Macrocyclic EGFR Inhibitors, Their Manufacturing Methods, and Applications in Pharmacy

Abstract

The present invention relates to macrocyclic EGFR inhibitors, methods for their production, and applications in pharmacy. In particular, the present invention relates to EGFR inhibitors having the structure of formula (I), their pharmaceutical compositions, their use as EGFR inhibitors, and their use in the manufacture of drugs for treating and / or preventing tumors or metastatic diseases that are at least partially related to EGFR L858R / C797S double mutations, EGFR Del19 / C797S double mutations, L858R / T790M / C797S triple mutations, and Del19 / T790M / C797S triple mutations, especially their use in the manufacture of drugs for treating and / or preventing hyperproliferative diseases and cell death induction disorder diseases. The definition of each substituent in formula (I) is the same as the definition in the specification. JPEG2025524038000148.jpg6074

Description

Technical Field

[0001] The present invention belongs to the field of drug synthesis, and specifically relates to a macrocyclic EGFR inhibitor, a method for producing the same, and an application in pharmacy.

Background Art

[0002] Lung cancer is the most lethal malignant tumor in the world, seriously threatening human health. Among them, non-small-cell lung cancer (NSCLC) accounts for about 85% of all lung cancers. At present, it has been confirmed that multiple molecular mechanisms such as gene mutations and abnormal expressions are related to the onset of NSCLC. However, EGFR is the main driver gene. The frequency of EGFR activating mutations in global NSCLC patients is about 17%, and the East Asian population is more sensitive, with a mutation frequency of about 50%. EGFR activating mutations mainly occur in exons 18-21, and the deletion mutation of exon 19 (Del19) and the L858R point mutation of exon 21 are the most common mutation subtypes, accounting for more than 80% of all mutation types. These mutations can cause ligand-independent activation of the receptor and promote the survival and proliferation of tumor cells. The first and second generations of EGFR tyrosine kinase inhibitors (TKIs) are mainly for these two activating mutations. Compared with platinum-based chemotherapy, the first and second generations of EGFR TKIs can significantly extend the progression-free survival period, but drug resistance often occurs after 10-12 months of administration. The EGFR T790M mutation is the main mechanism of resistance to the first and second generations of EGFR TKIs. Subsequently, the third-generation EGFR TKI osimertinib was developed to selectively inhibit EGFR T790M and common mutations of EGFR. In the results of the Phase III clinical FLAURA study, osimertinib showed a better therapeutic effect against the first-generation EGFR TKI, significantly improving the progression-free survival period (18.9 months vs. 10.2 months) and overall survival rate (38.6 months vs. 31.8 months), thereby directly promoting osimertinib to enter the first-choice therapy.

[0003] Despite the remarkable therapeutic effect of osimertinib, drug resistance inevitably appears and leads to the progression of the disease. Currently, there is no approved targeted therapeutic drug for patients with osimertinib resistance. Several EGFR-dependent and independent drug resistance mechanisms have been reported in both preclinical and clinical studies. The C797X (C797S is the most common) mutation in exon 20 has already become the most common EGFR-dependent osimertinib resistance mechanism. The C797X mutation is located in the tyrosine kinase domain of EGFR, which prevents osimertinib from forming a covalent bond within the ATP-binding domain of EGFR, resulting in drug resistance. In the phase III clinical AURA3 trial, the probability of the C797X mutation in patients receiving second-line treatment with osimertinib is 15%, while in the phase III clinical FLAURA trial, the probability of the C797X mutation in patients receiving first-line treatment with osimertinib is 7%. Therefore, the development of more potent and selective EGFR next-generation inhibitors targeting the double mutations consisting of EGFR activation mutation / C797S and the triple mutations consisting of EGFR activation mutation / T790M / C797S is extremely important for patients with resistance who use osimertinib as the first or second choice.

Summary of the Invention

[0004] An object of the present invention is to provide a macrocyclic EGFR inhibitor, a method for producing the same, and an application in pharmacy. A series of compounds of the present invention have a strong inhibitory effect on the cytological activities of EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation, and Del19 / T790M / C797S triple mutation, and are drugs for treating and / or preventing tumors or metastatic diseases at least partially related to EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation, and Del19 / T790M / C797S triple mutation, and can be widely applied to the manufacture of drugs for treating, in particular, hyperproliferative diseases and cell death induction disorder diseases, and the development of a new generation of EGFR inhibitors is expected.

[0005] The first aspect of the present invention provides a compound of formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof,

Chemical formula

[0006] R1 is hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C2-10 Alkenyl group, C 2-10 Alkynyl group, C 3-12 Cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 Aryl group, 5- to 10-membered heteroaryl group, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-O-S(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-O-R 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-S-C(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, wherein each of said groups is independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 Alkyl group, C 2-10 Alkenyl group, C 2-10 Alkynyl group, C3-12 Cycloalkyl group, 3- to 12-membered heterocyclic group, C 3-12 C substituted with a cycloalkyl group 1-10 C substituted with an alkyl group, 3- to 12-membered heterocyclic group 1-10 Alkyl group, C 6-10 Aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-N(R 13 )-S(O)2R 10 , -C 0-8 Alkyl-O-S(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-O-R 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-S-C(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12substituted with one or more substituents selected from the group consisting of, said groups being each independently optionally further one or more deuteriums, halogens, cyano groups, nitro groups, azide groups, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-N(R 13 )-S(O)2R 10 , -C 0-8 alkyl-O-S(O)2R 10 , -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with a substituent selected from the group consisting of,

[0007] each R2 is independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 and -C 0-8 alkyl-S(O) r R 10 and -C 0-8 alkyl-O-R 11 and -C 0-8 alkyl-C(O)OR 11 and -C 0-8 alkyl-C(O)SR 11 and -C 0-8 alkyl-S-C(O)R 12 and -C 0-8 alkyl-C(O)R 12 and -C 0-8 alkyl-O-C(O)R 12 and -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 and -C 0-8 alkyl-C(=NR 13 )R 12 and -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 and -C0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, said groups each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3-12 membered heterocyclic group, C 6-10 aryl group, 5-10 membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 and -C 0-8 alkyl-S(O) r R 10 and -C 0-8 alkyl-O-R 11 and -C 0-8 alkyl-C(O)OR 11 and -C 0-8 alkyl-C(O)SR 11 and -C 0-8 alkyl-S-C(O)R 12 and -C 0-8 alkyl-C(O)R 12 and -C 0-8 alkyl-O-C(O)R 12 and -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 and -C 0-8 alkyl-C(=NR 13 )R 12 and -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R12 、 -C 0-8 alkyl - C(O)NR 13 R 14 and -C 0-8 alkyl - N(R 13 ) - C(O)R 12 substituted with one or more substituents selected from the group consisting of,

[0008] each R3, R a and R b is independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen - substituted C 1-10 alkyl group, deuterium - substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3 - 12 - membered heterocyclic group, C 6-10 aryl group, 5 - 10 - membered heteroaryl group, -C 0-8 alkyl - SF5, -C 0-8 alkyl - S(O)(=N - R7)R8, -C 0-8 alkyl - N=S(O)R8R9, -C 0-8 alkyl - N=SR8R9, -C 0-8 alkyl - O - S(O)2R 10 、 -C 0-8 alkyl - S(O) r R 10 、 -C 0-8 alkyl - O - R 11 、 -C 0-8 alkyl - C(O)OR 11 、 -C 0-8 alkyl - C(O)SR 11 、 -C 0-8 alkyl - S - C(O)R 12 、 -C 0-8 alkyl - C(O)R 12 、 -C 0-8 alkyl - O - C(O)R 12 、 -C 0-8 alkyl - P(O)(R 12 )2、 -C 0-8 alkyl - NR 13 R 14 、 -C 0-8alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of,

[0009] R4 and R c are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 )2、-C0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 is selected from the group consisting of

[0010] R d is hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 Alkyl group, halogen-substituted C 1-10 Alkyl group, deuterium substituted C 1-10 Alkyl group, C 2-10 Alkenyl group, C 2-10 Alkynyl group, C 3-12 Cycloalkyl groups, 3-12 membered heterocyclic groups, C 6-10 Aryl groups, 5-10 membered heteroaryl groups, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-OS(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-OR 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-SC(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-OC(O)R12 , -C 0-8 alkyl - P(O)(R 12 )2, -C 0-8 alkyl - NR 13 R 14 , -C 0-8 alkyl - C(=NR 13 )R 12 , -C 0-8 alkyl - N(R 13 ) - C(=NR 14 )R 12 , -C 0-8 alkyl - C(O)NR 13 R 14 and -C 0-8 alkyl - N(R 13 ) - C(O)R 12 selected from the group consisting of, R 5a and R 5b are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3 - 12 membered heterocyclic group, C 6-10 aryl group, 5 - 10 membered heteroaryl group, -C 0-8 alkyl - SF5, -C 0-8 alkyl - S(O)(=N - R7)R8, -C 0-8 alkyl - N=S(O)R8R9, -C 0-8 alkyl - N=SR8R9, -C 0-8 alkyl - O - S(O)2R 10 , -C 0-8 alkyl - S(O) r R 10 , -C 0-8 alkyl - O - R 11 , -C 0-8 alkyl - C(O)OR 11 , -C 0-8 alkyl - C(O)SR 11 , -C 0-8 alkyl - S - C(O)R 12 , -C 0-8 alkyl - C(O)R 12 , -C 0-8 alkyl - O - C(O)R12 , -C 0-8 alkyl - P(O)(R 12 )2, -C 0-8 alkyl - NR 13 R 14 , -C 0-8 alkyl - C(=NR 13 )R 12 , -C 0-8 alkyl - N(R 13 ) - C(=NR 14 )R 12 , -C 0-8 alkyl - C(O)NR 13 R 14 and -C 0-8 alkyl - N(R 13 ) - C(O)R 12 selected from the group consisting of, or R 5a and R 5b together with the carbon atom directly connected thereto form C(O), C 3-6 cycloalkyl group, 4 - 10 membered heterocyclic group, C 6-10 aryl group or 5 - 10 membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen - substituted C 1-10 alkyl group, deuterium - substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3 - 12 membered heterocyclic group, C 6-10 aryl group, 5 - 10 membered heteroaryl group, =O, =S, -C 0-8 alkyl - SF5, -C 0-8 alkyl - S(O)(=N - R7)R8, -C 0-8 alkyl - N=S(O)R8R9, -C 0-8 alkyl - N=SR8R9, -C 0-8 alkyl - O - S(O)2R 10 , -C 0-8 alkyl - S(O) r R 10 , -C 0-8 alkyl - O - R 11 , -C 0-8 alkyl - C(O)OR 11, -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of:

[0011] each R 5c and R 5d is independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3 - 12 membered heterocyclic group, C 6-10 aryl group, 5 - 10 membered heteroaryl group, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 , -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11, -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or, R 5c and R 5d together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, a 4- to 10-membered heterocyclic group, a C 6-10 aryl group or a 5- to 10-membered heteroaryl group, said groups each independently optionally further being deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, a 3- to 12-membered heterocyclic group, a C 6-10 aryl group, a 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8Alkyl-N=SR8R9, -C 0-8 Alkyl-O-S(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-O-R 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-S-C(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, provided that when 5c R 5d or R 1-4 is H or a C 2-10 alkyl group, R1 is an optionally substituted C

[0012] R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C3-12 Cycloalkyl groups, 3-12 membered heterocyclic groups, C 6-10 Aryl groups, 5-10 membered heteroaryl groups, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-OS(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-OR 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-SC(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-OC(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 or R 5e and R 5f C together with the carbon atoms directly connected to them 3-6 Cycloalkyl groups, 4-10 membered heterocyclic groups, C 6-10forms an aryl group or a 5- to 10-membered heteroaryl group, and each said group is independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 )2、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of

[0013] R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 )2、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5g and R 5h together with the carbon atom directly connected thereto form a C 3-6 cycloalkyl group, a 4- to 10-membered heterocyclic group, a C 6-10 aryl group or a 5- to 10-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, a 3- to 12-membered heterocyclic group, a C 6-10 aryl group, a 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 , -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0- 8alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of

[0014] R 6a is hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3- to 6-membered heterocyclic groups and -OR 11 wherein each of said groups is independently optionally further selected from the group consisting of deuterium, halogen, cyano, hydroxyl, ═O, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium substituted C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 1-4 Alkoxy group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group, and -NR 13 R 14 and is substituted with one or more substituents selected from the group consisting of: R 6b are hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3- to 6-membered heterocyclic groups and -OR 11 wherein each of said groups is independently optionally further selected from the group consisting of deuterium, halogen, cyano, hydroxyl, ═O, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium substituted C1-4 an alkyl group, C 2-4 an alkenyl group, C 2-4 an alkynyl group, C 1-4 an alkoxy group, C 3-6 a cycloalkyl group, C 3-6 a cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, and -NR 13 R 14 substituted with one or more substituents selected from the group consisting of R 6c is hydrogen, deuterium, C 1-4 an alkyl group, C 2-4 an alkenyl group, C 2-4 an alkynyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group, and -O-R 11 selected from the group consisting of, and the groups are each independently optionally further deuterium, halogen, cyano group, hydroxyl group, =O, C 1-4 an alkyl group, halogen-substituted C 1-4 an alkyl group, deuterium-substituted C 1-4 an alkyl group, C 2-4 an alkenyl group, C 2-4 an alkynyl group, C 1-4 an alkoxy group, C 3-6 a cycloalkyl group, C 3-6 a cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, and -NR 13 R 14 substituted with one or more substituents selected from the group consisting of

[0015] each R7 is independently hydrogen, deuterium, C 1-10 an alkyl group, C 2-10 an alkenyl group, C 2-10 an alkynyl group, C 3-10 a cycloalkyl group, a 3- to 10-membered heterocyclic group, C 6-10 an aryl group, a 5- to 10-membered heteroaryl group, -C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)R 12 or -C 0-8Alkyl-C(O)NR 13 R 14 selected from the group consisting of, said group optionally further comprising deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 or -C 0-8 alkyl-N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of,

[0016] each of R8 and R9 is independently hydrogen, deuterium, hydroxyl group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10Selected from the group consisting of an aryl group or a 5- to 10-membered heteroaryl group, or R8 and R9 together with the sulfur atom directly connecting thereto form a 3- to 10-membered heterocyclic group, and said group is optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 or -C 0-8 alkyl-N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of

[0017] Each R 10 is independently hydrogen, deuterium, hydroxyl group, C 1-10 alkyl group, C 2-10 alkenyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10An aryl group, a 5- to 10-membered heteroaryl group, and -NR 13 R 14 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, hydroxyl group, =O, C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, a 3- to 12-membered heterocyclic group, a 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, a 5- to 10-membered heteroaryl group, a 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 selected from the group consisting of one or more substituents,

[0018] each R 11 is independently hydrogen, deuterium, C 1-10 alkyl group, C 2-10 alkenyl group, C 3-12 cycloalkyl group, a 3- to 12-membered heterocyclic group, C 6-10 aryl group, and a 5- to 10-membered heteroaryl group selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, hydroxyl group, =O, cyano group, C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, a 3- to 12-membered heterocyclic group, a 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, a 5- to 10-membered heteroaryl group, a 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 selected from the group consisting of one or more substituents,

[0019] each R 12 is independently hydrogen, deuterium, hydroxyl group, C 1-10 alkyl group, C 1-10 alkoxy group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12a cycloalkyl group, C 3-12 a cycloalkoxy group, a 3- to 12-membered heterocyclic group, a 3- to 12-membered heterocyclic oxy group, C 6-10 an aryl group, C 6-10 an aryloxy group, a 5- to 10-membered heteroaryl group, a 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 selected from the group consisting of, and each said group is independently optionally further deuterium, halogen, hydroxyl group, =O, cyano group, C 1-10 an alkyl group, C 1-10 an alkoxy group, C 3-12 a cycloalkyl group, C 3-12 a cycloalkoxy group, a 3- to 12-membered heterocyclic group, a 3- to 12-membered heterocyclic oxy group, C 6-10 an aryl group, C 6-10 an aryloxy group, a 5- to 10-membered heteroaryl group, a 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 substituted with one or more substituents selected from the group consisting of,

[0020] each R 13 and R 14 is independently hydrogen, deuterium, hydroxyl group, C 1-10 an alkyl group, C 2-10 an alkenyl group, C 2-10 an alkynyl group, C 3-12 a cycloalkyl group, a 3- to 12-membered heterocyclic group, C 6-10 an aryl group, a 5- to 10-membered heteroaryl group, a sulfinyl group, a sulfonyl group, a methylsulfonyl group, an isopropylsulfonyl group, a cyclopropylsulfonyl group, a p-toluenesulfonyl group, an aminosulfonyl group, a dimethylaminosulfonyl group, and C 1-10 an alkanoyl group, and each said group is independently optionally further deuterium, halogen, hydroxyl group, =O, C 1-10 an alkyl group, C 2-10 an alkenyl group, C 2-10 an alkynyl group, a halogen-substituted C 1-10 an alkyl group, a deuterium-substituted C 1-10 an alkyl group, C 1-10 an alkoxy group, C 3-12A cycloalkyl group, C 3-12 A cycloalkoxy group, a 3- to 12-membered heterocyclic group, a 3- to 12-membered heterocyclic oxy group, C 6-10 An aryl group, C 6-10 An aryloxy group, a 5- to 10-membered heteroaryl group, a 5- to 10-membered heteroaryloxy group, an amino group, a mono-C 1-10 An alkylamino group, a di-C 1-10 An alkylamino group and C 1-10 Is substituted with one or more substituents selected from the group consisting of an alkanoyl group,

[0021] Alternatively, R 13 And R 14 Together with the nitrogen atom directly connected thereto, form a 4- to 10-membered heterocyclic group or a 5- to 10-membered heteroaryl group, and the 4- to 10-membered heterocyclic group or 5- to 10-membered heteroaryl group may optionally further contain deuterium, halogen, a hydroxyl group, =O, C 1-10 An alkyl group, C 2-10 An alkenyl group, C 2-10 An alkynyl group, a halogen-substituted C 1-10 An alkyl group, a deuterium-substituted C 1-10 An alkyl group, C 1-10 An alkoxy group, C 3-12 A cycloalkyl group, C 3-12 A cycloalkoxy group, a 3- to 12-membered heterocyclic group, a 3- to 12-membered heterocyclic oxy group, C 6-10 An aryl group, C 6-10 An aryloxy group, a 5- to 10-membered heteroaryl group, a 5- to 10-membered heteroaryloxy group, methanesulfonylmethyl, an amino group, a mono-C 1-10 An alkylamino group, a di-C 1-10 An alkylamino group and C 1-10 Is substituted with one or more substituents selected from the group consisting of an alkanoyl group, m is 0, 1, 2, 3 or 4, n is 0, 1 or 2, p is 1 or 2, and Each r is independently 0, 1 or 2.

