, a 1,2,4-oxadiazolyl group, a 1,2,3-triazolyl group, a 1,2,3-thiodiazolyl group, a 1,3,4-thiodiazolyl group, a 1,2,5-thiodiazolyl group, a pyrazinyl group, a 1,3,5-triazinyl group, a benzimidazolyl group, a benzofuranyl group, a benzothienyl group, an indolyl group (e.g., a 2-indolyl group), a purinyl group, a quinolyl group (e.g., a 2-quinolyl group, a 3-quinolyl group, a 4-quinolyl group), an isoquinolyl group (e.g., Examples of aryl groups include, but are not limited to, 1-isoquinolyl, 3-isoquinolyl, and 4-isoquinolyl groups, imidazo[1,2-a]pyridyl, pyrazolo[1,5-a]pyridyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-b]pyridazinyl, [1,2,4]triazolo[4,3-b]pyridazinyl, [1,2,4]triazolo[1,5-a]pyrimidinyl, and [1,2,4]triazolo[1,5-a]pyridyl. When an aryl group is a linking group, the aryl group refers to the linked arylene group. The aryl groups can be independently and optionally substituted with one or more substituents described herein.

[0122] The term "carbon chain" refers to a saturated or unsaturated group that serves as a bond and is composed of carbon atoms. The carbon chain can be optionally substituted with one or more substituents described herein. In some embodiments, the carbon chain is saturated, and in other embodiments, the carbon chain contains one or more double or triple bonds. In some embodiments, the carbon chain has 2 to 6 atoms, in other embodiments, the carbon chain has 2 to 4 atoms, in other embodiments, the carbon chain has 2 to 3 atoms, in other embodiments, the carbon chain has 2 atoms, in other embodiments, the carbon chain has 3 atoms, and in other embodiments, the carbon chain has 4 atoms.

[0123] The term "heterochain" refers to a saturated or unsaturated group that serves as a linking group and is composed of carbon atoms and heteroatoms, and includes at least one heteroatom. The heterochain can be optionally substituted with one or more substituents described herein. In some embodiments, the heterochain is saturated, and in other embodiments, the heterochain includes one or more double or triple bonds. In some embodiments, the heterochain has 2 to 6 atoms, in other embodiments, the heterochain has 2 to 4 atoms, in other embodiments, the heterochain has 2 to 3 atoms, and in other embodiments, the heterochain has 2 atoms. In other embodiments, the heterochain has 3 atoms, and in other embodiments, the heterochain has 4 atoms.

[0124] The term "nitrogen protecting group" has the same meaning as "amino saturated group" and is used interchangeably with "amino saturated group." A nitrogen protecting group is a group that combines a substituent with an amino group to block or protect the functionality of the amino group in a compound. Suitable amino protecting groups include acetyl, trifluoroacetyl, t-butoxycarbonyl (BOC, Boc), benzyloxycarbonyl (CBZ, Cbz), and 9-fluorenemethyleneoxycarbonyl (Fmoc).

[0125] The term "leaving group" refers to an atom or functional group that separates from a larger molecule in a chemical reaction and is a term used in nucleophilic substitution and elimination reactions. In a nucleophilic substitution reaction, the reactant that is attacked by the nucleophile is called the substrate, and the atom or group of atoms that leaves the substrate molecule with a pair of electrons is called the leaving group. Common leaving groups include, but are not limited to, halogen atoms, ester groups, sulfonate ester groups, nitro groups, azide groups, or hydroxyl groups.

[0126] The term "carbon unit" refers to a CH2 or a substituted CH2.

[0127] As explained in the present invention, unless otherwise specified in detail, the bonding group used in the present invention includes, for example, a hydroxyalkyl group, an aminoalkyl group, a hydroxyalkoxy group, an aminoalkoxy group, an alkylamino group, a saturated or partially unsaturated carbocyclylalkyl group, a saturated or partially unsaturated heterocyclylalkyl group, an arylalkyl group, and a heteroarylalkyl group, such as an amino group, a hydroxyl group, an alkyl group, an alkoxy group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, and a heteroaryl group, each of which has the definition described in the present invention.

[0128] As described herein, unless otherwise specified, ring substituents such as saturated or partially unsaturated carbocyclyl groups, saturated or partially unsaturated heterocyclyl groups, aryl groups, and heteroaryl groups can be bonded to the rest of the molecule through any bondable position on the ring. For example, a piperidinyl group includes piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, and piperidin-4-yl. As described herein, a ring system formed on a ring with a substituent R bonded to the center by a single bond indicates that the substituent R can be substituted at any substitutable position or any reasonable position on the ring to which it is bonded. As described herein, a ring system formed by a single bond bonded to the center of the ring indicates that this bond can be bonded to the rest of the molecule at any bondable position on the ring system. As described herein, when two bond points on a ring are bonded to the rest of the molecule, the two bond points can be bonded to the rest of the molecule at any bondable position on the ring, and at the same time, the bonded ends can be interchanged.

[0129] As used herein, the term "pharmaceutically acceptable excipient" refers to a pharmaceutically acceptable material, mixture, or solvent related to the consistency of a dosage form or pharmaceutical composition. Each excipient must be compatible with the other components of the pharmaceutical composition when mixed to avoid interactions that would substantially reduce the efficacy of the compounds disclosed herein and result in a non-pharmaceutically acceptable pharmaceutical composition when administered to a patient. Furthermore, each excipient must be pharmaceutically acceptable, e.g., of sufficiently high purity. Suitable pharmaceutically acceptable excipients will vary depending on the specific dosage form selected. Furthermore, pharmaceutically acceptable excipients can be selected based on their specific function in the composition. For example, a specific pharmaceutically acceptable excipient can be selected to aid in the production of a uniform dosage form. A specific pharmaceutically acceptable excipient can be selected to aid in the production of a stable dosage form. A specific pharmaceutically acceptable excipient can be selected to aid in the transport or transportation of the compounds of the present invention from one organ or part of the body to another organ or part of the body when administered to a patient. A specific pharmaceutically acceptable excipient can be selected to enhance patient compliance.

[0130] Some examples of suitable excipients include lactose, glucose, sucrose, sorbitol, mannitol, starch, gum arabic, calcium phosphate, alginate, tragacanth, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, and methylcellulose. Suitable pharmaceutically acceptable excipients further include classes of excipients such as solvents, propellants, solubilizers, cosolvents, emulsifiers, colorants, binders, disintegrants, fillers, lubricants, wetting agents, osmolality regulators, stabilizers, glidants, flavorings, preservatives, suspending agents, coating materials, fragrances, anti-adherents, antioxidants, chelating agents, penetration enhancers, pH adjusters, plasticizers, surfactants, foaming agents, anti-foaming agents, thickeners, encapsulating agents, humectants, absorbents, diluents, flocculating agents, anti-flocculating agents, and filter aids. Those skilled in the art will recognize that a particular pharmaceutically acceptable excipient may serve more than one function and may serve alternative functions, depending on the extent to which that excipient is present in the formulation and the presence of other excipients in the formulation. The compounds of the invention can be formulated using methods known in the art to provide quick, sustained, or delayed release of the active ingredient after administration to a patient.

[0131] Those skilled in the art possess the knowledge and capabilities in the art to enable them to select appropriate amounts of suitable pharmaceutically acceptable excipients for use in the present invention. Furthermore, there are numerous resources available to those skilled in the art that describe pharmaceutically acceptable excipients and aid in selecting appropriate pharmaceutically acceptable excipients. Examples include Remington's Pharmaceutical Sciences (Mack Publishing Company), The Handbook of Pharmaceutical Additives (Gower Publishing Limited), and The Handbook of Pharmaceutical Excipients (the American Pharmaceutical Association and the Pharmaceutical Press).

[0132] As used herein, "pharmaceutically acceptable carriers" includes solvents and solvent mixtures, coatings, complexing agents, solid carriers, dispersion media, surfactants, antibacterial and antifungal agents, isotonic and absorption delaying agents for drug active substances, and mixtures thereof, which are also known in the art.

[0133] Remington: The Science and Practice of Pharmacy, 21st edition, 2005, ed. D.B. Troy, Lippincott Williams & Wilkins, Philadelphia, and Encyclopedia of Pharmaceutical Technology, eds. J. Swarbrick and J.C.B. Boylan, 1988-1999, Marcel Dekker, New York, disclose various carriers for preparing pharmaceutically acceptable compositions and well-known techniques for their preparation, the contents of each of which are incorporated herein by reference. In addition to any conventional carriers that are incompatible with the compounds by producing undesirable biological effects or by adversely interacting with other components of the pharmaceutically acceptable compositions, contemplated applications are also within the scope of the present invention.

[0134] Suitable pharmaceutically acceptable carriers depend on the pharmaceutical form and are known to those skilled in the art. Non-limiting examples of pharmaceutically acceptable carriers include lactose, gelatin, sugar alcohols (e.g., starch, mannitol, corn starch, etc.), vegetable oils, talc, magnesium stearate, colloidal silicon dioxide, carboxymethylcellulose, microcrystalline cellulose, sodium lauryl sulfate, Tween aqueous buffer, copovidone, polysorbate, ethanol, propylene glycol, polyglycols (preferably polyethylene glycols such as PEG 400), 80 (i.e., PEG (20), sorbitol monooleate), DMSO, mixtures of water and cosolvents, such as ethanol, and the like. and / or polyethylene glycol; esters of fatty acids with glycerin and / or polyols such as polyethylene glycol; surfactants such as anionic, cationic, nonionic and amphoteric surfactants; complexing agents such as cyclodextrins, e.g., α-cyclodextrin (α-CD) or hydroxypropyl-β-cyclodextrin (HP-β-CD); lipids, e.g., bile acids or salts of animal or vegetable phospholipids; micelle-forming agents; and oils, e.g., corn oil; or mixtures of two or more of the foregoing.

[0135] Unless otherwise stated, any structural formulas set forth in this invention are intended to represent both non-isotopically enriched and isotopically enriched forms of these compounds. Isotopically enriched compounds have structures depicted by the general formulas set forth in this invention, except that one or more atoms are replaced by atoms of selected atomic mass or mass number. Exemplary isotopes that can be incorporated into compounds of this invention include isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorus, sulfur, fluorine, and chlorine, e.g., 2 H, 3 H, 11 C. 13 C. 14 C. 15 N, 17 O. 18 O. 18 F, 31 P, 32 P, 35 S,36 Cl and 125 Includes I.

[0136] 3 H, 14 C and 18 Compounds containing radioactive isotopes such as F, or 2 H and 13 Compounds in which non-radioactive isotopes such as C exist. Such isotopically enriched compounds are useful for metabolic studies ( 14 C), reaction kinetic studies ( 2 H or 3 H), or positron emission tomography (PET) or single photon emission computed tomography (SPECT) including tissue distribution determination of drugs or substrates, or can be used in radiotherapy of patients. 18 F-enriched compounds are particularly suitable for PET or SPECT studies. Isotopically enriched compounds of Formulas I, II-1 to II-6, III, IV-1 to IV-6, V-1 to V-6, VI-1 to VI-5, VII-1 to VII-6, and VIII-1 to VIII-6 can be prepared by conventional techniques well known to those skilled in the art, or by substituting an appropriate isotopically labeled reagent for the unlabeled reagent originally used, as described in the examples and preparation processes herein.

[0137] Additionally, heavier isotopes, particularly deuterium (i.e. 2Substitution with H or D may offer certain therapeutic advantages due to greater metabolic stability. For example, this may be due to increased in vivo half-life, reduced dosage requirements, or improved therapeutic index. It should be understood that deuterium in the present invention is considered a substituent of compounds of Formulas I, II-1 to II-6, III, IV-1 to IV-6, V-1 to V-6, VI-1 to VI-5, VII-1 to VII-6, and VIII-1 to VIII-6. An isotopic enrichment factor can be used to define the concentration of a heavier isotope, specifically deuterium. As used herein, the term "isotopic enrichment factor" refers to the ratio between the isotopic abundance and the natural abundance of a specified isotope. When a substituent of a compound of the invention is designated as deuterium, the compound has an isotopic enrichment factor for each designated deuterium atom of at least 3500 (52.5% deuterium doping at each designated deuterium atom), at least 4000 (60% deuterium doping), at least 4500 (67.5% deuterium doping), at least 5000 (75% deuterium doping), at least 5500 (82.5% deuterium doping), at least 6000 (90% deuterium doping), at least 6333.3 (95% deuterium doping), at least 6466.7 (97% deuterium doping), at least 6600 (99% deuterium doping), or at least 6633.3 (99.5% deuterium doping). Pharmaceutically acceptable solvates of the present invention include those wherein the solvent of crystallization may be isotopically substituted, eg D2O, acetone-d6, DMSO-d6.

[0138] Compounds, Pharmaceutical Compositions, Formulations and Administration The present invention provides focal adhesion kinase (FAK) inhibitor compounds that have good therapeutic effects on cancer, pulmonary arterial hypertension, and pathological angiogenesis.

[0139] In one aspect, the present invention relates to a compound, wherein the compound is a compound of Formula I or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula I: JPEG2025500871000149.jpg33126 where M, A, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0140] In some embodiments, M is a covalent warhead. JPEG2025500871000150.jpg37128 JPEG2025500871000151.jpg36136 JPEG2025500871000152.jpg36138 JPEG2025500871000153.jpg35132, where Z, L 7 , L 8 , R M1 , R M2 , R M3 , R M4 , R M5 , q, r are as defined in the present invention.

[0141] In some embodiments, M is JPEG2025500871000154.jpg3621, JPEG2025500871000155.jpg3615, JPEG2025500871000156.jpg2924 or JPEG2025500871000157.jpg2911, where Z, L 7 , R M1, R M2 , R M3 is as defined in the present invention.

