PDE4b inhibitor, and pharmaceutical composition thereof and use thereof

Abstract

The present disclosure provides a compound of formula H having excellent PDE4B inhibitory activity, and a pharmaceutical composition thereof and a use thereof. The compound provided by the present disclosure can be used for effectively treating PDE4-related diseases and disorders, including but not limited to inflammatory respiratory diseases, inflammatory bowel diseases, inflammatory joint diseases, inflammatory skin diseases, inflammatory eye diseases, and diseases or cancers of the peripheral or central nervous system.

Description

PDE4B inhibitors and pharmaceutical compositions and uses thereof

[0001] This application claims priority to the following prior applications: Chinese invention patent application No. 202410144764.1, filed with the State Intellectual Property Office of China on February 1, 2024, entitled “PDE4B inhibitors, pharmaceutical compositions thereof, and uses thereof”; and Chinese invention patent application No. 202410637006.3, filed with the State Intellectual Property Office of China on May 21, 2024, entitled “PDE4B inhibitors, pharmaceutical compositions thereof, and uses thereof”. The entire contents of the above-mentioned prior applications are incorporated herein by reference. Technical Field

[0002] The present disclosure relates to a PDE4B inhibitor and a pharmaceutical composition and use thereof, and belongs to the field of chemical medicine. Background Art

[0003] Fibrosis is a general term for a broad range of diseases that can occur in almost all human tissues. Fibrotic tissues and organs gradually lose their normal function, severely impacting patients' quality of life and even becoming life-threatening. For example, pulmonary fibrosis, where fibrotic tissue loses its elasticity, makes it increasingly difficult for the lungs to expand and contract during breathing, reducing vital capacity and severely impairing the patient's ability to move.

[0004] Idiopathic pulmonary fibrosis (IPF) is a progressive pulmonary fibrosis disease that progresses rapidly and can lead to death within a few years, even shorter than the survival of many cancer patients. Due to the gradual worsening of pulmonary fibrosis and the unpredictable progression of the disease, IPF patients suffer from the unimaginable pain of being unable to breathe and may die from respiratory failure and / or heart failure at any time. At the same time, because the clinical manifestations of most IPF patients are atypical, they are easily missed and often misdiagnosed as chronic obstructive pulmonary disease, bronchial asthma, or other lung diseases. The median survival of patients after being diagnosed with IPF is only 2.5 to 5 years.

[0005] IPF is classified as a rare disease in China, the European Union, the United States, and Japan, with a combined global prevalence of approximately 3 million IPF patients. The disease primarily affects patients over 50 years of age, with men more likely to be affected than women. While there are no publicly available large-scale epidemiological studies on the incidence of IPF in China, the burden of IPF on individuals, families, society, and public health resources remains significant due to China's large population.

[0006] The PDE4 subfamily comprises four isoforms (PDE4A, PDE4B, PDE4C, and PDE4D), each with distinct tissue distributions: PDE4A is ubiquitous, with relatively high expression in adipose tissue, brain, heart, and testis; PDE4B is also widely distributed, with particularly high expression in the lung, immune cells, brain, heart, and skeletal muscle; PDE4C is primarily expressed in the testis and other tissues, with low expression in the lung and absent in blood and immune cells; and PDE4D is primarily expressed in the brain, immune cells, and skeletal muscle. Consequently, the PDE4B isoform is more highly expressed in the lung than the other isoforms. In vitro studies targeting PDE4B in pulmonary fibrosis have demonstrated the importance of PDE4B inhibition in anti-inflammatory and anti-fibrotic responses. PDE4B inhibition increases intracellular cAMP levels, subsequently activating protein kinase A (PKA) and cAMP-activated exchange protein (EPAC), reducing the synthesis and release of proinflammatory cytokines and increasing the synthesis of anti-inflammatory cytokines.

[0007] Although preclinical evidence suggests that PDE4 inhibitors are associated with anti-inflammatory and anti-fibrotic effects and have the potential to reduce inflammation and fibrotic remodeling in lung diseases, many PDE4 inhibitors have gastrointestinal side effects due to differences in selectivity, leading to the termination of clinical trials. Therefore, there is a need to develop PDE4B inhibitors that exhibit better selectivity and / or fewer gastrointestinal side effects.

[0008] SUMMARY OF THE INVENTION

[0009] In order to solve the above technical problems, the present disclosure provides a compound represented by the following formula H, its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug:

[0010] in:

[0011] X1 represents chemical bond, C 1-20 Alkylene, O, S, NR q , S(=O), S(=O)2 or C(=O);

[0012] R q selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3- 20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 );

[0013] L represents chemical bond, C 2-20 Alkynyl or Cy; wherein L can be at any position with X1 or R c connect;

[0014] Cy represents a 3-20 membered heterocyclic group, C 6-20 Aryl, 5-20 membered heteroaryl, wherein the 3-20 membered heterocyclic group, C 6-20 The aryl group and the 5-20 membered heteroaryl group may be optionally fused with a 4-7 membered cycloalkyl group, provided that when the heterocyclic group contains a N atom, the heterocyclic group may be bonded to the carbon atom at the 2-position of the pyrimidine ring in formula H through its N atom or C atom;

[0015] W represents a chemical bond, CH, O, S, N, -S(O)-, -S(O)2-, -C(O), sub-C 1-6 Alkyl, C 2-6 Alkenyl or C 2- 6-alkynyl;

[0016] R2 is selected from absent, H, unsubstituted or optionally replaced by 1, 2 or more R d1 Substituted with the following groups: C 6-20 Aryl, 5-20 membered heteroaryl;

[0017] R 2’ represents absence, H, halogen, OH, CN, unsubstituted or optionally replaced by 1, 2 or more R d2 Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2;

[0018] The condition is that R2 and R 2’ Not at the same time "does not exist";

[0019] Alternatively, R2, R 2’ It may be unsubstituted or optionally substituted with 1, 2 or more R d3 Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, 6-20 membered aryl;

[0020] R a represents H or -X-R3;

[0021] X represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-;

[0022] R3 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d4 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2;

[0023] R b represents H or -Y-R4;

[0024] Y represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-;

[0025] R4 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d5 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2;

[0026] The condition is R a 、R b Not at the same time H;

[0027] Or, R a 、R b Together with the atoms to which it is attached, it forms an unsubstituted or optionally substituted group consisting of 1, 2 or more R d6 Substituted with the following groups: C 5-20 Cycloalkenyl, 3-20 membered heterocyclyl, 5-20 membered heteroaryl, 6-20 membered aryl;

[0028] Every R d1 、R d2 、R d3 、R d4 、R d5 、R d6 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), SO, SO2, unsubstituted or optionally substituted by 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-CH2-C(O)R 31 、-C(O)OR 32 、-CH2C(O)OR 32 、-C(O)NHR 32 、-CH2C(O)NHR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 );

[0029] Alternatively, when there are two or more selected from R d1 、R d2 、R d3 、R d4 、R d5 、R d6 When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R e Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0030] Every R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R eSubstituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6-20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, 3-20 membered heterocyclyl, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 );

[0031] m is an integer selected from 1 to 10;

[0032] Every R e the same or different, independently selected from H, halogen, OH, CN, NO2, NH2, oxo (=O), thio (=S), O-CONH2, O-CONHR f , unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 );

[0033] Alternatively, when there are two or more selected from R e When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R f Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0034] Every R f the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R g Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 51 、-C(O)OR 52 、-OC(O)R 53 、-S(O)2R 54 、-S(O)2OR 55 、-OS(O)2R 56 、-P(O)(OR 57 )(OR 58 );

[0035] Alternatively, when there are two or more selected from R fWhen the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R g Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0036] Every R g the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2;

[0037] Every R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2;

[0038] The 3-20 membered heterocyclyl represents a saturated or unsaturated non-aromatic ring or ring system, such as a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, such as 1, 2, 3, 4, 5 or more heteroatoms independently selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2-;

[0039] The C 6-20 Aryl represents a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, or spirocyclic) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which may be a single aromatic ring or multiple aromatic rings fused together;

[0040] The 5-20 membered heteroaryl group represents a monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring system having 5 to 20 ring atoms and containing 1, 2, 3, 4, 5 or more heteroatoms independently selected from N, O and S.

[0041] According to a preferred embodiment in the context of the present disclosure, the compound does not comprise a compound selected from the group consisting of:

[0042] According to an embodiment of the present disclosure, the present disclosure provides a compound represented by the following formula G, its racemate, stereoisomer, tautomer, isotope label, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug:

[0043] in:

[0044] Cy represents a chemical bond, a 3-20 membered heterocyclic group, C 6-20 Aryl, 5-20 membered heteroaryl, provided that when the heterocyclic group contains a N atom, the heterocyclic group can be bonded to the carbon atom at the 2-position of the pyrimidine ring in formula G through its N atom or C atom;

[0045] W represents a chemical bond, CH, O, S, N, -S(O)-, -S(O)2-, -C(O), sub-C 1-6 Alkyl, C 2-6 Alkenyl or C 2- 6-alkynyl;

[0046] R2 is selected from absent, H, unsubstituted or optionally replaced by 1, 2 or more R d1 Substituted with the following groups: C 6-20 Aryl, 5-20 membered heteroaryl;

[0047] R 2’ represents absence, H, halogen, OH, CN, unsubstituted or optionally replaced by 1, 2 or more R d2 Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2;

[0048] The condition is that R2 and R 2’ Not at the same time "does not exist";

[0049] Alternatively, R2, R 2’ It may be unsubstituted or optionally substituted with 1, 2 or more R d3 Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, 6-20 membered aryl;

[0050] R a represents H or -X-R3;

[0051] X represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-;

[0052] R3 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d4Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2;

[0053] R b represents H or -Y-R4;

[0054] Y represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-;

[0055] R4 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d5 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2;

[0056] The condition is R a 、R b Not at the same time H;

[0057] Or, R a 、R b Together with the atoms to which it is attached, it forms an unsubstituted or optionally substituted group consisting of 1, 2 or more R d6 Substituted with the following groups: C 5-20 Cycloalkenyl, 3-20 membered heterocyclyl, 5-20 membered heteroaryl, 6-20 membered aryl;

[0058] Every R d1 、R d2 、R d3 、R d4 、R d5 、R d6 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3- 20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-CH2-C(O)R 31 、-C(O)OR 32 、-CH2C(O)OR 32 、-C(O)NHR 32 、-CH2C(O)NHR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 );

[0059] Alternatively, when there are two or more selected from R d1 、R d2 、R d3 、R d4 、R d5 、R d6 When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R e Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0060] Every R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 );

[0061] m is an integer selected from 1 to 10;

[0062] Every R e the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 );

[0063] Alternatively, when there are two or more selected from R e When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R f Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0064] Every R f the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R g Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 51 、-C(O)OR 52 、-OC(O)R 53 、-S(O)2R 54 、-S(O)2OR 55 、-OS(O)2R 56 、-P(O)(OR 57 )(OR 58 );

[0065] Alternatively, when there are two or more selected from R f When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R g Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0066] Every R g the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2;

[0067] Every R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2;

[0068] The 3-20 membered heterocyclyl represents a saturated or unsaturated non-aromatic ring or ring system, such as a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, such as 1, 2, 3, 4, 5 or more heteroatoms independently selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2-;

[0069] The C 6-20 Aryl represents a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, or spirocyclic) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which may be a single aromatic ring or multiple aromatic rings fused together;

[0070] The 5-20 membered heteroaryl group represents a monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring system having 5 to 20 ring atoms and containing 1, 2, 3, 4, 5 or more heteroatoms independently selected from N, O and S.