[0022] In a preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, X1 is CR a or N, X2 is CR b or N, X3 is CR c or N, X4 is CR d or N, L1 is CR 5a R 5b and, L2 is (CR 5c R 5d ) p , NR 6a , O, S, S(O), S(O)2 or C(O), L3 is a bond, CR 5e R 5f , NR 6b , O, S, S(O), S(O)2 or C(O), alternatively, L2 and L3 together form a C 4-6 cycloalkyl group, 4-6 membered heterocyclic group, C 6-8 aryl group or 5-8 membered heteroaryl group, and the C 4-6 cycloalkyl group, 4-6 membered heterocyclic group, C 6-8 aryl group or 5-8 membered heteroaryl group is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R11 , -C 0-4 alkyl - C(O)OR 11 , -C 0-4 alkyl - C(O)SR 11 , -C 0-4 alkyl - S - C(O)R 12 , -C 0-4 alkyl - C(O)R 12 , -C 0-4 alkyl - O - C(O)R 12 , -C 0-4 alkyl - P(O)(R 12 )2, -C 0-4 alkyl - NR 13 R 14 , -C 0-4 alkyl - C(=NR 13 )R 12 , -C 0-4 alkyl - N(R 13 ) - C(=NR 14 )R 12 , -C 0-4 alkyl - C(O)NR 13 R 14 and -C 0-4 alkyl - N(R 13 ) - C(O)R 12 is substituted with one or more substituents selected from the group consisting of, L4 is CR 5g R 5h , O, S, S(O), S(O)2, NR 6c or C(O), Ring A is C 4-6 cycloalkyl group, 4 - 6 membered heterocyclic group, C 6-8 aryl group or 5 - 8 membered heteroaryl group,

[0023] R1 is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3 - 8 membered heterocyclic group, C 6-8 aryl group, 5 - 8 membered heteroaryl group, -C 0-4 alkyl - SF5, -C 0-4 alkyl - S(O)(=N - R7)R8, -C 0-4Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-O-S(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 alkyl group substituted with a cycloalkyl group, C 1-4 alkyl group substituted with a 3-6 membered heterocyclic group, C 1-4 alkyl group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 0-4 Alkyl-SF5, -C0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-N(R 13 )-S(O)2R 10 , -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 )2, -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, said groups being each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group, 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 Alkyl-SF5, -C 0-4 Alkyl-S(O)(=N-R7)R8, -C 0-4 Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-N(R 13 )-S(O)2R 10 , -C 0-4 Alkyl-O-S(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of

[0024] Each R2 is independently hydrogen, deuterium, halogen, cyano group, C 1-4Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group, 5- to 8-membered heteroaryl group, -C 0-4 Alkyl-SF5, -C 0-4 Alkyl-S(O)(=N-R7)R8, -C 0-4 Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-O-S(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 ), 2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group, 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 Alkyl-SF5, -C 0-4 Alkyl-S(O)(=N-R7)R8, -C 0-4 Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-O-S(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of,

[0025] each R3, R a and R bis independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 )2, -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of,

[0026] R4 and R c are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 )2, -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4Alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of

[0027] R d is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 )2、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of

[0028] R 5a and R 5b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 )2、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4Alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5a and R 5b together with the carbon atom to which they are directly attached form a C(O), C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 )2、-C 0-4 alkyl-NR 13 R 14 、-C0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of:

[0029] Each R 5c and R 5d are independently hydrogen, deuterium, halogen, cyano group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups, C 6-8 Aryl groups, 5-8 membered heteroaryl groups, -C 0-4 Alkyl-SF5, -C 0-4 Alkyl-S(O)(=N-R7)R8, -C 0-4 Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-OS(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-OR 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-SC(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-OC(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR13 R 14 、 -C 0-4 alkyl - C(=NR 13 )R 12 、 -C 0-4 alkyl - N(R 13 ) - C(=NR 14 )R 12 、 -C 0-4 alkyl - C(O)NR 13 R 14 and -C 0-4 alkyl - N(R 13 ) - C(O)R 12 selected from the group consisting of, or R 5c and R 5d , together with the carbon atom directly connecting to them, form a C 3-6 cycloalkyl group, a 4 - 6 membered heterocyclic group, a C 6-8 aryl group or a 5 - 8 membered heteroaryl group, and the said groups may each independently optionally further have deuterium, halogen, cyano group, C 1-4 alkyl group, halogen - substituted C 1-4 alkyl group, deuterium - substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3 - 6 membered heterocyclic group, C 6-8 aryl group, a 5 - 8 membered heteroaryl group, =O, =S, -C 0-4 alkyl - SF5, -C 0-4 alkyl - S(O)(=N - R7)R8, -C 0-4 alkyl - N=S(O)R8R9, -C 0-4 alkyl - N=SR8R9, -C 0-4 alkyl - O - S(O)2R 10 、 -C 0-4 alkyl - S(O) r R 10 、 -C 0-4 alkyl - O - R 11 、 -C 0-4 alkyl - C(O)OR 11 、 -C 0-4 alkyl - C(O)SR 11 、 -C 0-4 alkyl - S - C(O)R 12 、 -C 0-4alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 )2, -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, provided that when R 5c or R 5d is H or a C 1-4 alkyl group, R1 is an optionally substituted C 2-10 alkynyl group, or, provided that L3 is O, S, S(O) or S(O)2,

[0030] R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or, R 5e and R 5f together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, a 4-6 membered heterocyclic group, a C 6-8 aryl group or a 5-8 membered heteroaryl group, said groups each independently optionally further comprising deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3-6 membered heterocyclic group, C 6-8 aryl group, a 5-8 membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-O-S(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of,

[0031] R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C0-4 Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-O-S(O)2R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-O-R 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 Alkyl-S-C(O)R 12 , -C 0-4 Alkyl-C(O)R 12 , -C 0-4 Alkyl-O-C(O)R 12 , -C 0-4 Alkyl-P(O)(R 12 )2, -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or, R 5g and R 5h together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, a 4- to 6-membered heterocyclic group, a C 6-8 aryl group or a 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C3-6 Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group, 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 Alkyl-SF5, -C 0-4 Alkyl-S(O)(=N-R7)R8, -C 0-4 Alkyl-N=S(O)R8R9, -C 0-4 Alkyl-N=SR8R9, -C 0-4 Alkyl-O-S(O)2R 10 、-C 0-4 Alkyl-S(O) r R 10 、-C 0-4 Alkyl-O-R 11 、-C 0-4 Alkyl-C(O)OR 11 、-C 0-4 Alkyl-C(O)SR 11 、-C 0-4 Alkyl-S-C(O)R 12 、-C 0-4 Alkyl-C(O)R 12 、-C 0-4 Alkyl-O-C(O)R 12 、-C 0-4 Alkyl-P(O)(R 12 )2、-C 0-4 Alkyl-NR 13 R 14 、-C 0-4 Alkyl-C(=NR 13 )R 12 、-C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, provided that R 6a 、R 6b 、R 6c 、R7、R8、R9、R 10 、R 11 、R 12 、R13 、R 14 、m, n, p, and r are as defined for the compounds of formula (I).

[0032] In a preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, each R7 is independently hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)R 12 or -C 0-4 alkyl-C(O)NR 13 R 14 selected from the group consisting of, and the groups may optionally further be deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 or -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of:

[0033] Each R8 and R9 is independently selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group or 5-8 membered heteroaryl group, or R8 and R9 together with the sulfur atom directly connecting them form a 3-6 membered heterocyclic group, and the said group is optionally further substituted with deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 Or -C 0-4 Alkyl-N(R 13 )-C(O)R 12 Substituted with one or more substituents selected from the group consisting of

[0034] Each R 10 Is independently hydrogen, deuterium, a hydroxyl group, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 3-6 Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group, 5- to 8-membered heteroaryl group, and -NR 13 R 14 Selected from the group consisting of, and the groups are each independently optionally further deuterium, halogen, hydroxyl group, =O, C 1-4 Alkyl group, C 1-4 Alkoxy group, C 3-6 Cycloalkyl group, C 3-6 Cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group, C 6-8 Aryl group, C 6-8 Aryloxy group, 5- to 8-membered heteroaryl group, 5- to 8-membered heteroaryloxy group, and -NR 13 R 14 Selected from the group consisting of, and substituted with one or more substituents selected from the group consisting of

[0035] Each R 11 Is independently hydrogen, deuterium, C 1-4 Alkyl group, C 2-4 Alkenyl group, C 3-6 Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group and 5- to 8-membered heteroaryl group selected from the group consisting of, and the groups are each independently optionally further deuterium, halogen, hydroxyl group, =O, cyano group, C 1-4 Alkyl group, C 1-4 Alkoxy group, C 3-6A cycloalkyl group, C 3-6 A cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 An aryl group, C 6-8 An aryloxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryloxy group, and -NR 13 R 14 substituted with one or more substituents selected from the group consisting of

[0036] Each R 12 is independently hydrogen, deuterium, a hydroxyl group, C 1-4 An alkyl group, C 1-4 An alkoxy group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, C 3-6 A cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 An aryl group, C 6-8 An aryloxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryloxy group, and -NR 13 R 14 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, hydroxyl group, =O, cyano group, C 1-4 An alkyl group, C 1-4 An alkoxy group, C 3-6 A cycloalkyl group, C 3-6 A cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 An aryl group, C 6-8 An aryloxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryloxy group, and -NR 13 R 14 substituted with one or more substituents selected from the group consisting of

[0037] Each R 13 and R 14 are each independently hydrogen, deuterium, a hydroxyl group, C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C6-8 An aryl group, a 5- to 8-membered heteroaryl group, a sulfinyl group, a sulfonyl group, a methylsulfonyl group, an isopropylsulfonyl group, a cyclopropylsulfonyl group, a p-toluenesulfonyl group, an aminosulfonyl group, a dimethylaminosulfonyl group, and C 1-4 Selected from the group consisting of alkanoyl groups, and each of said groups is optionally further independently deuterium, halogen, a hydroxyl group, =O, C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, a halogen-substituted C 1-4 An alkyl group, a deuterium-substituted C 1-4 An alkyl group, C 1-4 An alkoxy group, C 3-6 A cycloalkyl group, C 3-6 A cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 An aryl group, C 6-8 An aryloxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryloxy group, an amino group, a mono C 1-4 An alkylamino group, a di C 1-4 An alkylamino group, and C 1-4 Substituted with one or more substituents selected from the group consisting of alkanoyl groups,

[0038] Alternatively, R 13 and R 14 Together with the nitrogen atom directly connecting them, form a 4- to 6-membered heterocyclic group or a 5- to 8-membered heteroaryl group, and said 4- to 6-membered heterocyclic group or 5- to 8-membered heteroaryl group is optionally further deuterium, halogen, a hydroxyl group, =O, C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, a halogen-substituted C 1-4 An alkyl group, a deuterium-substituted C 1-4 An alkyl group, C 1-4 An alkoxy group, C 3-6 A cycloalkyl group, C 3-6 A cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 An aryl group, C 6-8An aryl oxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryl oxy group, methanesulfonylmethyl, an amino group, a mono-C 1-4 alkylamino group, di-C 1-4 alkylamino group and C 1-4 substituted with one or more substituents selected from the group consisting of an alkanoyl group, and each r is independently 0, 1 or 2.

[0039] In a more preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, the compound of formula (I) is a compound of formula (II) below,

Chemical formula

[0040] R1 is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 8-membered heterocyclic group, C 6-8An aryl group, a 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, wherein said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 3-6 alkyl group substituted with a cycloalkyl group, C 1-4 alkyl group substituted with a 3- to 6-membered heterocyclic group, C 1-4 alkyl group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -N(R 13 )-S(O)2R 10 , -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR13 R 14 ,-C(=NR 13 )R 12 ,-N(R 13 )-C(=NR 14 )R 12 ,-C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, said groups being each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-N(R 13 )-S(O)2R 10 , -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 )2, -C 0-4Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of:

[0041] R 2a are hydrogen, deuterium, and C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups, C 6-8 Aryl groups, 5-8 membered heteroaryl groups, -S(O) r R 10 , -OR 11 , -C(O)OR 11 , -C(O)SR 11 , -C(O)R 12 and -C(O)NR 13 R 14 wherein each of said groups is independently optionally further selected from the group consisting of deuterium, halogen, cyano group, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium-substituted C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups, C 6-8 Aryl groups, 5-8 membered heteroaryl groups, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -OS(O)2R 10 , -S(O) r R 10 , -OR 11 , -C(O)OR 11, -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of:

[0042] R 2b is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12selected from the group consisting of, wherein each of said groups is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of,

[0043] R 3a , R 3b , R a and R b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8An aryl group, a 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of

[0044] R4 and R c are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14, -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of,

[0045] R d is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, R 5a and R 5b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 An aryl group, a 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5a and R 5b together with the carbon atom to which they are directly attached form a C(O), C 3-6 cycloalkyl group, a 4- to 6-membered heterocyclic group, C 6-8 aryl group or a 5- to 8-membered heteroaryl group, and the said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11, -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of:

[0046] Each R 5c and R 5d is independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12selected from the group consisting of, or R 5c and R 5d together with the carbon atom directly linked thereto form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of one or more substituents, provided that when R 5c or R 5d is H or a C 1-4 alkyl group, R1 is an optionally substituted C 2-10 alkynyl group, provided that

[0047] R 5e and R 5fis independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5e and R 5f together with the carbon atom directly connecting them, form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and the groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of,

[0048] R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12, -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5g and R 5h together with the carbon atom directly linking them, form a C 3-6 cycloalkyl group, a 4-6 membered heterocyclic group, a C 6-8 aryl group or a 5-8 membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3-6 membered heterocyclic group, C 6-8 aryl group, a 5-8 membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of one or more substituents, provided that R 6a , R 6c , R7, R8, R9, R 10 , R 11 , R 12 , R13 , R 14 , p, and r are as defined for the compound of formula (I).

[0049] In a further preferred form, in the compound of formula (I), its stereoisomers or its pharmaceutically acceptable salts, the compound of formula (I) is a compound of the following formula (III),

Chemical formula

[0050] R1 is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 8-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12, -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, wherein said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 alkyl group substituted with a cycloalkyl group, C 1-4 alkyl group substituted with a 3-6 membered heterocyclic group, C 1-4 alkyl group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -N(R 13 )-S(O)2R 10 , -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12substituted with one or more substituents selected from the group consisting of, said groups each independently optionally further being one or more deuteriums, halogens, cyano groups, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF5, -C 0-4 alkyl-S(O)(=N-R7)R8, -C 0-4 alkyl-N=S(O)R8R9, -C 0-4 alkyl-N=SR8R9, -C 0-4 alkyl-N(R 13 )-S(O)2R 10 , -C 0-4 alkyl-O-S(O)2R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 )2, -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4Alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with a substituent selected from the group consisting of

[0051] R 2a is selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group and 3-6 membered heterocyclic group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of

[0052] R 2b is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group and -SF5, and the said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of

[0053] R 3a , R 3b , R a and R b are each independently hydrogen, deuterium, halogen, cyano group, C1-4 An alkyl group, a halogen-substituted C 1-4 An alkyl group, a deuterium-substituted C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 Selected from the group consisting of an aryl group, a 5- to 8-membered heteroaryl group, and -SF5, R c is hydrogen, deuterium, halogen, a cyano group, C 1-4 An alkyl group, a halogen-substituted C 1-4 An alkyl group, a deuterium-substituted C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 Selected from the group consisting of an aryl group, a 5- to 8-membered heteroaryl group, and -SF5, R d is hydrogen, deuterium, halogen, a cyano group, C 1-4 An alkyl group, a halogen-substituted C 1-4 An alkyl group, a deuterium-substituted C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 Selected from the group consisting of an aryl group, a 5- to 8-membered heteroaryl group, and -SF5,

[0054] R 5a and R 5b are each independently hydrogen, deuterium, halogen, a cyano group, C 1-4 An alkyl group, C 2-4 An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 Selected from the group consisting of an aryl group, a 5- to 8-membered heteroaryl group, and -SF5, or R 5a and R 5b together with the carbon atom directly connected thereto, C(O), C 3-6Cycloalkyl group, 4-6 membered heterocyclic group, C 6-8 forms an aryl group or a 5-8 membered heteroaryl group, and each of said groups is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of,

[0055] when p is 1, R 5c and R 5d together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group or a 4-6 membered heterocyclic group, and each of said groups is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C2-4 an alkynyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 an aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of

[0056] alternatively, when p is 2, one pair of R 5c and R 5d together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and when one pair of R 5c and R 5d together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, another pair of R 5c and R 5d are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8an aryl group, a 5- to 8-membered heteroaryl group, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of,

[0057] R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group and -SF5, or R 5e and R 5f together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and the said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6Cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 Aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of:

[0058] R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group and -SF5, or R 5g and R 5h together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further substituted with deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4An alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 An aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of

[0059] R 6c is hydrogen, deuterium, C 1-4 an alkyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group and -O-R 11 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, cyano group, hydroxyl group, =O, C 1-4 an alkyl group, halogen-substituted C 1-4 an alkyl group, deuterium-substituted C 1-4 an alkyl group, C 2-4 an alkenyl group, C 2-4 an alkynyl group, C 1-4 an alkoxy group, C 3-6 a cycloalkyl group, C 3-6 a cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group and -NR 13 R 14substituted with one or more substituents selected from the group consisting of provided that R7, R8, R9, R 10 , R 11 , R 12 , R 13 , R 14 , p and r are as defined for the compound of formula (I).

[0060] In a more preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, the compound of formula (I) is a compound of the following formula (IV),

Chemical formula

[0061] R1 is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-8 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group and -SF5, and the said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 alkyl group substituted with a cycloalkyl group, C 1-4 alkyl group substituted with a 3-6 membered heterocyclic group, C 1-4 alkyl group, C 6-8Aryl groups, 5-8 membered heteroaryl groups, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -N(R 13 )-S(O)2R 10 , -OS(O)2R 10 , -S(O) r R 10 , -OR 11 , -C(O)OR 11 , -C(O)SR 11 , -SC(O)R 12 , -C(O)R 12 , -OC(O)R 12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and each of said groups is independently optionally and further substituted with deuterium, halogen, cyano group, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium-substituted C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups, C 6-8 Aryl groups, 5-8 membered heteroaryl groups, =O, =S, -SF5, -S(O)(=N-R7)R8, -N=S(O)R8R9, -N=SR8R9, -N(R 13 )-S(O)2R 10 , -OS(O)2R 10 , -S(O) r R 10 , -OR 11 , -C(O)OR 11 , -C(O)SR 11 , -SC(O)R 12 , -C(O)R 12 , -OC(O)R12 , -P(O)(R 12 )2, -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of R 2a is hydrogen, deuterium, a hydroxyl group, a C 1-4 alkyl group, a C 2-4 alkenyl group, a C 2-4 alkynyl group, a C 3-6 cycloalkyl group and a 3- to 6-membered heterocyclic group, and said groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, a cyano group, a C 1-4 alkyl group, a halogen-substituted C 1-4 alkyl group, a deuterium-substituted C 1-4 alkyl group, a C 2-4 alkenyl group, a C 2-4 alkynyl group, a C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group, =O, =S and -SF5

[0062] R 2b is hydrogen, deuterium, halogen, a cyano group, a C 1-4 alkyl group, a C 2-4 alkenyl group, a C 2-4 alkynyl group, a C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group and -SF5, and said groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, a cyano group, a C 1-4 alkyl group, a halogen-substituted C 1-4 alkyl group, a deuterium-substituted C 1-4 alkyl group, a C 2-4 alkenyl group, a C 2-4 alkynyl group, a C 3-6Substituted with one or more substituents selected from the group consisting of a cycloalkyl group, a 3- to 6-membered heterocyclic group, =O, =S, and -SF5,

[0063] R 5a and R 5b are each independently hydrogen, deuterium, a halogen, a cyano group, C 1-4 alkyl group, C 3-6 cycloalkyl group, and a 3- to 6-membered heterocyclic group, or R 5a and R 5b together with the carbon atom directly connected thereto form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and the groups are each independently optionally further deuterium, a halogen, a cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group, =O, =S, and -SF5, substituted with one or more substituents selected from the group consisting of

[0064] R 5c and R 5d together with the carbon atom directly connected thereto form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and the groups are each independently optionally further deuterium, a halogen, a cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group, =O, =S, and -SF5, substituted with one or more substituents selected from the group consisting of

[0065] R 5e and R 5f are each independently hydrogen, deuterium, a halogen, a cyano group, C 1-4 alkyl group, C 3-6Selected from the group consisting of a cycloalkyl group and a 3- to 6-membered heterocyclic group, or R 5e and R 5f together with the carbon atom directly connected thereto form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and each of said groups is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, =O, =S and -SF5, and is substituted with one or more substituents selected from the group consisting of provided that R7, R8, R9, R 10 , R 11 , R 12 , R 13 , R 14 and r are as defined for the compound of formula (I).

[0066] More preferably, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, L1 is CR 5a R 5b wherein L2 is CR 5c R 5d wherein L3 is CR 5e R 5f wherein L4 is O,

[0067] R 5a and R 5bis independently selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, and each of said groups is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF5,

[0068] R 5c and R 5d together with the carbon atom directly connected thereto form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and each of said groups is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF5, and

[0069] R 5e and R 5fis independently selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, and each of said groups is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF5.

[0070] More preferably, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R 2a is selected from the group consisting of hydrogen, deuterium, hydroxyl group, methyl group, ethyl group, propyl group, isopropyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, and each of said groups is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF5, and

[0071] R 2bis selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group and -SF5, and the group is each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF5.