[0142] In some embodiments, L 7 is one bond, -O-, -S-, -NR L7a - or C 1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7a S(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a S(=O)2-, where each R L7a are independently hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and each R L7b are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b groups, combined with the atoms to which they are attached, form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, wherein each L 7 , R L7a , R L7bThe alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0143] In some embodiments, L 7 is one bond, -O-, -S-, -NH- or C 1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group are optionally independently replaced by -O-, -S-, -NH-, -NHC(=O)-, -C(=O)NH-, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NHC(=S)-, -C(=S)NH-, transCH=CH-, cisCH=CH-, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NH-, -NHS(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NH-, or -NHS(=O)2-.

[0144] In some embodiments, L 8 is one bond or C 1-4 is an alkyl group, where L 8 The alkyl groups in are optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo.

[0145] In some embodiments, each R M1 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a , -CHN(RM1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0146] In some embodiments, each R M1 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a , -CHN(R M1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group.

[0147] In some embodiments, each R M2 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0148] In some embodiments, each R M2 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group.

[0149] In some embodiments, each R M3 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a , -N(R M3a )2 or -SR M3a where each R M3a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; In some embodiments, each R M3 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a , -N(R M3a )2 or -SR M3a where each R M3a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group.

[0150] In some embodiments, optionally, R M1 and RM3 , or R M2 and R M3 , or R M1 and R M2 are optionally joined to form a saturated or partially unsaturated carbocyclyl group or a saturated or partially unsaturated heterocyclyl group, wherein the saturated or partially unsaturated carbocyclyl group or the saturated or partially unsaturated heterocyclyl group may each optionally independently comprise deuterium, halogen, hydroxyl, amino, cyano, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0151] In some embodiments, optionally, R M1 and R M3 , or R M2 and R M3 , or R M1 and R M2 are optionally joined to form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a saturated or 3- to 6-membered partially unsaturated heterocyclyl group, wherein the 3- to 6-membered saturated or partially unsaturated carbocyclyl group or the saturated or 3- to 6-membered partially unsaturated heterocyclyl group optionally each independently contain deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0152] In some embodiments, R M4 is a leaving group. In some embodiments, R M4 is a halogen, a p-toluenesulfonyl group, a phenylsulfonyl group, or a p-nitrobenzenesulfonyl group. M5 is a halogen.

[0153] In some embodiments, Z is O, S, or NR Z where R Z are hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and R ZThe alkyl group in is optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo. In some embodiments, Z is O, S, or NH.

[0154] In some embodiments, q is 0, 1, 2, 3, 4, 5, or 6.

[0155] In some embodiments, r is 1 or 2.

[0156] In some embodiments, M is JPEG2025500871000158.jpg711, JPEG2025500871000159.jpg1111, JPEG2025500871000160.jpg1120, JPEG2025500871000161.jpg1523, JPEG2025500871000162.jpg207, JPEG2025500871000163.jpg1313, JPEG2025500871000164.jpg1413, JPEG2025500871000165.jpg1623, JPEG2025500871000166.jpg1728 or JPEG2025500871000167.jpg1619. In some embodiments, A is an aryl group or a heteroaryl group. In some embodiments, A is a 6- to 10-membered aryl group or a 5- to 10-membered heteroaryl group.

[0157] In some further embodiments, A is a 6- to 10-membered aryl group or a 5- to 10-membered azaaryl group. In some further embodiments, A is a phenyl group or a 6-membered azaaryl group. In some further embodiments, A is a phenyl group, an imidazolyl group, a pyrazolyl group, a triazolyl group, a tetrazolyl group, an oxazolyl group, a thiazolyl group, a furyl group, a thienyl group, a pyrrolyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, a pyridazinyl group, or JPEG2025500871000168.jpg1523, JPEG2025500871000169.jpg1623, JPEG2025500871000170.jpg1524, JPEG2025500871000171.jpg1523, JPEG2025500871000172.jpg1523, JPEG2025500871000173.jpg1523, JPEG2025500871000174.jpg1723, JPEG2025500871000175.jpg1324, JPEG2025500871000176.jpg1723, JPEG2025500871000177.jpg1523, JPEG2025500871000178.jpg1723, JPEG2025500871000179.jpg1324, JPEG2025500871000180.jpg1723, JPEG2025500871000181.jpg1723, JPEG2025500871000182.jpg1224, JPEG2025500871000183.jpg1226, JPEG2025500871000184.jpg1426 or It is based on JPEG2025500871000185.jpg1525 etc.

[0158] In some further embodiments, A is a phenyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, or a pyridazinyl group. In some further embodiments, A is a phenyl group or a pyrazinyl group.

[0159] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, or a nitrogen protecting group, where R L1a The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in the formula (I) are optionally substituted with one or more substituents each independently selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo.

[0160] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, deuterium, and C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 a haloheteroalkyl group or a nitrogen protecting group, where R L1aThe alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in the formula (I) are optionally substituted with one or more substituents each independently selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo.

[0161] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 Haloalkyl group, C 1-4 a haloheteroalkyl group or a nitrogen protecting group, where R L1a The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in are optionally substituted with one or more substituents each independently selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo. 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, methyl, ethyl, vinyl, ethynyl, or trifluoromethyl. 1 is a bond, —C(═O)—, —S(═O)—, —S(═O)2—, —C(═O)NH—, —NHC(═O)—, —S(═O)2NH—, or —NHS(═O)2—. In some other embodiments, L 1is one bond, -C(=O)- or -C(=O)NH-.

[0162] In some embodiments, L 2 is a bond, an alkyl group, a heteroalkyl group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where L 2 The alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the formula (I) are optionally substituted with one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, alkyl, alkenyl, alkynyl, heteroalkyl, or haloheteroalkyl groups.

[0163] In some other embodiments, L 2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl group, heteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 and substituted by one or more substituents selected from haloheteroalkyl groups.

[0164] In some other embodiments, L 2 is one bond, C 1-4 Alkyl group, C 1-4a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl group, heteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 and substituted by one or more substituents selected from haloheteroalkyl groups.

[0165] In some other embodiments, L 2 is one bond, C 1-4 Alkyl group, C 1-4 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the formula (I) are each optionally substituted with a substituent selected from deuterium, hydroxyl, amino, cyano, fluorine, chlorine, oxo, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy and methylamino.

[0166] In some other embodiments, L 2 is a bond, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where L 2The saturated or partially unsaturated carbocyclyl group and the saturated or partially unsaturated heterocyclyl group in the formula (I) are each optionally substituted with one or more substituents independently selected from hydroxyl, amino, cyano, fluorine, chlorine, oxo, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy, and methylamino groups. 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group.

[0167] In some embodiments, L 3 is a bond, an aryl group, or a heteroaryl group, where L 3 The aryl or heteroaryl groups in the formula (I) are each optionally substituted with one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, or haloheteroalkyl groups.

[0168] In some other embodiments, L 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 In some other embodiments, L is substituted by one or more substituents selected from haloheteroalkyl groups. 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3The aryl or heteroaryl groups in L are each optionally substituted with a substituent independently selected from deuterium, hydroxyl, amino, cyano, fluorine, chlorine, methyl, ethyl, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy, and methylamino. 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in L are optionally substituted with one or more hydroxyl, amino, cyano, fluorine, chlorine, methyl, ethyl, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy, or methylamino substituents. 3 is a bond, a phenyl group, or a pyridyl group.

[0169] In some embodiments, L 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 The carbon or hetero chains for are optionally substituted with one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, alkenyl, alkynyl, alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, hydroxyalkoxy, aminoalkoxy, alkylamino, and nitrogen protecting groups.

[0170] In some other embodiments, L 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 The carbon chain or hetero chain for each of the groups may optionally each independently be selected from the group consisting of deuterium, hydroxyl, amino, cyano, halogen, oxo, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Alkyl group, C 1-6 Haloalkyl group, C 1-6 Hydroxyalkyl group, C 1-6Aminoalkyl group, C 1-6 Alkoxy group, C 1-6 Haloalkoxy group, C 1-6 Hydroxyalkoxy group, C 1-6 Aminoalkoxy group, C 1-6 In some other embodiments, L is substituted with one or more substituents selected from an alkylamino group, a nitrogen protecting group, and an alkylamino group. 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 The carbon chain or hetero chain for each of the groups may optionally each independently be selected from the group consisting of deuterium, hydroxyl, amino, cyano, halogen, oxo, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Alkyl group, C 1-4 Haloalkyl group, C 1-4 Hydroxyalkyl group, C 1-4 Aminoalkyl group, C 1-4 Alkoxy group, C 1-4 Haloalkoxy group, C 1-4 Hydroxyalkoxy group, C 1-4 Aminoalkoxy group, C 1-4 In some other embodiments, L is substituted with one or more substituents selected from an alkylamino group, a nitrogen protecting group, and an alkylamino group. 4 is a carbon chain or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains for are optionally substituted with one or more substituents, each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, and nitrogen protecting groups.

[0171] In some other embodiments, L 4are -NHCH2-, -CH2NH-, -OCH2-, -CH2O-, -SCH2-, -CH2S-, -NHCH2CH2-, -CH2NHCH2-, -CH2CH2NH-, -OCH2CH2-, -CH2OCH2-, -CH2CH2O-, -SCH2CH2-, -CH2SCH2-, -CH2CH2S-, -NHCH2CH2CH2-, -CH2NHCH2CH2-, -CH2CH2NHCH2-, -CH2CH2 CH2NH-, -OCH2CH2CH2-, -CH2OCH2CH2-, -CH2CH2OCH2-, -CH2CH2CH2O-, -SCH2CH2CH2-, -CH2SCH2CH2-, -CH2CH2SCH2-, -CH2CH2CH2S-, -CH2OCH2O-, -OCH2OCH2-, -NHCH2CH2O-, -CH2NHCH2O- or -NHCH2OCH2-, wherein L 4 wherein the hydrogen atoms of CH2 are each optionally and independently replaced by a substituent selected from the group consisting of hydrogen, deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, and methylamino; and wherein L 4 The hydrogens of NH in L are optionally each independently replaced by hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group. 4 is -NHCH2-, -CH2NHCH2-, -NHC(=O)-, -CH2NHC(=O)-, -C(=O)NHCH2- or -NHCH(CH3)-.

[0172] In some embodiments, L 5 is -NR L5a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 5The alkyl and heteroalkyl groups in L5a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group.

[0173] In some embodiments, L 5 is -NR L5a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 heteroalkyl group, where L 5 The alkyl and heteroalkyl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, and each R L5a are independently hydrogen, deuterium, and C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 It is a haloalkyl group or a nitrogen protecting group.

[0174] In some other embodiments, L 5 is -NR L5a , -CR L5b R L5c -, -O-, -S-, -CR L5b R L5c NR L5a -, -NR L5a CR L5b R L5c -, -CR L5b R L5c O-, -OCR L5b R L5c -, -CRL5b R L5c S- or -SCR L5b R L5c -, where each R L5b and R L5c are each independently hydrogen, deuterium, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen, or C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L5a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 In some other embodiments, L is a haloalkyl group or a nitrogen protecting group. 5 In some other embodiments, L is -NH-, -O-, -S-, -NHCH-, -OCH-, -SCH-, -CHNH-, -CHO-, or -CHS-. 5 is -NH-.

[0175] In some embodiments, L 6 is -NR L6a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 6 The alkyl and heteroalkyl groups in L6a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group.

[0176] In some other embodiments, L 6 is -NR L6a -, -O-, -S-, C 1-6 Alkyl group or C 1-6heteroalkyl group, where L 6 The alkyl and heteroalkyl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, and each R L6a are independently hydrogen, deuterium, and C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 It is a haloalkyl group or a nitrogen protecting group.

[0177] In some other embodiments, L 6 is -NR L6a , -CR L6b R L6c -, -O-, -S-, -CR L6b R L6c NR L6a -, -NR L6a CR L6b R L6c -, -CR L6b R L6c O-, -OCR L6b R L6c -, -CR L6b R L6c S- or -SCR L6b R L6c -, where each R L6b and R L6c are each independently hydrogen, deuterium, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen, or C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L6aare independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 In some other embodiments, L is a haloalkyl group or a nitrogen protecting group. 6 In some other embodiments, L is -NH-, -O-, -S-, -NHCH-, -OCH-, -SCH-, -CHNH-, -CHO-, or -CHS-. 6 is —NH— or —NHCH2—.

[0178] In some embodiments, X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y 5 are each independently CH or N.

[0179] In some embodiments, each R 1 are independently hydrogen, deuterium, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 1The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, and heteroarylalkyl group in the above are optionally substituted with one or more substituents each independently selected from deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, and alkyl group.

[0180] In some embodiments, each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group may each independently optionally contain deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0181] In some other embodiments, each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above may each independently optionally contain deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0182] In some other embodiments, each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 a haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in each R are optionally substituted with one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, and oxo. 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 a haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in each R are optionally substituted with one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, and oxo. 1are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, fluorine, chlorine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC (=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2- , CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3 )2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)- , CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(C H3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH 2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2 CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-. ,

[0183] In some embodiments, each R 2 are independently hydrogen, deuterium, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 2 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl groups in the above are optionally substituted by one or more substituents each independently selected from one or more hydroxyl, amino, cyano, halogen, oxo and alkyl groups.

[0184] In some other embodiments, each R2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group may each independently optionally contain deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0185] In some other embodiments, each R 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above may each independently optionally contain deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 In some other embodiments, each R is substituted with one or more substituents selected from alkyl groups. 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 a haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in each R are optionally substituted with one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, and oxo. 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 a haloheteroalkyl group, where R 2The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in the formula (I) are each optionally substituted with one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, and oxo.