[0071] According to an embodiment of the present invention, the cycloalkyl group may be saturated or partially saturated.

[0072] According to an embodiment of the present invention, the compound represented by formula G, its racemate, stereoisomer, tautomer, isotope label, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug can be selected from the following compounds represented by formula I, II, III, IV, V, VI, VII, VIII or IX, its racemate, stereoisomer, tautomer, isotope label, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug:

[0073] The groups in the above formulae I to IX may independently have the definitions in the context of the present disclosure.

[0074] According to an embodiment of the present invention, the compound of formula I may have the following definition:

[0075] in:

[0076] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0077] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0078] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0079] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0080] R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in;

[0081] Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6-alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0082] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0083] The heteroaryl ring is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0084] Cycloalkyl groups may be saturated or partially saturated;

[0085] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substituted with an aryl substituent,

[0086] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or

[0087] R2 represents hydrogen, a mono- or polycyclic C 6-20- Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, C 1-3-alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in .

[0088] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0089] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0090] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0091] Cycloalkyl groups may be saturated or partially saturated;

[0092] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substituted with an aryl substituent;

[0093] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted with a substituent, or

[0094] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0095] Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0096] R3 represents H, C 1-6 -alkyl, F, chlorine, bromine, hydroxyl, -CN, -CH2CN, -CH2COOR, -COOR, -CO-NH(CH3)C 1-3 -fluoroalkyl, (C 1-6 -alkyl)-OH, (C 1-6 -alkyl)-OCH3, (C 1-6 -alkyl)-NH2, (C 1-6 -alkyl)-N(C 1-3 -alkyl) or (C 1-6 -alkyl)-NH;

[0097] R 3’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-20- Aryl, C 6-20- Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- Alkyl groups are substituted.

[0098] Alternatively, R3 and R 3’ Together they represent oxo, methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 -alkyl) is substituted with a substituent;

[0099] R4 represents H, C 1-6 -alkyl, F, chlorine, bromine, hydroxyl, -CN, -CH2CN, -CH2COOR, -COOR, -CO-NH(CH3)C 1-3 -fluoroalkyl, (C 1-6 -alkyl)-OH, (C 1-6 -alkyl)-OCH3, (C 1-6 -alkyl)-NH2, (C 1-6 -alkyl)-N(C 1-3 -alkyl) or (C 1-6 -alkyl)-NH;

[0100] R 4’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-20- Aryl, C 6-20- Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- Alkyl groups are substituted.

[0101] Alternatively, R4 and R 4’ Together they represent oxo, methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3- alkyl) is substituted by a substituent;

[0102] R5 and R6 independently represent H, F, or C 1-6 -alkyl, C 1-3 -fluoroalkyl, C 1-6 -alkyl-OH, C 1-6 -Alkenyl-OCH3, C 1-6 -alkyl-NH2, C 1-6 -alkynyl-NH(C 1-3 -alkyl) and C 1-6 -alkyl-N(C 1-3 -alkyl)2;

[0103] Alternatively, R1 and R3 together with the C- and N-atoms of piperidine form a saturated or partially saturated 5- or 7-membered heterocyclic group containing two or three nitrogen atoms, which may be optionally selected from -CH3, -CH2CH3, -CH2CH2CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3- alkyl) group,

[0104] Alternatively, R3 and R6 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution;

[0105] Alternatively, R3 and R5 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution;

[0106] Alternatively, R3 and R4 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution;

[0107] Alternatively, R4 and R6 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution;

[0108] Alternatively, R4 and R7 together with the carbon atom to which they are attached form a double bond.

[0109] According to an embodiment of the present invention, examples of R1 may be selected from the following groups:

[0110] According to an embodiment of the present invention, -W-R2R 2’ Examples of can be selected from the following groups:

[0111] According to an embodiment of the present invention, the compound of formula II has the following definition:

[0112] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0113] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0114] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0115] R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in

[0116] Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3-alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0117] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0118] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0119] Cycloalkyl groups may be saturated or partially saturated;

[0120] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 5-10 substituted with an aryl substituent;

[0121] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group which may be optionally replaced by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 Substituents substituted;

[0122] R2 represents hydrogen, a mono- or polycyclic C 6-20- Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in;

[0123] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1- 3-Alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0124] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0125] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0126] Cycloalkyl groups may be saturated or partially saturated;

[0127] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substituted with an aryl substituent;

[0128] R2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 5-10 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or

[0129] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-20- Aryl, C 6-20- Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0130] or,

[0131] R2 and R 2’ together form a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O,

[0132] R3 represents a group selected from aryl and heteroaryl, which is independently optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or is independently optionally substituted by one, two or more groups selected from OR1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0133] R4 represents a group selected from aryl and heteroaryl, which is independently optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or is independently optionally substituted by one, two or more groups selected from OR 1.1、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0134] A ring represents a chemical bond, a mono- or polycyclic C 6-20- Aryl may be optionally substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or,

[0135] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0136] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0137] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0138] Cycloalkyl groups may be saturated or partially saturated;

[0139] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10-cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20- aryl;

[0140] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent.

[0141] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0142] According to an embodiment of the present invention, -W-R2R 2’ Examples of can be selected from the following groups:

[0143] According to an embodiment of the present invention, examples of -X-R3 substituents may be selected from the following groups:

[0144] According to an embodiment of the present invention, the compound of formula III has the following definition:

[0145] in:

[0146] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0147] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0148] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0149] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0150] R1 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in

[0151] Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0152] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0153] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0154] Cycloalkyl groups may be saturated or partially saturated;

[0155] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0156] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted with a substituent, or

[0157] R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20-Aryl and NR 2.2 R 2.3 substituted by a substituent in

[0158] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20 Aryl, C 1-6 -alkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 2.2 R2.3 substituted by 1, 2 or more substituents;

[0159] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0160] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally associated heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0161] Cycloalkyl groups may be saturated or partially saturated;

[0162] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic CC 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0163] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted with a substituent, or

[0164] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0165] Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0166] A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10-aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20 Aryl and NR 1.2 R 1.3 Substituents in substituted;

[0167] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20 Aryl, C 1-6 -alkyl, CC 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20 Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0168] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0169] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0170] Cycloalkyl groups may be saturated or partially saturated;

[0171] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 aryl;

[0172] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent.

[0173] Alternatively, according to an embodiment of the present invention,

[0174] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0175] According to an embodiment of the present invention, -W-R2R 2’ Examples of can be selected from the following groups:

[0176] According to an embodiment of the present invention, the compound of formula IV has the following definition:

[0177] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0178] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0179] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0180] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0181] V represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0182] R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20 Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20 Aryl and NR 1.2 R 1.3 substituted by a substituent in

[0183] Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20 Aryl, C 1-6 -alkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20 Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0184] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0185] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0186] Cycloalkyl groups may be saturated or partially saturated;

[0187] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0188] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group which may be optionally replaced by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 or

[0189] R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in

[0190] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0191] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0192] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0193] Cycloalkyl groups may be saturated or partially saturated;

[0194] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0195] R2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 2.1 substituted with a substituent, or

[0196] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0197] Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3-alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0198] A ring represents a chemical bond, a mono- or polycyclic C 6-20 Aryl may be optionally substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 , CH2CH2CO-NR 1.1 ,CH=CHCO-NR1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or,

[0199] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0200] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0201] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0202] Cycloalkyl groups may be saturated or partially saturated;

[0203] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 aryl substitution;

[0204] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent.

[0205] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0206] According to an embodiment of the present invention, -W-R2R 2’ Examples of can be selected from the following groups:

[0207] According to an embodiment of the present invention, the compound of formula V has the following definition:

[0208] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0209] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0210] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0211] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0212] V represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0213] R1 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in;

[0214] or,

[0215] R1 represents a group selected from heterocyclic and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1- 6-alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0216] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0217] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0218] Cycloalkyl groups may be saturated or partially saturated;

[0219] where R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6- 20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 substituted with an aryl substituent;

[0220] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or

[0221] R2 represents hydrogen, a mono- or polycyclic C6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in

[0222] or,

[0223] R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3-alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1- 6-alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0224] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0225] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0226] Cycloalkyl groups may be saturated or partially saturated;

[0227] where R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6- 20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 substituted with an aryl substituent,

[0228] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted with a substituent, or

[0229] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0230] or,

[0231] R2 and R 2’ together form a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O,

[0232] A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10-aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or,

[0233] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0234] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0235] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0236] Cycloalkyl groups may be saturated or partially saturated;

[0237] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 Aryl,

[0238] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3-alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent.

[0239] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0240] According to an embodiment of the present invention, -W-R2R 2’ Examples of substituents may be selected from the following groups:

[0241] According to an embodiment of the present invention, the compound of formula VI has the following definition:

[0242] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0243] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0244] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0245] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0246] R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in

[0247] or,

[0248] R1 represents a group selected from heterocyclic and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1- 6-alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0249] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0250] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0251] Cycloalkyl groups may be saturated or partially saturated;

[0252] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20-aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0253] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or

[0254] R2 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in;

[0255] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0256] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0257] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0258] Cycloalkyl groups may be saturated or partially saturated;

[0259] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0260] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 Substituents substituted;

[0261] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0262] Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0263] A ring represents a chemical bond, a mono- or polycyclic C 6-20 Aryl may be optionally substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 or

[0264] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0265] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0266] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0267] Cycloalkyl groups may be saturated or partially saturated;

[0268] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 aryl;

[0269] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent.