[0072] In a more preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, the compound of formula (I) is a compound of the following formula (V),

Chemical formula

[0073] R 2a are hydrogen, deuterium, and C 1-4 Alkyl group, C 3-6 cycloalkyl groups and 3-6 membered heterocyclic groups, each of which is independently optionally further selected from the group consisting of deuterium, halogen, cyano group, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium-substituted C 1-4 Alkyl group, C 3-6 Substituted with one or more substituents selected from the group consisting of cycloalkyl groups and 3- to 6-membered heterocyclic groups; R 5c and R 5d together with the carbon atom directly linked thereto form C 3-6 a cycloalkyl group or a 4- to 6-membered heterocyclic group, and each of said groups is independently optionally further substituted with deuterium, halogen, a cyano group, C 1-4 an alkyl group, a halogen-substituted C 1-4 an alkyl group, a deuterium-substituted C 1-4 an alkyl group, C 2-4 an alkenyl group, C 2-4 an alkynyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group, =O, =S and -SF5, and is substituted with one or more substituents selected from the group consisting of provided that R 10 , R 11 , R 12 , R 13 , R 14 and r are as defined for the compound of formula (I).

[0074] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R 5c and R 5d together with the carbon atom directly linked thereto form C 3-6 a cycloalkyl group or a 4- to 6-membered heterocyclic group.

[0075] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R 5c and R 5d together with the carbon atom directly linked thereto form a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, an oxetanyl group, an oxolanyl group or an oxanyl group.

[0076] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R1 is C 2-4 an alkynyl group, and said C 2-4 alkynyl is further substituted with deuterium, C 1-4 an alkyl group, C 3-6Substituted with a substituent selected from the group consisting of a cycloalkyl group and a 3- to 6-membered heterocyclic group, and each of said groups is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 substituted with one or more substituents selected from the group consisting of a cycloalkyl group and a 3- to 6-membered heterocyclic group.

[0077] In a more preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R1 is an ethynyl group, and said ethynyl group is optionally further deuterium, methyl group, ethyl group, propyl group, isopropyl group, butyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridyl group, azetidinyl group, azolidyl group and azonanil group. Substituted with one or more substituents selected from the group consisting of, and each of said groups is independently optionally further deuterium, fluorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, butyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridyl group, azetidinyl group, azolidyl group and azonanil group Substituted with one or more substituents selected from the group consisting of.

[0078] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R1 is an ethynyl group, and the ethynyl group is optionally further substituted with one or more substituents selected from the group consisting of a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, an oxiranyl group, an oxetanyl group, an oxolanyl group, an oxanyl group, an aziridinyl group, an azetidinyl group, an azolidyl group and an azonanyl group, and each of the groups is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, bromine, a cyano group, a methyl group, an ethyl group, a propyl group, an isopropyl group, a monofluoromethyl group, a difluoromethyl group, a trifluoromethyl group, a monodeuteromethyl group, a dideuteromethyl group and a trideuteromethyl group.

[0079] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R1 is

Chemical formula

[0080] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R1 is a 4- to 8-membered nitrogen-containing heterocyclic group, and the 4- to 8-membered nitrogen-containing heterocyclic group is optionally further deuterium, halogen, cyano, C 1-4 alkyl group, =O, -N(R 13 )-S(O)2R 10, -S(O) r R 10 , -O-R 11 , -O-C(O)R 12 , -NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of, said C 1-4 alkyl group is optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, -N(R 13 )-S(O)2R 10 , -O-S(O)2R 10 , -S(O) r R 10 , -O-R 11 , -O-C(O)R 12 , -NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of, provided that R 10 , R 11 , R 12 , R 13 , R 14 and r are as defined for the compound of formula (I).

[0081] More preferably, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, the structure of R1 is

Chemical formula

[0082] More preferably, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, the structure of R1 is

Chemical formula

[0083] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, the structure of R1 is

Chemical formula

[0084] In a more preferred form, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R 2a is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 cycloalkyl group and 3- to 6-membered heterocyclic group.

[0085] In a more preferred embodiment, in the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, R 2a is selected from the group consisting of hydrogen, deuterium, methyl group, ethyl group, propyl group, isopropyl group, butyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group.

[0086] In a most preferred embodiment, the compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt includes, but is not limited to, the following compounds.

[0087] [Chemical formula] [Chemical formula] [Chemical formula] [Chemical formula] [Chemical formula]

[0088] The second aspect of the present invention provides a method for producing a compound of formula (I), its stereoisomer or its pharmaceutically acceptable salt, which includes the following steps.

[0089] [Chemical formula] However, ring A, X1, X2, X3, X4, L1, L2, L3, L4, R1, R2, R3, R4, m and n are as defined for the compound of formula (I).

[0090] A third aspect of the present invention provides a pharmaceutical composition comprising a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

[0091] The present invention also relates to the use of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for treating and / or preventing a tumor or metastatic disease that is at least partially associated with an EGFR L858R / C797S double mutation, an EGFR Del19 / C797S double mutation, an L858R / T790M / C797S triple mutation and a Del19 / T790M / C797S triple mutation.

[0092] The present invention also relates to the use of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for preventing and / or treating a tumor and / or metastatic disease due to excessive proliferation and impaired induction of cell death.

[0093] The present invention also relates to the use of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for preventing and / or treating lung cancer, colon cancer, pancreatic cancer, head and neck cancer, breast cancer, ovarian cancer, uterine cancer, gastric cancer, non-small cell lung cancer, leukemia, myelodysplastic syndrome, malignant lymphoma, head and neck tumor, thoracic tumor, gastrointestinal tumor, endocrine tumor, breast and other gynecological tumors, urological tumors, skin tumors, sarcoma, nasal inverted papilloma or squamous cell carcinoma of the nasal cavity associated with nasal inverted papilloma that is at least partially associated with an EGFR L858R / C797S double mutation, an EGFR Del19 / C797S double mutation, an L858R / T790M / C797S triple mutation and a Del19 / T790M / C797S triple mutation.

[0094] The present invention also relates to a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof for use as a medicament.

[0095] The present invention also relates to the use of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof for treating and / or preventing a tumor or metastatic disease that is at least partially associated with an EGFR L858R / C797S double mutation, an EGFR Del19 / C797S double mutation, an L858R / T790M / C797S triple mutation and a Del19 / T790M / C797S triple mutation.

[0096] The present invention also relates to the use of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof for preventing and / or treating a tumor and / or metastatic disease caused by excessive proliferation and impaired induction of cell death.

[0097] The present invention also relates to the use of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof for treating and / or preventing lung cancer, colon cancer, pancreatic cancer, head and neck cancer, breast cancer, ovarian cancer, uterine cancer, gastric cancer, non-small cell lung cancer, leukemia, myelodysplastic syndrome, malignant lymphoma, head and neck tumor, thoracic tumor, gastrointestinal tumor, endocrine tumor, breast and other gynecological tumors, urological tumors, skin tumors, sarcoma, nasal inverted papilloma or squamous cell carcinoma of the nasal cavity associated with nasal inverted papilloma that is at least partially associated with an EGFR L858R / C797S double mutation, an EGFR Del19 / C797S double mutation, an L858R / T790M / C797S triple mutation and a Del19 / T790M / C797S triple mutation.

[0098] The present invention also relates to a method for treating and / or preventing a tumor or metastatic disease that is at least partially associated with an EGFR L858R / C797S double mutation, an EGFR Del19 / C797S double mutation, an L858R / T790M / C797S triple mutation and a Del19 / T790M / C797S triple mutation, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

[0099] The present invention also relates to a method for preventing and / or treating tumors and / or metastatic diseases caused by excessive proliferation and cell death induction disorders, which comprises administering to a patient in need thereof a therapeutically effective amount of the compound of formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

[0100] The present invention also relates to a method for treating and / or preventing lung cancer, colon cancer, pancreatic cancer, head and neck cancer, breast cancer, ovarian cancer, uterine cancer, gastric cancer, non-small cell lung cancer, leukemia, myelodysplastic syndrome, malignant lymphoma, head and neck tumors, thoracic tumors, gastrointestinal tumors, endocrine tumors, breast and other gynecological tumors, urological tumors, skin tumors, sarcomas, nasal cavity inverted papillomas or squamous cell carcinomas of the nasal cavity associated with nasal cavity inverted papillomas, which comprises administering to a patient in need thereof a therapeutically effective amount of the compound of formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and which is at least partially related to EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation and Del19 / T790M / C797S triple mutation.

Mode for Carrying Out the Invention

[0101] The inventors of the present application, through extensive and in-depth research, for the first time developed an EGFR inhibitor having the structure of formula (I). A series of compounds of the present invention can be widely applied to the manufacture of drugs for treating and / or preventing tumors or metastatic diseases that are at least partially related to EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation and Del19 / T790M / C797S triple mutation, and are expected to be developed as a new generation of EGFR inhibitors. Based on this, the present invention has been completed.

[0102] Detailed Description: Unless otherwise stated or otherwise indicated, the following terms used in the specification and claims have the following meanings.

[0103] The term "alkyl group" refers to a saturated aliphatic hydrocarbon group containing a straight-chain or branched chain, preferably a straight-chain alkyl group and a branched-chain alkyl group containing 1 to 10 or 1 to 6 or 1 to 4 carbon atoms, including a methyl group, an ethyl group, an n-propyl group, an isopropyl group, an n-butyl group, an isobutyl group, a t-butyl group, an s-butyl group, an n-pentyl group, a 1,1-dimethylpropyl group, a 1,2-dimethylpropyl group, a 2,2-dimethylpropyl group, a 1-ethylpropyl group, a 2-methylbutyl group, a 3-methylbutyl group, an n-hexyl group, a 1-ethyl-2-methylpropyl group, a 1,1,2-trimethylpropyl group, a 1,1-dimethylbutyl group, a 1,2-dimethylbutyl group, a 2,2-dimethylbutyl group, a 1,3-dimethylbutyl group, a 2-ethylbutyl group, a 2-methylpentyl group, a 3-methylpentyl group, a 4-methylpentyl group, a 2,3-dimethylbutyl group, an n-heptyl group, a 2-methylhexyl group, a 3-methylhexyl group, a 4-methylhexyl group, a 5-methylhexyl group, a 2,3-dimethylpentyl group, a 2,4-dimethylpentyl group, a 2,2-dimethylpentyl group, a 3,3-dimethylpentyl group, a 2-ethylpentyl group, a 3-ethylpentyl group, an n-octyl group, a 2,3-dimethylhexyl group, a 2,4-dimethylhexyl group, a 2,5-dimethylhexyl group, a 2,2-dimethylhexyl group, a 3,3-dimethylhexyl group, a 4,4-dimethylhexyl group, a 2-ethylhexyl group, a 3-ethylhexyl group, a 4-ethylhexyl group, a 2-methyl-2-ethylpentyl group, a 2-methyl-3-ethylpentyl group or various branched-chain isomers thereof, etc., but is not limited thereto. The "C 1-10 alkyl group" refers to a straight-chain alkyl group and a branched-chain alkyl group containing 1 to 10 carbon atoms, and the "C 1-4 alkyl group" refers to a straight-chain alkyl group and a branched-chain alkyl group containing 1 to 4 carbon atoms, and the "C 0-8 alkyl group" refers to a straight-chain alkyl group and a branched-chain alkyl group containing 0 to 8 carbon atoms, and the "C 0-4 alkyl group" refers to a straight-chain alkyl group and a branched-chain alkyl group containing 0 to 4 carbon atoms.

[0104] The alkyl group may be optionally substituted or unsubstituted. In the case of a substituted alkyl group, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 , -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8An alkyl-N(R 13 )-C(O)R 12 It is preferably one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of.

[0105] The "cycloalkyl group" or "carbocyclic ring" refers to a saturated or partially unsaturated monocyclic or polycyclic cyclic hydrocarbon substituent. The partially unsaturated cyclic hydrocarbon means that the cyclic hydrocarbon may contain one or more (preferably 1, 2 or 3) double bonds, but none of the rings has a completely conjugated π electron system. The cycloalkyl group is divided into a monocyclic cycloalkyl group and a polycyclic cycloalkyl group, and is preferably a cycloalkyl group containing 3 to 12 or 3 to 8 or 3 to 6 carbon atoms. For example, the "C 3-12 cycloalkyl group" refers to a cycloalkyl group containing 3 to 12 carbon atoms, the "C 4-12 cycloalkyl group" refers to a cycloalkyl group containing 4 to 12 carbon atoms, the "C 4-8 cycloalkyl group" refers to a cycloalkyl group containing 4 to 8 carbon atoms, the "C 3-8 cycloalkyl group" refers to a cycloalkyl group containing 3 to 8 carbon atoms, the "C 3-6 cycloalkyl group" refers to a cycloalkyl group containing 3 to 6 carbon atoms, the "C 4-6 cycloalkyl group" refers to a cycloalkyl group containing 4 to 6 carbon atoms. Among them, The monocyclic cycloalkyl group includes, but is not limited to, a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclopentenyl group, a cyclohexyl group, a cyclohexenyl group, a cyclohexadienyl group, a cycloheptyl group, a cycloheptatrienyl group, a cyclooctyl group, etc.

[0106] The polycyclic cycloalkyl group includes spirocyclic, fused-ring, and bridged-ring cycloalkyl groups. The "spirocycloalkyl group" refers to a polycyclic group that shares one carbon atom (referred to as the spiro atom) between monocyclic rings. These groups may contain one or more (preferably 1, 2, or 3) double bonds, but there is no ring having a completely conjugated π-electron system. Depending on the number of spiro atoms shared between rings, the spirocycloalkyl group is divided into a monospirocycloalkyl group, a dispirocycloalkyl group, or a polyspirocycloalkyl group, and the spirocycloalkyl group includes, but is not limited to, the following.

[0107]

Chem.

[0108] The "fused cycloalkyl group" refers to an all-carbon polycyclic group in which each ring in the system shares a pair of adjacent carbon atoms with another ring in the system. One or more of its rings may contain one or more (preferably 1, 2, or 3) double bonds, but there is no ring having a completely conjugated π-electron system. It can be divided into bicyclic, tricyclic, tetracyclic, or polycyclic fused cycloalkyl groups depending on the number of constituent rings, and the fused cycloalkyl group includes, but is not limited to, the following.

[0109]

Chem.

[0110] The "bridged cycloalkyl group" refers to an all-carbon polycyclic group that shares two carbon atoms that are not directly connected between any two rings. These groups may contain one or more (preferably 1, 2, or 3) double bonds, but there is no ring having a completely conjugated π-electron system. It can be divided into bicyclic, tricyclic, tetracyclic, or polycyclic bridged cycloalkyl groups depending on the number of constituent rings, and the bridged cycloalkyl group includes, but is not limited to, the following.

[0111]

Chem.

[0112] The ring of the cycloalkyl group may be condensed with an aryl group, a heteroaryl group or a heterocycloalkyl ring. Here, the ring linked to the parent structure is a cycloalkyl group, including but not limited to an indanyl group, a tetrahydronaphthyl group, a benzocycloheptyl group, etc.

[0113] The cycloalkyl group may be optionally substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 )2、-C 0-8 alkyl-NR 13R 14 、 -C 0-8 alkyl - C(=NR 13 )R 12 、 -C 0-8 alkyl - N(R 13 ) - C(=NR 14 )R 12 、 -C 0-8 alkyl - C(O)NR 13 R 14 and -C 0-8 alkyl - N(R 13 ) - C(O)R 12 It is preferably one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of.

[0114] The "heterocyclic group" or "heterocycle" refers to a saturated or partially unsaturated monocyclic or polycyclic cyclic hydrocarbon substituent. The partially unsaturated cyclic hydrocarbon means that the cyclic hydrocarbon may contain one or more (preferably 1, 2 or 3) double bonds, but none of the rings have a completely conjugated π - electron system. One or more (preferably 1, 2, 3 or 4) of the ring atoms of the heterocyclic group are heteroatoms selected from the group consisting of N, O, N·O or S(O) r (where r is an integer 0, 1, 2), and does not contain a ring moiety of -O - O -, -O - S - or -S - S -, and the remaining ring atoms are carbon. Preferably, it is a heterocyclic group containing 3 to 12 or 3 to 8 or 3 to 6 ring atoms. For example, the "3 - 6 membered heterocyclic group" refers to a heterocyclic group containing 3 to 6 ring atoms, the "3 - 8 membered heterocyclic group" refers to a heterocyclic group containing 3 to 8 ring atoms, the "4 - 6 membered heterocyclic group" refers to a heterocyclic group containing 4 to 6 ring atoms, the "4 - 8 membered heterocyclic group" refers to a heterocyclic group containing 4 to 8 ring atoms, the "4 - 10 membered heterocyclic group" refers to a heterocyclic group containing 4 to 10 ring atoms, the "4 - 12 membered heterocyclic group" refers to a heterocyclic group containing 4 to 12 ring atoms, the "5 - 8 membered heterocyclic group" refers to a heterocyclic group containing 5 to 8 ring atoms, and the "3 - 12 membered heterocyclic group" refers to a heterocyclic group containing 3 to 12 ring atoms.

[0115] The monocyclic heterocyclic group includes, but is not limited to, a pyrrolidyl group, a piperidyl group, a piperazinyl group, a morpholyl group, a thiomorpholyl group, a homopiperazinyl group, an oxetane group, a tetrahydrofuran group, etc.

[0116] The polycyclic heterocycle includes a spiro ring, a fused ring, and a bridged ring heterocyclic group. The "spiro heterocyclic group" is a polycyclic heterocyclic group that shares one atom (referred to as a spiro atom) between monocyclic rings, and one or more (preferably 1, 2, 3, or 4) of its ring atoms are N, O, N·O, or S(O) r (where r is an integer of 0, 1, or 2), which is a heteroatom selected from the group consisting of, and the remaining ring atoms are carbon. These groups may contain one or more double bonds (preferably 1, 2, or 3), but there is no ring having a completely conjugated π electron system. Depending on the number of spiro atoms shared between rings, the spiro heterocyclic group is divided into a monospiro heterocyclic group, a dispiro heterocyclic group, or a polyspiro heterocyclic group. The spiro heterocyclic group includes, but is not limited to, the following.

[0117]

Chemical formula

[0118] The "fused heterocyclic group" refers to a polycyclic heterocyclic group in which each ring in the system shares a pair of atoms adjacent to another ring in the system. One or more (preferably 1, 2, 3, or 4) of the rings may contain one or more (preferably 1, 2, or 3) double bonds, but there is no ring having a completely conjugated π electron system, and one or more (preferably 1, 2, 3, or 4) of its ring atoms are N, O, N·O, or S(O) r (where r is an integer of 0, 1, or 2), which is a heteroatom selected from the group consisting of, and the remaining ring atoms are carbon. Depending on the number of constituent rings, it can be divided into a bicyclic, tricyclic, tetracyclic, or polycyclic fused heterocyclic group. The fused heterocyclic group includes, but is not limited to, the following.

[0119]

Chemical formula

[0120] The "bridged heterocyclic group" refers to a polycyclic heterocyclic group that shares two atoms where any two rings are not directly connected. These rings may contain one or more (preferably 1, 2, or 3) double bonds, but there is no ring having a completely conjugated π - electron system, and one or more (preferably 1, 2, 3, or 4) of its ring atoms are N, O, N·O, or S(O) r (where r is an integer 0, 1, 2) and is selected from the group consisting of heteroatoms, and the remaining ring atoms are carbon. It can be divided into bicyclic, tricyclic, tetracyclic, or polycyclic bridged heterocyclic groups according to the number of constituent rings. The bridged heterocyclic group includes, but is not limited to, the following.

[0121]

Chemical formula

[0122] The ring of the heterocyclic group may be condensed with the ring of an aryl group, heteroaryl group, or cycloalkyl group. Here, the ring connected to the parent structure is a heterocyclic group, including, but not limited to, the following.

[0123]

Chemical formula

[0124] The heterocyclic group may be optionally substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen - substituted C 1-10 alkyl group, deuterium - substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3 - 12 - membered heterocyclic group, C 6-10 aryl group, 5 - 10 - membered heteroaryl group, =O, =S, -C 0-8 alkyl - SF5, -C 0-8Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-O-S(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-O-R 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-S-C(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 It is preferably one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of.