[0186] In some other embodiments, each R 2are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, fluorine, chlorine, bromine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)N H-, CH3NHC(=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH 3)2CHS(=O)2-, CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2 NHS(=O)2-, (CH3)2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH 3)2CHN(CH3)C(=O)-, CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS (=O)2N(CH3)-, CH3N(CH3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC (=O)N(CH2CH3)-, CH3N(CH2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-,(CH3)2CHON(CH2CH3)C(=O)-, CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-. ,

[0187] In some embodiments, each R 3 are independently hydrogen, deuterium, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 3 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl groups in the above are optionally substituted by one or more substituents each independently selected from one or more hydroxyl, amino, cyano, halogen, oxo and alkyl groups.

[0188] In some other embodiments, each R 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group may each independently optionally contain deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0189] In some other embodiments, each R 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above may each independently optionally contain deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 In some other embodiments, each R is substituted with one or more substituents selected from alkyl groups. 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, and 3- to 6-membered saturated or partially unsaturated heterocyclyl group may each independently optionally be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 In some other embodiments, each R is substituted with one or more substituents selected from alkyl groups. 3are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, and 3- to 6-membered saturated or partially unsaturated heterocyclyl group in the above formula (I) are each optionally substituted with one or more substituents independently selected from deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, methyl group, ethyl group, and isopropyl group.

[0190] In some other embodiments, each R 3are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, fluorine, chlorine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC (=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2- , CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3 )2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)- , CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(C H3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH 2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3) S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and two adjacent R, 3 If there are two adjacent R 3 together with the atoms to which they are attached, and optionally JPEG2025500871000186.jpg1918, JPEG2025500871000187.jpg1919, JPEG2025500871000188.jpg1921, JPEG2025500871000189.jpg1921, JPEG2025500871000190.jpg2018, JPEG2025500871000191.jpg2019, JPEG2025500871000192.jpg2023, JPEG2025500871000193.jpg2023, JPEG2025500871000194.jpg1921 or Form JPEG2025500871000195.jpg1919. In some embodiments, n, m, and p are each independently 0, 1, 2, 3, or 4.

[0191] In some embodiments, the saturated or partially unsaturated carbocyclyl group includes a saturated or partially unsaturated monocarbocyclyl group, a saturated or partially unsaturated spirocarbocyclyl group, a saturated or partially unsaturated fused carbocyclyl group, or a saturated or partially unsaturated bridged carbocyclyl group.

[0192] In some embodiments, the saturated or partially unsaturated carbocyclyl group is selected from formulas ii-1 to ii-6, wherein formulas ii-1 to ii-6 are monovalent when they are connected to the rest of the molecule by one bond, and wherein formulas ii-1 to ii-6 are divalent when they are connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated carbocyclyl groups represented by formulas ii-1 to ii-6 are each optionally and independently substituted with one or more substituents described herein; JPEG2025500871000196.jpg1410, JPEG2025500871000197.jpg1810, JPEG2025500871000198.jpg2111, JPEG2025500871000199.jpg2214, JPEG2025500871000200.jpg2221 or JPEG2025500871000201.jpg2314, wherein each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5.

[0193] In some embodiments, the saturated or partially unsaturated heterocyclyl group includes a saturated or partially unsaturated monoheterocyclyl group, a saturated or partially unsaturated spiroheterocyclyl group, a saturated or partially unsaturated fused heterocyclyl group, or a saturated or partially unsaturated bridged heterocyclyl group. In some embodiments, the saturated or partially unsaturated heterocyclyl group is selected from Formulae iii-1 to iii-16, where Formulae iii-1 to iii-16 are monovalent when they are bonded to the rest of the molecule by one bond, and where Formulae iii-1 to iii-16 are divalent when they are bonded to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl groups represented by Formulae iii-1 to iii-16 are optionally substituted, each independently, with one or more substituents described herein; JPEG2025500871000202.jpg1711, JPEG2025500871000203.jpg1711, JPEG2025500871000204.jpg1611, JPEG2025500871000205.jpg1813, JPEG2025500871000206.jpg2313, JPEG2025500871000207.jpg1913, JPEG2025500871000208.jpg2414, JPEG2025500871000209.jpg2614, JPEG2025500871000210.jpg2321, JPEG2025500871000211.jpg2321, JPEG2025500871000212.jpg2321, JPEG2025500871000213.jpg2321, JPEG2025500871000214.jpg2221, JPEG2025500871000215.jpg2521, JPEG2025500871000216.jpg2016 or JPEG2025500871000217.jpg2118, wherein each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5.

[0194] In some other embodiments, the saturated or partially unsaturated carbocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by one bond, and the following groups are divalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated carbocyclyl groups represented below are optionally substituted, each independently, with one or more substituents described herein: JPEG2025500871000218.jpg12139.

[0195] In some other embodiments, the saturated or partially unsaturated heterocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated heterocyclyl group is connected to the rest of the molecule by one bond, and the following groups are divalent when the saturated or partially unsaturated heterocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl groups represented below are optionally substituted, each independently, with one or more substituents described herein.

[0196] JPEG2025500871000219.jpg21141 JPEG2025500871000220.jpg21137 JPEG2025500871000221.jpg15123 In some embodiments, the compound of the present invention is a compound of Formula II-1 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula II-1: JPEG2025500871000223.jpg29114Here, each R M1 , R M2 , R M3 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0197] In some embodiments, the compound of the present invention is a compound of Formula II-2 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula II-2: JPEG2025500871000224.jpg27113Here, each R M1 , R M2 , R M3 , R L1a , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R2 , R 3 , A, n, m, p are as defined in the present invention.

[0198] In some embodiments, the compound of the present invention is a compound of Formula II-3 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula II-: JPEG2025500871000225.jpg27113 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, wherein each R M1 , R M2 , R M3 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0199] In some embodiments, the compound of the present invention is a compound of Formula II-4 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula II-4: JPEG2025500871000226.jpg28108Here, each R M1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0200] In some embodiments, the compound of the present invention is a compound of Formula II-5 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula II-5: JPEG2025500871000227.jpg27109Here, each R M1 , R L1a , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0201] In some embodiments, the compound of the present invention is a compound of Formula II-6 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula II-6: JPEG2025500871000228.jpg28114 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, wherein each R M1 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0202] In some embodiments, the compound of the present invention is a compound of Formula III or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula III: JPEG2025500871000229.jpg24117 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4eare each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; k and v are each independently 0, 1, or 2; and 1 , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0203] In some embodiments, the compound of the present invention is a compound of formula IV-1 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula IV-1: JPEG2025500871000230.jpg22114 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4band R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; k and v are each independently 0, 1, or 2; and M1 , R M2 , R M3 , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0204] In some embodiments, the compound of the present invention is a compound of formula IV-2 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula (IV-2): JPEG2025500871000231.jpg28147 where, R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy or a nitrogen protecting group; Each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4eoptionally forms oxo; k and v are each independently 0, 1, or 2; and M1 , R M2 , R M3 , R L1a , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0205] In some embodiments, the compound of the present invention is a compound of formula IV-3 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula IV-3: JPEG2025500871000232.jpg22109 where, B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy or a nitrogen protecting group; Each R L4b , R L4c , RL4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo; k and v are each independently 0, 1, or 2; Here, each R M1 , R M2 , R M3 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0206] In some embodiments, the compound of the present invention is a compound of formula IV-4 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula IV-4: JPEG2025500871000233.jpg23114 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4eare each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; k and v are each independently 0, 1, or 2; and M1 , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0207] In some embodiments, the compound of the present invention is a compound of formula IV-5 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula IV-5: JPEG2025500871000234.jpg22112 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4band R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; k and v are each independently 0, 1, or 2; and M1 , R L1a , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0208] In some embodiments, the compound of the present invention is a compound of formula IV-6 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula IV-6: JPEG2025500871000235.jpg23112 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , RL4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; k and v are each independently 0, 1, or 2; Here, each R M1 , L 3 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0209] In some embodiments, the compound of the present invention is a compound of formula V-1 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-1: JPEG2025500871000236.jpg32125Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0210] In some embodiments, the compound of the present invention is a compound of formula V-2 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-2: JPEG2025500871000237.jpg31118Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0211] In some embodiments, the compound of the present invention is a compound of formula V-3 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-3: JPEG2025500871000238.jpg30116Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0212] In some embodiments, the compound of the present invention is a compound of formula V-4 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-4: JPEG2025500871000239.jpg31119Here, each M, L 1 , L 2 , L 3 , L 4 , L 5, L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0213] In some embodiments, the compound of the present invention is a compound of formula V-5 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-5: JPEG2025500871000240.jpg30114Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0214] In some embodiments, the compound of the present invention is a compound of formula V-6 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-6: JPEG2025500871000241.jpg30117Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0215] In some embodiments, the compound of the present invention is a compound of formula V-7 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula V-7: JPEG2025500871000242.jpg30117Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , A, n, m, p are as defined in the present invention.

[0216] In some embodiments, the compound of the present invention is a compound of formula VI-1 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VI-1: JPEG2025500871000243.jpg27114Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0217] In some embodiments, the compound of the present invention is a compound of formula VI-2 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Equation VI-2: JPEG2025500871000244.jpg26109Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0218] In some embodiments, the compound of the present invention is a compound of formula VI-3 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Equation VI-3: JPEG2025500871000245.jpg27114Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0219] In some embodiments, the compound of the present invention is a compound of formula VI-4, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Equation VI-4: JPEG2025500871000246.jpg27115Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0220] In some embodiments, the compound of the present invention is a compound of formula VI-5 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Equation VI-5: JPEG2025500871000247.jpg29117Here, each M, L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0221] In some embodiments, the compound of the present invention is a compound of formula VII-1 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VII-1: JPEG2025500871000248.jpg26135where, R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R M2 , R M3 , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0222] In some embodiments, the compound of the present invention is a compound of formula VII-2 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VII-2: JPEG2025500871000249.jpg20107 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each RL4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R M2 , R M3 , R L1a , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0223] In some embodiments, the compound of the present invention is a compound of formula VII-3 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VII-3: JPEG2025500871000250.jpg20106 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R M2 , R M3 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0224] In some embodiments, the compound of the present invention is a compound of formula VII-4 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VII-4: JPEG2025500871000251.jpg30152 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , RL4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0225] In some embodiments, the compound of the present invention is a compound of formula VII-5 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VII-5: JPEG2025500871000252.jpg20109where, R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4coptionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R L1a , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0226] In some embodiments, the compound of the present invention is a compound of Formula VII-6 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VII-6: JPEG2025500871000253.jpg22109 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4eare each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0227] In some embodiments, the compound of the present invention is a compound of formula VIII-1 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VIII-1: JPEG2025500871000254.jpg24107 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4eoptionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R M2 , R M3 , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0228] In some embodiments, the compound of the present invention is a compound of formula VIII-2 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VIII-2: JPEG2025500871000255.jpg32141 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R M2 , R M3 , RL1a , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0229] In some embodiments, the compound of the present invention is a compound of formula VIII-3 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VIII-3: JPEG2025500871000256.jpg30139 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R M2 , R M3 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0230] In some embodiments, the compound of the present invention is a compound of formula VIII-4 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VIII-4: JPEG2025500871000257.jpg33139 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , L 2 , L 3 , L 5 , L 6 , X 1, X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0231] In some embodiments, the compound of the present invention is a compound of formula VIII-5 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VIII-5: JPEG2025500871000258.jpg30144 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , R L1a , L 2 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3 , n, m, p are as defined in the present invention.

[0232] In some embodiments, the compound of the present invention is a compound of formula VIII-6 or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula VIII-6: JPEG2025500871000259.jpg32141 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2, where each R M1 , L 3 , L 5 , L 6 , X 1 , X 2 , R 1 , R 2 , R 3, n, m, p are as defined in the present invention.

[0233] In one aspect, the present invention provides a compound, wherein the compound is a compound of Formula I or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula (I): JPEG2025500871000260.jpg29113where, M is a covalent warhead, A is an aryl or heteroaryl group; L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, or a nitrogen protecting group, where R L1a wherein the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups are each optionally substituted with one or more substituents independently selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo; L 2 is a bond, an alkyl group, a heteroalkyl group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where L 2 wherein the alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl group is optionally substituted by one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, alkyl, alkenyl, alkynyl, heteroalkyl, or haloheteroalkyl groups; L3 is a bond, an aryl group, or a heteroaryl group, where L 3 wherein the aryl or heteroaryl groups are each optionally substituted by one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, or haloheteroalkyl groups; L 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 wherein the carbon or hetero chain is optionally substituted with one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, alkenyl, alkynyl, alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, hydroxyalkoxy, aminoalkoxy, alkylamino, and nitrogen protecting groups; L 5 is -NR L5a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 5 The alkyl and heteroalkyl groups in L5a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; L 6 is -NR L6a -, -O-, -S-, an alkyl group, or a heteroalkyl group, wherein L 6 The alkyl and heteroalkyl groups in L6a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; X1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y 5 are each independently CH or N, Each R 1 are independently hydrogen, deuterium, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 1 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, heteroarylalkyl group are optionally substituted by one or more substituents each independently selected from deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group; Each R 2are independently hydrogen, deuterium, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 2 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group or heteroarylalkyl group is optionally substituted by one or more substituents each independently selected from hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, Each R 3 are independently hydrogen, deuterium, amino, hydroxyl, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R3 wherein the alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group is optionally substituted by one or more substituents each independently selected from hydroxyl group, amino group, cyano group, halogen, oxo, alkyl group, and m and p are each independently 0, 1, 2, 3, or 4.