[0270] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0271] According to an embodiment of the present invention, -W-R2R 2’ Examples of substituents may be selected from the following groups:

[0272] According to an embodiment of the present invention, the compound of formula VII has the following definition:

[0273] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0274] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0275] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0276] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0277] R1 represents hydrogen, a mono- or polycyclic C 6-20-aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in;

[0278] Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0279] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0280] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0281] Cycloalkyl groups may be saturated or partially saturated;

[0282] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0283] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 Substituents substituted;

[0284] R2 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in

[0285] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1- 3-Alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0286] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0287] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0288] Cycloalkyl groups may be saturated or partially saturated;

[0289] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0290] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted with a substituent, or

[0291] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0292] Alternatively, R2 and R 2’Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0293] A ring represents a chemical bond, a mono- or polycyclic C 6-20- aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 or

[0294] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3-alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0295] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0296] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0297] Cycloalkyl groups may be saturated or partially saturated;

[0298] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 aryl;

[0299] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent.

[0300] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0301] According to an embodiment of the present invention, -W-R2R 2’ Examples of groups may be selected from the following groups:

[0302] According to an embodiment of the present invention, the compound of formula VIII has the following definition:

[0303] W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl;

[0304] X represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0305] Y represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0306] Z represents CH2, O, S, NH, S(O), S(O)2 or C(O);

[0307] R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in;

[0308] Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1, oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0309] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0310] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0311] Cycloalkyl groups may be saturated or partially saturated;

[0312] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0313] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C1-6 -alkyl, C 6-20- Aryl and COOR 1.1 Substituents substituted;

[0314] R2 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in

[0315] Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents;

[0316] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0317] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0318] Cycloalkyl groups may be saturated or partially saturated;

[0319] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent;

[0320] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 Substituents substituted;

[0321] R 2’ Indicates H, F, Me, C 1-6- Alkyl, C2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 6-20 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 6-20 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0322] Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0323] R4 represents a group selected from aryl and heteroaryl, which is independently optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or is independently optionally substituted by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20-aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents;

[0324] A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 or

[0325] Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0326] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0327] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0328] Cycloalkyl groups may be saturated or partially saturated;

[0329] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 aryl;

[0330] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent.

[0331] According to an embodiment of the present invention, examples of Ring A may be selected from the following groups:

[0332] According to an embodiment of the present invention, -W-R2R 2’ Examples of groups may be selected from the following groups:

[0333] According to an embodiment of the present invention, the compound of formula IX has the following definition:

[0334] in:

[0335] X1 represents chemical bond, C 1-20 Alkylene, O, S, NR q , S(=O), S(=O)2 or C(=O);

[0336] U stands for -(CH2) t -, O, S, NR q , S(=O), S(=O)2 or C(=O), wherein t represents 0, 1, 2 or 3;

[0337] R q selected from H, halogen, OH, CN, NO2, NH2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 );

[0338] v represents 0, 1, 2, 3, 4, or 5;

[0339] L represents chemical bond, C 2-20 Alkynyl or Cy; wherein L can be at any position with X1 or R c connect;

[0340] Cy represents a chemical bond, a 3-20 membered heterocyclic group, C 6-20 Aryl, 5-20 membered heteroaryl, wherein the 3-20 membered heterocyclic group, C 6-20 The aryl group and the 5-20 membered heteroaryl group may be optionally fused with a 4-7 membered cycloalkyl group, provided that when the heterocyclic group contains a N atom, the heterocyclic group may be bonded to the carbon atom at the 2-position of the pyrimidine ring in formula IX through its N atom or C atom;

[0341] R a represents H or -X-R3;

[0342] X represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-;

[0343] R3 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d4 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2;

[0344] R b represents H or -Y-R4;

[0345] Y represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-;

[0346] R4 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d5 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2;

[0347] The condition is R a 、R b Not at the same time H;

[0348] Or, R a 、R b Together with the atoms to which it is attached, it forms an unsubstituted or optionally substituted group consisting of 1, 2 or more R d6 Substituted with the following groups: C 5-20 Cycloalkenyl, 3-20 membered heterocyclyl, 5-20 membered heteroaryl, 6-20 membered aryl;

[0349] Every R d2 、R d4 、R d5 、R d6 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), SO, SO2, unsubstituted or optionally substituted by 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-CH2-C(O)R 31 、-C(O)OR 32 、- CH2C(O)OR 32 、-C(O)NHR 32 、-CH2C(O)NHR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 );

[0350] Alternatively, when there are two or more selected from R d2 、R d4 、R d5 、R d6 When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R e Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0351] Every R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C6-20 Aryl-, C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6-20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, 3-20 membered heterocyclyl, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 );

[0352] For example, the 4-10 membered heterocycloalkyl or 4-10 membered heterocycloalkenyl group may be: 1-methylpyrrolidinyl, 1-ethylpyrrolidinyl, 1-cyclopropylpyrrolidinyl, 1-cyclopropylmethylpyrrolidinyl, 5-methyl-4,5-dihydropyridazin-3(2H)-onyl, 1-methylazetidinyl, 1-methylpiperidinyl;

[0353] m is an integer selected from 1 to 10;

[0354] Every R e the same or different, independently selected from H, halogen, OH, CN, NO2, NH2, oxo (=O), thio (=S), O-CONH2, O-CONHR f , unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 );

[0355] Alternatively, when there are two or more selected from R e When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R f Substituted with the following groups: C 3-20Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0356] Every R f the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R g Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 51 、-C(O)OR 52 、-OC(O)R 53 、-S(O)2R 54 、-S(O)2OR 55 、-OS(O)2R 56 、-P(O)(OR 57 )(OR 58 );

[0357] Alternatively, when there are two or more selected from R f When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R g Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl;

[0358] Every R g the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2;

[0359] Every R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2;

[0360] The 3-20 membered heterocyclyl represents a saturated or unsaturated non-aromatic ring or ring system, such as a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, such as 1, 2, 3, 4, 5 or more heteroatoms independently selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2-;

[0361] The C 6-20 Aryl represents a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, or spirocyclic) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which may be a single aromatic ring or multiple aromatic rings fused together;

[0362] The 5-20 membered heteroaryl group represents a monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring system having 5 to 20 ring atoms and containing 1, 2, 3, 4, 5 or more heteroatoms independently selected from N, O and S.

[0363] According to an embodiment of the present disclosure, L represents an alkynyl group; a mono- or polycyclic C 6-20- Aryl or a mono- or polycyclic C 6-20 - aryl and 4-7 membered cycloalkyl, which may be independently substituted at the ortho, para or meta positions by one, two, or three independent fluorine, chlorine, bromine, hydroxyl, CN, NH2 groups, or by one, two or more substituted groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, C 1-6 -alkyl, C1-3 -fluoroalkyl, C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 , CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or,

[0364] L represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more substituted groups selected from OR 1.1 、C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 , mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents;

[0365] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0366] Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; in some embodiments, L is selected from a 5-membered monocyclic heteroaryl, a 5-membered heteroarylacene ring, a 5-membered heteroaryl and 5-10 membered heteroaryl, a 5-membered heteroaryl and 4-7 membered cycloalkyl, a 5-membered heteroaryl and 4-7 membered heterocycloalkyl, a 6-membered heteroarylacene ring, a 6-membered heteroaryl and 5-10 membered heteroaryl, a 6-membered heteroaryl and 6-membered heteroaryl, a 6-membered heteroaryl and 4-7 membered cycloalkyl, and a 6-membered heteroaryl and 4-7 membered heterocycloalkyl;

[0367] Cycloalkyl groups may be saturated or partially saturated;

[0368] R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, C 3-11-mono- or biheterocyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1- 10- Alkyl and C 6-20- aryl;

[0369] R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20- Aryl, 3-10 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent.

[0370] According to an embodiment of the present disclosure, examples of L may be selected from the following groups:

[0371] According to an embodiment of the present disclosure, each R d2 The same or different, independently of each other, represent hydrogen, halogen, cyano, hydroxyl, CF3, C 1-6 -alkyl, C 1-3 -Fluoroalkyl, CHF2, CH2F, SO2-CH3, SO2-CH2CH3, SO2-NR 1.2 R 1.3 , C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3-alkyl-NH2 or C 1-3 -alkyl-NHR 1.1 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in;

[0372] According to an embodiment of the present disclosure, R e Can be selected from OH;

[0373] Every R d6 The same or different, independently represent H, F, Me, C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 , C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, a mono- or polycyclic C 6- 20- Aryl or a mono- or polycyclic C 6-20 -aryl and 4-7 membered cycloalkyl, a mono- or polycyclic C6-20-heteroaryl and 4-7 membered cycloalkyl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent; or

[0374] Every R d6 The same or different, independently represent H, F, Me, C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3-alkyl-NH2, C 1-3 -alkyl-NHR 1.1 , C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1- 6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent.

[0375] Or, two and R d6 together with the atoms to which it is attached, form a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged cycloalkyl, or a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 , CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6- 20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6- 20- Aryl and NR 2.2 R 2.3 ;

[0376] R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substitution of aryl groups by substituents;

[0377] R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20- Aryl, 3-10 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH -CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted by a substituent.

[0378] Every R c the same or different, independently of each other, represents hydrogen, a mono- or polycyclic C 6-20 -aryl or a mono- or polycyclic C 6-20 - aryl and 4-7 membered cycloalkyl, such as C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6- 20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, or selected from 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, the above groups may be substituted at the ortho, para or meta positions by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 4.1 ,COOR 4.1 CH2COOR 4.1 ,CH2CH2COOR 4.1 ,CH=CHCOOR 4.1 ,CO-NR 4.1 CH2CO-NR 4.1 ,CH2CH2CO-NR 4.1 ,CH=CHCO-NR4.1 ,NR 4.2 R 4.3 ,CH2-NR 4.2 R 4.3 ,CH2CH2-NR 4.2 R 4.3 ,C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 4.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 4.1 , C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 4.2 R 4.3 Substituents substituted;

[0379] Or, each R c are identical or different and independently represent a group selected from heterocycle and heteroaryl, which may be optionally substituted in the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 4.1 、C 1-3 -alkyl-OR 4.1 SR 4.1 、C 1-3 -alkyl-SR 4.1 ,SO-R 4.1 ,C 1-3 -alkyl-SOR 4.1 ,SO2-R 4.1 ,C 1-3 -alkyl-SO2R 4.1 ,COOR 4.1 ,CH2COOR 4.1 ,CH2CH2COOR 4.1 ,CH=CHCOOR 4.1 ,CO-NR4.1 CH2CO-NR 4.1 ,CH2CH2CO-NR 4.1 ,CH=CHCO-NR 4.1 ,COR 4.1 ,CH2COR 4.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 4.1 and NR 4.2 R 4.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 4.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 4.2 R 4.3 substituted by 1, 2 or more substituents;

[0380] Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O;

[0381] The heteroaryl ring is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group including 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; in some embodiments R4 is selected from a 5-membered monocyclic heteroaryl, a 5-membered heteroarylacene ring, a 5-membered heteroaryl and 5-10 membered heteroaryl, a 5-membered heteroaryl and 4-7 membered cycloalkyl, a 5-membered heteroaryl and 4-7 membered heterocycloalkyl, a 6-membered heteroarylacene ring, a 6-membered heteroaryl and 5-10 membered heteroaryl, a 6-membered heteroaryl and 6-membered heteroaryl, a 6-membered heteroaryl and 4-7 membered cycloalkyl, and a 6-membered heteroaryl and 4-7 membered heterocycloalkyl;

[0382] Cycloalkyl groups may be saturated or partially saturated;

[0383] R 4.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 5-10 substituted with an aryl substituent;

[0384] R 4.2 and R 4.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-10 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 4.1 and COOR 4.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 4.1 substituted by a substituent.