[0125] The "aryl group" or "aromatic ring" refers to a group of a monocyclic or condensed polycyclic (i.e., rings sharing adjacent carbon atom pairs) of all carbon atoms, a group of a polycyclic (i.e., rings having adjacent carbon atom pairs) having a conjugated π electron system, preferably an all-carbon aryl group containing 6 to 10 or 6 to 8 carbon atoms. For example, "C 6-10The term "aryl group" refers to a fully carbon aryl group containing 6 to 10 carbons, including phenyl group and naphthyl group, but not limited thereto. "C" 6-8 The term "aryl group" refers to a fully carbon aryl group containing 6 to 8 carbons. The ring of the aryl group may be condensed with a heteroaryl group, a heterocyclic group or a cycloalkyl ring. Here, the ring connected to the parent structure is an aryl ring, including but not limited to the following.

[0126]

Chemical formula

[0127] The "aryl group" may be substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C0-8 Alkyl - O - C(O)R 12 , - C 0-8 Alkyl - P(O)(R 12 )2, - C 0-8 Alkyl - NR 13 R 14 , - C 0-8 Alkyl - C(=NR 13 )R 12 , - C 0-8 Alkyl - N(R 13 ) - C(=NR 14 )R 12 , - C 0-8 Alkyl - C(O)NR 13 R 14 and - C 0-8 Alkyl - N(R 13 ) - C(O)R 12 is preferably one or more (preferably 1, 2, 3, or 4) groups selected from the group consisting of.

[0128] The "heteroaryl group" refers to a heteroaromatic system containing one or more (preferably 1, 2, 3, or 4) heteroatoms, where the heteroatoms are heteroatoms including N, O, N·O, and S(O)r (where r is an integer of 0, 1, or 2), preferably a heteroaromatic system containing 5 - 10 or 5 - 8 or 5 - 6 ring atoms. For example, the "5 - 8 - membered heteroaryl group" refers to a heteroaromatic system containing 5 - 8 ring atoms, the "5 - 10 - membered heteroaryl group" refers to a heteroaromatic system containing 5 - 10 ring atoms, and includes, but is not limited to, furyl group, thienyl group, pyridyl group, pyrrolyl group, N - alkylpyrrolyl group, pyrimidinyl group, pyrazinyl group, imidazolyl group, tetrazolyl group, etc. The ring of the heteroaryl group may be condensed with an aryl group, a heterocyclic group, or a cycloalkyl ring. Here, the ring connected to the parent structure is a heteroaryl ring, including, but not limited to, the following.

[0129]

Chemical formula

[0130] The "heteroaryl group" may be optionally substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 , -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8An alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of one or more (preferably 1, 2, 3, or 4) groups.

[0131] The "alkenyl group" refers to an alkyl group as defined above, consisting of at least two carbon atoms and at least one carbon-carbon double bond, preferably a linear or branched alkenyl group containing 2-10 or 2-4 carbons. For example, "C 2-10 alkenyl group" refers to a linear or branched alkenyl group containing 2-10 carbons, and "C 2-4 alkenyl group" refers to a linear or branched alkenyl group containing 2-4 carbons. It includes, but is not limited to, vinyl group, 1-propenyl group, 2-propenyl group, 1-butenyl group, 2-butenyl group, 3-butenyl group, etc.

[0132] The "alkenyl group" may be substituted or unsubstituted. In the case of a substituted one, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3-12 membered heterocyclic group, C 6-10 aryl group, 5-10 membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11, -C 0-8 alkyl - C(O)SR 11 , -C 0-8 alkyl - S - C(O)R 12 , -C 0-8 alkyl - C(O)R 12 , -C 0-8 alkyl - O - C(O)R 12 , -C 0-8 alkyl - P(O)(R 12 )2, -C 0-8 alkyl - NR 13 R 14 , -C 0-8 alkyl - C(=NR 13 )R 12 , -C 0-8 alkyl - N(R 13 ) - C(=NR 14 )R 12 , -C 0-8 alkyl - C(O)NR 13 R 14 and -C 0-8 alkyl - N(R 13 ) - C(O)R 12 It is preferably one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of

[0133] The "alkynyl group" refers to an alkyl group as defined above, consisting of at least two carbon atoms and at least one carbon - carbon triple bond, preferably a linear or branched - chain alkynyl group containing 2 - 10 or 2 - 4 carbon atoms. For example, the "C 2-10 alkynyl group" refers to a linear or branched - chain alkynyl group containing 2 - 10 carbon atoms, and the "C 2-4 alkynyl group" refers to a linear or branched - chain alkynyl group containing 2 - 4 carbon atoms. It includes, but is not limited to, ethynyl group, 1 - propynyl group, 2 - propynyl group, 1 - butynyl group, 2 - butynyl group, 3 - butynyl group, etc.

[0134] The "alkynyl group" may be substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10Alkyl group, halogen-substituted C 1-10 Alkyl group, deuterium-substituted C 1-10 Alkyl group, C 2-10 Alkenyl group, C 2-10 Alkynyl group, C 3-12 Cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 Aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-O-S(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-O-R 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-S-C(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 ), -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 It is preferable that it is one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of.

[0135] "Alkoxy group" refers to an -O-alkyl group, and the definition of the alkyl group is as described above. For example, "C 1-10 Alkoxy group" refers to an alkyloxy group containing 1 to 10 carbons, "C 1-4 Alkoxy group" refers to an alkyloxy group containing 1 to 4 carbons, "C 1-2 Alkoxy group" refers to an alkyloxy group containing 1 to 2 carbons, and includes, but is not limited to, methoxy group, ethoxy group, propoxy group, butoxy group, etc.

[0136] The "alkoxy group" may be optionally substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 Alkyl group, halogen-substituted C 1-10 Alkyl group, deuterium-substituted C 1-10 Alkyl group, C 2-10 Alkenyl group, C 2-10 Alkynyl group, C 3-12 Cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 Aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-O-S(O)2R 10 、-C 0-8 Alkyl-S(O) r R 10 、-C 0-8 Alkyl-O-R 11 、-C 0-8 Alkyl-C(O)OR 11 、-C 0-8 Alkyl-C(O)SR 11 、-C 0-8 Alkyl-S-C(O)R 12 、-C 0-8 Alkyl-C(O)R 12 、-C 0-8Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 It is preferably one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of.

[0137] The "cycloalkoxy group" or "cycloalkyloxy group" refers to an -O-cycloalkyl group, and the definition of the cycloalkyl group is as described above. For example, "C 3-12 cycloalkoxy group" refers to a cycloalkyloxy group containing 3-12 carbons, and "C 3-6 cycloalkoxy group" refers to a cycloalkyloxy group containing 3-6 carbons, and includes, but is not limited to, cyclopropoxy group, cyclobutoxy group, cyclopentyloxy group, cyclohexyloxy group, etc.

[0138] The "cycloalkoxy group" or "cycloalkyloxy group" may be optionally substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3-12 membered heterocyclic group, C 6-10An aryl group, a 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 Alkyl-SF5, -C 0-8 Alkyl-S(O)(=N-R7)R8, -C 0-8 Alkyl-N=S(O)R8R9, -C 0-8 Alkyl-N=SR8R9, -C 0-8 Alkyl-O-S(O)2R 10 , -C 0-8 Alkyl-S(O) r R 10 , -C 0-8 Alkyl-O-R 11 , -C 0-8 Alkyl-C(O)OR 11 , -C 0-8 Alkyl-C(O)SR 11 , -C 0-8 Alkyl-S-C(O)R 12 , -C 0-8 Alkyl-C(O)R 12 , -C 0-8 Alkyl-O-C(O)R 12 , -C 0-8 Alkyl-P(O)(R 12 )2, -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 It is preferably one or more (preferably 1, 2, 3 or 4) groups selected from the group consisting of.

[0139] The "heterocyclic oxy group" or "heterocyclyloxy group" refers to an -O-heterocyclic group, and the definition of the heterocyclic group is as described above, including, but not limited to, an azetidinyl oxy group, an oxetanyl oxy group, an azacyclopentaoxy group, nitrogen, an oxanyl oxy group, etc.

[0140] The "heterocyclic oxy group" or "heterocyclic group oxy group" may be optionally substituted or unsubstituted. In the case of being substituted, the substituents are independently deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF5, -C 0-8 alkyl-S(O)(=N-R7)R8, -C 0-8 alkyl-N=S(O)R8R9, -C 0-8 alkyl-N=SR8R9, -C 0-8 alkyl-O-S(O)2R 10 , -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 )2, -C 0-8 alkyl-NR 13 R 14 , -C 0-8alkyl-C(=NR 13 )R 12 、 -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、 -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of one or more (preferably 1, 2, 3 or 4) groups.

[0141] "C 1-10 alkanoyl group" refers to a monovalent atomic group remaining after removing a hydroxy group from C 1-10 alkanoic acid, and is usually represented as "C0-9alkyl-C(O)-". For example, "C1alkyl-C(O)-" refers to an acetyl group, "C2alkyl-C(O)-" refers to a propionyl group, and "C3alkyl-C(O)-" refers to a butyryl group or an isobutyryl group.

[0142] "-C 0-8 alkyl-S(O)(=N-R7)R8" refers to a group in which the sulfur atom in -S(O)(=N-R7)R8 is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0143] "-C 0-8 alkyl-N=S(O)R8R9" refers to a group in which the nitrogen atom in -N=S(O)R8R9 is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0144] "-C 0-8 alkyl-N=SR8R9" refers to a group in which the nitrogen atom in -N=SR8R9 is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0145] "-C 0-8 alkyl-N(R 13 )-S(O)2R 10 " means -N(R 13 )-S(O)2R 10 wherein the nitrogen atom in is connected to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0146] "-C 0-8 alkyl-O-S(O)2R 10 " means -O-S(O)2R 10 wherein the oxygen atom in is connected to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0147] "-C 0-8 alkyl-S(O) r R 10 " means -S(O) r R 10 wherein the sulfur atom in is connected to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0148] "-C 0-8 alkyl-P(O)(R 12 )2" means -P(O)(R 12 )2 wherein the phosphorus atom in is connected to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0149] "-C 0-8 alkyl-O-R 11 " means -O-R 11 wherein the oxygen atom in is connected to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0150] "-C 0-8 alkyl-C(O)OR 11"-C(O)OR" 11 refers to a carbonyl group in 11 0-8 linked to a C alkyl group, where the definition of the C alkyl group is as described above. 0-8 The definition of the alkyl group is as described above.

[0151] "-C" 0-8 alkyl-C(O)SR 11 "-C(O)SR" 11 refers to a carbonyl group in 11 0-8 linked to a C alkyl group, where the definition of the C alkyl group is as described above. 0-8 The definition of the alkyl group is as described above.

[0152] "-C" 0-8 alkyl-S-C(O)R 12 "-S-C(O)R" 12 refers to a sulfur atom in 12 0-8 linked to a C alkyl group, where the definition of the C alkyl group is as described above. 0-8 The definition of the alkyl group is as described above.

[0153] "-C" 0-8 alkyl-C(O)R 12 "-C(O)R" 12 refers to a carbonyl group in 12 0-8 linked to a C alkyl group, where the definition of the C alkyl group is as described above. 0-8 The definition of the alkyl group is as described above.

[0154] "-C" 0-8 alkyl-O-C(O)R 12 "-O-C(O)R" 12 refers to an oxygen atom in 12 0-8 linked to a C alkyl group, where the definition of the C alkyl group is as described above. 0-8 The definition of the alkyl group is as described above.

[0155] "-C" 0-8 alkyl-NR 13 R 14 "-NR" 13 R 14 refers to a nitrogen atom in 14 0-8 linked to a C alkyl group, where the definition of the C alkyl group is as described above. 0-8The definition of the alkyl group is as described above.

[0156] 「-C 0-8 alkyl-C(=NR 13 )R 12 」 means -C(=NR 13 )R 12 wherein the carbon atom in is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0157] 「-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 」 means -N(R 13 )-C(=NR 14 )R 12 wherein the nitrogen atom in is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0158] 「-C 0-8 alkyl-C(O)NR 13 R 14 」 means -C(O)NR 13 R 14 wherein the carbonyl group in is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0159] 「-C 0-8 alkyl-N(R 13 )-C(O)R 12 」 means -N(R 13 )-C(O)R 12 wherein the nitrogen atom in is linked to a C 0-8 alkyl group, and the definition of the C 0-8 alkyl group is as described above.

[0160] 「Halogen-substituted C 1-10The term "alkyl group" refers to an alkyl group having 1 to 10 carbon atoms in which hydrogen in the alkyl group is optionally substituted with an atom of fluorine, chlorine, bromine, or iodine, including, but not limited to, a difluoromethyl group, a dichloromethyl group, a dibromomethyl group, a trifluoromethyl group, a trichloromethyl group, a tribromomethyl group, etc.

[0161] "Halogen-substituted C 1-10 The term "alkoxy group" refers to an alkoxy group having 1 to 10 carbon atoms in which hydrogen in the alkyl group is optionally substituted with an atom of fluorine, chlorine, bromine, or iodine. It includes, but is not limited to, a difluoromethoxy group, a dichloromethoxy group, a dibromomethoxy group, a trifluoromethoxy group, a trichloromethoxy group, a tribromomethoxy group, etc.

[0162] "Deuterium-substituted C 1-10 The term "alkyl group" refers to an alkyl group having 1 to 10 carbon atoms in which hydrogen in the alkyl group is optionally substituted with a deuterium atom. It includes, but is not limited to, a deuteromethyl group, a dideuteromethyl group, a trideuteromethyl group, etc.

[0163] "Halogen" refers to fluorine, chlorine, bromine, or iodine.

[0164] The term "optional" or "optionally" means that it is possible depending on the matters or circumstances described below but does not necessarily occur. The description includes the cases where the matters or circumstances occur or do not occur, that is, it includes both the cases where substitution has occurred and the cases where substitution has not occurred. For example, the term "heterocyclic group optionally substituted with an alkyl group" means that an alkyl group may exist but does not necessarily exist, and the description includes the cases where the heterocyclic group is substituted with an alkyl group and the cases where the heterocyclic group is not substituted with an alkyl group.

[0165] "Substitution" means that one or more "hydrogen atoms" in the base are independently substituted by corresponding numbers of substituents. Of course, the substituents are only at positions where these are chemically possible, conform to the theory of chemical valence bonds, and those skilled in the art can confirm whether substitution is possible or not without any special effort (either experimentally or theoretically). For example, an amino group or a hydroxy group having free hydrogen may be unstable when bonded to a carbon atom having an unsaturated bond (such as an olefin).

[0166] "Stereoisomer" in English refers to stereoisomer, which refers to isomers caused by differences in the spatial arrangement of atoms within a molecule, and can be divided into two types: cis-trans isomers and enantiomers, and can also be divided into two types: enantiomers and diastereoisomers. Stereoisomers caused by the rotation of a single bond are called conformational stereo-isomers and also rotamers. Stereoisomers caused by bond length, bond angle, double bonds within a molecule, the presence of a ring, etc. are called configuration stereo-isomers, and configuration stereo-isomers are divided into two types. Among them, isomers caused by the inability of a double bond or a single bond of a ring-forming carbon atom to rotate freely are geometric isomers, also called cis-trans isomers, and are divided into two structures: Z and E. For example, cis-2-butene and trans-2-butene are a pair of geometric isomers, and stereoisomers with different optical properties caused by the lack of anti-axis symmetry within a molecule are called optical isomers and are divided into structures R and S. In the present invention, the "stereoisomer" may be understood to include one or more of the enantiomers, configuration stereo-isomers, and conformational stereo-isomers unless otherwise specified.

[0167] In the present invention, "pharmaceutically acceptable salts" refer to pharmaceutically acceptable acid addition salts, including inorganic acid salts and organic acid salts, and these salts can be prepared by methods known in this field.

[0168] The term "pharmaceutical composition" refers to a mixture of one or more compounds described in this specification, or their physiologically / pharmaceutically acceptable salts or prodrugs, and other chemical components, together with other components such as physiologically / pharmaceutically acceptable carriers and excipients. The purpose of the pharmaceutical composition is to facilitate administration to an organism and exert biological activity by contributing to the absorption of the active ingredient.

[0169] Hereinafter, the present invention will be described in more detail and comprehensively with reference to examples, which do not limit the present invention, and the present invention is not limited only to the content of the examples.

[0170] The structure of the compounds of the present invention was confirmed by nuclear magnetic resonance (NMR) or / and liquid chromatography-mass spectrometry (LC-MS). The chemical shift (δ) of NMR is expressed in units of parts per million (ppm). The NMR measurements were performed using a Bruker AVANCE-400 / 500 nuclear magnetic resonance spectrometer, and the solvents for the measurements were deuterated dimethyl sulfoxide (DMSO-d6), deuterated methanol (CD3OD), and deuterated chloroform (CDCl3), with tetramethylsilane (TMS) as the internal standard.

[0171] The LC-MS measurements were performed using an Agilent 6120 mass spectrometer. The HPLC measurements were performed using an Agilent 1200DAD high-pressure liquid chromatograph (Sunfire C18 150 × 4.6 mm chromatographic column) and a Waters 2695-2996 high-pressure liquid chromatograph (Gimini C18 150 × 4.6 mm chromatographic column).

[0172] For thin layer chromatography, silica gel plates from Yantai Huanghai HSGF254 or Qingdao GF254 were used. The specifications used for TLC were 0.15 mm - 0.20 mm, and the specifications used for the separation and purification of products by thin layer chromatography were 0.4 mm - 0.5 mm. For column chromatography, silica gel with a mesh size of 200 - 300 from Yantai Huanghai was usually used as the carrier.

[0173] The starting materials in the examples of the present invention are known commercially available products or those that can be synthesized by methods known in this field.

[0174] Unless otherwise specified, all reactions of the present invention are carried out under continuous magnetic stirring in an atmosphere of dry nitrogen or argon. The solvent is a dry solvent, and the unit of the reaction temperature is degrees Celsius (°C).

[0175] I. Production of Intermediate Intermediate 1-1: Production of (S)-3-bromo-1-(4-((tert-butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-1H-pyrazolo[4,3-c]pyridine

Chemical formula

[0176] First step: Synthesis of 3-bromo-6-chloro-1H-pyrazolo[4,3-c]pyridine

Chemical formula

[0177] Second step: Synthesis of (R)-4-((tert-butyldimethylsilyl)oxy)butan-2-ol

Chemical formula

[0178] Step 3: Synthesis of (R)-4-((tert-butyldimethylsilyl)oxy)butan-2-yl 4-methylbenzene-1-sulfonate

Chemical formula

[0179] Step 4: Synthesis of (S)-3-bromo-1-(4-((tert-butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-1H-pyrazolo[4,3-c]pyridine

Chemical formula

[0180] Intermediates 1-2 to 1-6 can be produced by referring to the synthesis method of Intermediate 1-1 and selecting the corresponding raw materials.

Table 1

[0181] Intermediate 1-7: Preparation of (1-((3-bromo-6-chloro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol

Chem.

[0182] First step: Synthesis of methyl 1-(iodomethyl)cyclopentane-1-carboxylate

Chem.

[0183] Second step: Synthesis of methyl 1-((3-bromo-6-chloro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentane-1-carboxylate

Chemical formula

[0184] Step 3: Synthesis of (1-((3-bromo-6-chloro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol

Chemical formula

[0185] Intermediates 1-8 to 1-10 are prepared by referring to the synthetic route of Intermediate 1-7 and selecting the corresponding raw materials.