[0234] In some embodiments, M is JPEG2025500871000261.jpg37128 JPEG2025500871000262.jpg35137 JPEG2025500871000263.jpg36138 JPEG2025500871000264.jpg35132, where: L 7 is one bond, -O-, -S-, -NR L7a - or C 1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7aS(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a S(=O)2-, where each R L7a are independently hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and each R L7b are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b groups, combined with the atoms to which they are attached, form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, wherein each L 7 , R L7a , R L7b The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; L 8 is one bond or C 1-4 is an alkyl group, where L 8 wherein the alkyl group is optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a, -CHN(R M1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M2 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a , -N(R M3a )2 or -SR M3a where each R M3a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3aThe alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Optionally, R M1 and R M3 , or R M2 and R M3 , or R M1 and R M2 are optionally joined to form a saturated or partially unsaturated carbocyclyl group or a saturated or partially unsaturated heterocyclyl group, wherein the saturated or partially unsaturated carbocyclyl group or the saturated or partially unsaturated heterocyclyl group may each optionally independently comprise deuterium, halogen, hydroxyl, amino, cyano, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; R M4 is a leaving group and R M5 is a halogen and Z is O, S or NR Z where R Z are hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and R Z wherein the alkyl group is optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo; q is 0, 1, 2, 3, 4, 5, or 6; and r is 1 or 2; In some embodiments, M is JPEG2025500871000265.jpg3621, JPEG2025500871000266.jpg3615, JPEG2025500871000267.jpg2924 or JPEG2025500871000268.jpg2911, L 7 is one bond, -O-, -S-, -NR L7a- or C 1-4 alkyl group, wherein the C 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a -, -NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, SysCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a -, -NR L7a S(=O)-, -S(=O)2-, -S(=O)2O-, -OS(=O)2-, -S(=O)2NR L7a -or-NR L7a S(=O)2-, where each R L7a are independently hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and R L7b are hydrogen, deuterium, halogens, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each L 7 , R L7a , R L7b The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4substituted by one or more substituents selected from alkyl groups; Z is O, S or NR Z where R Z are hydrogen, deuterium, and C 1-4 is an alkyl group or a nitrogen protecting group, and R Z wherein the alkyl group is optionally substituted with one or more substituents selected from hydrogen, deuterium, halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M1a , -CHN(R M1a )2, -CH2SR M1a , -OR M1a , -N(R M1a )2, -Si(R M1a )3 or -SR M1a where each R M1a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M1a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each RM2 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M2a , -CHN(R M2a )2, -CH2SR M2a , -OR M2a , -N(R M2a )2 or -SR M2a where each R M2a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M2a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, -CN, -CHOR M3a , -CHN(R M3a )2, -CH2SR M3a , -OR M3a, -N(R M3a )2 or -SR M3a where each R M3a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two R M3a Groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl group, alkenyl group, alkynyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, halogen, hydroxyl group, amino group, cyano group, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; In some embodiments, M is JPEG2025500871000269.jpg712, JPEG2025500871000270.jpg1112, JPEG2025500871000271.jpg1120, JPEG2025500871000272.jpg1523, JPEG2025500871000273.jpg207, JPEG2025500871000274.jpg1313, JPEG2025500871000275.jpg1413, JPEG2025500871000276.jpg1624, JPEG2025500871000277.jpg1728 or JPEG2025500871000278.jpg1619. In some embodiments, A is a 6- to 10-membered aryl group or a 5- to 10-membered heteroaryl group. In some embodiments, A is a 6- to 10-membered aryl group or a 5- to 10-membered azaaryl group. In some embodiments, A is a phenyl group or a 6-membered azaaryl group. In some embodiments, A is a phenyl group, an imidazolyl group, a pyrazolyl group, a triazolyl group, a tetrazolyl group, an oxazolyl group, a thiazolyl group, a furyl group, a thienyl group, a pyrrolyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, a pyridazinyl group, or JPEG2025500871000279.jpg1523, JPEG2025500871000280.jpg1623, JPEG2025500871000281.jpg1524, JPEG2025500871000282.jpg1523, JPEG2025500871000283.jpg1523, JPEG2025500871000284.jpg1523, JPEG2025500871000285.jpg1723, JPEG2025500871000286.jpg1324, JPEG2025500871000287.jpg1723, JPEG2025500871000288.jpg1523, JPEG2025500871000289.jpg1723, JPEG2025500871000290.jpg1324, JPEG2025500871000291.jpg1723, JPEG2025500871000292.jpg1723, JPEG2025500871000293.jpg1224, JPEG2025500871000294.jpg1226, JPEG2025500871000295.jpg1326 or JPEG2025500871000296.jpg1525, In some embodiments, A is a phenyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, or a pyridazinyl group. In some embodiments, A is a phenyl group or a pyrazinyl group.

[0235] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)2NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 Haloalkyl group, C 1-4 a haloheteroalkyl group or a nitrogen protecting group, where R L1a The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl group, heteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group, or heteroaryl group may each independently optionally be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C1-4 substituted by one or more substituents selected from haloheteroalkyl groups; 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; 4 is a carbon chain or hetero chain having 2 to 6 atoms, where L 4 The carbon chain or hetero chain for each of the groups may optionally each independently be selected from the group consisting of deuterium, hydroxyl, amino, cyano, halogen, oxo, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Alkyl group, C 1-4 Haloalkyl group, C 1-4 Hydroxyalkyl group, C 1-4 Aminoalkyl group, C 1-4 Alkoxy group, C 1-4 Haloalkoxy group, C 1-4 Hydroxyalkoxy group, C 1-4 Aminoalkoxy group, C 1-4 It is substituted with one or more substituents selected from alkylamino groups, nitrogen protecting groups.

[0236] In some embodiments, L 1 represents one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NR L1a -, -NR L1a C(=O)-, -S(=O)2NR L1a -or-NR L1a S(=O)2-, where each R L1a are independently hydrogen, methyl, ethyl, vinyl, ethynyl, or trifluoromethyl; L2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 4 is a carbon chain or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains for are optionally substituted with one or more substituents, each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, and nitrogen protecting groups.

[0237] In some embodiments, L 1 is one bond, -C(=O)-, -S(=O)-, -S(=O)2-, -C(=O)NH-, -NHC(=O)-, -S(=O)2NH- or -NHS(=O)2-, and L 2 is a bond, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where L 2The saturated or partially unsaturated carbocyclyl group and the saturated or partially unsaturated heterocyclyl group in the formula (I) are each optionally substituted by one or more substituents independently selected from hydroxyl, amino, cyano, fluorine, chlorine, oxo, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy, and methylamino groups; and L 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 4 is a carbon chain or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains for are optionally substituted with one or more substituents, each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, and nitrogen protecting groups.

[0238] In some embodiments, L 1 is one bond, —C(═O)— or —C(═O)NH—, and L 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group, and L 3 is a bond, a phenyl group, or a pyridyl group, and L 4are -NHCH2-, -CH2NH-, -OCH2-, -CH2O-, -SCH2-, -CH2S-, -NHCH2CH2-, -CH2NHCH2-, -CH2CH2NH-, -OCH2CH2-, -CH2OCH2-, -CH2CH2O-, -SCH2CH2-, -CH2SCH2-, -CH2CH2S-, -NHCH2CH2CH2-, -CH2NHCH2CH2-, -CH2CH2NHCH2-, -CH2CH2 CH2NH-, -OCH2CH2CH2-, -CH2OCH2CH2-, -CH2CH2OCH2-, -CH2CH2CH2O-, -SCH2CH2CH2-, -CH2SCH2CH2-, -CH2CH2SCH2-, -CH2CH2CH2S-, -CH2OCH2O-, -OCH2OCH2-, -NHCH2CH2O-, -CH2NHCH2O- or -NHCH2OCH2-, wherein L 4 wherein the hydrogen atoms of CH2 are each optionally and independently replaced by a substituent selected from the group consisting of hydrogen, deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, and methylamino; and wherein L 4 The hydrogen of NH in is optionally replaced by each independently hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group substituent.

[0239] In some embodiments, L 1 is one bond, —C(═O)— or —C(═O)NH—, and L 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group, and L 3 is a bond, a phenyl group, or a pyridyl group, and L 4 is -NHCH2-, -CH2NHCH2-, -NHC(=O)-, -CH2NHC(=O)-, -C(=O)NHCH2- or -NHCH(CH3)-.

[0240] In some embodiments, L5 is -NR L5a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 heteroalkyl group, where L 5 The alkyl and heteroalkyl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, and each R L5a are independently hydrogen, deuterium, and C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 is a haloalkyl group or a nitrogen protecting group, and L 6 is -NR L6a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 heteroalkyl group, where L 6 The alkyl and heteroalkyl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups, and each R L6a are independently hydrogen, deuterium, and C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 It is a haloalkyl group or a nitrogen protecting group.

[0241] In some embodiments, L 5 is -NR L5a , -CR L5b R L5c -, -O-, -S-, -CR L5b R L5c NR L5a -, -NR L5a CR L5b R L5c -, -CR L5b R L5c O-, -OCR L5b R L5c -, -CR L5b R L5c S- or -SCR L5b R L5c -, where each R L5b and R L5c are each independently hydrogen, deuterium, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen, or C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L5a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 is a haloalkyl group or a nitrogen protecting group, and L 6 is -NR L6a , -CR L6b R L6c -, -O-, -S-, -CR L6b R L6c NR L6a -, -NR L6a CR L6b R L6c -, -CR L6b R L6c O-, -OCR L6b R L6c -, -CR L6b R L6c S- or -SCR L6b R L6c -, where each R L6band R L6c are each independently hydrogen, deuterium, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen, or C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L6a are independently hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 It is a haloalkyl group or a nitrogen protecting group.

[0242] In some embodiments, L 5 is -NH-, -O-, -S-, -NHCH2-, -OCH2-, -SCH2-, -CH2NH-, -CH2O- or -CH2S-, and L 6 is -NH-, -O-, -S-, -NHCH2-, -OCH2-, -SCH2-, -CH2NH-, -CH2O- or -CH2S-.

[0243] In some embodiments, L 5 is -NH-, and L 6 is —NH— or —NHCH2—.

[0244] In some embodiments, Each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group may each independently optionally contain deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C1-6 is an alkyl group, and two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group may each independently optionally contain deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 Alkyl group, 6- to 10-membered heteroaryl group or 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 3 If there are two adjacent R 3together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group may each independently optionally contain deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0245] In some embodiments, each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 1 If there are two adjacent R 1 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above may each independently optionally contain deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4alkyl groups, and each R 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 2 If there are two adjacent R 2 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above may each independently optionally contain deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 alkyl groups, and each R 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl groups, C 1-6 Haloalkyl group, C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above may each independently optionally contain deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0246] In some embodiments, each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 a haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 a haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-6 Alkyl group, C 1-6 Heteroalkyl groups, C 1-6 haloalkyl group or C 1-6 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, and 3- to 6-membered saturated or partially unsaturated heterocyclyl group may each independently optionally be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 It is substituted by one or more substituents selected from alkyl groups.

[0247] In some embodiments, each R 1 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 a haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 a haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 3 are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, halogen, C 1-4 Alkyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C1-4 A haloheteroalkyl group is a group consisting of two adjacent R 3 If there are two adjacent R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, and 3- to 6-membered saturated or partially unsaturated heterocyclyl group in the above formula (I) are each optionally substituted with one or more substituents independently selected from deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, methyl group, ethyl group, and isopropyl group.