[0385] For example, the 4-10 membered heterocyclic group or 4-10 membered heterocycloalkenyl group can be: 1-methylpyrrolidinyl, 1-ethylpyrrolidinyl, 1-cyclopropylpyrrolidinyl, 1-cyclopropylmethylpyrrolidinyl, 5-methyl-4,5-dihydropyridazin-3(2H)-one, 1-methylazetidinyl, 1-methylpiperidinyl.

[0386] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound, when present, R1 represents hydrogen, a mono- or polycyclic C 6-20 Aryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, -NHOH, -C 1-3- Alkyl-NHOH, -C1-3 -CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, CN, NO2, NH2, or substituted by 1, 2 or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6- 20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO-NHOH, -CO-NHOH, -C 1-3 -alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8-cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 、-OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in; wherein R 1.1 、R 1.2 、R 1.3 has the meaning given in the context of this document.

[0387] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound thereof, when present, R1 represents a group selected from heterocyclic and heteroaryl, which may be optionally substituted at the ortho, para or meta position by one, two or three halogens, OH, CN, NH2, -NHOH, -C 1-3 -alkyl-NHOH, -C 1- 3-alkyl-CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, nitro, oxo, CF3, CHF2 and CH2F, or substituted by 1, 2 or more selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3 -alkyl-NHOH, -C 1-3- Alkyl-CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 , OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by one, two or more substituents; wherein R 1.1 、R 1.2 、R 1.3 has the meaning given in the context of this document.

[0388] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound, when present, R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,C(CH3)2COOR 2.1 ,CF2COOR 2.1 ,CHFCOOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 ,CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, COOR 2.1 -C 3-8- Cycloalkyl, CO-NR 2.1 -C 3-8- Cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2- CH2CH3 and SO2-NR 2.2 R2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO-NHOH, -CO-NHOH, -C 1-3 -alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 , OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 2.2 R 2.3 Substituted by the substituent in CCOOR 2.1 ; Among them, R 2.1 、R 2.2 、R 2.3 has the meaning given in the context of this document.

[0389] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound thereof, when present, R2 represents a group selected from heterocyclic and heteroaryl groups, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogens, OH, CN, NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1- 3- Alkyl-CO - NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, nitro, oxo, CF3, CHF2 and CH2F, or substituted by 1, 2 or more selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,COOR 2.1 -C 3-8 -cycloalkyl, CO-NR 2.1 -C 3-8 -cycloalkyl, CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20 Aryl, C 1-6 -alkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 2.2 R 2.3 substituted by one, two or more substituents; wherein R 2.1 、R 2.2 、R 2.3 has the meaning given in the context of this document.

[0390] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound, when present, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 、C 1-3 -alkyl-OC 1-3 -alkyl-COOH, C 1-3 -alkyl-OC 1-3 -alkyl-CONR 2.1 、C 1-3 -alkyl-phosphoric acid, C 1-3 -alkyl-OC(O)-OR 2.1 、C 1-3 -alkyl-OC(O)-NR 2.1 、C 1-3 -alkyl-OC(=O)-C 1-3 -alkyl-(OC 1-3 -alkyl)v, C 1-3 -alkyl-OC(=O)-C 1-6 -alkyl-COOR 2.1 、C 1-3 -alkyl-NC(=O)-C 1-6 -alkyl-COOR 2.1 、C 1-3 -alkyl-NC(=O)-OC 1-6 -alkyl-COOR 2.1 、C 1-3 -alkyl-NC(=O)-NC 1-6 -alkyl-COOR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 ,CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 Each of the substituents may be optionally replaced by one, two or more substituents selected from OH, CN, C 1-3 -alkyl-CN, C 1-3 -alkyl-NH2, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 、-OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3substituted by a substituent in which R 2.1 、R 1.2 、R 1.3 , v has the meaning given in the context of this document.

[0391] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound, when present, each R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, NH2; each of the above groups may be optionally replaced by OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO - NHOH, -CO - NHOH, -C 1-3- Alkyl-NH - CO - NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC3- 8-cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 , OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by one, two or more substituents; wherein R 1.1 、R 1.2 、R 2.1 、R 2.3 has the meaning given in the context of this document.

[0392] Alternatively, according to the compound represented by Formula H or Formula G of the present disclosure (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt or prodrug compound, when present, each R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, C 1-6 Alkyl-C 4-10 Heterocycloalkyl, C 1-6 Alkyl-C 4-10 Heterocycloalkenyl, C 1-6 Alkyl-C 6-20 Aryl, C 1-6 Alkyl-C 5-20 Heteroaryl, 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6-20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, 3-20 membered heterocyclyl, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); where R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 has the meaning given in the context of this document.

[0393] Unless otherwise defined, in the compounds of any one of Formulas I to IX in the context of the present disclosure, when some substituents are defined as two connected groups (such as the form of "group 1-group 2", wherein group 1 and group 2 are the same or different), the position at which the substituents form a bond in the compound of any one of Formulas I to IX is not particularly limited, for example, group 1 may be bonded to the connection position in the compound of any one of Formulas I to IX, or group 2 may be bonded to the connection position in the compound of any one of Formulas I to IX, as long as the above-mentioned bonding conforms to the valence bond theory. In addition, the connection position between the two connected groups (such as group 1 and group 2) is not particularly limited, as long as the above-mentioned connection conforms to the valence bond theory.

[0394] For the purpose of illustration, for example, 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 、3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl groups, which may represent C 6-20- Aryl-C 1-6 -alkyl-, 5-20 membered heteroaryl-C 1-6 Alkyl-, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl)-, 3-20 membered heterocyclyl-C 6-20- Aryl-, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 -, 3-20 membered heterocyclic-C 1-6 -alkyl-, C 3-10 -cycloalkyl-C 1-6 -alkyl-, can also represent -C 6-20- Aryl-C 1-6 -alkyl, -5-20 membered heteroaryl-C 1-6 Alkyl, -C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), -3-20 membered heterocyclyl-C 6-20- Aryl, -5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 、-3-20 membered heterocyclic-C 1-6 -alkyl, -C 3-10-cycloalkyl-C 1-6 -alkyl.

[0395] It should be understood that, for the above-mentioned "group 1-group 2" form, if a chemical bond "-" is added to the left side of group 1 or the right side of group 2, it means that its connection position in the compound described in any one of Formulas I to IX has been determined, and the position where it forms a bond in the compound described in any one of Formulas I to IX is the corresponding group to which the chemical bond is added.

[0396] The present disclosure also provides a method for preparing a compound represented by Formula H, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt, or prodrug, wherein the preparation method comprises reacting a compound of Formula A1 with a compound of Formula B1 to obtain a compound of Formula G:

[0397] Wherein, LG is a leaving group, such as Cl, Br or I;

[0398] X1, L, W, R a 、R b 、R c , R2, R 2’ , m independently have the definitions given above.

[0399] The present disclosure also provides a method for preparing a compound represented by Formula G, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt, or prodrug, wherein the preparation method comprises reacting a compound of Formula A with a compound of Formula B to obtain a compound of Formula G:

[0400] and optionally, derivatizing the compound of formula G into a stereoisomer, tautomer, isotopically labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt, or prodrug thereof;

[0401] Wherein, LG is a leaving group, such as Cl, Br or I;

[0402] Cy, W, R a 、R b 、R c , R2, R 2’ , m independently have the definitions given above.

[0403] According to the embodiment of the present disclosure, if necessary, the reaction can be carried out in the presence of a protective group on the compound of formula A1, compound A2, compound B1 or compound B2. For example, the protective group can be selected from an amino protective group, a hydroxyl protective group, etc. Suitable protective groups can be selected from C 1-40Alkyl, C 6-20 Aryl C 1-40 Alkyl-, for example tert-butyl, isopropyl, benzyl, tert-butoxycarbonyl (Boc), 2-biphenyl-2-propoxycarbonyl, benzyloxycarbonyl, fluorenylmethyloxycarbonyl (Fmoc), trifluoroacetyl.

[0404] According to an embodiment of the present disclosure, the preparation method can be carried out in the presence of a solvent such as an organic solvent. For example, the organic solvent can be selected from at least one of the following: alcohols, such as methanol, ethanol, isopropyl alcohol, and n-butanol; ethers, such as ethyl propyl ether, n-butyl ether, anisole, phenethyl ether, cyclohexyl methyl ether, dimethyl ether, diethyl ether, dimethyl glycol, biphenyl ether, dipropyl ether, diisopropyl ether, di-n-butyl ether, diisobutyl ether, diisoamyl ether, ethylene glycol dimethyl ether, isopropyl ethyl ether, methyl tert-butyl ether, tetrahydrofuran, methyltetrahydrofuran, dioxane, dichlorodiethyl ether, and Polyethers of ethylene oxide and / or propylene oxide; aliphatic, cycloaliphatic or aromatic hydrocarbons, such as pentane, hexane, heptane, octane, nonane, and those possibly substituted by fluorine and chlorine atoms, such as methylene chloride, dichloromethane, chloroform, carbon tetrachloride, fluorobenzene, chlorobenzene or dichlorobenzene; cyclohexane, methylcyclohexane, petroleum ether, octane, benzene, toluene, chlorobenzene, bromobenzene, xylene; esters such as methyl acetate, ethyl acetate, butyl acetate, isobutyl acetate and dimethyl carbonate, dibutyl carbonate or ethylene carbonate.

[0405] The present disclosure also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by Formula H or Formula G (e.g., any one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt, or at least one of its prodrug compounds.