Table 2

[0186] Preparation of Intermediate 2-1: (S)-1-(4-((tert-butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-3-(prop-1-yn-1-yl)-1H-pyrazolo[4,3-c]pyridine

Chemical formula

[0187] Intermediate 2-2: Preparation of 1-((S)-4-((tert-butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-3-(((S)-1-methylpyrrolidin-2-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridine

Chemical formula

[0188] First step: Synthesis of tert-butyl (S)-2-ethynylpyrrolidine-1-carboxylate

Chemical formula

[0189] Second step: Synthesis of (S)-2-((1-((S)-4-((tert-butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-1H-pyrazolo[4,3-c]pyridin-3-yl)ethynyl)pyrrolidine-1-carboxylic acid tert-butyl ester

Chemical formula

[0190] Step 3: Synthesis of 1-((S)-4-((tert-butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-3-(((S)-pyrrolidin-2-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridine [Chemical formula] (S)-2-((1-((S)-4-((tert-Butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-1H-pyrazolo[4,3-c]pyridin-3-yl)ethynyl)pyrrolidine-1-carboxylic acid tert-butyl ester (720 mg, 1.35 mmol) was dissolved in hexafluoroisopropanol (20 mL), and then TFA (1.0 mL, 13.50 mmol) was added dropwise, followed by reaction at room temperature for 1 hour. After completion of the reaction, CH2Cl2 was added for dilution, and the mixture was washed successively with saturated aqueous NaHCO3, pure water, and saturated brine, and dried over anhydrous sodium sulfate. After filtration, the filtrate was concentrated to obtain a crude product, which was used directly in the next reaction. MS m / z (ESI): 433.2 [M+H] + 。

[0191] Step 4: Synthesis of 1-((S)-4-((tert-Butyldimethylsilyl)oxy)butan-2-yl)-6-chloro-3-(((S)-1-methylpyrrolidin-2-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridine

Chemical Structure

[0192] Production of Intermediate 2-3: (1-((6-Chloro-3-((1-methylpiperidin-4-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol

Chemical formula

[0193] First Step: Synthesis of tert-butyl 4-((1-((1-(((tert-butyldimethylsilyl)oxy)methyl)cyclopentyl)methyl)-6-chloro-1H-pyrazolo[4,3-c]pyridin-3-yl)ethynyl)piperidine-1-carboxylate

Chemical formula

[0194] Second Step: Synthesis of (1-((6-Chloro-3-(piperidin-4-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol [Chemical formula] t-Butyl 4-((1-((1-(((t-butyldimethylsilyl)oxy)methyl)cyclopentyl)methyl)-6-chloro-1H-pyrazolo[4,3-c]pyridin-3-yl)ethynyl)piperidine-1-carboxylate (450 mg, 0.766 mmol) was dissolved in CH2Cl2 (15 mL), then TFA (0.57 mL, 7.662 mmol) was added dropwise, and the mixture was stirred at room temperature for 2 hours. After completion of the reaction, saturated aqueous sodium bicarbonate solution was added to the reaction solution, and the mixture was extracted with dichloromethane. The combined organic phases were washed successively with water and saturated brine, and dried over anhydrous sodium sulfate. After filtration and concentration, the crude product (1-((6-chloro-3-(piperidin-4-ylethynyl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol (260 mg, 0.697 mmol, yield: 91.0%) was obtained. MS m / z (ESI): 373.2 [M+H] + .

[0195] Third step: Synthesis of (1-((6-chloro-3-((1-methylpiperidin-4-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol [Chemical formula] 1 - ((6 - chloro - 3 - (piperidin - 4 - ylethynyl)-1H - pyrazolo[4,3 - c]pyridin - 1 - yl)methyl)cyclopentyl)methanol (260 mg, 0.697 mmol) was dissolved in CH2Cl2 (20 mL), then 33% aqueous formaldehyde solution (299 mg, 3.486 mmol) and NaBH(OAc)3 (739 mg, 3.486 mmol) were added, and the mixture was stirred at room temperature for 18 h. After completion of the reaction, saturated aqueous NaHCO3 solution was added to quench the reaction, and the mixture was extracted three times with dichloromethane. The combined organic phases were concentrated and then separated by column chromatography to obtain (1 - ((6 - chloro - 3 - ((1 - methylpiperidin - 4 - yl)ethynyl)-1H - pyrazolo[4,3 - c]pyridin - 1 - yl)methyl)cyclopentyl)methanol (260 mg, 0.672 mmol, yield: 96.4%). MS m / z (ESI): 387.2 [M + H] + 。

[0196] Intermediates 2 - 4 to 2 - 23 can be prepared by referring to the synthesis methods of Intermediate 2 - 2 or 2 - 3 and selecting the corresponding raw materials.

Table 3 - 1

Table 3 - 2

Table 3 - 3

Table 3 - 4

Table 3 - 5

[0197] Preparation of Intermediate 3 - 1: t - butyl 3 - ((methanesulfonyl)methyl)azetidine - 1 - carboxylate

Chem.

[0198] Intermediate 3-2: Preparation of t-butyl (S)-3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidine-1-carboxylate

Chemical formula

[0199] First step: Synthesis of t-butyl (S)-3-(((trifluoromethyl)thio)methyl)pyrrolidine-1-carboxylate

Chemical formula

[0200] Second step: Synthesis of t-butyl (S)-3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidine-1-carboxylate

Chemical formula

[0201] Intermediate 3-3: Preparation of t-butyl (S)-3-((ethylsulfonyl)methyl)pyrrolidine-1-carboxylate

Chemical formula

[0202] First step: Synthesis of t-butyl (S)-3-((tosyloxy)methyl)pyrrolidine-1-carboxylate

Chemical formula

[0203] Second step: Synthesis of tert-butyl (S)-3-((ethylsulfonyl)methyl)-1-pyrrolidinecarboxylate

Chemical formula

[0204] Intermediate 3-4: Preparation of (S)-3-((cyclobutylsulfonyl)methyl)pyrrolidine-1-carboxylic acid tert-butyl ester

Chemical formula

[0205] First step: Synthesis of cyclobutanesulfonyl chloride

Chemical formula

[0206] Second Step: Synthesis of Sodium Cyclobutanesulfinate

Chem.

[0207] Third Step: Synthesis of t-Butyl (S)-3-((Cyclobutylsulfonyl)methyl)pyrrolidine-1-carboxylate

Chem.

[0208] Intermediates 3-5 to 3-15 are prepared by referring to part of the route of Intermediate 3-3 or 3-4 and selecting the corresponding raw materials.

Table 4

[0209] Intermediate 4-1: Preparation of 1-((1-(((t-butyldimethylsilyl)oxy)methyl)cyclobutyl)methyl)-6-chloro-3-(3-((methanesulfonyl)methyl)azetidin-1-yl)-1H-pyrazolo[4,3-c]pyridine

Chemical formula

[0210] First step: Synthesis of 3-((methanesulfonyl)methyl)azetidine hydrochloride

Chemical formula

[0211] Second Step: Synthesis of 1-((1-(((t-Butyldimethylsilyl)oxy)methyl)cyclobutyl)methyl)-6-chloro-3-(3-((methanesulfonyl)methyl)azetidin-1-yl)-1H-pyrazolo[4,3-c]pyridine

Chemical Structure

[0212] Preparation of Intermediate 4-2: (S)-(1-((6-Chloro-3-(3-((ethylsulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol

Chem.

[0213] First Step: Synthesis of (S)-3-((ethylsulfonyl)methyl)pyrrolidine hydrochloride

Chem.

[0214] Second Step: Synthesis of methyl (S)-1-((6-chloro-3-(3-((ethylsulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentane-1-carboxylate

Chem.

[0215] Step 3: Synthesis of (S)-(1-((6-chloro-3-(3-((ethylsulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol

Chemical formula

[0216] Intermediates 4-3 to 4-23 can be prepared by referring to the synthesis methods of Intermediate 4-1 or 4-2 and selecting the corresponding raw materials.

Table 5-1

Table 5-2

Table 5-3

Table 5-4

[0217] Preparation of Intermediate 5-1: 4-(4-Aminopyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one

Chemical formula

[0218] First Step: Synthesis of 2-Methyl-1-((2-(Trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one

Chemical Structure

[0219] Second Step: Synthesis of 4-Bromo-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one

Chemical Structure

[0220] Step 3: Synthesis of tert-Butyl (t-Butoxycarbonyl)(2-Chloropyrimidin-4-yl)Carbamate

Chem.

[0221] Step 4: Synthesis of tert-Butyl (t-Butoxycarbonyl)(2-(2-Methyl-3-oxo-1-((2-(Trimethylsilyl)ethoxy)methyl)-2,3-dihydro-1H-pyrazol-4-yl)pyrimidin-4-yl)Carbamate

Chem.

[0222] Step 5: Synthesis of 4-(4-aminopyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one

Chemical formula

[0223] II. Preparation of the compounds of the examples Example A1: (S)-1 1 ,5-dimethyl-4 3 -(prop-1-yn-1-yl)-1 1 H,4 1 Preparation of H-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimidino-1(4,5)-pyrazole heterocyclooctafane

Chemical formula

[0224] First step: Synthesis of (S)-4-(4-((1-(4-((t-butyldimethylsilyl)oxy)butan-2-yl)-3-(prop-1-yn-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one

Chemical formula

[0225] Second step: Synthesis of (S)-4-(4-((1-(4-Hydroxybutan-2-yl)-3-(prop-1-yn-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1,2-dihydro-3H-pyrazol-3-one

Chemical formula

[0226] Step 3: Synthesis of (S)-1 1 ,5-dimethyl-4 3 -(prop-1-yn-1-yl)-1 1 H,4 1 H-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimidino-1(4,5)-pyrazole heterocyclooctaphane

Chemical Structure

[0227] Examples A2 to A3 can be produced by referring to the synthesis method of Example A1 and selecting the corresponding raw materials.

Table 6

[0228] Example 1: Preparation of 1'-Methyl-3'-((1-methylpiperidin-4-yl)ethynyl)spiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazole heterocyclooctafane)

Chemical Structure

[0229] First Step: Synthesis of 4-(4-((1-((1-(Hydroxymethyl)cyclopentyl)methyl)-3-((1-methylpiperidin-4-yl)ethynyl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one

Chemical Structure

[0230] Second step: Synthesis of 4-(4 - ((1 - ((1 - (hydroxymethyl)cyclopentyl)methyl)-3 - ((1 - methylpiperidin - 4 - yl)ethynyl)-1H - pyrazolo[4,3 - c]pyridin - 6 - yl)amino)pyrimidin - 2 - yl)-2 - methyl - 1,2 - dihydro - 3H - pyrazol - 3 - one

Chemical Structure

[0231] Step 3: Synthesis of 1'-methyl-3'-((1-methylpiperidin-4-yl)ethynyl)spiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimidino-1(4,5)-pyrazole heterocyclooctafane)

Chem.

[0232] Examples 2 to 12 can be prepared by referring to the synthesis method of Example 1 or A1 and selecting the corresponding raw materials.

Table 7-1

Table 7-2

Table 7-3

[0233] Example 13: Preparation of (R)-2-(1-(1'-methylspiro[cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane]-3'-yl)pyrrolidin-3-yl)propan-2-ol

Chemical Structure

[0234] First Step: Synthesis of (R)-2-(1-(6-chloro-1-((1-(hydroxymethyl)cyclopentyl)methyl)-1H-pyrazolo[4,3-c]pyridin-3-yl)pyrrolidin-3-yl)propan-2-ol

Chemical Structure

[0235] Second step: Synthesis of (R)-4-(4-((1-((1-(hydroxymethyl)cyclopentyl)methyl)-3-(3-(2-hydroxypropyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one [Chemical formula] (R)-2-(1-(6-chloro-1-((1-(hydroxymethyl)cyclopentyl)methyl)-1H-pyrazolo[4,3-c]pyridin-3-yl)pyrrolidin-3-yl)propan-2-ol (0.40 g, 0.74 mmol) and 4-(4-aminopyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one (0.24 g, 0.74 mmol) were dissolved in 1,4-dioxane (8 mL), then Cs2CO3 (0.48 g, 1.47 mmol) and Brettphos-Pd-G3 (0.13 g, 0.15 mmol) were added. After purging with nitrogen, the mixture was heated by microwave to 130 °C and reacted for 2 hours. After the reaction solution was cooled, ethyl acetate was added for dilution, and it was washed once with water and saturated brine respectively. The organic layer was separated, dried over anhydrous sodium sulfate, concentrated, and the obtained crude product was separated by column chromatography (eluent: CH2Cl2 / MeOH 0 - 6%) to obtain (R)-4-(4-((1-((1-(hydroxymethyl)cyclopentyl)methyl)-3-(3-(2-hydroxypropyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one (0.38 g, purity: 62.6%, yield: 47.6%). MS m / z (ESI): 678.6 [M+H] + 。

[0236] Step 3: Synthesis of (R)-4-(4-((1-((1-(hydroxymethyl)cyclopentyl)methyl)-3-(3-(2-hydroxypropyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-1-methyl-1H-pyrazol-5-ol

Chemical Structure

[0237] Step 4: Synthesis of (R)-2-(1-(1'-methylspiro[cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimidino-1(4,5)-pyrazoleheterocyclooctaphane]-3'-yl)pyrrolidin-3-yl)propan-2-ol [Chemical Structure] (R)-4-(4-((1-((1-(Hydroxymethyl)cyclopentyl)methyl)-3-(3-(2-Hydroxypropyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-1-methyl-1H-pyrazol-5-ol (180 mg, purity: 85.4%, 0.28 mmol) was dissolved in toluene (5 mL), CMBP (542 mg, 2.25 mmol) was added, and the mixture was heated to 130 °C and reacted for 24 hours. The reaction was completed, cooled to room temperature, and saturated aqueous NaHCO3 solution was added to quench the reaction. The mixture was extracted twice with ethyl acetate, the organic phase layers were combined, washed with saturated brine, and dried over anhydrous sodium sulfate. After filtration and concentration, separation by column chromatography (eluent: CH2Cl2 / MeOH 0 - 5%) gave (R)-2-(1-(1'-methylspiro[cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimidin-1(4,5)-pyrazoleheterocyclooctafane]-3'-yl)pyrrolidin-3-yl)propan-2-ol (34.4 mg, yield: 22.9%). MS m / z (ESI): 530.4 [M+H] + 。 1 HNMR (400 MHz, DMSO-d6) δ 10.26 (s,1H), 9.18 (s,1H), 8.71 (s,1H), 8.29 (d, J = 5.8 Hz,1H), 8.00 (s,1H), 6.77 (d, J = 5.9 Hz,1H), 4.37 (s,1H), 3.80 (s,3H), 3.71 - 3.61 (m,1H), 3.60 - 3.38 (m,3H), 2.41 - 2.28 (m,1H), 1.92 (q, J = 9.4 Hz,4H), 1.70 (brs,2H), 1.17 (brs,3H), 1.15 (s,3H).

[0238] Example 14: Preparation of (S)-1'-methyl-3'-(3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidin-1-yl)spiro[cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazole heterocyclooctafane) [Chemical formula]

[0239] First step: Synthesis of (S)-4-(4-((1-((1-(hydroxymethyl)cyclopentyl)methyl)-3-(3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one [Chemical formula] (S)-(1-((6-chloro-3-(3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)cyclopentyl)methanol (0.48 g, 0.98 mmol) and 4-(4-aminopyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one (330 mg, 1.03 mmol) were dissolved in 1,4-dioxane (8 mL). After that, Cs2CO3 (0.64 g, 1.95 mmol) and Brettphos-Pd-G3 (0.18 g, 0.195 mmol) were added. After purging with nitrogen, the mixture was heated by microwave to 130 °C and reacted for 2 hours. After the reaction solution was cooled, ethyl acetate was added for dilution, and it was washed once with water and saturated brine in sequence. The organic layer was separated and dried over anhydrous sodium sulfate. After filtration and concentration, the obtained crude product was separated by column chromatography to obtain (S)-4-(4-((1-((1-(hydroxymethyl)cyclopentyl)methyl)-3-(3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1,2-dihydro-3H-pyrazol-3-one (0.32 g, purity: 73.6%, yield: 31.5%). MS m / z (ESI): 766.4 [M+H] + 。

[0240] Second step: Synthesis of (S)-4-(4-((1-((1-(hydroxymethyl)cyclopentyl)methyl)-3-(3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)amino)pyrimidin-2-yl)-2-methyl-1,2-dihydro-3H-pyrazol-3-one

Chemical formula

[0241] Step 3: Synthesis of (S)-1'-methyl-3'-(3-(((trifluoromethyl)sulfonyl)methyl)pyrrolidin-1-yl)spiro[cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimidino-1(4,5)-pyrazole heterocyclooctafane)

Chemical Structure

[0242] Examples 15 to 47 and Example A4 are prepared by referring to the routes of Example A1, 1, 13 or 14 and selecting the corresponding raw materials.

Table 8-1

Table 8-2

Table 8-3

Table 8-4

Table 8-5

Table 8-6

Table 8-7

Table 8-8

Table 8-9

[0243] Example 48: Preparation of (R)-N-(1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane)-3'-yl)pyrrolidin-3-yl)methanesulfonamide

Chemical Structure

[0244] First Step: Synthesis of (R)-1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane)-3'-yl)pyrrolidin-3-amine

Chemical Structure

[0245] Second step: Synthesis of (R)-N-(1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane)-3'-yl)pyrrolidin-3-yl)methanesulfonamide [Chemical formula] The crude product obtained in the previous step was dissolved in dry CH2Cl2 (3.0 mL), and triethylamine (0.10 mL, 0.74 mmol) and methanesulfonic anhydride (32 mg, 0.18 mmol) were added with cooling in an ice bath, followed by reaction at room temperature for 1 hour. After adding saturated aqueous NaHCO3 solution to quench the reaction, extraction was performed twice with CH2Cl2. The combined organic phases were successively washed with saturated brine and dried over anhydrous sodium sulfate. Filtration, concentration, and separation by column chromatography gave (R)-N-(1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazole heterocyclooctafane)-3'-yl)pyrrolidin-3-yl)methanesulfonamide (7.3 mg, yield: 13%). MS m / z (ESI): 565.3 [M+H] + 。 1 H NMR (400 MHz, DMSO-d6) δ 10.26 (s, 1H), 9.21 (s, 1H), 8.71 (d, J = 0.9 Hz, 1H), 8.30 (d, J = 5.8 Hz, 1H), 8.00 (s, 1H), 6.77 (dd, J = 5.8, 1.3 Hz, 1H), 4.61 (brs, 2H), 4.08 (p, J = 6.3 Hz, 1H), 3.80 (s, 4H), 3.68 (dd, J = 8.7, 5.9 Hz, 1H), 3.58 (q, J = 7.8 Hz, 1H), 3.41 (dd, J = 9.9, 5.5 Hz, 1H), 3.00 (s, 3H), 2.35 - 2.24 (m, 2H), 2.04 - 1.85 (m, 4H), 1.70 (s, 2H).

[0246] Example 49: Preparation of (R)-N-(1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazole heterocyclooctafane)-3'-yl)pyrrolidin-3-yl)acetamide

Chemical Structure

[0247] Example 50: Preparation of (R)-2,2,2-Trifluoro-N-(1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane)-3'-yl)pyrrolidin-3-yl)acetamide

Chemical formula

[0248] First step: Synthesis of (R)-1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane)-3'-yl)pyrrolidin-3-amine

Chemical formula

[0249] Second step: Synthesis of (R)-2,2,2-Trifluoro-N-(1-(1'-methylspiro(cyclopentane-1,6'-8-oxa-3-aza-4(6,1)-pyrazolo[4,3-c]pyridino-2(2,4)-pyrimido-1(4,5)-pyrazoleheterocyclooctafane)-3'-yl)pyrrolidin-3-yl)acetamide

Chemical formula

[0250] Examples 51 to 58 can be produced by referring to the synthesis methods of Examples 48, 49 or 50 and selecting the corresponding raw materials.

Table 9-1

Table 9-2

[0251] The nuclear magnetic data of the compounds produced in the above examples are as follows.

Table 10-1

Table 10-2

Table 10-3

Table 10-4

Table 10-5

Table 10-6

Table 10-7

Table 10-8

[0252] III. Biological Measurement and Evaluation (Cell Proliferation Experiment) (I) Reagents and Consumables DMEM Medium (Gibco, Cat#11965118) RPMI1640 Medium (Gibco, Cat#11875119) Fetal Bovine Serum FBS (GBICO, Cat#10099-141) CellTiter-Glo® Luminescent Cell Viability Assay Kit (Promega, Cat# G7572) Black clear-bottom 96-well plate (Corning®, Cat# 3603)

[0253] (2) Instruments SpectraMax multi-label microplate reader (MD, 2104-0010A) Carbon dioxide incubator (Thermo Scientific 3100 series) Biological safety cabinet (Thermo Scientific, 1300 series type A2) Inverted microscope (Olympus, CKX41SF) Siemens refrigerator (KK25E76TI)

[0254] (3) Cell lines and culture conditions

Table 11

[0255] (4) Experimental procedures 1. Cell culture and seeding (1) Cells in the logarithmic growth phase were obtained and counted using a platelet counter. The cell viability was detected by the trypan blue exclusion method to ensure that the cell viability was 90% or higher. (2) The cell concentration was adjusted to reach the desired final density, and 90 μL of the cell suspension was added to the 96-well plate. (3) The cells were incubated overnight in the 96-well plate at 37°C, 5% CO2, and 95% humidity.