[0248] In some embodiments, each R 1are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, fluorine, chlorine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC (=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2- , CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3 )2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)- , CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(C H3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH 2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and each R 2are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, fluorine, chlorine, bromine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)N H-, CH3NHC(=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH 3)2CHS(=O)2-, CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2 NHS(=O)2-, (CH3)2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH 3)2CHN(CH3)C(=O)-, CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS (=O)2N(CH3)-, CH3N(CH3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC (=O)N(CH2CH3)-, CH3N(CH2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-,(CH3)2CHON(CH2CH3)C(=O)-, CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3)S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and each R 3are independently hydrogen, deuterium, amino group, hydroxyl group, cyano group, fluorine, chlorine, methyl group, ethyl group, propyl group, isopropyl group, t-butyl, methoxy group, ethoxy group, isopropoxy group, t-butoxy group, trifluoromethyl group, trifluoromethoxy group, CH3C(=O)-, CH3CH2C(=O)-, (CH3)2CHC(=O)-, CH3C(=O)O-, CH3CH2C(=O)O-, (CH3)2CHC(=O)O-, CH3C(=O)NH-, CH3CH2C(=O)NH-, (CH3)2CHC(=O)NH-, CH3NHC (=O)-, CH3CH2NHC(=O)-, (CH3)2CHNHC(=O)-, CH3ONHC(=O)-, CH3CH2ONHC(=O)-, (CH3)2CHONHC(=O)-, CH3S(=O)2-, CH3CH2S(=O)2-, (CH3)2CHS(=O)2- , CH3S(=O)2O-, CH3CH2S(=O)2O-, (CH3)2CHS(=O)2O-, CH3S(=O)2NH-, CH3CH2S(=O)2NH-, (CH3)2CHS(=O)2NH-, CH3NHS(=O)2-, CH3CH2NHS(=O)2-, (CH3 )2CHNHS(=O)2-, CH3C(=O)N(CH3)-, CH3CH2C(=O)N(CH3)-, (CH3)2CHC(=O)N(CH3)-, CH3N(CH3)C(=O)-, CH3CH2N(CH3)C(=O)-, (CH3)2CHN(CH3)C(=O)- , CH3ON(CH3)C(=O)-, CH3CH2ON(CH3)C(=O)-, (CH3)2CHON(CH3)C(=O)-, CH3S(=O)2N(CH3)-, CH3CH2S(=O)2N(CH3)-, (CH3)2CHS(=O)2N(CH3)-, CH3N(C H3)S(=O)2-, CH3CH2N(CH3)S(=O)2-, (CH3)2CHN(CH3)S(=O)2-, CH3C(=O)N(CH2CH3)-, CH3CH2C(=O)N(CH2CH3)-, (CH3)2CHC(=O)N(CH2CH3)-, CH3N(CH 2CH3)C(=O)-, CH3CH2N(CH2CH3)C(=O)-, (CH3)2CHN(CH2CH3)C(=O)-, CH3ON(CH2CH3)C(=O)-, CH3CH2ON(CH2CH3)C(=O)-, (CH3)2CHON(CH2CH3)C(=O)-,CH3S(=O)2N(CH2CH3)-, CH3CH2S(=O)2N(CH2CH3)-, (CH3)2CHS(=O)2N(CH2CH3)-, CH3N(CH2CH3)S(=O)2-, CH3CH2N(CH2CH3)S(=O)2-, (CH3)2CHN(CH2CH3) S(=O)2-, (CH3)2P(=O)-, CH3CH2(CH3)P(=O)-, (CH3)2CH(CH3)P(=O)-, (CH3CH2)2P(=O)-, CH3CH2(CH3)P(=O)- or (CH3)2CH(CH3CH2)P(=O)-, and two adjacent R, 3 If there are two adjacent R 3 together with the atoms to which they are attached, and optionally JPEG2025500871000297.jpg1918, JPEG2025500871000298.jpg1919, JPEG2025500871000299.jpg1921, JPEG2025500871000300.jpg1921, JPEG2025500871000301.jpg2019, JPEG2025500871000302.jpg2019, JPEG2025500871000303.jpg2023, JPEG2025500871000304.jpg2023, JPEG2025500871000305.jpg1921 or Form JPEG2025500871000306.jpg1919. In some embodiments, the saturated or partially unsaturated carbocyclyl group is selected from formulas ii-1 to ii-6, wherein when formulas ii-1 to ii-6 are linked to the remainder of the molecule by one bond, formulas ii-1 to ii-6 are monovalent, and when formulas ii-1 to ii-6 are linked to the remainder of the molecule by two bonds, formulas ii-1 to ii-6 are divalent; and the saturated or partially unsaturated carbocyclyl groups represented by formulas ii-1 to ii-6 are optionally substituted, each independently, by one or more substituents as defined in the corresponding claim above; JPEG2025500871000307.jpg1410, JPEG2025500871000308.jpg1810, JPEG2025500871000309.jpg2111, JPEG2025500871000310.jpg2214, JPEG2025500871000311.jpg2221 or JPEG2025500871000312.jpg2314 The saturated or partially unsaturated heterocyclyl group is selected from formulae iii-1 to iii-16, wherein formulae iii-1 to iii-16 are monovalent when they are linked to the remainder of the molecule by one bond, and are divalent when they are linked to the remainder of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl groups represented by formulae iii-1 to iii-16 are optionally substituted, each independently, by one or more substituents as defined in the corresponding claim above; JPEG2025500871000313.jpg1710, JPEG2025500871000314.jpg1711, JPEG2025500871000315.jpg1610, JPEG2025500871000316.jpg1813, JPEG2025500871000317.jpg2313, JPEG2025500871000318.jpg2013, JPEG2025500871000319.jpg2414, JPEG2025500871000320.jpg2714, JPEG2025500871000321.jpg2421, JPEG2025500871000322.jpg2321, JPEG2025500871000323.jpg2321, JPEG2025500871000324.jpg2221, JPEG2025500871000325.jpg2221, JPEG2025500871000326.jpg2521, JPEG2025500871000327.jpg2016 or JPEG2025500871000328.jpg2118 where each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5.

[0249] In some embodiments, the saturated or partially unsaturated carbocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by one bond, and the following groups are divalent when the saturated or partially unsaturated carbocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated carbocyclyl groups represented below are optionally substituted, each independently, by one or more substituents defined in the corresponding claim above: JPEG2025500871000329.jpg13141, The saturated or partially unsaturated heterocyclyl group is selected from the following groups, where the following groups are monovalent when the saturated or partially unsaturated heterocyclyl group is connected to the rest of the molecule by one bond, and where the following groups are divalent when the saturated or partially unsaturated heterocyclyl group is connected to the rest of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl groups shown below are optionally substituted, each independently, by one or more substituents defined in the corresponding claim above.

[0250] JPEG2025500871000330.jpg21141 JPEG2025500871000331.jpg21137 JPEG2025500871000332.jpg15122 In some embodiments, the compound of the present invention is a compound represented by any one of Formulas II-1 to II-6, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof, Formula II-1: JPEG2025500871000334.jpg30116, Formula II-2: JPEG2025500871000335.jpg27113, Formula II-3: JPEG2025500871000336.jpg25104, Formula II-4: JPEG2025500871000337.jpg29111, Formula II-5: JPEG2025500871000338.jpg28110 or Formula II-6: JPEG2025500871000339.jpg29114 wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 and substituted by one or more substituents selected from haloheteroalkyl groups.

[0251] In some embodiments, the compound of the present invention is a compound of Formula III or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof: Formula (III): JPEG2025500871000340.jpg33161 where R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; and k and v are each independently 0, 1, or 2.

[0252] In some embodiments, the compound of the present invention is a compound represented by any one of Formulas IV-1 to IV-6, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof, Formula IV-1: JPEG2025500871000341.jpg23114, Formula IV-2: JPEG2025500871000342.jpg21113, Formula IV-3: JPEG2025500871000343.jpg23113, Formula IV-4: JPEG2025500871000344.jpg23112, Formula IV-5: JPEG2025500871000345.jpg20101 or Formula IV-6: JPEG2025500871000346.jpg23113, wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms oxo; and k and v are each independently 0, 1, or 2.

[0253] In some embodiments, the compound of the present invention is a compound represented by any one of Formulas V-1 to V-7, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof.

[0254] Formula V-1: JPEG2025500871000347.jpg29112, Formula V-2: JPEG2025500871000348.jpg30116, Formula V-3: JPEG2025500871000349.jpg28108, Formula V-4: JPEG2025500871000350.jpg30116, Formula V-5: JPEG2025500871000351.jpg30117, Formula V-6: JPEG2025500871000352.jpg2597 or Formula V-7: JPEG2025500871000353.jpg30115In some embodiments, the compound of the present invention is a compound represented by any one of Formulas VI-1 to VI-5, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof.

[0255] Formula VI-1: JPEG2025500871000354.jpg27113, Equation VI-2: JPEG2025500871000355.jpg26110, Equation VI-3: JPEG2025500871000356.jpg27111, Equation VI-4: JPEG2025500871000357.jpg26109 or Equation VI-5: In some embodiments, the compound of the present invention is a compound represented by any one of Formulas VII-1 to VII-6, or a stereoisomer, tautomer, nitroxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug thereof, Formula VII-1: JPEG2025500871000359.jpg21109, Formula VII-2: JPEG2025500871000360.jpg20106, Formula VII-3: JPEG2025500871000361.jpg21109, Formula VII-4: JPEG2025500871000362.jpg21106, Formula VII-5: JPEG2025500871000363.jpg19101 or Formula VII-6: JPEG2025500871000364.jpg22111, wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, and the 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group may optionally contain deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, an oxo group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl groups, C 1-4 haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group, and each R L4b , R L4c , R L4d and R L4eare each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, and L4b and R L4c optionally forms an oxo, and R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1, or 2.

[0256] In some embodiments, the compound of the present invention is a compound represented by any one of Fo...

Claims

1. A compound which is a compound of formula I or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof, Formula I: Where: M is a covalent warhead; A is an aryl or heteroaryl group; L 1 is one bond, -C(=O)-, -S(=O)-, -S(=O) 2 -, -C(=O)NR L1a --, --NR L1a C(=O)-, -S(=O) 2 N.R. L1a -or-NR L1a S (=O) 2 -, where each R L1a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, or a nitrogen protecting group, where R L1a wherein the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups are optionally substituted with one or more substituents each independently selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo; L 2 is a bond, an alkyl group, a heteroalkyl group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where L 2 wherein the alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl group is optionally substituted by one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, alkyl, alkenyl, alkynyl, heteroalkyl, or haloheteroalkyl; L 3 is a bond, an aryl group, or a heteroaryl group, where L 3 wherein the aryl or heteroaryl groups are optionally substituted with one or more substituents independently selected from deuterium, hydroxyl, amino, cyano, halogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, or haloheteroalkyl groups; L 4 is a carbon or hetero chain having 2 to 6 atoms, where L 4 wherein the carbon or hetero chain is optionally substituted with one or more substituents, each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, alkenyl, alkynyl, alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, hydroxyalkoxy, aminoalkoxy, alkylamino, nitrogen protecting groups; L 5 is -NR L5a -, -O-, -S-, an alkyl group or a heteroalkyl group, 5 The alkyl and heteroalkyl groups for each R are optionally substituted with a substituent selected from deuterium, amino, hydroxyl, oxo, cyano, halogen, alkenyl, or alkynyl; L5a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; L 6 is -NR L6a -, -O-, -S-, an alkyl group or a heteroalkyl group, 6 The alkyl and heteroalkyl groups for each R are optionally substituted with a substituent selected from deuterium, amino, hydroxyl, oxo, cyano, halogen, alkenyl, or alkynyl; L6a are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, or a nitrogen protecting group; X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 and Y 5 are each independently CH or N; Each R 1 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, an alkoxy group, a haloalkoxy group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated carbocyclylalkyl group, a saturated or partially unsaturated heterocyclyl group, a saturated or partially unsaturated heterocyclylalkyl group, an aryl group, an arylalkyl group, a heteroaryl group, or a heteroarylalkyl group; 1 When R 1 together with the atoms to which they are attached, optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 1 the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl groups are optionally substituted by one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, and alkyl groups; Each R 2 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, an alkoxy group, a haloalkoxy group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated carbocyclylalkyl group, a saturated or partially unsaturated heterocyclyl group, a saturated or partially unsaturated heterocyclylalkyl group, an aryl group, an arylalkyl group, a heteroaryl group, or a heteroarylalkyl group; 2 When R 2 together with the atoms to which they are attached, optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 2 wherein the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl groups are each optionally substituted by one or more substituents, each independently, hydroxyl, amino, cyano, halogen, oxo, alkyl, Each R 3 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, an alkyl group, an alkenyl group, an alkynyl group, a heteroalkyl group, a haloalkyl group, a haloheteroalkyl group, an alkoxy group, a haloalkoxy group, a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated carbocyclylalkyl group, a saturated or partially unsaturated heterocyclyl group, a saturated or partially unsaturated heterocyclylalkyl group, an aryl group, an arylalkyl group, a heteroaryl group, or a heteroarylalkyl group; 3 When R 3 together with the atoms to which they are attached, optionally form a saturated or partially unsaturated carbocyclyl group, a saturated or partially unsaturated heterocyclyl group, an aryl group, or a heteroaryl group, where R 3 wherein the alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated carbocyclylalkyl, saturated or partially unsaturated heterocyclyl, saturated or partially unsaturated heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl groups are optionally substituted, each independently, by one or more substituents of hydroxyl, amino, cyano, halogen, oxo, alkyl, and wherein n, m and p are each independently 0, 1, 2, 3 or 4; or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitrogen oxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt or prodrug thereof;