[0406] According to an embodiment of the present disclosure, the pharmaceutical composition further comprises one or more pharmaceutically acceptable excipients.

[0407] According to an embodiment of the present disclosure, the pharmaceutical composition may further contain one or more additional therapeutic agents. The additional therapeutic agent may be selected from therapeutic agents having the same or different targets as the disclosed compound, such as cancer therapeutic agents.

[0408] The present disclosure also provides the use of at least one of the compounds represented by Formula H or Formula G (e.g., one of the compounds represented by Formulas I to IX), their racemates, stereoisomers, tautomers, isotope-labeled substances, solvates, polymorphs, pharmaceutically acceptable salts, or prodrug compounds thereof in the preparation of a drug.

[0409] The medicament can be used to prevent or treat a disease.

[0410] The present invention also provides a method for preventing or treating a disease, comprising administering to a patient in need thereof at least one of a compound represented by Formula H or Formula G (e.g., one of the compounds represented by Formulas I to IX), its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, pharmaceutically acceptable salt, or a prodrug compound thereof.

[0411] According to an embodiment of the present invention, the disease may be a PDE4B-mediated disease, or at least a disease mediated by PDE4.

[0412] For example, the disease mediated at least by PDE4 is selected from diseases mediated by PDE4, or diseases mediated by at least one (eg, 1, 2, 3, or 4) of PDE1, PDE2, PDE3, and PDE5.

[0413] For example, the medicament can be used to prevent or treat a disease mediated by PDE4 and at least one (eg, 1, 2, 3, or 4) selected from PDE1, PDE2, PDE3, and PDE5.

[0414] According to embodiments of the present disclosure, the PDE4 is selected from the group consisting of PDE4A, PDE4B (eg, PDE4B2), PDE4C, and PDE4D (eg, PDE4D2).

[0415] According to an embodiment of the present disclosure, the PDEl is selected from the group consisting of PDElA, PDElB and PDElC.

[0416] According to an embodiment of the present disclosure, the PDE2 is selected from PDE2A.

[0417] According to an embodiment of the present disclosure, the PDE3 is selected from PDE3A and PDE3B.

[0418] According to an embodiment of the present disclosure, the PDE5 is selected from PDE5A.

[0419] According to an embodiment of the present invention, the disease includes but is not limited to respiratory inflammatory diseases, inflammatory bowel diseases, arthritic diseases, skin inflammatory diseases, eye inflammatory diseases, diseases of the peripheral or central nervous system, degenerative lesions of the central nervous system, Alzheimer's Disease (AD), non-alcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) or pulmonary hypertension associated therewith, chronic obstructive pulmonary disease (COPD) or pulmonary hypertension associated therewith, hepatic fibrosis (HF), renal fibrosis, benign prostatic hyperplasia (BPH), gastroesophageal reflux disease, obstructive sleep apnea and coronary artery disease or cancer.

[0420] According to an embodiment of the present invention, the cancer includes but is not limited to one selected from the following: gastric cancer, bladder cancer, blood cancer, bone cancer, brain cancer, breast cancer, central nervous system cancer, cervical cancer, colon cancer, endometrial cancer, esophageal cancer, gallbladder cancer, gastrointestinal cancer, external genital cancer, urogenital tract cancer, head cancer, kidney cancer, laryngeal cancer, liver cancer, lung cancer, muscle tissue cancer, neck cancer, oral or nasal mucosal cancer, ovarian cancer, pancreatic cancer, prostate cancer, skin cancer, spleen cancer, small intestine cancer, large intestine cancer, testicular cancer and / or thyroid cancer.

[0421] According to an embodiment of the present invention, since the compounds disclosed herein have specific tissue distribution and / or low hERG inhibitory effect, the diseases are preferably selected from those diseases that are particularly advantageous when prevented or treated with compounds having specific tissue distribution and / or low hERG inhibitory effect.

[0422] For example, the focus of the disease (i.e., the part where pathological changes occur) includes the respiratory system, digestive system, excretory system and / or reproductive system, such as liver, kidney and / or prostate. For this purpose, the medicine can be a targeted drug for the respiratory system, digestive system, excretory system and / or reproductive system, such as a liver targeted drug, a kidney targeted drug and / or a prostate targeted drug.

[0423] When used as a drug, the compounds of the present disclosure can be administered in the form of a pharmaceutical composition. These compositions can be prepared in a manner well known in the pharmaceutical field and can be administered by a variety of routes, depending on whether local or systemic treatment is required and the area to be treated. Administration can be topical (e.g., transdermal, skin, eye and mucous membranes including intranasal, vaginal and rectal delivery), pulmonary (e.g., by inhalation or insufflation of powders or aerosols, including by nebulizer; intratracheal, intranasal), oral or parenteral. Parenteral administration includes intravenous, intraarterial, subcutaneous, intraperitoneal or intramuscular injection or infusion; or intracranial, such as intrathecal or intraventricular administration. It can be administered parenterally in a single bolus form, or it can be administered by, for example, a continuous infusion pump. Topically administered pharmaceutical compositions and preparations may include transdermal patches, ointments, lotions, creams, gels, drops, suppositories, sprays, liquids and powders. Conventional pharmaceutical carriers, water, powders or oily bases, thickeners, etc. may be necessary or required.

[0424] In preparing the compositions of the present disclosure, the active ingredient is typically mixed with an excipient, diluted by the excipient, or enclosed in a carrier such as a capsule, sachet, paper, or other container. When the excipient serves as a diluent, it can be a solid, semisolid, or liquid substance that acts as a solvent, carrier, or medium for the active ingredient. Thus, the compositions can be in the form of tablets, pills, powders, lozenges, sachets, cachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols (solid or dissolved in a liquid medium), ointments containing, for example, up to 10% by weight of the active compound, soft and hard gelatin capsules, suppositories, sterile injectable solutions, and sterile packaged powders.

[0425] Some examples of suitable excipients include lactose, glucose, sucrose, sorbitol, mannitol, starch, gum arabic, calcium phosphate, alginates, tragacanth gum, gelatin, calcium silicate, microcrystalline cellulose, polyvinyl pyrrolidone, cellulose, water, syrup, and methylcellulose. The formulation may also contain: lubricants such as talc, magnesium stearate, and mineral oil; wetting agents; emulsifiers and suspending agents; preservatives such as methyl benzoate and hydroxypropyl benzoate; sweeteners and flavoring agents. The compositions of the present disclosure can be formulated using methods known in the art so as to provide immediate, sustained, or delayed release of the active ingredient after administration to the patient.

[0426] The compositions can be formulated in unit dosage form, each dose containing about 5 to 1000 mg, more usually about 100 to 500 mg, of the active ingredient. The term "unit dosage form" refers to physically discrete units suitable as single dosage units for human patients and other mammals, each unit containing a predetermined quantity of active material calculated to produce the desired therapeutic effect, in admixture with a suitable pharmaceutical excipient.

[0427] The effective dosage of the active compound can range widely, and is generally administered in a pharmaceutically effective amount. However, it will be understood that the actual amount of compound administered is generally determined by the physician based on relevant circumstances, including the condition being treated, the route of administration chosen, the actual compound being administered; the age, weight, and response of the individual patient; the severity of the patient's symptoms, etc.

[0428] For preparing solid compositions such as tablets, the principal active ingredient is mixed with a pharmaceutical excipient to form a solid preformulation composition comprising a homogeneous mixture of a compound of the present disclosure. When these preformulation compositions are referred to as homogeneous, it is meant that the active ingredient is generally evenly distributed throughout the composition, such that the composition can be readily divided into equally effective unit dosage forms such as tablets, pills, and capsules. This solid preformulation is then divided into unit dosage forms of the type described above, containing, for example, about 0.1 to 1000 mg of the active ingredient of the present disclosure.

[0429] The tablets or pills of the present disclosure may be coated or compounded to provide dosage forms that offer the advantage of prolonged action. For example, a tablet or pill may contain an inner dosage component and an outer dosage component, the outer dosage component being in the form of a film coating the outer dosage component. The two components may be separated by an enteric layer that serves to prevent disintegration in the stomach, thereby allowing the inner component to pass intact into the duodenum or to be released later. A variety of materials may be used for such enteric layers or coatings, including a variety of polymeric acids and mixtures of polymeric acids with such materials, such as shellac, cetyl alcohol, and cellulose acetate.

[0430] Liquid forms for oral or parenteral administration in which the disclosed compounds and compositions can be incorporated include aqueous solutions, appropriately flavored syrups, aqueous or oily suspensions; and emulsions flavored with edible oils such as cottonseed oil, sesame oil, coconut oil, or peanut oil; as well as elixirs and similar pharmaceutically acceptable vehicles.

[0431] Compositions for inhalation or insufflation include solutions, suspensions, and powders dissolved in pharmaceutically acceptable water or organic solvents, or mixtures thereof. Liquid or solid compositions may contain suitable pharmaceutically acceptable excipients as described above. In certain embodiments, the compositions are administered by the oral or nasal respiratory route for local or systemic effect. The compositions may be aerosolized using an inert gas. Aerosolized solutions may be inhaled directly from a nebulizing device, or the nebulizing device may be connected to a mask curtain or intermittent positive pressure breathing machine. Solution, suspension, or powder compositions may be administered orally or nasally using a device that delivers the formulation in an appropriate manner.

[0432] The amount of compound or composition administered to a patient is not fixed and depends on the agent being administered, the purpose of administration, e.g., prevention or treatment; the patient's condition; the mode of administration; and the like. In therapeutic applications, the composition may be administered to a patient already suffering from a disease in an amount sufficient to cure or at least partially arrest the symptoms of the disease and its complications. The effective dose will depend on the disease being treated and the judgment of the attending clinician, which will depend on factors such as the severity of the disease, the patient's age, weight, and general condition.

[0433] The compositions administered to patients can be in the form of pharmaceutical compositions as described above. These compositions can be sterilized by conventional sterilization techniques or by filtration. Aqueous solutions can be packaged for use as is or lyophilized, and the lyophilized formulation can be mixed with a sterile aqueous carrier prior to administration. The pH of the compound formulation is typically 3 to 11, more preferably 5 to 9, and most preferably 7 to 8. It will be appreciated that the use of some of the aforementioned excipients, carriers, or stabilizers may result in the formation of pharmaceutical salts.