[0256] 2. T0 benchmark data (1) 10 μL of PBS was added to each well of the T0 plate containing cells. (2) The CTG reagent was thawed, and the cell plate was equilibrated at room temperature for 30 minutes. (3) An equal volume of the CTG solution was added to each well. (4) The cells were lysed by shaking with an orbital shaker for 5 minutes. (5) The cell plate was placed at room temperature for 20 minutes to stabilize the luminescence signal. (6) The T0 fluorescence signal value was read.

[0257] 3. Dilution and addition of the compound (1) Based on the compound information table, the corresponding volume of DMSO was added to the corresponding compound powder to prepare a 10 mM stock solution. (2) Compound solutions diluted 1000-fold and 3.16-fold were prepared. (3) The compound solution diluted 1000× was further diluted 100-fold with PBS to prepare a 10-fold compound solution. The highest concentration was set at 10 μM, with nine concentrations. After dilution 3.16-fold, 10 μL of the drug solution was added to each well of a 96-well plate for inoculation, and the cells were inoculated. Three duplicate wells were set for each compound concentration, and the final concentration of DMSO was set at 0.1%. (4) The cells were placed in the 96-well plate containing the drug and continuously cultured at a temperature of 37 °C, 5% CO2, and 95% humidity for 72 hours, followed by CTG analysis.

[0258] 4. Reading of the fluorescence signal (1) The CTG reagent was thawed, and the cell plate was equilibrated at room temperature for 30 minutes. (2) An equal volume of CTG solution was added to each well. (3) The cells were lysed by shaking with an orbital shaker for 5 minutes. (4) The cell plate was placed at room temperature for 20 minutes to stabilize the fluorescence signal. (5) The fluorescence value was read.

[0259] 5. Data processing The data was analyzed using GraphPad Prism 7.0 software, and the data was fitted by non-linear S-curve regression to obtain a dose-effect curve. Based on this, the IC 50 value (unit: nM) was calculated. For specific experimental results, refer to Table 1.

[0260] Cell survival rate (%) = (Lum test drug - Lum culture medium control) / (Lum cell control - Lum culture medium control) × 100%.

[0261]

Table 12-1

Table 12-2

[0262] The "positive compound" used in the biological measurement, evaluation and mouse pharmacokinetic experiment of this application is one of the compounds (Compound 101) with the best activity range in WO2021168074A1, and its chemical structural formula is as follows.

Chemical formula

[0263] From the biological activity data of the compounds in specific examples of the present invention, a series of compounds of the present invention have a strong inhibitory effect on various mutations of C797S with EGFR drug resistance, including EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation and Del19 / T790M / C797S triple mutation at the cell level, and have high selectivity for EGFR WT.

[0264] IV. Mouse pharmacokinetic experiment (I) Purpose of the study The purpose of this test is to study the pharmacokinetic behavior of some compounds of the present invention, and the administration method is single oral (PO) administration to ICR mice. (II) Test protocol 1. Test drug The compounds used in this test are derived from the compounds in specific examples of the present invention and the listed positive compounds. 2. Test animals ICR male mice, N = 9, and the supplier is Shanghai Xipu'er-Bikai Experimental Animal Co., Ltd. 3. Preparation and Administration of Drugs The compounds were weighed and dissolved in their respective solvents (10% PG + 10% Solutol® + 80% pH 3 citrate buffer), shaken and sonicated to obtain a 1 mg / mL solution. After fasting nine mice overnight, they were orally administered at a dose of 10 mg / kg (or IV 2 mg / kg). 4. Sample Collection Blood was collected from the submandibular vein at approximately 90 μL per time point, anticoagulated with sodium heparin, placed on ice after collection, and centrifuged within 1 hour to separate plasma (centrifugation conditions: 8000 revolutions per minute, 6 minutes, 2 - 8°C). The blood collection time points were 0, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 hours. The samples were stored in a -20°C refrigerator.

[0265] 40 μL of plasma sample was added to 160 μL of ice-cold acetonitrile containing an internal standard, vortexed for 3 minutes, and centrifuged at 11000 revolutions per minute for 5 minutes. 100 μL of the supernatant was added to 100 μL of water, and 5 μL was injected into LC / MS / MS for analysis.

[0266] 5. Test Results

Table 13

[0267] From the pharmacokinetic data of the compounds in the above specific examples, a series of compounds of the present invention enter the mouse body through single oral (10 mg / kg) absorption and have very good pK data. Compared with the positive compounds, the AUC of a series of compounds of the present invention is improved by at least 5 times, and the AUC of the compounds in some examples is further improved by dozens of times. Experiments prove that the oral exposure of a series of compounds of the present invention is significantly improved and has good oral bioavailability, and it is expected to solve the problem that the pK of the positive compounds decreases and they are not suitable for oral administration.

[0268] All documents related to the present invention are cited for reference in this application so that each document is cited independently. Further, after reading the above content of the present invention, those skilled in the art can make various changes and modifications to the present invention, and it should be understood that those equivalent forms are included in the scope of the claims of the present invention.

Claims

1. Formula (I): 【Chemical 1】 (wherein: X 1 is CR a or N, and X 2 is CR b or N, and X 3 is CR c or N, and X 4 is CR d or N, and L 1 is CR 5a R 5b and L 2 is (CR 5c R 5d ) p , NR 6a , O, S, S(O), S(O) 2 or C(O), and L 3 is a bond, CR 5e R 5f , NR 6b , O, S, S(O), S(O) 2 or C(O), and Alternatively, L 2 and L 3 both form a C 4-12 cycloalkyl group, a 4- to 12-membered heterocyclic group, a C 6-10 aryl group or a 5- to 10-membered heteroaryl group, and the C 4-12 cycloalkyl group, a 4- to 12-membered heterocyclic group, a C 6-10 aryl group or a 5- to 10-membered heteroaryl group are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, a 3- to 12-membered heterocyclic group, a C 6-10 aryl group, a 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 , -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 may be substituted by one or more substituents selected from the group consisting of L 4 is CR 5g R 5h , O, S, S(O), S(O) 2 , NR 6c or C(O), and Ring A is C 4-12 a cycloalkyl group, a 4- to 12-membered heterocyclic group, C 6-10 an aryl group or a 5- to 10-membered heteroaryl group, and R 1 is hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, said groups each independently optionally further having one or more deuteriums, halogens, cyano groups, nitro groups, azide groups, C 1-10 alkyl groups, C 2-10 alkenyl groups, C 2-10 alkynyl groups, C 3-12 cycloalkyl groups, 3- to 12-membered heterocyclic groups, C 3-12 alkyl groups substituted with a cycloalkyl group, C 1-10 alkyl groups substituted with a 3- to 12-membered heterocyclic group, C 1-10 alkyl groups, C 6-10 aryl groups, 5- to 10-membered heteroaryl groups, =O, =S, -C 0-8 alkyl-SF 5 -C 0-8 alkyl-S(O)(=N-R 7 )R 8 -C 0-8 alkyl-N=S(O)R 8 R 9 -C 0-8 alkyl-N=SR 8 R 9 -C 0-8 alkyl-N(R 13 )-S(O) 2 R 10 -C 0-8 alkyl-O-S(O) 2 R 10 -C 0-8 alkyl-S(O) r R 10 -C 0-8 alkyl-O-R 11 -C 0-8 alkyl-C(O)OR 11 -C 0-8 alkyl-C(O)SR 11 -C 0-8 alkyl-S-C(O)R 12 -C 0-8 alkyl-C(O)R 12 -C 0-8 alkyl-O-C(O)R 12 -C 0-8 alkyl-P(O)(R 12 ) 2 , -C 0-8 alkyl - NR 13 R 14 , -C 0-8 alkyl - C(=NR 13 )R 12 , -C 0-8 alkyl - N(R 13 )(-C(=NR 14 )R 12 , -C 0-8 alkyl - C(O)NR 13 R 14 and -C 0-8 alkyl - N(R 13 )(-C(O)R 12 substituted with one or more substituents selected from the group consisting of, and each of said groups is independently optionally further substituted with one or more deuteriums, halogens, cyano groups, nitro groups, azide groups, C 1-10 alkyl group, halogen - substituted C 1-10 alkyl group, deuterium - substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3 - 12 - membered heterocyclic group, C 6-10 aryl group, 5 - 10 - membered heteroaryl group, =O, =S, -C 0-8 alkyl - SF 5 , -C 0-8 alkyl - S(O)(=N - R 7 )R 8 , -C 0-8 alkyl - N=S(O)R 8 R 9 , -C 0-8 alkyl - N=SR 8 R 9 , -C 0-8 alkyl - N(R 13 )(-S(O) 2 R 10 , -C 0-8 alkyl - O - S(O) 2 R 10 , -C 0-8 alkyl - S(O) r R 10 , -C 0-8 alkyl - O - R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)SR 11 , -C 0-8 alkyl-S-C(O)R 12 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-P(O)(R 12 ) 2 , -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with a substituent selected from the group consisting of Each R 2 is independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, said groups are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、 -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、 -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of: Each R 3 、R a and R b are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of R 4 and R c are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 ), R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of R d is hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of R 5a and R 5b are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5a and R 5b together with the carbon atom directly linking them, form C(O), C 3-6 cycloalkyl group, 4- to 10-membered heterocyclic group, C 6-10 aryl group or 5- to 10-membered heteroaryl group, and each of said groups is independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF 5 ,-C 0-8 alkyl-S(O)(=N-R 7 )R 8 ,-C 0-8 alkyl-N=S(O)R 8 R 9 ,-C 0-8 alkyl-N=SR 8 R 9 ,-C 0-8 alkyl-O-S(O) 2 R 10 ,-C 0-8 alkyl-S(O) r R 10 ,-C 0-8 alkyl-O-R 11 ,-C 0-8 alkyl-C(O)OR 11 ,-C 0-8 alkyl-C(O)SR 11 ,-C 0-8 alkyl-S-C(O)R 12 ,-C 0-8 alkyl-C(O)R 12 ,-C 0-8 alkyl-O-C(O)R 12 ,-C 0-8 Alkyl-P(O)(R 12 ) 2 , -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C (=NR 13 ) R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 ) R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of: Each R 5c and R 5d are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5c and R 5d together with the carbon atom directly connecting them form a C 3-6 cycloalkyl group, 4- to 10-membered heterocyclic group, C 6-10 aryl group or 5- to 10-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF 5 -C 0-8 alkyl-S(O)(=N-R 7 )R 8 -C 0-8 alkyl-N=S(O)R 8 R 9 -C 0-8 alkyl-N=SR 8 R 9 -C 0-8 alkyl-O-S(O) 2 R 10 -C 0-8 alkyl-S(O) r R 10 -C 0-8 alkyl-O-R 11 -C 0-8 alkyl-C(O)OR 11 -C 0-8 alkyl-C(O)SR 11 -C 0-8 alkyl-S-C(O)R 12 -C 0-8 alkyl-C(O)R 12 -C 0-8 alkyl-O-C(O)R 12 -C 0-8 alkyl-P(O)(R 12 ), -C 2 alkyl-NR 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 ), -C 12 alkyl-N(R 0-8 alkyl-N(R 13 alkyl-N(R 14 alkyl-N(R 12 ), -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 alkyl-N(R 12 ), and is substituted with one or more substituents selected from the group consisting of, provided that when R 5c or R 5d is H or a C 1-4 alkyl group, R 1 is an optionally substituted C 2-10 alkynyl group, or, L 3 is O, S, S(O) or S(O) 2 ), provided that R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5e and R 5f together with the carbon atom directly connecting them form a C 3-6 cycloalkyl group, 4- to 10-membered heterocyclic group, C 6-10 aryl group or 5- to 10-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF 5 ,-C 0-8 alkyl-S(O)(=N-R 7 )R 8 ,-C 0-8 alkyl-N=S(O)R 8 R 9 ,-C 0-8 alkyl-N=SR 8 R 9 ,-C 0-8 alkyl-O-S(O) 2 R 10 ,-C 0-8 alkyl-S(O) r R 10 ,-C 0-8 alkyl-O-R 11 ,-C 0-8 alkyl-C(O)OR 11 ,-C 0-8 alkyl-C(O)SR 11 ,-C 0-8 alkyl-S-C(O)R 12 ,-C 0-8 alkyl-C(O)R 12 ,-C 0-8 alkyl-O-C(O)R 12 ,-C 0-8 Alkyl-P(O)(R 12 ) 2 , -C 0-8 Alkyl-NR 13 R 14 , -C 0-8 Alkyl-C(=NR 13 )R 12 , -C 0-8 Alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 Alkyl-C(O)NR 13 R 14 and -C 0-8 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ) 2 、-C 0-8 alkyl-NR 13 R 14 、-C 0-8 alkyl-C(=NR 13 )R 12 、-C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5g and R 5h together with the carbon atom directly connecting them, form a C 3-6 cycloalkyl group, 4- to 10-membered heterocyclic group, C 6-10 aryl group or 5- to 10-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, =O, =S, -C 0-8 alkyl-SF 5 、-C 0-8 alkyl-S(O)(=N-R 7 )R 8 、-C 0-8 alkyl-N=S(O)R 8 R 9 、-C 0-8 alkyl-N=SR 8 R 9 、-C 0-8 alkyl-O-S(O) 2 R 10 、-C 0-8 alkyl-S(O) r R 10 、-C 0-8 alkyl-O-R 11 、-C 0-8 alkyl-C(O)OR 11 、-C 0-8 alkyl-C(O)SR 11 、-C 0-8 alkyl-S-C(O)R 12 、-C 0-8 alkyl-C(O)R 12 、-C 0-8 alkyl-O-C(O)R 12 、-C 0-8 alkyl-P(O)(R 12 ), -C 2 alkyl-NR 0-8 R 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 and -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, R 6a is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group and -O-R 11 and is optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, cyano group, hydroxyl group, =O, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3-6 membered heterocyclic group, 3-6 membered heterocyclic oxy group and -NR 13 R 14 and is substituted with one or more substituents selected from the group consisting of R 6b is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group and -O-R 11 and is optionally further substituted by one or more substituents selected from the group consisting of deuterium, halogen, cyano group, hydroxyl group, =O, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3-6 membered heterocyclic group, 3-6 membered heterocyclic oxy group and -NR 13 R 14 and is substituted by one or more substituents selected from the group consisting of R 6c is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group and -O-R 11 and is optionally further substituted by one or more substituents selected from the group consisting of deuterium, halogen, cyano group, hydroxyl group, =O, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3-6 membered heterocyclic group, 3-6 membered heterocyclic oxy group and -NR 13 R 14 and is substituted by one or more substituents selected from the group consisting of Each R 7 is independently hydrogen, deuterium, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)R 12 or -C 0-8 alkyl-C(O)NR 13 R 14 selected from the group consisting of, and said groups may optionally further be deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 or -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, Each R 8 and R 9 are each independently selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10 aryl group or 5- to 10-membered heteroaryl group, or R 8 and R 9 together with a sulfur atom directly linking them form a 3- to 10-membered heterocyclic group, and the group may optionally further have deuterium, halogen, cyano group, nitro group, azide group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 3-10 cycloalkyl group, 3- to 10-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, -C 0-8 alkyl-S(O) r R 10 , -C 0-8 alkyl-O-R 11 , -C 0-8 alkyl-C(O)OR 11 , -C 0-8 alkyl-C(O)R 12 , -C 0-8 alkyl-O-C(O)R 12 , -C 0-8 alkyl-NR 13 R 14 , -C 0-8 alkyl-C(=NR 13 )R 12 , -C 0-8 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-8 alkyl-C(O)NR 13 R 14 or -C 0-8 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of Each R 10 is independently selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-10 alkyl group, C 2-10 alkenyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, and -NR 13 R 14 and is optionally further independently substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, =O, C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, 3- to 12-membered heterocyclic group, 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 ; Each R 11 is independently selected from the group consisting of hydrogen, deuterium, C 1-10 alkyl group, C 2-10 alkenyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group and 5- to 10-membered heteroaryl group, and said groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, =O, cyano group, C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, 3- to 12-membered heterocyclic group, 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryloxy group and -NR 13 R 14 and is substituted with one or more substituents selected from the group consisting of Each R 12 is independently hydrogen, deuterium, a hydroxyl group, C 1-10 alkyl group, C 1-10 alkoxy group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, 3- to 12-membered heterocyclic group, 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 is selected from the group consisting of, and each said group is independently optionally further deuterium, halogen, hydroxyl group, =O, cyano group, C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, 3- to 12-membered heterocyclic group, 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryloxy group, and -NR 13 R 14 is substituted with one or more substituents selected from the group consisting of, Each R 13 and R 14 are each independently hydrogen, deuterium, a hydroxyl group, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, C 3-12 cycloalkyl group, 3- to 12-membered heterocyclic group, C 6-10 aryl group, 5- to 10-membered heteroaryl group, a sulfinyl group, a sulfonyl group, a methylsulfonyl group, an isopropylsulfonyl group, a cyclopropylsulfonyl group, a p-toluenesulfonyl group, an aminosulfonyl group, a dimethylaminosulfonyl group, and C 1-10 alkanoyl group, and are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, a hydroxyl group, =O, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, 3- to 12-membered heterocyclic group, 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryloxy group, an amino group, mono-C 1-10 alkylamino group, di-C 1-10 alkylamino group, and C 1-10 alkanoyl group, and are substituted with one or more substituents selected from the group consisting thereof, Alternatively, R 13 and R 14 form, together with a nitrogen atom directly linked thereto, a 4- to 10-membered heterocyclic group or a 5- to 10-membered heteroaryl group, and the 4- to 10-membered heterocyclic group or 5- to 10-membered heteroaryl group is optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, =O, C 1-10 alkyl group, C 2-10 alkenyl group, C 2-10 alkynyl group, halogen-substituted C 1-10 alkyl group, deuterium-substituted C 1-10 alkyl group, C 1-10 alkoxy group, C 3-12 cycloalkyl group, C 3-12 cycloalkoxy group, 3- to 12-membered heterocyclic group, 3- to 12-membered heterocyclic oxy group, C 6-10 aryl group, C 6-10 aryloxy group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryloxy group, methanesulfonylmethyl, amino group, mono-C 1-10 alkylamino group, di-C 1-10 alkylamino group and C 1-10 alkanoyl group, m is 0, 1, 2, 3 or 4, n is 0, 1 or 2, p is 1 or 2, and each r is independently 0, 1 or 2) a compound, its stereoisomers or its pharmaceutically acceptable salts thereof.