2. M is, and Where: L 7 represents one bond, -O-, -S-, -NR L7a - or C 1-4 is an alkyl group, 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a --, --NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, cisCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a --, --NR L7a S(=O)-, -S(=O) 2 -, -S(=O) 2 O-, -OS (=O) 2 -, -S(=O) 2 N.R. L7a -or-NR L7a S (=O) 2 -, where each R L7a are independently hydrogen, deuterium, C 1-4 is an alkyl group or a nitrogen protecting group, L7b are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b The groups combine with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each L 7 , R L7a , R L7b The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; L 8 is one bond or C 1-4 is an alkyl group, 8 wherein the alkyl group is optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl groups, 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, 5- to 10-membered heteroaryl groups, -CN, -CH 2 OR M1a , -CH 2 N (R M1a ) 2 , -CH 2 S.R. M1a , -OR M1a , -N(R M1a ) 2 , -Si(R M1a ) 3 Or -SR M1a where each R M1a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group; or M1a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; Each R M2 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl groups, 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, 5- to 10-membered heteroaryl groups, -CN, -CH 2 OR M2a , -CH 2 N (R M2a ) 2 , -CH 2 S.R. M2a , -OR M2a , -N(R M2a ) 2 Or -SR M2a where each R M2a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group; or M2a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl groups, 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, 5- to 10-membered heteroaryl groups, -CN, -CH 2 OR M3a , -CH 2 N (R M3a ) 2 , -CH 2 S.R. M3a , -OR M3a , -N(R M3a ) 2 Or -SR M3a where each R M3a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group; or M3a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; Optionally, R M1 and R M3 , or R M2 and R M3 , or R M1 and R M2 are optionally joined to form a saturated or partially unsaturated carbocyclyl group or a saturated or partially unsaturated heterocyclyl group, where the saturated or partially unsaturated carbocyclyl group or the saturated or partially unsaturated heterocyclyl group are each optionally independently selected from deuterium, halogen, hydroxyl, amino, cyano, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; R M4 is a leaving group, R M5 is a halogen, Z is O, S or NR Z where R Z is hydrogen, deuterium, C 1-4 is an alkyl group or a nitrogen protecting group; R Z wherein the alkyl group is optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, amino, cyano, and oxo; q is 0, 1, 2, 3, 4, 5 or 6; r is 1 or 2; or M is, 、 、 or and L 7 represents one bond, -O-, -S-, -NR L7a - or C 1-4 is an alkyl group, 1-4 One or more carbon units of the alkyl group may optionally be independently selected from -O-, -S-, -NR L7a --, --NR L7a C(=O)-, -C(=O)NR L7a -, -SC(=O)-, -C(=O)S-, -OC(=O)-, -C(=O)O-, -NR L7a C(=S)-, -C(=S)NR L7a -, TransCR L7b =CR L7b -, cisCR L7b =CR L7b -, -C≡C-, -S(=O)-, -S(=O)O-, -OS(=O)-, -S(=O)NR L7a --, --NR L7a S(=O)-, -S(=O) 2 -, -S(=O) 2 O-, -OS (=O) 2 -, -S(=O) 2 N.R. L7a -or-NR L7a S (=O) 2 -, where each R L7a are independently hydrogen, deuterium, C 1-4 is an alkyl group or a nitrogen protecting group, L7b are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, or two adjacent R L7b The groups are optionally combined with the atoms to which they are attached to form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each L 7 , R L7a , R L7b The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; Z is O, S or NR Z where R Z is hydrogen, deuterium, C 1-4 is an alkyl group or a nitrogen protecting group; R Z The alkyl group in the formula (I) is optionally substituted with one or more substituents selected from hydrogen, deuterium, halogen, hydroxyl, amino, cyano, and oxo; Each R M1 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl groups, 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, 5- to 10-membered heteroaryl groups, -CN, -CH 2 OR M1a , -CH 2 N (R M1a ) 2 , -CH 2 S.R. M1a , -OR M1a , -N(R M1a ) 2 , -Si(R M1a ) 3 Or -SR M1a where each R M1a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group; or M1a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M1 , R M1a The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; Each R M2 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl groups, 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, 5- to 10-membered heteroaryl groups, -CN, -CH 2 OR M2a , -CH 2 N (R M2a ) 2 , -CH 2 S.R. M2a , -OR M2a , -N(R M2a ) 2 Or -SR M2a where each R M2a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group; or M2a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M2 , R M2a The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; Each R M3 are independently hydrogen, deuterium, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl groups, 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, 5- to 10-membered heteroaryl groups, -CN, -CH 2 OR M3a , -CH 2 N (R M3a ) 2 , -CH 2 S.R. M3a , -OR M3a , -N(R M3a ) 2 Or -SR M3a where each R M3a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 an alkynyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group; or M3a The groups are optionally combined with the atom to which they are attached to form a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where each R M3 , R M3a The alkyl, alkenyl, alkynyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 1-4 substituted by one or more substituents selected from alkyl groups; or M is, 、 、 、 、 、 、 、 、 or characterized in that 2. A compound according to claim 1 or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof.

3. A is a 6- to 10-membered aryl group or a 5- to 10-membered heteroaryl group, or A is a 6- to 10-membered aryl group or a 5- to 10-membered azaaryl group, or A is a phenyl group or a 6-membered azaaryl group, or A is a phenyl group, an imidazolyl group, a pyrazolyl group, a triazolyl group, a tetrazolyl group, an oxazolyl group, a thiazolyl group, a furyl group, a thienyl group, a pyrrolyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, a pyridazinyl group, or 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 or and A and L 6 and is one end of the or A is a phenyl group, a pyridyl group, a pyrimidinyl group, a pyrazinyl group, or a pyridazinyl group; or A is a phenyl group or a pyrazinyl group; 2. A compound according to claim 1 or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof.

4. L 1 is one bond, -C(=O)-, -S(=O)-, -S(=O) 2 -, -C(=O)NR L1a --, --NR L1a C(=O)-, -S(=O) 2 N.R. L1a -or-NR L1a S (=O) 2 -, where each R L1a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group, C 1-4 a haloheteroalkyl group or a nitrogen protecting group, where R L1a The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl group, heteroalkyl group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated heterocyclyl group, aryl group or heteroaryl group in the formula (I) may each optionally independently be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 substituted by one or more substituents selected from haloheteroalkyl groups; 4 is a carbon or hetero chain having 2 to 6 atoms, where L 4 The carbon or hetero chains for each are optionally independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Alkyl group, C 1-4 Haloalkyl group, C 1-4 Hydroxyalkyl group, C 1-4 Aminoalkyl group, C 1-4 Alkoxy group, C 1-4 Haloalkoxy group, C 1-4 Hydroxyalkoxy group, C 1-4 Aminoalkoxy group, C 1-4 substituted by one or more substituents selected from an alkylamino group, a nitrogen protecting group, or L 1 is one bond, -C(=O)-, -S(=O)-, -S(=O) 2 -, -C(=O)NR L1a --, --NR L1a C(=O)-, -S(=O) 2 N.R. L1a -or-NR L1a S (=O) 2 -, where each R L1a are independently hydrogen, a methyl group, an ethyl group, a vinyl group, an ethynyl group, or a trifluoromethyl group; L 2 is one bond, C 1-6 Alkyl group, C 1-6 a heteroalkyl group, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, wherein L 2 The alkyl, heteroalkyl, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in 4 is a carbon or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains for are optionally substituted with one or more substituents, each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, nitrogen protecting groups, or L 1 is one bond, -C(=O)-, -S(=O)-, -S(=O) 2 -, -C(=O)NH-, -NHC(=O)-, -S(=O) 2 NH- or -NHS(=O) 2 - and L 2 is a bond, a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, or a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where L 2 The saturated or partially unsaturated carbocyclyl group and the saturated or partially unsaturated heterocyclyl group in the formula (I) are each optionally substituted by one or more substituents independently selected from a hydroxyl group, an amino group, a cyano group, a fluorine group, a chlorine group, an oxo group, a vinyl group, an ethynyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, and a methylamino group; 3 is a bond, a 6- to 10-membered aryl group, or a 5- to 10-membered heteroaryl group, where L 3 The aryl or heteroaryl groups in are optionally substituted with one or more hydroxyl, amino, cyano, fluorine, chlorine, methyl, ethyl, vinyl, ethynyl, methoxy, ethoxy, trifluoromethoxy, methylamino substituents; L 4 is a carbon or hetero chain having 2 to 4 atoms, where L 4 The carbon or hetero chains for are optionally substituted with one or more substituents, each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, methylamino, nitrogen protecting groups, or L 1 is a bond, —C(═O)— or —C(═O)NH—, and L 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group; L 3 is a bond, a phenyl group or a pyridyl group, L 4 is -NHCH 2 --, --CH 2 NH-, -OCH 2 --, --CH 2 O-, -SCH 2 --, --CH 2 S-, -NHCH 2 CH 2 --, --CH 2 N.H.C.H. 2 --, --CH 2 CH 2 NH-, -OCH 2 CH 2 --, --CH 2 OCH 2 --, --CH 2 CH 2 O-, -SCH 2 CH 2 --, --CH 2 SCH 2 --, --CH 2 CH 2 S-, -NHCH 2 CH 2 CH 2 --, --CH 2 N.H.C.H. 2 CH 2 --, --CH 2 CH 2 N.H.C.H. 2 --, --CH 2 CH 2 CH 2 NH-, -OCH 2 CH 2 CH 2 --, --CH 2 OCH 2 CH 2 --, --CH 2 CH 2 OCH 2 --, --CH 2 CH 2 CH 2 O-, -SCH 2 CH 2 CH 2 --, --CH 2 SCH 2 CH 2 --, --CH 2 CH 2 SCH 2 --, --CH 2 CH 2 CH 2 S-, -CH 2 OCH 2 O-, -OCH 2 OCH 2 --, --OCH 2 CH 2 O-, -NHCH 2 CH 2 O-, -CH 2 N.H.C.H. 2 O- or -NHCH 2 OCH 2 -, where L 4 Related CH 2 hydrogen is optionally replaced by a substituent selected from the group consisting of hydrogen, deuterium, hydroxyl, amino, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, and methylamino; 4 wherein the hydrogen of the NH is optionally replaced, each independently, by a hydrogen, a deuterium, a hydroxyl group, a cyano group, a halogen, an oxo, a vinyl group, an ethynyl group, a methyl group, a ethyl group, a isopropyl group, a methoxy group, a ethoxy group, a trifluoromethoxy group, a nitrogen protecting group substituent; or L 1 is a bond, —C(═O)— or —C(═O)NH—, and L 2 is a bond, a cyclohexyl group, a piperidinyl group, a phenyl group, or a pyridyl group; L 3 is a bond, a phenyl group or a pyridyl group, L 4 is -NHCH 2 --, --CH 2 N.H.C.H. 2 -, -NHC(=O)-, -CH 2 NHC(=O)-, -C(=O)NHCH 2 - or -NHCH(CH 3 )- 2. A compound according to claim 1 or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof.

5. L 5 is -NR L5a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 Heteroalkyl groups, where L 5 The alkyl and heteroalkyl groups in the formula (I) are each optionally independently selected from deuterium, amino, hydroxyl, oxo, cyano, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 haloheteroalkyl groups, each R L5a are independently hydrogen, deuterium, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 is a haloalkyl group or a nitrogen protecting group, and L 6 is -NR L6a -, -O-, -S-, C 1-6 Alkyl group or C 1-6 Heteroalkyl groups, where L 6 The alkyl and heteroalkyl groups in the formula (I) are each optionally independently selected from deuterium, amino, hydroxyl, oxo, cyano, halogen, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 haloheteroalkyl groups, each R L6a are independently hydrogen, deuterium, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 is a haloalkyl group or a nitrogen protecting group, or L 5 is -NR L5a , -CR L5b R L5c -, -O-, -S-, -CR L5b R L5c N.R. L5a --, --NR L5a CR L5b R L5c -, -CR L5b R L5c O-, -OCR L5b R L5c -, -CR L5b R L5c S- or -SCR L5b R L5c -, where each R L5b and R L5c are each independently hydrogen, deuterium, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen, 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L5a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 is a haloalkyl group or a nitrogen protecting group, and L 6 is -NR L6a , -CR L6b R L6c -, -O-, -S-, -CR L6b R L6c N.R. L6a --, --NR L6a CR L6b R L6c -, -CR L6b R L6c O-, -OCR L6b R L6c -, -CR L6b R L6c S- or -SCR L6b R L6c -, where each R L6b and R L6c are each independently hydrogen, deuterium, an amino group, a hydroxyl group, an oxo group, a cyano group, a halogen, 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 is a haloheteroalkyl group, and each R L6a are independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 is a haloalkyl group or a nitrogen protecting group, Or L 5 is -NH-, -O-, -S-, -NHCH 2 --, --OCH 2 -, -SCH 2 --, --CH 2 NH-, -CH 2 O- or -CH 2 S- and L 6 is -NH-, -O-, -S-, -NHCH 2 --, --OCH 2 -, -SCH 2 --, --CH 2 NH-, -CH 2 O- or -CH 2 S-, or L 5 is -NH-, and L 6 is -NH- or -NHCH 2 - characterized in that 2. A compound according to claim 1 or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof.