[0434] The therapeutic dose of the disclosed compounds may depend on, for example, the specific use of the treatment, the manner in which the compound is administered, the patient's health and condition, and the judgment of the prescribing physician. The proportion or concentration of the disclosed compounds in the pharmaceutical composition may not be fixed and depends on a variety of factors, including dosage, chemical properties (e.g., hydrophobicity), and route of administration. For example, the disclosed compounds may be provided in a physiologically buffered aqueous solution containing about 0.1 to 10% w / v of the compound for parenteral administration. Some typical dosage ranges are about 1 μg / kg to about 1 g / kg body weight / day. In certain embodiments, the dosage range is about 0.01 mg / kg to about 100 mg / kg body weight / day. The dosage is likely to depend on such variables as the type and extent of the disease or condition, the general health status of the particular patient, the relative biological efficacy of the selected compound, the excipient formulation, and its route of administration. The effective dose can be obtained by extrapolation of a dose-response curve derived from an in vitro or animal model test system. Beneficial effects

[0435] The present disclosure provides novel compounds comprising a novel pyrimidine-fused ring as a core, novel side chains, novel linkers, and substituents. The compounds disclosed herein exhibit excellent PDE4B inhibitory activity, even at the pmol level. The compounds disclosed herein also exhibit selective PDE4B inhibitory activity, particularly PDE4B / 4D selective inhibitory activity. Some compounds also surprisingly exhibit dual- or multi-target inhibitory activity.

[0436] The compounds disclosed herein can be used to treat respiratory inflammatory diseases, inflammatory bowel disease, arthritic diseases, inflammatory skin diseases, inflammatory eye diseases, and diseases or cancers of the peripheral or central nervous system. Furthermore, the compounds disclosed herein have specific tissue distribution and / or low hERG inhibition, thus possessing promising potential as tissue-targeted drugs and improved tissue toxicity.

[0437] Definitions and Explanations of Terms

[0438] Unless otherwise indicated, the definitions of groups and terms in this specification and claims, including definitions used as examples, exemplary definitions, preferred definitions, definitions in tables, and definitions of specific compounds in the Examples, may be arbitrarily combined and coupled with one another. The group definitions and compound structures resulting from such combinations and couplings should be understood to be within the scope of this specification and / or claims.

[0439] Unless otherwise indicated, the numerical ranges recited in this specification and claims are equivalent to reciting at least each specific integer value therein. For example, the numerical range "1-20" is equivalent to reciting each integer value in the numerical range "1-10," namely, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, and each integer value in the numerical range "11-40," namely, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20. In addition, when certain numerical ranges are described as "numbers," it should be understood that the two endpoints of the range, each integer within the range, and each decimal within the range are recited. For example, "a number from 0 to 10" should be understood to recite not only each integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10, but also at least the sum of each integer therein and 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, or 0.9, respectively.

[0440] It should be understood that herein, when describing 1, 2 or more, "more" should refer to an integer greater than 2, such as an integer greater than or equal to 3, such as 3, 4, 5, 6, 7, 8, 9 or 10.

[0441] The term "halogen" refers to fluorine, chlorine, bromine and iodine.

[0442] The term "C 1-20 "Alkyl" is understood to mean a straight-chain or branched saturated monovalent hydrocarbon group having 1 to 20 carbon atoms. For example, "C 1-10 "Alkyl" means straight-chain and branched alkyl groups having 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms, "C 1-6The term "alkyl" refers to straight-chain and branched alkyl groups having 1, 2, 3, 4, 5 or 6 carbon atoms. The alkyl group is, for example, methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, isobutyl, sec-butyl, tert-butyl, isopentyl, 2-methylbutyl, 1-methylbutyl, 1-ethylpropyl, 1,2-dimethylpropyl, neopentyl, 1,1-dimethylpropyl, 4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl, 2-ethylbutyl, 1-ethylbutyl, 3,3-dimethylbutyl, 2,2-dimethylbutyl, 1,1-dimethylbutyl, 2,3-dimethylbutyl, 1,3-dimethylbutyl or 1,2-dimethylbutyl, or the like or isomers thereof.

[0443] The term "C 2-20 "Alkenyl" is understood to mean preferably a linear or branched monovalent hydrocarbon radical containing one, two or more double bonds and having 2 to 20 carbon atoms, preferably "C 2-10 Alkenyl". "C 2-10 "Alkenyl" is understood to mean preferably a linear or branched monovalent hydrocarbon radical containing 1, 2 or more double bonds and having 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms, for example having 2, 3, 4, 5 or 6 carbon atoms (i.e., C 2-6 alkenyl), having 2 or 3 carbon atoms (i.e., C 2-3It is understood that when the alkenyl group contains more than one double bond, the double bonds may be separated from one another or conjugated. The alkenyl group is, for example, vinyl, allyl, (E)-2-methylvinyl, (Z)-2-methylvinyl, (E)-but-2-enyl, (Z)-but-2-enyl, (E)-but-1-enyl, (Z)-but-1-enyl, pent-4-enyl, (E)-pent-3-enyl, (Z)-pent-3-enyl, (E)-pent-2-enyl, (Z)-pent-2-enyl, (E)- Pent-1-enyl, (Z)-pent-1-enyl, hex-5-enyl, (E)-hex-4-enyl, (Z)-hex-4-enyl, (E)-hex-3-enyl, (Z)-hex-3-enyl, (E)-hex-2-enyl, (Z)-hex-2-enyl, (E)-hex-1-enyl, (Z)-hex-1-enyl, isopropenyl, 2-methylprop-2-enyl, 1-methylprop-2-enyl , 2-methylprop-1-enyl, (E)-1-methylprop-1-enyl, (Z)-1-methylprop-1-enyl, 3-methylbut-3-enyl, 2-methylbut-3-enyl, 1-methylbut-3-enyl, 3-methylbut-2-enyl, (E)-2-methylbut-2-enyl, (Z)-2-methylbut-2-enyl, (E)-1-methylbut-2-enyl, (Z)-1-methyl But-2-enyl, (E)-3-methylbut-1-enyl, (Z)-3-methylbut-1-enyl, (E)-2-methylbut-1-enyl, (Z)-2-methylbut-1-enyl, (E)-1-methylbut-1-enyl, (Z)-1-methylbut-1-enyl, 1,1-dimethylprop-2-enyl, 1-ethylprop-1-enyl, 1-propylvinyl, 1-isopropylvinyl.

[0444] The term "C 2-20 "Alkynyl" is understood to mean a linear or branched monovalent hydrocarbon radical containing one, two or more triple bonds and having 2 to 20 carbon atoms, preferably "C 2-10 Alkynyl". The term "C 2-10 "Alkynyl" is understood to mean preferably a linear or branched monovalent hydrocarbon radical containing one, two or more triple bonds and having 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms, for example having 2, 3, 4, 5 or 6 carbon atoms (i.e., "C 2-6 Alkynyl”), having 2 or 3 carbon atoms (“C 2-3The alkynyl group is, for example, ethynyl, prop-1-ynyl, prop-2-ynyl, but-1-ynyl, but-2-ynyl, but-3-ynyl, pent-1-ynyl, pent-2-ynyl, pent-3-ynyl, pent-4-ynyl, hex-1-ynyl, hex-2-ynyl, hex-3-ynyl, hex-4-ynyl, hex-5-ynyl, 1-methylprop-2-ynyl, 2-methylbut-3-ynyl, 1-methylbut-3-ynyl, 1-methylbut-2-ynyl, 3-methylbut-1-ynyl, 1-ethylprop-2-ynyl, 3-methylpent-4-ynyl, 2-methylpent-4-ynyl, 1-methylpent-4-ynyl, In some embodiments, the alkynyl group is ethynyl, prop-1-ynyl or prop-2-ynyl.

[0445] The term "C 3-20 "Cycloalkyl" is understood to mean a saturated or unsaturated (such as partially unsaturated) monovalent monocyclic, bicyclic (such as condensed ring, bridged ring, spiro ring) hydrocarbon ring or tricyclic alkane having 3 to 20 carbon atoms, preferably "C 3-10 Cycloalkyl". The term "C 3-10 "Cycloalkyl" is understood to mean a saturated monovalent monocyclic, bicyclic (eg bridged, spiro) hydrocarbon ring or tricyclic alkane having 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms. 3-10 The cycloalkyl group may be a monocyclic hydrocarbon group such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl or cyclodecyl, or a bicyclic hydrocarbon group such as borneol, indolyl, hexahydroindolyl, tetrahydronaphthyl, decahydronaphthyl, bicyclo[2.1.1]hexyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, 6,6-dimethylbicyclo[3.1.1]heptyl, 2,6,6-trimethylbicyclo[3.1.1]heptyl, bicyclo[2.2.2]octyl, 2,7-diazaspiro[3,5]nonyl, 2,6-diazaspiro[3,4]octyl, or a tricyclic hydrocarbon group such as adamantyl.

[0446] It should be understood by those skilled in the art that the term "C 3-20 Cycloalkyl" does not have aromaticity. Moreover, when the above "C 3-20 When the cycloalkyl group is unsaturated, it may have one or more carbon-carbon double bonds and / or one or more carbon-carbon triple bonds. 3-20When a cycloalkyl group has a carbon-carbon double bond, it can also be called a "C 3-20 Cycloalkenyl"; when "C 3-20 When a cycloalkyl group has a carbon-carbon triple bond, it can also be called a "C 3-20 Cycloalkynyl".