2. X 1 is CR a or N, and X 2 is CR b or N, and X 3 is CR c or N, and X 4 is CR d or N, and L 1 is CR 5a R 5b and L 2 is (CR 5c R 5d ) p , NR 6a , O, S, S(O), S(O) 2 or C(O), and L 3 is a bond, CR 5e R 5f , NR 6b , O, S, S(O), S(O) 2 or C(O), and Alternatively, L 2 and L 3 both form a cycloalkyl group, a 4-6 membered heterocyclic group, a C 4-6 aryl group or a 5-8 membered heteroaryl group, and the C 6-8 cycloalkyl group, 4-6 membered heterocyclic group, C 4-6 aryl group or 5-8 membered heteroaryl group may each independently optionally further have deuterium, halogen, cyano group, C 6-8 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 1-4 alkenyl group, C 2-4 alkynyl group, C 2-4 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 6-8 alkyl-SF 0-4 、-C 5 alkyl-S(O)(=N-R 0-4 ), -C 7 alkyl-N=S(O)R 8 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 8 R 9 、-C 0-4 alkyl-S(O) 2 R 10 、-C 0-4 alkyl-O-R r R 10 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 11 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 、-C 0-4 ), -C 12 ), -C 2 、-C 0-4 Alkyl-NR 13 R 14 、 -C 0-4 Alkyl-C(=NR 13 )R 12 、 -C 0-4 Alkyl-N(R 13 )-C(=NR 14 )R 12 、 -C 0-4 Alkyl-C(O)NR 13 R 14 And -C 0-4 Alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of L 4 is CR 5g R 5h , O, S, S(O), S(O) 2 , NR 6c or C(O), and Ring A is C 4-6 a cycloalkyl group, a 4- to 6-membered heterocyclic group, C 6-8 an aryl group or a 5- to 8-membered heteroaryl group, R 1 is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 8-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, said groups each independently optionally further being deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 alkyl group substituted with a cycloalkyl group, C 1-4 alkyl group substituted with a 3-6 membered heterocyclic group, C 1-4 alkyl group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF 5 -C 0-4 alkyl-S(O)(=N-R 7 )R 8 -C 0-4 alkyl-N=S(O)R 8 R 9 -C 0-4 alkyl-N=SR 8 R 9 -C 0-4 alkyl-N(R 13 )-S(O) 2 R 10 -C 0-4 alkyl-O-S(O) 2 R 10 -C 0-4 alkyl-S(O) r R 10 -C 0-4 alkyl-O-R 11 -C 0-4 alkyl-C(O)OR 11 -C 0-4 alkyl-C(O)SR 11 -C 0-4 alkyl-S-C(O)R 12 -C 0-4 alkyl-C(O)R 12 -C 0-4 alkyl-O-C(O)R 12 -C 0-4 alkyl-P(O)(R 12 ) 2 -C 0-4 Alkyl-NR 13 R 14 , -C 0-4 Alkyl-C (=NR 13 ) R 12 , -C 0-4 Alkyl-N(R 13 )-C(=NR 14 ) R 12 , -C 0-4 Alkyl-C(O)NR 13 R 14 and -C 0-4 Alkyl-N(R 13 )-C(O)R 12 and each of said groups is independently optionally and further substituted with deuterium, halogen, cyano group, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium-substituted C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups, C 6-8 Aryl groups, 5-8 membered heteroaryl groups, =O, =S, -C 0-4 Alkyl-SF 5 , -C 0-4 Alkyl-S(O)(=NR 7 ) R 8 , -C 0-4 Alkyl-N=S(O)R 8 R 9 , -C 0-4 Alkyl-N=SR 8 R 9 , -C 0-4 Alkyl-N(R 13 )-S(O) 2 R 10 , -C 0-4 Alkyl-OS(O) 2 R 10 , -C 0-4 Alkyl-S(O) r R 10 , -C 0-4 Alkyl-OR 11 , -C 0-4 Alkyl-C(O)OR 11 , -C 0-4 Alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 ) 2 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of: Each R 2 is independently hydrogen, deuterium, a halogen, a cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, said groups each independently optionally further comprising deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF 5 , -C 0-4 alkyl-S(O)(=N-R 7 )R 8 , -C 0-4 alkyl-N=S(O)R 8 R 9 , -C 0-4 alkyl-N=SR 8 R 9 , -C 0-4 alkyl-O-S(O) 2 R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 ) 2 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 Alkyl-N(R 13 ),-C(=NR 14 )R 12 ,-C 0-4 Alkyl-C(O)NR 13 R 14 and-C 0-4 Alkyl-N(R 13 ),-C(O)R 12 substituted with one or more substituents selected from the group consisting of, Each R 3 、R a and R b is independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 ), R 12 , -C 0-4 alkyl - C(O)NR 13 R 14 and -C 0-4 alkyl - N(R 13 ), -C(O)R 12 selected from the group consisting of R 4 and R c are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of R d is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of R 5a and R 5b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5a and R 5b together with the carbon atom directly connected to them, form C(O), C 3-6 cycloalkyl group, 4-6 membered heterocyclic group, C 6-8 aryl group or 5-8 membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ), 2 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )(-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )(-C(O)R 12 substituted with one or more substituents selected from the group consisting of, Each R 5c and R 5d are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5c and R 5d together with the carbon atom directly connected thereto, form a C 3-6 cycloalkyl group, a 4- to 6-membered heterocyclic group, a C 6-8 aryl group or a 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF 5 , -C 0-4 alkyl-S(O)(=N-R 7 )R 8 , -C 0-4 alkyl-N=S(O)R 8 R 9 , -C 0-4 alkyl-N=SR 8 R 9 , -C 0-4 alkyl-O-S(O) 2 R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 ), 2 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )(-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )(-C(O)R 12 substituted with one or more substituents selected from the group consisting of, provided that when R 5c or R 5d is H or a C 1-4 alkyl group, R 1 is an optionally substituted C 2-10 alkynyl group, or alternatively, L 3 is O, S, S(O) or S(O) 2 , R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5e and R 5f together with the carbon atom directly linked thereto form a C 3-6 cycloalkyl group, a 4- to 6-membered heterocyclic group, a C 6-8 aryl group or a 5- to 8-membered heteroaryl group, said groups each independently optionally further being deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF 5 ,-C 0-4 alkyl-S(O)(=N-R 7 )R 8 ,-C 0-4 alkyl-N=S(O)R 8 R 9 ,-C 0-4 alkyl-N=SR 8 R 9 ,-C 0-4 alkyl-O-S(O) 2 R 10 ,-C 0-4 alkyl-S(O) r R 10 ,-C 0-4 alkyl-O-R 11 ,-C 0-4 alkyl-C(O)OR 11 ,-C 0-4 alkyl-C(O)SR 11 ,-C 0-4 alkyl-S-C(O)R 12 ,-C 0-4 alkyl-C(O)R 12 ,-C 0-4 alkyl-O-C(O)R 12 ,-C 0-4 alkyl-P(O)(R 12 ), 2 -C 0-4 alkyl-NR 13 R 14 -C 0-4 alkyl-C(=NR 13 )R 12 -C 0-4 alkyl-N(R 13 )(-C(=NR 14 )R 12 -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )(-C(O)R 12 substituted with one or more substituents selected from the group consisting of: R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-SF 5 、-C 0-4 alkyl-S(O)(=N-R 7 )R 8 、-C 0-4 alkyl-N=S(O)R 8 R 9 、-C 0-4 alkyl-N=SR 8 R 9 、-C 0-4 alkyl-O-S(O) 2 R 10 、-C 0-4 alkyl-S(O) r R 10 、-C 0-4 alkyl-O-R 11 、-C 0-4 alkyl-C(O)OR 11 、-C 0-4 alkyl-C(O)SR 11 、-C 0-4 alkyl-S-C(O)R 12 、-C 0-4 alkyl-C(O)R 12 、-C 0-4 alkyl-O-C(O)R 12 、-C 0-4 alkyl-P(O)(R 12 ) 2 、-C 0-4 alkyl-NR 13 R 14 、-C 0-4 alkyl-C(=NR 13 )R 12 、-C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、-C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5g and R 5h together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, said groups each independently optionally further being deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -C 0-4 alkyl-SF 5 , -C 0-4 alkyl-S(O)(=N-R 7 )R 8 , -C 0-4 alkyl-N=S(O)R 8 R 9 , -C 0-4 alkyl-N=SR 8 R 9 , -C 0-4 alkyl-O-S(O) 2 R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 ) 2 、 -C 0-4 alkyl-NR 13 R 14 、 -C 0-4 alkyl-C(=NR 13 )R 12 、 -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、 -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, Here, R 6a 、R 6b 、R 6c 、R 7 、R 8 、R 9 、R 10 、R 11 、R 12 、R 13 、R 14 、m, n, p and r are as described in claim 1, characterized in that The compound of formula (I) according to Claim 1, its stereoisomers or its pharmaceutically acceptable salts thereof.

3. Each R 7 is independently hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)R 12 or -C 0-4 alkyl-C(O)NR 13 R 14 selected from the group consisting of, and said groups may optionally further be deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 or -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of Each R 8 and R 9 are each independently selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, or R 8 and R 9 form a 3- to 6-membered heterocyclic group together with a sulfur atom directly connecting them, and the group is optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 or -C 0-4 alkyl-N(R 13 )-C(O)R 12 and are substituted with one or more substituents selected from the group consisting of Each R 10 is independently selected from the group consisting of hydrogen, deuterium, a hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, and -NR 13 R 14 and is optionally further independently substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, =O, C 1-4 alkyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group, C 6-8 aryl group, C 6-8 aryloxy group, 5- to 8-membered heteroaryl group, 5- to 8-membered heteroaryloxy group, and -NR 13 R 14 ; Each R 11 is independently selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group and 5- to 8-membered heteroaryl group, and the said groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, =O, cyano group, C 1-4 alkyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group, C 6-8 aryl group, C 6-8 aryloxy group, 5- to 8-membered heteroaryl group, 5- to 8-membered heteroaryloxy group and -NR 13 R 14 and is substituted with one or more substituents selected from the group consisting of Each R 12 is independently hydrogen, deuterium, a hydroxyl group, C 1-4 alkyl group, C 1-4 alkoxy group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 aryl group, C 6-8 aryloxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryloxy group and -NR 13 R 14 is selected from the group consisting of, and each of said groups is independently optionally further deuterium, halogen, hydroxyl group, =O, cyano group, C 1-4 alkyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, a 3- to 6-membered heterocyclic group, a 3- to 6-membered heterocyclic oxy group, C 6-8 aryl group, C 6-8 aryloxy group, a 5- to 8-membered heteroaryl group, a 5- to 8-membered heteroaryloxy group and -NR 13 R 14 is substituted with one or more substituents selected from the group consisting of, Each R 13 and R 14 are each independently hydrogen, deuterium, a hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, sulfinyl group, sulfonyl group, methylsulfonyl group, isopropylsulfonyl group, cyclopropylsulfonyl group, p-toluenesulfonyl group, aminosulfonyl group, dimethylaminosulfonyl group, and C 1-4 alkanoyl group, and are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, =O, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group, C 6-8 aryl group, C 6-8 aryloxy group, 5- to 8-membered heteroaryl group, 5- to 8-membered heteroaryloxy group, amino group, mono-C 1-4 alkylamino group, di-C 1-4 alkylamino group, and C 1-4 alkanoyl group, and are substituted with one or more substituents selected from the group consisting thereof, Alternatively, R 13 and R 14 together with the nitrogen atom directly linked thereto form a 4- to 6-membered heterocyclic group or a 5- to 8-membered heteroaryl group, and the 4- to 6-membered heterocyclic group or 5- to 8-membered heteroaryl group is optionally further deuterium, halogen, hydroxyl group, =O, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group, C 6-8 aryl group, C 6-8 aryloxy group, 5- to 8-membered heteroaryl group, 5- to 8-membered heteroaryloxy group, methanesulfonylmethyl, amino group, mono-C 1-4 alkylamino group, di-C 1-4 alkylamino group and C 1-4 alkanoyl group, and is substituted with one or more substituents selected from the group consisting of, and The compound of formula (I) according to Claim 1, its stereoisomers or its pharmaceutically acceptable salts thereof, characterized in that each r is independently 0, 1 or 2.

4. Formula (II): [Chemical 2] (wherein: X 1 is CR a or N, and X 2 is CR b or N, and X 3 is CR c or N, and X 4 is CR d or N, and L 1 is CR 5a R 5b and L 2 is (CR 5c R 5d ), p NR 6a , O, S, S(O), S(O) 2 or C(O), and L 3 is a bond, CR 5e R 5f or C(O), and L 4 is CR 5g R 5h , O, S, S(O), S(O) 2 , NR 6c or C(O), and R 1 is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-8 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and is independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 cycloalkyl group-substituted C 1-4 alkyl group, 3-6 membered heterocyclic group-substituted C 1-4 alkyl group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 ) R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -N(R 13 )-S(O) 2 R 10 , -OS(O) 2 R 10 , -S(O) r R 10 , -OR 11 , -C(O)OR 11 , -C(O)SR 11 , -SC(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C (=NR 13 ) R 12 , -N(R 13 )-C(=NR 14 ) R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and each of said groups is independently optionally and further substituted with deuterium, halogen, cyano group, C 1-4 Alkyl group, halogen-substituted C 1-4 Alkyl group, deuterium-substituted C 1-4 Alkyl group, C 2-4 Alkenyl group, C 2-4 Alkynyl group, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups, C 6-8 Aryl groups, 5-8 membered heteroaryl groups, =O, =S, -C 0-4 Alkyl-SF 5 , -C 0-4 Alkyl-S(O)(=NR 7 ) R 8 , -C 0-4 Alkyl-N=S(O)R 8 R 9 , -C 0-4 Alkyl-N=SR 8 R 9 , -C 0-4 alkyl-N(R 13 ), -S(O) 2 R 10 , -C 0-4 alkyl-O-S(O) 2 R 10 , -C 0-4 alkyl-S(O) r R 10 , -C 0-4 alkyl-O-R 11 , -C 0-4 alkyl-C(O)OR 11 , -C 0-4 alkyl-C(O)SR 11 , -C 0-4 alkyl-S-C(O)R 12 , -C 0-4 alkyl-C(O)R 12 , -C 0-4 alkyl-O-C(O)R 12 , -C 0-4 alkyl-P(O)(R 12 ) 2 , -C 0-4 alkyl-NR 13 R 14 , -C 0-4 alkyl-C(=NR 13 )R 12 , -C 0-4 alkyl-N(R 13 ), -C(=NR 14 )R 12 , -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 ), -C(O)R 12 substituted with one or more substituents selected from the group consisting of R 2a is hydrogen, deuterium, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -C(O)R 12 and -C(O)NR 13 R 14 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of R 2b is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 、 -N=SR 8 R 9 、 -O-S(O) 2 R 10 、 -S(O) r R 10 、 -O-R 11 、 -C(O)OR 11 、 -C(O)SR 11 、 -S-C(O)R 12 、 -C(O)R 12 、 -O-C(O)R 12 、 -P(O)(R 12 ) 2 、 -NR 13 R 14 、 -C(=NR 13 )R 12 、 -N(R 13 )-C(=NR 14 )R 12 、 -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of R 3a 、R 3b 、R a and R b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF 5 、-S(O)(=N-R 7 )R 8 、-N=S(O)R 8 R 9 、-N=SR 8 R 9 、-O-S(O) 2 R 10 、-S(O) r R 10 、-O-R 11 、-C(O)OR 11 、-C(O)SR 11 、-S-C(O)R 12 、-C(O)R 12 、-O-C(O)R 12 、-P(O)(R 12 ) 2 、-NR 13 R 14 、-C(=NR 13 )R 12 、-N(R 13 )-C(=NR 14 )R 12 、-C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, R 4 and R c are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, R d is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 ), R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ), 2 , -NR 13 R 14 , -C(=NR 13 ), R 12 , -N(R 13 )-C(=NR 14 ), R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and is selected from the group consisting of R 5a and R 5b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5a and R 5b together with the carbon atom directly connecting thereto, form C(O), C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 An alkynyl group, C 3-6 A cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 An aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of, Each R 5c and R 5d are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 are selected from the group consisting of, or R 5c and R 5d together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 an alkynyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 an aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 is substituted with one or more substituents selected from the group consisting of, provided that when R 5c or R 5d is H or a C 1-4 alkyl group, R 1 is an optionally substituted C 2-10 alkynyl group, R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5e and R 5f together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 an alkynyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 an aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF 5 -, -S(O)(=N-R 7 )R 8 -, -N=S(O)R 8 R 9 -, -N=SR 8 R 9 -, -O-S(O) 2 R 10 -, -S(O) r R 10 -, -O-R 11 -, -C(O)OR 11 -, -C(O)SR 11 -, -S-C(O)R 12 -, -C(O)R 12 -, -O-C(O)R 12 -, -P(O)(R 12 ) 2 -, -NR 13 R 14 -, -C(=NR 13 )R 12 -, -N(R 13 )-C(=NR 14 )R 12 -, -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, or R 5g and R 5h together with the carbon atom to which they are directly attached form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 an alkynyl group, C 3-6 a cycloalkyl group, a 3- to 6-membered heterocyclic group, C 6-8 an aryl group, a 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of Here, R 6a 、R 6c 、R 7 、R 8 、R 9 、R 10 、R 11 、R 12 、R 13 、R 14 、p and r are as described in claim 1) The compound of formula (I) according to Claim 1, its stereoisomers or its pharmaceutically acceptable salts thereof, characterized in that it is a compound of).

5. Formula (III): [Chemical Formula 3] (wherein: X 1 is CR a or N, and X 2 is CR b or N, and X 3 is CR c or N, and X 4 is CR d or N, and L 1 is CR 5a R 5b and L 2 is (CR 5c R 5d ) p and L 3 is a bond, CR 5e R 5f or C(O), and L 4 is CR 5g R 5h , O, NR 6c or C(O), and R 1 is hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-8 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 cycloalkyl group-substituted C 1-4 alkyl group, 3-6 membered heterocyclic group-substituted C 1-4 alkyl group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 ), R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -N(R 13 ), -S(O) 2 R 10 , -O - S(O) 2 R 10 , -S(O) r R 10 , -O - R 11 , -C(O)OR 11 , -C(O)SR 11 , -S - C(O)R 12 , -C(O)R 12 , -O - C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 ), -C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 ), -C(O)R 12 substituted with one or more substituents selected from the group consisting of, said groups being each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen - substituted C 1-4 alkyl group, deuterium - substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3 - 6 membered heterocyclic group, C 6-8 aryl group, 5 - 8 membered heteroaryl group, =O, =S, -C 0-4 alkyl - SF 5 , -C 0-4 alkyl - S(O)(=N - R 7 )R 8 , -C 0-4 alkyl - N=S(O)R 8 R 9 , -C 0-4 alkyl - N=SR 8 R 9 、 -C 0-4 alkyl-N(R 13 )-S(O) 2 R 10 、 -C 0-4 alkyl-O-S(O) 2 R 10 、 -C 0-4 alkyl-S(O) r R 10 、 -C 0-4 alkyl-O-R 11 、 -C 0-4 alkyl-C(O)OR 11 、 -C 0-4 alkyl-C(O)SR 11 、 -C 0-4 alkyl-S-C(O)R 12 、 -C 0-4 alkyl-C(O)R 12 、 -C 0-4 alkyl-O-C(O)R 12 、 -C 0-4 alkyl-P(O)(R 12 ) 2 、 -C 0-4 alkyl-NR 13 R 14 、 -C 0-4 alkyl-C(=NR 13 )R 12 、 -C 0-4 alkyl-N(R 13 )-C(=NR 14 )R 12 、 -C 0-4 alkyl-C(O)NR 13 R 14 and -C 0-4 alkyl-N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of: R 2a is selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group and 3-6 membered heterocyclic group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of R 2b is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, and -SF 5 and is optionally further substituted by one or more substituents selected from the group consisting of deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and is substituted by one or more substituents selected from the group consisting of R 3a 、R 3b 、R a and R b are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, and -SF 5 selected from the group consisting of, R c is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group and -SF 5 and is selected from the group consisting of R d is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group and -SF 5 and is selected from the group consisting of R 5a and R 5b each independently represents hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, and -SF 5 and is selected from the group consisting of, or R 5a and R 5b together with the carbon atom directly connecting thereto forms C(O), C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups each independently may further optionally be deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 、-C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with one or more substituents selected from the group consisting of, When p is 1, R 5c and R 5d together with the carbon atom directly linked thereto form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and said groups are each independently optionally further substituted with deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 and is substituted with one or more substituents selected from the group consisting of Alternatively, when p is 2, the pair of R 5c and R 5d together with the carbon atom directly connecting them form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, or when the pair of R 5c and R 5d form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group together with the directly connecting carbon atom, another pair of R 5c and R 5d are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, -SF 5 -, -S(O)(=N-R 7 )R 8 -, -N=S(O)R 8 R 9 -, -N=SR 8 R 9 -, -O-S(O) 2 R 10 -, -S(O) r R 10 -, -O-R 11 -, -C(O)OR 11 -, -C(O)SR 11 -, -S-C(O)R 12 -, -C(O)R 12 -, -O-C(O)R 12 -, -P(O)(R 12 ) 2 -, -NR 13 R 14 -, -C(=NR 13 )R 12 -, -N(R 13 )-C(=NR 14 )R 12 -, -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 selected from the group consisting of, R 5e and R 5f are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group and -SF 5 selected from the group consisting of, or R 5e and R 5f together with the carbon atom directly linking them, form a C 3-6 cycloalkyl group, 4-6 membered heterocyclic group, C 6-8 aryl group or 5-8 membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 ), R 12 , -C(O)NR 13 R 14 and -N(R 13 ), -C(O)R 12 substituted with one or more substituents selected from the group consisting of R 5g and R 5h are each independently hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, and -SF 5 selected from the group consisting of, or R 5g and R 5h together with the carbon atom directly linked thereto form a C 3-6 cycloalkyl group, 4- to 6-membered heterocyclic group, C 6-8 aryl group or 5- to 8-membered heteroaryl group, and said groups are each independently optionally further deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, C 6-8 aryl group, 5- to 8-membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 ), R 12 , -C(O)NR 13 R 14 and -N(R 13 ), -C(O)R 12 substituted with one or more substituents selected from the group consisting of: R 6c is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group and -O-R 11 and is optionally further substituted independently by one or more substituents selected from the group consisting of deuterium, halogen, cyano group, hydroxyl group, =O, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 1-4 alkoxy group, C 3-6 cycloalkyl group, C 3-6 cycloalkoxy group, 3- to 6-membered heterocyclic group, 3- to 6-membered heterocyclic oxy group and -NR 13 R 14 and is substituted by one or more substituents selected from the group Here, R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , p and r are as described in claim 1), the compound of formula (I) according to claim 1, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