6. Each R 1 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, C 1-6 Alkoxy group, C 1-6 haloalkoxy group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 an alkyl group, a 6- to 10-membered heteroaryl group, or a 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 1 When R 1 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, alkoxy group, haloalkoxy group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group in the above-mentioned formula (I) may optionally each independently be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; Each R 2 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, C 1-6 Alkoxy group, C 1-6 haloalkoxy group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 an alkyl group, a 6- to 10-membered heteroaryl group, or a 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 2 When R 2 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, alkoxy group, haloalkoxy group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group in the above-mentioned formula (I) may optionally each independently be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups, Each R 3 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group, C 1-6 Alkoxy group, C 1-6 haloalkoxy group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl C 1-6 Alkyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl group, 3- to 6-membered saturated or partially unsaturated heterocyclyl C 1-6 Alkyl group, 6- to 10-membered aryl group, 6- to 10-membered aryl C 1-6 an alkyl group, a 6- to 10-membered heteroaryl group, or a 6- to 10-membered heteroaryl C 1-6 is an alkyl group, and two adjacent R 3 When R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3 The alkyl group, alkenyl group, alkynyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, alkoxy group, haloalkoxy group, saturated or partially unsaturated carbocyclyl group, saturated or partially unsaturated carbocyclylalkyl group, saturated or partially unsaturated heterocyclyl group, saturated or partially unsaturated heterocyclylalkyl group, aryl group, arylalkyl group, heteroaryl group, or heteroarylalkyl group in the above-mentioned formula (I) may optionally each independently be selected from the group consisting of deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 substituted by one or more substituents selected from alkyl groups; or Each R 1 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group or C 1-6 Alkoxy group, C 1-6 A haloalkoxy group, and two adjacent R 1 When R 1 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 1 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above are optionally each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 each R is substituted by one or more substituents selected from alkyl groups; 2 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group or C 1-6 Alkoxy group, C 1-6 A haloalkoxy group, and two adjacent R 2 When R 2 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 2 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above are optionally each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 each R is substituted by one or more substituents selected from alkyl groups; 3 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group, C 1-6 Haloheteroalkyl group or C 1-6 Alkoxy group, C 1-6 A haloalkoxy group, and two adjacent R 3 When R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, a 6- to 10-membered aryl group, or a 6- to 10-membered heteroaryl group, where R 3 The alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, haloheteroalkyl, alkoxy, haloalkoxy, saturated or partially unsaturated carbocyclyl, saturated or partially unsaturated heterocyclyl, aryl or heteroaryl groups in the above are optionally each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 or substituted by one or more substituents selected from alkyl groups; Each R 1 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group or C 1-6 haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group or C 1-6 haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 3 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-6 Alkyl group, C 1-6 Heteroalkyl group, C 1-6 Haloalkyl group or C 1-6 A haloheteroalkyl group, and two adjacent R 3 When R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl group, heteroalkyl group, haloalkyl group, haloheteroalkyl group, 3- to 6-membered saturated or partially unsaturated carbocyclyl group, and 3- to 6-membered saturated or partially unsaturated heterocyclyl group in the above-mentioned formula (I) are each optionally independently selected from deuterium, hydroxyl group, amino group, cyano group, halogen, oxo, C 1-4 or substituted by one or more substituents selected from alkyl groups; Each R 1 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-4 Alkyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 haloheteroalkyl group, where R 1 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 2 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-4 Alkyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 haloheteroalkyl group, where R 2 The alkyl, heteroalkyl, haloalkyl, and haloheteroalkyl groups in 3 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, a halogen, 1-4 Alkyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group or C 1-4 A haloheteroalkyl group, and two adjacent R 3 When R 3 together with the atoms to which they are attached, optionally form a 3- to 6-membered saturated or partially unsaturated carbocyclyl group, a 3- to 6-membered saturated or partially unsaturated heterocyclyl group, where R 3 The alkyl, heteroalkyl, haloalkyl, haloheteroalkyl, 3- to 6-membered saturated or partially unsaturated carbocyclyl, and 3- to 6-membered saturated or partially unsaturated heterocyclyl groups in the formula (I) are optionally substituted by one or more substituents each independently selected from deuterium, hydroxyl, amino, cyano, halogen, oxo, methyl, ethyl, and isopropyl; Each R 1 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, fluorine, chlorine, a methyl group, an ethyl group, a propyl group, an isopropyl group, a t-butyl group, a methoxy group, an ethoxy group, an isopropoxy group, a t-butoxy group, a trifluoromethyl group, a trifluoromethoxy group, a CH 3 C(=O)-, CH 3 CH 2 C(=O)-, (CH 3 ) 2 CHC(=O)-, CH 3 C(=O)O-, CH 3 CH 2 C(=O)O-, (CH 3 ) 2 CHC(=O)O-, CH 3 C(=O)NH-, CH 3 CH 2 C(=O)NH-, (CH 3 ) 2 CHC(=O)NH-,CH 3 NHC(=O)-, CH 3 CH 2 NHC(=O)-, (CH 3 ) 2 CHNHC(=O)-, CH 3 ONHC(=O)-, CH 3 CH 2 ONHC(=O)-, (CH 3 ) 2 CHONHC(=O)-, CH 3 S (=O) 2 -, CH 3 CH 2 S (=O) 2 -, (CH 3 ) 2 CHS(=O) 2 -, CH 3 S (=O) 2 O-, CH 3 CH 2 S (=O) 2 O-, (CH 3 ) 2 CHS(=O) 2 O-, CH 3 S (=O) 2 NH-, CH 3 CH 2 S (=O) 2 NH-、(CH 3 ) 2 CHS(=O) 2 NH-、CH 3 NHS(=O) 2 -、CH 3 CH 2 NHS(=O) 2 -、(CH 3 ) 2 CHNHS(=O) 2 -、CH 3 C(=O)N(CH 3 )-、CH 3 CH 2 C(=O)N(CH 3 )-、(CH 3 ) 2 CHC(=O)N(CH 3 )-、CH 3 N(CH 3 )C(=O)-、CH 3 CH 2 N(CH 3 )C(=O)-、(CH 3 ) 2 CHN(CH 3 )C(=O)-、CH 3 ON(CH 3 )C(=O)-、CH 3 CH 2 ON(CH 3 )C(=O)-、(CH 3 ) 2 CHON(CH 3 )C(=O)-、CH 3 S(=O) 2 N(CH 3 )-、CH 3 CH 2 S(=O) 2 N(CH 3 )-、(CH 3 ) 2 CHS(=O) 2 N(CH 3 )-、CH 3 N(CH 3 )S(=O) 2 -、CH 3 CH 2 N(CH 3 )S(=O) 2 -、(CH 3 ) 2 CHN(CH 3 )S(=O) 2 -、CH 3 C(=O)N(CH 2 CH 3 )-、CH 3 CH 2 C(=O)N(CH 2 CH 3 )-、(CH 3 ) 2 CHC(=O)N(CH 2 CH 3 )-、CH 3 N(CH 2 CH 3 )C(=O)-、CH 3 CH 2 N(CH 2 CH 3 )C(=O)-、(CH 3 ) 2 CHN(CH 2 CH 3 )C(=O)-、CH 3 ON(CH 2 CH 3 )C(=O)-、CH 3 CH 2 ON(CH 2 CH 3 )C(=O)-、(CH 3 ) 2 CHON(CH 2 CH 3 )C(=O)-、CH 3 S(=O) 2 N(CH 2 CH 3 )-、CH 3 CH 2 S(=O) 2 N(CH 2 CH 3 )-、(CH 3 ) 2 CHS(=O) 2 N(CH 2 CH 3 )-、CH 3 N(CH 2 CH 3 )S(=O) 2 -、CH 3 CH 2 N(CH 2 CH 3 )S(=O) 2 -,(CH 3 ) 2 CHN(CH 2 CH 3 )S(=O) 2 -,(CH 3 ) 2 P(=O)-,CH 3 CH 2 (CH 3 )P(=O)-,(CH 3 ) 2 CH(CH 3 )P(=O)-,(CH 3 CH 2 ) 2 P(=O)-,CH 3 CH 2 (CH 3 )P(=O)-or(CH 3 ) 2 CH(CH 3 CH 2 )P(=O)-and Each R 2 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, fluorine, chlorine, bromine, a methyl group, an ethyl group, a propyl group, an isopropyl group, a t-butyl group, a methoxy group, an ethoxy group, an isopropoxy group, a t-butoxy group, a trifluoromethyl group, a trifluoromethoxy group, a CH 3 C(=O)-, CH 3 CH 2 C(=O)-, (CH 3 ) 2 CHC(=O)-, CH 3 C(=O)O-, CH 3 CH 2 C(=O)O-, (CH 3 ) 2 CHC(=O)O-, CH 3 C(=O)NH-, CH 3 CH 2 C(=O)NH-, (CH 3 ) 2 CHC(=O)NH-,CH 3 NHC(=O)-, CH 3 CH 2 NHC(=O)-, (CH 3 ) 2 CHNHC(=O)-, CH 3 ONHC(=O)-, CH 3 CH 2 ONHC(=O)-, (CH 3 ) 2 CHONHC(=O)-, CH 3 S (=O) 2 -, CH 3 CH 2 S (=O) 2 -, (CH 3 ) 2 CHS(=O) 2 -, CH 3 S (=O) 2 O-, CH 3 CH 2 S (=O) 2 O-, (CH 3 ) 2 CHS(=O) 2 O-, CH 3 S (=O) 2 NH-, CH 3 CH 2 S(=O) 2 NH-、(CH 3 ) 2 CHS(=O) 2 NH-、CH 3 NHS(=O) 2 -、CH 3 CH 2 NHS(=O) 2 -、(CH 3 ) 2 CHNHS(=O) 2 -、CH 3 C(=O)N(CH 3 )-、CH 3 CH 2 C(=O)N(CH 3 )-、(CH 3 ) 2 CHC(=O)N(CH 3 )-、CH 3 N(CH 3 )C(=O)-、CH 3 CH 2 N(CH 3 )C(=O)-、(CH 3 ) 2 CHN(CH 3 )C(=O)-、CH 3 ON(CH 3 )C(=O)-、CH 3 CH 2 ON(CH 3 )C(=O)-、(CH 3 ) 2 CHON(CH 3 )C(=O)-、CH 3 S(=O) 2 N(CH 3 )-、CH 3 CH 2 S(=O) 2 N(CH 3 )-、(CH 3 ) 2 CHS(=O) 2 N(CH 3 )-、CH 3 N(CH 3 )S(=O) 2 -、CH 3 CH 2 N(CH 3 )S(=O) 2 -、(CH 3 ) 2 CHN(CH 3 )S(=O) 2 -、CH 3 C(=O)N(CH 2 CH 3 )-、CH 3 CH 2 C(=O)N(CH 2 CH 3 )-、(CH 3 ) 2 CHC(=O)N(CH 2 CH 3 )-、CH 3 N(CH 2 CH 3 )C(=O)-、CH 3 CH 2 N(CH 2 CH 3 )C(=O)-、(CH 3 ) 2 CHN(CH 2 CH 3 )C(=O)-、CH 3 ON(CH 2 CH 3 )C(=O)-、CH 3 CH 2 ON(CH 2 CH 3 )C(=O)-、(CH 3 ) 2 CHON(CH 2 CH 3 )C(=O)-、CH 3 S(=O) 2 N(CH 2 CH 3 )-、CH 3 CH 2 S(=O) 2 N(CH 2 CH 3 )-、(CH 3 ) 2 CHS(=O) 2 N(CH 2 CH 3 )-、CH 3 N(CH 2 CH 3 )S(=O) 2 -、CH 3 CH 2 N(CH 2 CH 3 )(S(=O) 2 -), (CH 3 )) 2 CHN(CH 2 CH 3 ))(S(=O) 2 -), (CH 3 )) 2 P(=O)-, CH 3 CH 2 (CH 3 ))P(=O)-, (CH 3 )) 2 CH(CH 3 ))P(=O)-, (CH 3 CH 2 )) 2 P(=O)-, CH 3 CH 2 (CH 3 ))P(=O)- or (CH 3 )) 2 CH(CH 3 CH 2 ))P(=O)- and Each R 3 are independently hydrogen, deuterium, an amino group, a hydroxyl group, a cyano group, fluorine, chlorine, a methyl group, an ethyl group, a propyl group, an isopropyl group, a t-butyl group, a methoxy group, an ethoxy group, an isopropoxy group, a t-butoxy group, a trifluoromethyl group, a trifluoromethoxy group, a CH 3 C(=O)-, CH 3 CH 2 C(=O)-, (CH 3 ) 2 CHC(=O)-, CH 3 C(=O)O-, CH 3 CH 2 C(=O)O-, (CH 3 ) 2 CHC(=O)O-, CH 3 C(=O)NH-, CH 3 CH 2 C(=O)NH-, (CH 3 ) 2 CHC(=O)NH-,CH 3 NHC(=O)-, CH 3 CH 2 NHC(=O)-, (CH 3 ) 2 CHNHC(=O)-, CH 3 ONHC(=O)-, CH 3 CH 2 ONHC(=O)-, (CH 3 ) 2 CHONHC(=O)-, CH 3 S (=O) 2 -, CH 3 CH 2 S (=O) 2 -, (CH 3 ) 2 CHS(=O) 2 -, CH 3 S (=O) 2 O-, CH 3 CH 2 S (=O) 2 O-, (CH 3 ) 2 CHS(=O) 2 O-, CH 3 S (=O) 2 NH-, CH 3 CH 2 S (=O) 2 NH-、(CH 3 ) 2 CHS(=O) 2 NH-、CH 3 NHS(=O) 2 -、CH 3 CH 2 NHS(=O) 2 -、(CH 3 ) 2 CHNHS(=O) 2 -、CH 3 C(=O)N(CH 3 )-、CH 3 CH 2 C(=O)N(CH 3 )-、(CH 3 ) 2 CHC(=O)N(CH 3 )-、CH 3 N(CH 3 )C(=O)-、CH 3 CH 2 N(CH 3 )C(=O)-、(CH 3 ) 2 CHN(CH 3 )C(=O)-、CH 3 ON(CH 3 )C(=O)-、CH 3 CH 2 ON(CH 3 )C(=O)-、(CH 3 ) 2 CHON(CH 3 )C(=O)-、CH 3 S(=O) 2 N(CH 3 )-、CH 3 CH 2 S(=O) 2 N(CH 3 )-、(CH 3 ) 2 CHS(=O) 2 N(CH 3 )-、CH 3 N(CH 3 )S(=O) 2 -、CH 3 CH 2 N(CH 3 )S(=O) 2 -、(CH 3 ) 2 CHN(CH 3 )S(=O) 2 -、CH 3 C(=O)N(CH 2 CH 3 )-、CH 3 CH 2 C(=O)N(CH 2 CH 3 )-、(CH 3 ) 2 CHC(=O)N(CH 2 CH 3 )-、CH 3 N(CH 2 CH 3 )C(=O)-、CH 3 CH 2 N(CH 2 CH 3 )C(=O)-、(CH 3 ) 2 CHN(CH 2 CH 3 )C(=O)-、CH 3 ON(CH 2 CH 3 )C(=O)-、CH 3 CH 2 ON(CH 2 CH 3 )C(=O)-、(CH 3 ) 2 CHON(CH 2 CH 3 )C(=O)-、CH 3 S(=O) 2 N(CH 2 CH 3 )-、CH 3 CH 2 S(=O) 2 N(CH 2 CH 3 )-、(CH 3 ) 2 CHS(=O) 2 N(CH 2 CH 3 )-、CH 3 N(CH 2 CH 3 )S(=O) 2 -、CH 3 CH 2 N(CH 2 CH 3 ) S(=O) 2 -, (CH 3 ) 2 CHN (CH 2 CH 3 ) S(=O) 2 -, (CH 3 ) 2 P(=O)-, CH 3 CH 2 (CH 3 )P(=O)-, (CH 3 ) 2 CH (CH 3 )P(=O)-, (CH 3 CH 2 ) 2 P(=O)-, CH 3 CH 2 (CH 3 ) P(=O)- or (CH 3 ) 2 CH (CH 3 CH 2 ) P(=O)-, and two adjacent R 3 When R 3 together with the atoms to which they are attached, and optionally 、 、 、 、 、 、 、 、 or The present invention is characterized in that A compound according to any one of claims 1 to 5, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt or prodrug thereof.