[0447] Unless otherwise defined, the term "3-20 membered heterocyclyl" refers to a saturated or unsaturated non-aromatic ring or ring system, for example, a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, for example 1, 2, 3, 4, 5 or more heteroatoms selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2- states. Preferably, the heterocyclyl may be selected from "3-10 membered heterocyclyl". The term "3-10 membered heterocyclyl" means a saturated or unsaturated non-aromatic ring or ring system, and contains at least one heteroatom selected from O, S and N. The heterocyclic group can be connected to the rest of the molecule by any one of the carbon atoms or nitrogen atom (if present). The heterocyclic group can include fused or bridged rings and spirocyclic rings. In particular, the heterocyclic group can include but is not limited to: 4-membered rings, such as azetidinyl, oxetane; 5-membered rings, such as tetrahydrofuranyl, dioxolyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, pyrrolinyl; or 6-membered rings, such as tetrahydropyranyl, piperidinyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl or trithianyl; or 7-membered rings, such as diazepanyl. Optionally, the heterocyclic group can be benzo-fused. The heterocyclic group may be bicyclic, for example, but not limited to, a 5,5-membered ring such as a hexahydrocyclopenta[c]pyrrol-2(1H)-yl ring, or a 5,6-membered bicyclic ring such as a hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl ring. The heterocyclic group may be partially unsaturated, i.e., it may contain one, two, or more double bonds, for example, but not limited to, dihydrofuranyl, dihydropyranyl, 2,5-dihydro-1H-pyrrolyl, 4H-[1,3,4]thiadiazinyl, 4,5-dihydrooxazolyl, or 4H-[1,4]thiazinyl, or it may be benzo-fused, for example, but not limited to, dihydroisoquinolinyl. When the 3-20-membered heterocyclic group is linked to other groups to form the compounds of the present disclosure, the carbon atoms on the 3-20-membered heterocyclic group may be linked to the other groups, or heteroatoms on the 3-20-membered heterocyclic group may be linked to the other groups. For example, when the 3-20 membered heterocyclic group is selected from piperazinyl, the nitrogen atom on the piperazinyl group may be linked to another group. Or when the 3-20 membered heterocyclic group is selected from piperidinyl, the nitrogen atom on the piperidinyl ring and the carbon atom at the para position thereof may be linked to another group. For example, the substituted 4-10 membered heterocyclic group may be selected from: 1-methylpyrrolidinyl, 1-ethylpyrrolidinyl, 1-cyclopropylpyrrolidinyl, 1-cyclopropylmethylpyrrolidinyl, 5-methyl-4,5-dihydropyridazin-3(2H)-one, 1-methylazetidinyl, 1-methylpiperidinyl;

[0448] The term "C6-20 "Aryl" should be understood to preferably mean a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, spiro) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which can be a single aromatic ring or a polyaromatic ring fused together, preferably "C 6- 14 Aryl". The term "C 6-14 "Aryl" is understood to mean preferably a monovalent aromatic or partially aromatic monocyclic, bicyclic or tricyclic hydrocarbon ring ("C 6-14 or a ring having 9 carbon atoms ("C9 aryl"), for example indanyl or indenyl, or a ring having 10 carbon atoms ("C 10 aryl) such as tetrahydronaphthyl, dihydronaphthyl or naphthyl, or a ring having 13 carbon atoms ("C 13 aryl), such as fluorenyl, or a ring having 14 carbon atoms ("C 14 aryl”), such as anthracenyl. When the C 6-20 When the aryl group is substituted, it may be monosubstituted or polysubstituted. Furthermore, there is no limitation on the position of substitution, and for example, substitution may be at the ortho, para or meta position.

[0449] The term "5-20 membered heteroaryl" is understood to include monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring systems having 5 to 20 ring atoms and containing 1 to 5 heteroatoms independently selected from N, O and S, for example "5-14 membered heteroaryl". The term "5-14 membered heteroaryl" is understood to include monovalent monocyclic, bicyclic or tricyclic aromatic ring systems having 5, 6, 7, 8, 9, 10, 11, 12, 13 or 14 ring atoms, in particular 5 or 6 or 9 or 10 carbon atoms, and containing 1 to 5, preferably 1 to 3, heteroatoms each independently selected from N, O and S and, in each case, may be benzofused. "Heteroaryl" also refers to a radical in which a heteroaromatic ring is fused to one, two or more aryl, alicyclic or heterocyclyl rings, wherein the radical or point of attachment is on the heteroaromatic ring. Non-limiting examples of the term heteroaryl include, for example, pyridyl, pyrazinyl, furanyl, thienyl, pyrimidinyl, isoxazolyl, isothiazolyl, oxazolyl, thiazolyl, pyrazolyl, furazanyl, pyrrolyl, pyrazolyl, triazolyl, tetrazolyl, 1,2,and 1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-indolizinyl, 1-, 3-, 4-, 5-, 6-, or 7-isoindolyl, 2-, 3-, 4-, 5-, 6-, or 7-indolyl, 2-, 3-, 4-, 5-, 6-, or 7-indazolyl, 2-, 4-, 5-, 6-, 7-, or 8-purinyl, 1-, 2-, 3-, 4-, 6-, 7-, 8-, or 9-quinolizinyl, 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl, 1-, 3-, 4-, 5-, 6-, 7-, or 8-isoquinolyl, 1-, 4-, 5-, 6-, 7-, or 8-phthalazinyl, 2-, 3-, 4-, 5-, or 6-naphthyridinyl, 2- , 3-, 5-, 6-, 7-, or 8-quinazolinyl, 3-, 4-, 5-, 6-, 7-, or 8-cinnolinyl, 2-, 4-, 6-, or 7-pteridinyl, 1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-4aHcarbazolyl, 1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-carbazolylcarbazolyl, 1-, 3-, 4-, 5-, 6-, 7-, 8-, or 9-carbolinyl, 1-, 2-, 3-, 4-, 6-, 7-, 8-, 9-, or 10-phenanthridinyl, 1-, 2-, 3-, 4 1-, 2-, 3-, 4-, 6-, 7-, 8-, or 9-phenanthroline, 1-, 2-, 3-, 4-, 6-, 7-, 8-, or 9-phenanthroline, 1-, 2-, 3-, 4-, 6-, 7-, 8-, or 9-phenanthroline, 1-, 2-, 3-, 4-, 6-, 7-, 8-, 9-, or 10-phenothiazinyl, 1-, 2-, 3-, 4-, 6-, 7-, 8-, 9-, or 10-phenanthroline, 2-, 3-, 4-, 5-, 6-, 7-, 8-, or 9-phenanthroline, 1-, 3-, 4-, 5-, 6-, 7-, 8-, 9-, or 10-benzoisoquinolyl, 2-, 3-, 4-, or thieno[2,3-b]furanyl, 2-, 3-, 5-, 6-, 7-, 8-, 9-, 10-, or 11-7H-pyrazino[2,3-c]carbazolyl, 2-, 3-, 5-, 6-, or 7-2H-furo[3,2-b]pyranyl, 2-, 3-, 4-, 5-, 7-, or 8-5H-pyrido[2,3-d]-o-oxazinyl, 1-, 3-, or 5-1H-pyrazolo[4,3 -d]-thiazolyl, 2-, 4- or 5-1H-imidazo[4,5-d]thiazolyl, 3-, 5- or 8-pyrazino[2,3-d]pyridazinyl, 2-, 3-, 5- or 6-imidazo[2,1-b]thiazolyl, 1-, 3-, 6-, 7-, 8- or 9-furo[3,4-c]cinnolinyl, 1-, 2-, 3-, 4-, 5-, 6-, 8-, 9-, 10 or 11-4H-pyrido[2,3-c]carbazolyl, 2-, 3-, 6- or 7-imidazo[1,2-b][1,2,4-, 5-, 6-, 7-, 8-, or 9-benzoxapinyl, 2-, 4-, 5-, 6-, 7-, or 8-benzoxazinyl, 1-, 2-, 3-, 5-, 6-, 7-, 8-, 9-, 10-, or 11-1H-pyrrolo[1,2-b][2]benzazepinyl. Typical fused heteroaryl groups include, but are not limited to, 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl, 1-, 3-, 4-, 5-, 6-, 7-, or 8-isoquinolyl, 2-, 3-, 4-, 5-, 6-, or 7-indolyl, 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thienyl, 2-, 4-, 5-, 6-, or 7-benzoxazolyl, 2-, 4-, 5-, 6-, or 7-benzimidazolyl, and 2-, 4-, 5-, 6-, or 7-benzothiazolyl. When the 5- to 20-membered heteroaryl group is linked to other groups to form the compounds of the present disclosure, it can be a carbon atom on the 5- to 20-membered heteroaryl ring linked to the other groups, or it can be a heteroatom on the 5- to 20-membered heteroaryl ring linked to the other groups. When the 5- to 20-membered heteroaryl group is substituted, it can be monosubstituted or polysubstituted. Furthermore, there is no limitation on the substitution site, for example, a hydrogen atom connected to a carbon atom on a heteroaryl ring may be substituted, or a hydrogen atom connected to a heteroatom on a heteroaryl ring may be substituted.

[0450] The term "spirocyclic" refers to a ring system in which two rings share one ring atom.

[0451] The term "fused ring" refers to a ring system in which two rings share two ring atoms.

[0452] The term "bridged ring" refers to a ring system in which two rings share three or more ring atoms.

[0453] Unless otherwise specified, heterocyclyl, 5-20 membered heteroaryl or heteroarylene includes all possible isomeric forms thereof, such as positional isomers thereof. Thus, for some illustrative non-limiting examples, 1-, 2-, 3-, 4-, 5-, 6-, 7-, 8-, 9-, 10-, 11-, 12-positions, etc. (if present) may include 1, 2 or more substituted or bonded to other groups, including pyridin-2-yl, pyridin-2-ylene, pyridin-3-yl, pyridin-3-ylene, pyridin-4-ylene and pyridin-4-ylene; thienyl or thienylene includes thien-2-yl, thien-2-ylene, thien-3-ylene and thien-3-ylene; pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl.

[0454] The term "oxo (=O)" refers to the replacement of hydrogen or lone electron pairs on non-oxygen atoms with oxygen, for example, After being oxygenated After being oxygenated

[0455] Unless otherwise stated, the definitions of terms herein also apply to groups containing the term, e.g. 1-6 The definition of alkyl also applies to C 1-6 Alkyloxy, C 3-8 Cycloalkyl-C 1-6 Alkyl- etc.

[0456] In the context of this disclosure, "-", "--", "---" or " All are intended to mark the chemical bonds for attachment of the substituents;

[0457] Those skilled in the art will appreciate that the compounds of Formula I may exist in the form of various pharmaceutically acceptable salts. If these compounds have a basic center, they may form acid addition salts; if these compounds have an acidic center, they may form base addition salts; if these compounds contain both an acidic center (e.g., a carboxyl group) and a basic center (e.g., an amino group), they may also form internal salts.

[0458] The compounds of the present disclosure may exist in the form of solvates (e.g., hydrates), wherein the compounds of the present disclosure contain a polar solvent, such as water, methanol, or ethanol, as a structural element of the crystal lattice of the compound. The amount of the polar solvent, particularly water, may be present in a stoichiometric or non-stoichiometric ratio.

[0459] As used herein, the term "pharmaceutically acceptable" refers to a substance (such as a carrier or diluent) that does not affect the biological activity or properties of the compounds of the present invention and is relatively non-toxic, that is, the substance can be administered to a subject without causing an adverse biological response or interacting in an adverse manner with any components contained in the composition.

[0460] It will be appreciated by those skilled in the art that the compounds of the present disclosure may exist in the form of various pharmaceutically acceptable salts. If these compounds have a basic center, they may form acid addition salts; if these compounds have an acidic center, they may form base addition salts; if these compounds contain both an acidic center (e.g., a carboxyl group) and a basic center (e.g., an amino group), they may also form internal salts.