6. The compound of formula (I) is a compound of the following formula (IV), [Chemical Formula 4] wherein, L 1 is CR 5a R 5b and L 2 is CR 5c R 5d and L 3 is CR 5e R 5f and L 4 is O, R 1 is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-8 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group and -SF 5 and is optionally further independently one or more deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 3-6 alkyl group substituted with a cycloalkyl group, C 1-4 alkyl group substituted with a 3-6 membered heterocyclic group, C 1-4 alkyl group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -N(R 13 )-S(O) 2 R 10 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with a substituent selected from the group consisting of, said groups each independently optionally further one or more deuteriums, halogens, cyano groups, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, C 6-8 aryl group, 5-8 membered heteroaryl group, =O, =S, -SF 5 , -S(O)(=N-R 7 )R 8 , -N=S(O)R 8 R 9 , -N=SR 8 R 9 , -N(R 13 )-S(O) 2 R 10 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -C(O)OR 11 , -C(O)SR 11 , -S-C(O)R 12 , -C(O)R 12 , -O-C(O)R 12 , -P(O)(R 12 ) 2 , -NR 13 R 14 , -C(=NR 13 )R 12 , -N(R 13 )-C(=NR 14 )R 12 , -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with a substituent selected from the group consisting of, R 2a is selected from the group consisting of hydrogen, deuterium, hydroxyl group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group and 3- to 6-membered heterocyclic group, and each of said groups is independently optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, =O, =S and -SF 5 and is substituted with a substituent selected from the group consisting of R 2b is selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group and -SF 5 and is optionally further substituted, independently of one another, by one or more deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3-6 membered heterocyclic group, =O, =S and -SF 5 with a substituent selected from the group consisting of, R 5a and R 5b are each independently selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 3-6 cycloalkyl group and 3- to 6-membered heterocyclic group, or R 5a and R 5b together with the directly connected carbon atoms form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and the groups are each independently optionally further substituted with one or more deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, =O, =S and -SF 5 and are substituted with a substituent selected from the group consisting of R 5c and R 5d together with the directly connected carbon atom form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and each of said groups is independently optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl groups, halogen-substituted C 1-4 alkyl groups, deuterium-substituted C 1-4 alkyl groups, C 2-4 alkenyl groups, C 2-4 alkynyl groups, C 3-6 cycloalkyl groups, 3- to 6-membered heterocyclic groups, =O, =S and -SF 5 and is substituted with a substituent selected from the group consisting of R 5e and R 5f are each independently selected from the group consisting of hydrogen, deuterium, halogen, cyano group, C 1-4 alkyl group, C 3-6 cycloalkyl group and 3- to 6-membered heterocyclic group, or R 5e and R 5f together with the directly linked carbon atoms form a C 3-6 cycloalkyl group or 4- to 6-membered heterocyclic group, and the groups are each independently optionally further substituted with one or more deuterium, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 2-4 alkenyl group, C 2-4 alkynyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, =O, =S and -SF 5 and are substituted with a substituent selected from the group consisting of Here, R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 and r are as described in claim 1, a compound of formula (I) according to claim 1, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

7. L 1 is CR 5a R 5b and L 2 is CR 5c R 5d and L 3 is CR 5e R 5f and L 4 is O, R 5a and R 5b are each independently selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, and said groups are each independently optionally further substituted with one or more of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF 5 and are substituted with a substituent selected from the group consisting of R 5c and R 5d together with the directly connected carbon atom form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and each of said groups is independently optionally further substituted with one or more deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF 5 substituted with a substituent selected from the group consisting of and R 5e and R 5f are each independently selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, and the groups are each independently optionally further one or more of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF 5 The compound of formula (I) according to claim 6, its stereoisomer or its pharmaceutically acceptable salt, characterized in that it is substituted with a substituent selected from the group consisting of

8. R 2a is selected from the group consisting of hydrogen, deuterium, hydroxyl group, methyl group, ethyl group, propyl group, isopropyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, and said groups are each independently optionally further one or more of deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF 5 substituted with a substituent selected from the group consisting of and R 2b is selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group and -SF 5 and is optionally further substituted, independently of one another, by one or more deuterium, fluorine, chlorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, vinyl group, ethynyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group, azetidinyl group, =O, =S and -SF 5 The compound of formula (I) according to claim 6, its stereoisomer or its pharmaceutically acceptable salt, characterized in that it is substituted by a substituent selected from the group consisting of

9. The compound of formula (I) is a compound of the following formula (V), 【Chemical Formula 5】 wherein, R 1 is selected from the group consisting of a C 2-4 alkenyl group, a C 2-4 alkynyl group, and a 3- to 8-membered heterocyclic group, and each of said groups is independently optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl groups, C 2-4 alkenyl groups, C 2-4 alkynyl groups, C 3-6 cycloalkyl groups, 3- to 6-membered heterocyclic groups, C 3-6 alkyl groups substituted with a cycloalkyl group, C 1-4 alkyl groups substituted with a 3- to 6-membered heterocyclic group, C 1-4 alkyl groups, =O, =S, -SF 5 , -N(R 13 ), -S(O) 2 R 10 , -O - S(O) 2 R 10 , -S(O) r R 10 , -O - R 11 , -C(O)OR 11 , -S - C(O)R 12 , -C(O)R 12 , -O - C(O)R 12 , -NR 13 R 14 , -C(O)NR 13 R 14 and -N(R 13 ), -C(O)R 12 selected from the group consisting of substituents, and each of said groups is independently optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl groups, halogen-substituted C 1-4 alkyl groups, deuterium-substituted C 1-4 alkyl groups, C 2-4 alkenyl groups, C 2-4 alkynyl groups, C 3-6 cycloalkyl groups, 3- to 6-membered heterocyclic groups, C 6-8 aryl groups, 5- to 8-membered heteroaryl groups, =O, =S, -SF 5 , -N(R 13 ), -S(O) 2 R 10 , -O - S(O) 2 R 10 , -S(O) r R 10 、 -O-R 11 、 -C(O)OR 11 、 -C(O)R 12 、 -O-C(O)R 12 、 -NR 13 R 14 、 -C(O)NR 13 R 14 and -N(R 13 )-C(O)R 12 substituted with a substituent selected from the group consisting of R 2a is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, C 3-6 cycloalkyl group and 3-6 membered heterocyclic group, and the groups are each independently optionally further substituted with one or more deuterium, halogen, cyano group, C 1-4 alkyl group, halogen substituted C 1-4 alkyl group, deuterium substituted C 1-4 alkyl group, C 3-6 cycloalkyl group and 3-6 membered heterocyclic group, and is substituted with a substituent selected from the group consisting of R 5c and R 5d together with the directly linked carbon atom form a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and said groups are each independently optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl groups, halogen-substituted C 1-4 alkyl groups, deuterium-substituted C 1-4 alkyl groups, C 2-4 alkenyl groups, C 2-4 alkynyl groups, C 3-6 cycloalkyl groups, 3- to 6-membered heterocyclic groups, =O, =S and -SF 5 and are substituted with substituents selected from the group consisting of Here, R 10 , R 11 , R 12 , R 13 , R 14 and r are as described in claim 1, and the compound of formula (I) according to claim 1, its stereoisomers or its pharmaceutically acceptable salts.

10. R 5c and R 5d together with the directly connected carbon atom forms a C 3-6 cycloalkyl group or a 4- to 6-membered heterocyclic group, and a compound of formula (I) according to claim 9, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

11. R 5c and R 5d form, together with the directly linked carbon atom, a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, an oxetanyl group, an oxolanyl group or an oxanyl group, a compound of formula (I) according to claim 9, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

12. R 1 is C 2-4 an alkynyl group, and said C 2-4 alkynyl group is optionally further substituted with one or more deuteriums, C 1-4 alkyl group, C 3-6 cycloalkyl group and a substituent selected from the group consisting of 3- to 6-membered heterocyclic groups, and said groups are each independently optionally further substituted with one or more deuteriums, halogen, cyano group, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 cycloalkyl group, 3- to 6-membered heterocyclic group, and the compound of formula (I) according to claim 9, a stereoisomer thereof or a pharmaceutically acceptable salt thereof, characterized in that it is substituted with a substituent selected from the group consisting of

13. R 1 is an ethynyl group, and the ethynyl group is optionally further substituted with one or more substituents selected from the group consisting of deuterium, methyl group, ethyl group, propyl group, isopropyl group, butyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridyl group, azetidinyl group, azolidyl group and azonanyl group, and the groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, bromine, cyano group, methyl group, ethyl group, propyl group, isopropyl group, butyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridyl group, azetidinyl group, azolidyl group and azonanyl group. The compound of formula (I) according to claim 9, its stereoisomer or its pharmaceutically acceptable salt, characterized in that.

14. R 1 is an ethynyl group, and the ethynyl group is optionally further substituted with one or more substituents selected from the group consisting of a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, an oxiranyl group, an oxetanyl group, an oxolanyl group, an oxanyl group, an aziridinyl group, an azetidinyl group, an azolidyl group, and an azonanyl group, and the groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, bromine, a cyano group, a methyl group, an ethyl group, a propyl group, an isopropyl group, a monofluoromethyl group, a difluoromethyl group, a trifluoromethyl group, a monodeuteromethyl group, a dideuteromethyl group, and a trideuteromethyl group, A compound of formula (I) according to claim 9, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

15. R 1 is [Chemical Formula 6] being, R 1a is selected from the group consisting of hydrogen, a methyl group, an ethyl group, a propyl group, an isopropyl group, a monofluoromethyl group, a difluoromethyl group, a trifluoromethyl group, a monodeuteromethyl group, a dideuteromethyl group, and a trideuteromethyl group, R 1b is a compound of formula (I) according to claim 9, a stereoisomer thereof or a pharmaceutically acceptable salt thereof, characterized in that it is selected from the group consisting of hydrogen, methyl group, ethyl group, propyl group, isopropyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group and trideuteromethyl group.

16. R 1 is a 4- to 8-membered nitrogen-containing heterocyclic group, and the 4- to 8-membered nitrogen-containing heterocyclic group is optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl groups, =O, -N(R 13 ), -S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -O-C(O)R 12 , -NR 13 R 14 and -N(R 13 ), -C(O)R 12 selected from the group consisting of substituents, and the C 1-4 alkyl group is optionally further substituted with one or more deuteriums, halogens, cyano groups, C 1-4 alkyl groups, halogen-substituted C 1-4 alkyl groups, deuterium-substituted C 1-4 alkyl groups, -N(R 13 ), -S(O) 2 R 10 , -O-S(O) 2 R 10 , -S(O) r R 10 , -O-R 11 , -O-C(O)R 12 , -NR 13 R 14 and -N(R 13 ), -C(O)R 12 selected from the group consisting of substituents, Here, R 10 , R 11 , R 12 , R 13 , R 14 and r are as described in claim 9, a compound of formula (I) according to claim 9, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

17. R 1 The structure of [Chemical Formula 7] being, R 1c is selected from the group consisting of hydrogen, deuterium, halogen, C 1-4 alkyl group, -N(R 13a )-S(O) 2 R 10a , -O-R 11a and -N(R 13a )-C(O)R 12a and the C 1-4 alkyl group is optionally further substituted with one or more substituents selected from the group consisting of deuterium, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, -S(O) r R 10b and -O-R 11a 11a R 1d is selected from the group consisting of hydrogen, deuterium, halogen, C 1-4 alkyl group, -N(R 13a ), -S(O) 2 R 10a , -O-R 11a and -N(R 13a ), -C(O)R 12a and is selected from the group consisting of R 1e is selected from the group consisting of hydrogen, deuterium, halogen, C 1-4 alkyl group, -N(R 13a ), -S(O) 2 R 10a , -O-R 11a and -N(R 13a ), -C(O)R 12a ; the C 1-4 alkyl group is optionally further substituted with one or more substituents selected from the group consisting of deuterium, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, -S(O) r R 10b and -O-R 11a . R 1f is selected from the group consisting of hydrogen, deuterium, halogen, C 1-4 alkyl group, -N(R 13a )-S(O) 2 R 10a , -O-R 11a and -N(R 13a )-C(O)R 12a and is selected from the group consisting of; the C 1-4 alkyl group is optionally further substituted with one or more substituents selected from the group consisting of deuterium, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, -S(O) r R 10b and -O-R 11a 11a Each R 10a is independently selected from the group consisting of hydrogen, C 1-4 alkyl group, C 3-6 cycloalkyl group and 3- to 6-membered heterocyclic group, Each R 10b is independently selected from the group consisting of hydrogen, C 1-4 alkyl group, C 3-6 cycloalkyl group and 3-6 membered heterocyclic group, and said groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl group, C 1-4 alkyl group and C 1-4 alkoxy group, Each R 11a is independently hydrogen or a C 1-4 alkyl group, Each R 12a is independently selected from the group consisting of hydrogen, C 1-4 alkyl group, C 1-4 alkoxy group and C 3-6 cycloalkyl group, and the group is independently optionally further substituted with a substituent selected from the group consisting of one or more deuteriums, halogens, hydroxyl groups and cyano groups, Each R 13a is independently hydrogen or a C 1-4 alkyl group, and The compound of formula (I) according to Claim 9, its stereoisomers or its pharmaceutically acceptable salts thereof, characterized in that each r is independently 0, 1 or 2.

18. R 1 The structure of 【Chemical 8】 being, R 1c is selected from the group consisting of hydrogen, deuterium, fluorine, bromine, methyl group, ethyl group, propyl group, isopropyl group, butyl group, -N(R 13a ), -S(O) 2 R 10a , -O-R 11a and -N(R 13a ), -C(O)R 12a wherein the methyl group, ethyl group, propyl group, isopropyl group or butyl group is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, methyl group, ethyl group, propyl group, isopropyl group, butyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, -S(O) r R 10b and -O-R 11a 11a R 1d is selected from the group consisting of hydrogen, deuterium, fluorine, bromine, methyl group, ethyl group, propyl group, isopropyl group and butyl group, R 1e is selected from the group consisting of hydrogen, deuterium, fluorine, bromine, methyl group, ethyl group, propyl group, isopropyl group, butyl group, -N(R 13a ), -S(O) 2 R 10a , -O-R 11a and -N(R 13a ), -C(O)R 12a ; wherein the methyl group, ethyl group, propyl group, isopropyl group or butyl group is independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, methyl group, ethyl group, propyl group, isopropyl group, butyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, -S(O) r R 10b and -O-R 11a . Each R 10a is independently selected from the group consisting of hydrogen, a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, an oxiranyl group, an oxetanyl group, an oxolanyl group, an oxanyl group, an aziridinyl group, an azetidinyl group, an azolidyl group, and an azonanyl group, Each R 10b is independently selected from the group consisting of hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridyl group, azetidinyl group, azolidyl group and azonanyl group, and the groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, hydroxyl group, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methoxy group, ethoxy group and proxy group, Each R 11a is independently selected from the group consisting of hydrogen, a methyl group, an ethyl group, a propyl group, an isopropyl group, and a butyl group, Each R 12a is independently selected from the group consisting of hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methoxy group, ethoxy group, propoxy group, t-butoxy group, cyclopropyl group, cyclobutyl group, cyclopentyl group and cyclohexyl group, and said groups are each independently optionally further substituted with a substituent selected from the group consisting of one or more deuteriums, fluorine, chlorine, hydroxyl group and cyano group, Each R 13a is independently hydrogen, characterized in that each r is independently 0, 1 or 2, The compound of formula (I) according to Claim 9, its stereoisomers or its pharmaceutically acceptable salts thereof.

19. R 1 The structure of 【Chemical Formula 9】 being, R 1g is hydrogen, deuterium or a methyl group, and R 1h is hydrogen, deuterium or a methyl group, and R 1j is hydrogen, deuterium or a methyl group, and q is 0, 1 or 2, R 10a is selected from the group consisting of hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridinyl group, azetidinyl group, azolidyl group and azonanyl group, R 10b is selected from the group consisting of hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, oxiranyl group, oxetanyl group, oxolanyl group, oxanyl group, aziridyl group, azetidinyl group, azolidyl group and azonanyl group, and the groups are each independently optionally further substituted with one or more substituents selected from the group consisting of deuterium, fluorine, chlorine, hydroxyl group, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methoxy group, ethoxy group and proxy group, Each R 11a is independently selected from the group consisting of hydrogen, a methyl group, an ethyl group, a propyl group, an isopropyl group, and a butyl group, R 12a is selected from the group consisting of hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methoxy group, ethoxy group, propoxy group, t-butoxy group, cyclopropyl group, cyclobutyl group, cyclopentyl group and cyclohexyl group, and the groups are each independently optionally further substituted with a substituent selected from the group consisting of one or more deuteriums, fluorine, chlorine, hydroxyl group and cyano group. The compound of formula (I) according to Claim 9, its stereoisomers or its pharmaceutically acceptable salts thereof.

20. R 2a is selected from the group consisting of hydrogen, deuterium, C 1-4 alkyl group, halogen-substituted C 1-4 alkyl group, deuterium-substituted C 1-4 alkyl group, C 3-6 The compound of formula (I) according to claim 9, its stereoisomer or its pharmaceutically acceptable salt, characterized in that it is selected from the group consisting of cycloalkyl group and 3-6 membered heterocyclic group.

21. R 2a is selected from the group consisting of hydrogen, deuterium, methyl group, ethyl group, propyl group, isopropyl group, butyl group, monofluoromethyl group, difluoromethyl group, trifluoromethyl group, monodeuteromethyl group, dideuteromethyl group, trideuteromethyl group, cyclopropyl group, cyclobutyl group, oxiranyl group, oxetanyl group, aziridyl group and azetidinyl group, a compound of formula (I) according to claim 9, a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

22. The compound of formula (I) according to Claim 1, its stereoisomers or its pharmaceutically acceptable salts thereof, characterized in that it is selected from the group consisting of the following compounds. 【Chemical Formula 10】 【Chemical 11】 【Chemical 12】 【Chemical 13】 【Chemical Formula 14】 【Chemical Formula 15】

23. A pharmaceutical composition comprising the compound of formula (I) according to any one of Claims 1 to 22, its stereoisomers or its pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier.

24. Use of the compound of formula (I) according to any one of Claims 1 to 22, its stereoisomers or its pharmaceutically acceptable salts thereof in the manufacture of a drug for treating and / or preventing tumors or metastatic diseases at least partially associated with EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation and Del19 / T790M / C797S triple mutation.

25. The use according to claim 24, wherein the tumor or metastatic disease is a tumor and / or metastatic disease characterized by excessive proliferation and impaired induction of cell death.

26. The use according to claim 24, wherein the tumor or metastatic disease is selected from the group consisting of lung cancer, colon cancer, pancreatic cancer, head and neck cancer, breast cancer, ovarian cancer, uterine cancer, gastric cancer, non-small cell lung cancer, leukemia, myelodysplastic syndrome, malignant lymphoma, head and neck tumor, thoracic tumor, gastrointestinal tumor, endocrine tumor, breast and other gynecological tumors, urological tumors, skin tumors, sarcomas, nasal inverted papilloma or squamous cell carcinoma of the nasal cavity associated with nasal inverted papilloma.

27. A compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 22 for the treatment and / or prevention of lung cancer, colon cancer, pancreatic cancer, head and neck cancer, breast cancer, ovarian cancer, uterine cancer, gastric cancer, non-small cell lung cancer, leukemia, myelodysplastic syndrome, malignant lymphoma, head and neck tumor, thoracic tumor, gastrointestinal tumor, endocrine tumor, breast and other gynecological tumors, urological tumors, skin tumors, sarcomas, nasal inverted papilloma or squamous cell carcinoma of the nasal cavity associated with nasal inverted papilloma, which is at least partially related to EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S triple mutation and Del19 / T790M / C797S triple mutation.

Images