7. the saturated or partially unsaturated carbocyclyl group is selected from formulae ii-1 to ii-6, where ii-1 to ii-6 are monovalent when ii-1 to ii-6 are linked to the remainder of the molecule by one bond, and ii-1 to ii-6 are divalent when ii-1 to ii-6 are linked to the remainder of the molecule by two bonds; and the saturated or partially unsaturated carbocyclyl groups represented by formulae ii-1 to ii-6 are optionally substituted, each independently, by one or more substituents as defined in the corresponding claim above; 、 、 、 、 or The saturated or partially unsaturated heterocyclyl group is selected from formulae iii-1 to iii-16, where formulae iii-1 to iii-16 are monovalent when they are linked to the remainder of the molecule by one bond, and where formulae iii-1 to iii-16 are divalent when they are linked to the remainder of the molecule by two bonds, and the saturated or partially unsaturated heterocyclyl groups represented by formulae iii-1 to iii-16 are optionally substituted, each independently, by one or more substituents as defined in the corresponding claim above; 、 、 、 、 、 、 、 、 、 、 、 、 、 、 or 、 wherein each t1 is independently 0, 1, 2, 3, 4, or 5, and each t2 and t3 is independently 1, 2, 3, 4, or 5; or the saturated or partially unsaturated carbocyclyl group is selected from the following groups, which are monovalent when the saturated or partially unsaturated carbocyclyl group is linked to the remainder of the molecule by one bond, and which are divalent when the saturated or partially unsaturated carbocyclyl group is linked to the remainder of the molecule by two bonds, and each of the saturated or partially unsaturated carbocyclyl groups represented below is optionally substituted, each independently, by one or more substituents as defined in the corresponding claim above, 、 The saturated or partially unsaturated heterocyclyl group is selected from the following groups, which are monovalent when the saturated or partially unsaturated heterocyclyl group is linked to the remainder of the molecule by one bond, and which are divalent when the saturated or partially unsaturated heterocyclyl group is linked to the remainder of the molecule by two bonds, and wherein the saturated or partially unsaturated heterocyclyl groups represented below are optionally substituted, each independently, by one or more substituents as defined in the corresponding claim above. A compound according to any one of claims 1 to 6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt or prodrug thereof.

8. The compound is a compound represented by any one of formulas II-1 to II-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitrogen oxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof; Formula II-1: Formula II-2: Formula II-3: Formula II-4: Formula II-5: Formula II-6: wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, said 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally containing deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group, C 1-4 Haloheteroalkyl group, C 1-4 Alkoxy group or C 1-4 substituted by one or more substituents selected from haloalkoxy groups; The compound according to any one of claims 1 to 7.

9. The compound is a compound of formula III or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof, Formula III: Here, R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group; L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, L4b and R L4c optionally forms an oxo, R L4d and R L4e optionally forms an oxo; and k and v are each independently 0, 1, or 2. The compound according to any one of claims 1 to 7.

10. The compound is a compound represented by any one of formulas IV-1 to IV-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitrogen oxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof; Formula IV-1: Formula IV-2: Formula IV-3: Formula IV-4: Formula IV-5: or Formula IV-6: wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, said 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally containing deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group, C 1-4 Haloheteroalkyl group, C 1-4 Alkoxy group or C 1-4 haloalkoxy groups; R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group; L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, L4b and R L4c optionally forms an oxo, R L4d and R L4e optionally forms an oxo; and k and v are each independently 0, 1, or 2. The compound according to any one of claims 1 to 7.

11. The compound is a compound represented by any one of formulas V-1 to V-7, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitrogen oxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof. The compound according to any one of claims 1 to 7. Formula V-1: Formula V-2: Formula V-3: Formula V-4: Formula V-5: Formula V-6: or Formula V-7:

12. The compound is a compound represented by any one of formulas VI-1 to VI-5, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitrogen oxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof. The compound according to any one of claims 1 to 7. Formula VI-1: Formula VI-2: Formula VI-3: Formula VI-4: or Formula VI-5:

13. The compound is a compound represented by any one of formulas VII-1 to VII-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof; Formula VII-1: Formula VII-2: Formula VII-3: Formula VII-4: Formula VII-5: or Formula VII-6: wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, said 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally containing deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group, C 1-4 Haloheteroalkyl group, C 1-4 Alkoxy group or C 1-4 haloalkoxy groups; R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group; L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, L4b and R L4c optionally forms an oxo, R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1 or 2. The compound according to any one of claims 1 to 7.

14. The compound is a compound represented by any one of formulas VIII-1 to VIII-6, or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitrogen oxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof; Formula VIII-1: Formula VIII-2: Formula VIII-3: Formula VIII-4: Formula VIII-5: or Formula VIII-6: wherein B is a 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group, said 3- to 6-membered saturated or partially unsaturated N-containing heterocyclyl group optionally containing deuterium, hydroxyl, amino, cyano, halogen, oxo, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Heteroalkyl group, C 1-4 Haloalkyl group, C 1-4 Haloheteroalkyl group, C 1-4 Alkoxy group or C 1-4 haloalkoxy groups; R L4a is hydrogen, deuterium, hydroxyl, cyano, halogen, oxo, vinyl, ethynyl, methyl, ethyl, isopropyl, methoxy, ethoxy, trifluoromethoxy, or a nitrogen protecting group; L4b , R L4c , R L4d and R L4e are each independently hydrogen, deuterium, a hydroxyl group, an amino group, a cyano group, a halogen, a vinyl group, an ethynyl group, a methyl group, an ethyl group, an isopropyl group, a methoxy group, an ethoxy group, a trifluoromethoxy group, or a methylamino group, L4b and R L4c optionally forms an oxo, R L4d and R L4e optionally forms an oxo, G 1 and G 2 are each independently CH or N, and k and v are each independently 0, 1 or 2. The compound according to any one of claims 1 to 7.

15. The compound is characterized in that it is a compound shown below or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt, or prodrug thereof. The compound according to any one of claims 1 to 14.

16. 1. A pharmaceutical composition comprising:

16. A pharmaceutical composition comprising a compound according to any one of claims 1 to 15 or a stereoisomer, tautomer, enantiomer, diastereomer, racemate, geometric isomer, nitroxide, solvate, hydrate, crystal form, ester, isotopically labeled compound (preferably deuterated), metabolite, pharma- ceutically acceptable salt or prodrug thereof, and a pharma- ceutically acceptable excipient thereof.

17. Use of a compound according to any one of claims 1 to 15 or a pharmaceutical composition according to claim 16 in the preparation of a medicament for preventing or treating a FAK-related disease.

18. The FAK-related disease is selected from cancer, pulmonary arterial hypertension, or pathological angiogenesis, and preferably, the cancer comprises lung cancer, bone cancer, pancreatic cancer, skin cancer, head and neck cancer, cutaneous or intraocular melanoma, uterine cancer, ovarian cancer, rectal cancer, cancer of the anal region, gastric cancer, colon cancer, breast cancer, uterine cancer, fallopian tube cancer, endometrial cancer, cervical cancer, trichilemmal carcinoma, vulvar cancer, Hodgkin's disease, esophageal cancer, small intestine cancer, endocrine system cancer, thyroid cancer, parathyroid cancer, adrenal cancer, soft tissue sarcoma, urethral cancer, penile cancer, prostate cancer, chronic or acute leukemia, lymphocytic lymphoma, bladder cancer, kidney or ureter cancer, renal cell carcinoma, renal pelvis cancer, central nervous system (CNS) tumor, primary CNS lymphoma, spinal axis cancer, brain stem glioma, pituitary adenoma, or a combination of one or more of the aforementioned cancers.

18. The use according to claim 17.

19. Use of a compound according to any one of claims 1 to 15 or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite or a pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof, or a pharmaceutical composition according to claim 16, in the preparation of a medicament for modulating or treating a YAP-related disease, comprising Preferably, the YAP-related disease is selected from cancer, including skin cancer, bone cancer, glioma, breast cancer, adrenal gland cancer, bladder cancer, esophageal cancer, head and neck cancer, liver cancer, parathyroid cancer, penile cancer, small intestine cancer, thyroid cancer, urethral cancer, cervical cancer, endometrial cancer, fallopian tube cancer, renal pelvis cancer, vaginal cancer, vulvar cancer, chronic or acute leukemia, colon cancer, melanoma, hematological malignancies, Hodgkin's lymphoma, lung cancer, lymphocytic lymphoma, central nervous system tumors (CNS), ovarian cancer, pancreatic cancer, pituitary adenoma, prostate cancer, soft tissue sarcoma, gastric cancer, and uterine cyst. and more preferably, the cancer is selected from one or more of lung cancer, colon cancer, ovarian cancer, prostate cancer, and liver cancer.

20. Use of a compound according to any one of claims 1 to 15 or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite or a pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof or a pharmaceutical composition according to claim 16 in the preparation of a medicament for modulating or treating a FAK and YAP-related disease, comprising Use of a compound according to any one of claims 1 to 15 or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite or a pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof or a pharmaceutical composition according to claim 16 in the preparation of a medicament for regulating or treating a FAK- and YAP-associated disease, preferably characterized in that the FAK- and YAP-associated disease is selected from cancer.

21. 1. A method for modulating the Hippo-YAP signaling pathway, comprising: A method for regulating the Hippo-YAP signaling pathway, comprising administering a compound according to any one of claims 1 to 15, or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite, or a pharma- ceutically acceptable salt, hydrate, isotope, or prodrug thereof, or a pharmaceutical composition according to claim 16.

22. Use of the compound according to any one of claims 1 to 15 or its enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite or pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof or the pharmaceutical composition according to claim 16 in the preparation of a Hippo-YAP signaling pathway inhibitor.

23. A method for preventing or treating a YAP-associated disease, comprising: Administering a compound according to any one of claims 1 to 15 or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite or a pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof, or a pharmaceutical composition according to claim 16, Preferably, the method for preventing or treating a YAP-associated disease is characterized in that the YAP-associated disease includes one or a combination of two or more of skin cancer, bone cancer, glioma, breast cancer, adrenal cancer, bladder cancer, esophageal cancer, head and neck cancer, liver cancer, parathyroid cancer, penile cancer, small intestine cancer, thyroid cancer, urethral cancer, cervical cancer, endometrial cancer, fallopian tube cancer, renal pelvis cancer, vaginal cancer, vulvar cancer, chronic or acute leukemia, colon cancer, melanoma, hematological malignancies, Hodgkin's lymphoma, lung cancer, lymphocytic lymphoma, central nervous system tumors (CNS), ovarian cancer, pancreatic cancer, pituitary adenoma, prostate cancer, soft tissue sarcoma, gastric cancer, and uterine cancer.

24. A method for preventing or treating a FAK-related disease, comprising: A method for preventing or treating a FAK-associated disease, comprising administering a compound according to any one of claims 1 to 15, or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite, or a pharma- ceutically acceptable salt, hydrate, isotope, or prodrug thereof, or a pharmaceutical composition according to claim 16, wherein the FAK-associated disease is preferably selected from cancer, pulmonary arterial hypertension, or pathological angiogenesis.

25. 1. A method for inhibiting FAK kinase and / or YAP protein activity in a cell or a subject, comprising:

17. A method for inhibiting FAK kinase and / or YAP protein activity in a cell or a subject, the method comprising contacting a cell with a compound of any one of claims 1 to 15 or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitroxide, metabolite or a pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof, or a pharmaceutical composition of claim 16, or administering to a subject a compound of any one of claims 1 to 15 or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitroxide, metabolite or a pharma- ceutically acceptable salt, hydrate, isotope or prodrug thereof, or a pharmaceutical composition of claim 16.

26. A process for the preparation of a compound according to any one of claims 1 to 15, comprising the steps of: It comprises one or more of the following steps (1) to (3), or it comprises one or more of the following steps (4) to (9), (1) reacting a compound of formula a1 with a compound of formula a2 to produce a compound of formula a3; (2) reacting a compound of formula a3 with a compound of formula a4 to produce a compound of formula a5; (3) reacting a compound of formula a5 with a compound of formula a6 to produce a compound of formula a7; (4) reacting a compound of formula b1 with a compound of formula b2 to produce a compound of formula b3; (5) converting the compound of formula b3 to a compound of formula b4; (6) converting the compound of formula b4 to a compound of formula b5; (7) reacting the compound of formula b5 with a compound of formula b3 to form a compound of formula b6; (8) converting the compound of formula b6 to a compound of formula b7; (9) converting the compound of formula b7 to a compound of formula b8; wherein Hal is a halogen, Cy represents various ring systems, preferably 3- to 6-membered saturated or partially unsaturated carbocyclyl groups, 3- to 6-membered saturated or partially unsaturated heterocyclyl groups, 6- to 10-membered aryl groups, or 5- to 10-membered heteroaryl groups, Pg represents a protecting group, A, R 1 , R 2 , R 3 , R 4 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , L 1 , L 2 , L 5 , L 6 16. A process for the preparation of a compound according to any one of claims 1 to 15, characterized in that M, n, m, p are as defined in claim 1.

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