[0461] The term "tautomer" refers to functional group isomers resulting from the rapid shift of an atom between two positions in a molecule. Compounds of the present disclosure may exhibit tautomerism. Tautomeric compounds may exist as two or more interconvertible species. Prototropic tautomers arise from the migration of a covalently bonded hydrogen atom between two atoms. Tautomers generally exist in equilibrium, and attempts to isolate a single tautomer usually result in a mixture whose physical and chemical properties are consistent with a mixture of compounds. The position of equilibrium depends on the chemical properties within the molecule. For example, in many aliphatic aldehydes and ketones such as acetaldehyde, the keto form predominates, while in phenols, the enol form predominates. The present disclosure encompasses all tautomeric forms of the compounds.

[0462] Depending on their molecular structure, the compounds of the present invention may be chiral and therefore may exist in various enantiomeric forms. Thus, these compounds may exist in racemic or optically active forms. The compounds of the present invention encompass isomers or mixtures thereof, racemates, in which each chiral carbon is in the R or S configuration. The compounds of the present invention or the intermediates can be separated into enantiomeric compounds by chemical or physical methods well known to those skilled in the art, or used in this form for synthesis. In the case of racemic amines, diastereomers are prepared from the mixture by reaction with an optically active resolving agent. Examples of suitable resolving agents are optically active acids, such as R and S forms of tartaric acid, diacetyltartaric acid, dibenzoyltartaric acid, mandelic acid, malic acid, lactic acid, suitable N-protected amino acids (e.g., N-benzoylproline or N-phenylsulfonylproline) or various optically active camphorsulfonic acids. Chromatographic enantiomer resolution can also be advantageously performed with the aid of optically active resolving agents (e.g., dinitrobenzoylphenylglycine, cellulose triacetate, or other carbohydrate derivatives or chirally derivatized methacrylate polymers immobilized on silica gel). Suitable eluents for this purpose are aqueous or alcoholic solvent mixtures, for example, hexane / isopropanol / acetonitrile. The corresponding stable isomers can be separated according to known methods, for example, by extraction, filtration, or column chromatography.

[0463] "Isotopes" are all isotopes of atoms that occur in the compounds of the present invention. Isotopes include those atoms having the same atomic number but different mass numbers. Examples of isotopes suitable for incorporation into the compounds of the present invention are hydrogen, carbon, nitrogen, oxygen, phosphorus, fluorine, and chlorine, such as, but not limited to, 2 H. 3 H. 13 C. 14 C. 15 N. 18 O. 31 P. 32 P. 35 S. 18 F and 36C1. Isotopically labeled compounds of the present invention can generally be prepared by conventional techniques known to those skilled in the art, or by methods analogous to those described in the accompanying Examples, using appropriate isotopically labeled reagents in place of non-isotopically labeled reagents. Such compounds have a variety of potential uses, for example, as standards and reagents in assays for biological activity. In the case of stable isotopes, such compounds have the potential to favorably alter biological, pharmacological, or pharmacokinetic properties.

[0464] The term "prodrug" refers to a compound of the present disclosure that can be converted to biologically active compounds under physiological conditions or by solvolysis. Prodrugs of the present disclosure are prepared by modifying functional groups within the compound. These modifications can be removed by conventional procedures or in vivo to yield the parent compound. Prodrugs include compounds in which a hydroxyl group or an amino group within a compound of the present disclosure is linked to any group. When a prodrug of a compound of the present disclosure is administered to a mammalian subject, the prodrug is cleaved to form free hydroxyl groups and free amino groups, respectively.

[0465] The term "patient" refers to any animal including mammals, preferably mice, rats, other rodents, rabbits, dogs, cats, pigs, cows, sheep, horses or primates, and most preferably humans.

[0466] The term "therapeutically effective amount" refers to that amount of an active compound or drug that will elicit the biological or medical response that a researcher, veterinarian, physician, or other clinician is seeking in a tissue, system, animal, individual, or human, and includes one or more of the following: (1) prevents disease, e.g., prevents a disease, disorder, or condition in an individual who is susceptible to the disease, disorder, or condition but who is not yet experiencing or developing the pathology or symptoms of the disease. (2) inhibits disease, e.g., inhibits the disease, disorder, or condition (i.e., prevents further development of the pathology and / or symptoms) in an individual who is experiencing or developing the pathology or symptoms of the disease, disorder, or condition. (3) alleviates disease, e.g., alleviates the disease, disorder, or condition (i.e., reverses the pathology and / or symptoms) in an individual who is experiencing or developing the pathology or symptoms of the disease, disorder, or condition. DETAILED DESCRIPTION

[0467] The technical solutions of the present disclosure will be further described in detail below with reference to specific embodiments. It should be understood that the following embodiments are merely illustrative and explanations of the present disclosure and should not be construed as limiting the scope of protection of the present disclosure. All technologies implemented based on the above content of the present disclosure are included within the scope of protection intended by the present disclosure.

[0468] Unless otherwise specified, the raw materials and reagents used in the following examples are commercially available or can be prepared by known methods.

[0469] Abbreviations DMF: N,N-dimethylformamide DCM: dichloromethane DIEA: N,N-diisopropylethylamine TEA: triethylamine PE: petroleum ether EA: ethyl acetate MeCN: acetonitrile Et2O: diethyl ether DMSO: dimethyl sulfoxide EtOAc: ethyl acetate THF: tetrahydrofuran TFA: trifluoroacetic acid MeOH: methanol EtOH: ethanol NaH: sodium hydride MeI: iodomethane EtI: ethyl iodide HFP: 1,1,1,3,3,3-hexafluoro-2-propanol DHP: 3,4-dihydro-2H-pyran PPTS: 4-methylbenzenesulfonic acid pyridine PPh3: triphenylphosphine DEAD: diethyl azodicarboxylate MsCl: methanesulfonyl chloride TMSOTf: trimethylsilyl trifluoromethanesulfonate m-CPBA: m-chloroperbenzoic acid

[0470] Analytical methods

[0471] 1. Nuclear magnetic resonance (NMR) spectra were recorded on a 400 MHz British AVANCE 500 instrument. Chemical shifts are reported in ppm using tritiated residual solvent as the internal standard. Peak magnifications are indicated as follows: s, singlet; d, doublet; dd, doublet of doublet; t, triplet; dt, triplet of doublet; q, quartet; m, multiplet; br s, broad singlet.

[0472] 2. Purity analysis of samples was performed on a Waters HPLC / Waters MS system.

[0473] Chromatographic conditions 1:

[0474] Chromatographic column Waters X-Bridge-C18 50mm*4.6mm*3.5μm

[0475] The column temperature was 40°C.

[0476] Sample temperature: room temperature

[0477] Detection of UV 214 nm, UV 254 nm

[0478] Flow rate: 2 mL / min: 2 mL / minute.

[0479] Mobile phase A: water (0.05% TFA)

[0480] Mobile phase B: MeCN (0.05% TFA)

[0481] Gradient program: B from 5% to 100% in 1.6 min, hold at 100% for 1.4 min.

[0482] Chromatographic condition 2:

[0483] Chromatographic column: Waters X Brdige C18 Waters X Brdige C18: 4.6mm*50mm*3.5μm

[0484] The column temperature was 40°C.

[0485] Sample temperature: room temperature

[0486] Detection of UV 214 nm, UV 254 nm

[0487] Flow rate: 2 mL / min.

[0488] Mobile phase A: water (0.01 mol / L NH4HCO3) B: MeCN

[0489] Mobile phase B: MeCN

[0490] Gradient program: B from 5% to 100% in 1.6 min, hold at 100% for 1.4 min.

[0491] 3. Preparative HPLC was performed on a Gilson 281.

[0492] Flow rate: 20 mL / min: 20 mL / min.

[0493] Chromatographic column: X-Select 10μm 19X-Select 10μm 19*250mm chromatographic column

[0494] Wavelength: 254nM or 214nM

[0495] Solvent A: water (10 mM NH4HCO3) and solvent B: MeCN.

[0496] Example 1: Synthesis Example

[0497] 1. Synthesis scheme:

[0498] 2. Experimental part:

[0499] 2.1

[0500] (S)-tert-Butyl 4-(5-chloropyrimidin-2-yl)-3-(cyanomethyl)piperazine-1-carboxylate (02010-1)

[0501] To a solution of 2,5-dichloropyrimidine (66 mg, 0.671 mmol) and DIEA (346.4 mg, 2.685 mmol) in NMP (3 mL) at room temperature was added tert-butyl 3-(cyanomethyl)piperazine-1-carboxylate (100 mg, 0.671 mmol). The mixture was then stirred at 100°C overnight, water (10 mL) was added, and the mixture was extracted twice with DCM (10 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0 / 1 to 1 / 4, silica gel-CS 12 g, 30 mL / min, silica gel, UV 254) to give the product as a yellow solid (46 mg, 30.7% yield).

[0502] ESI-MS m / z calcd for [C 15 H 20 ClN5O2][M-56+H] + :282.1; found:282.2

[0503] 2.2

[0504] 2-((S)-1-(5-chloropyrimidin-2-yl)-4-((R)-4-((1-(hydroxymethyl)cyclobutyl)amino)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperazin-2-yl)acetonitrile (MX02010)

[0505] A solution of (S)-tert-butyl 4-(5-chloropyrimidin-2-yl)-3-(cyanomethyl)piperazine-1-carboxylate (60 mg, 0.178 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (51 mg, 0.178 mmol) in HFP (3 mL) was stirred at 120 °C under microwave conditions for 2 h. Water (10 mL) was then added to the mixture, and the mixture was extracted twice with DCM (10 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered and concentrated, and the crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give a white solid compound (16.6 mg, yield 19.1%).

[0506] ESI-MS m / z calcd for [C 21 H 25 ClN8O2S][M+H] +:489.2; found:489.0

[0507] 1 H NMR (400MHz, DMSO-d6) δ8.53(s,2H),7.49(s,1H),5.11(s,1H),4.82(t,J=5.2Hz,1H),4.61–4.47(m,3H),3.76–3.68(m, 2H),3.46–3.35(m,1H),3.30–3.16(m,2H),3.10–3.05(m,1H),2.98–2.80(m,4H),2.46–2.20(m,5H),1.82–1.71(m,2H),

[0508] 1. Synthesis scheme:

[0509] 2. Experimental part:

[0510] 2.1

[0511] Tert-Butyl 3-((5-chloropyrimidin-2-yl)oxy)azetidine-1-carboxylate (02019-1)

[0512] To a solution of tert-butyl 3-hydroxyazetidine-1-carboxylate (500 mg, 2.89 mmol) in THF (8 mL) was added 2,5-dichloropyrimidine (430 mg, 2.89 mmol) and t-BuOK (647 mg, 5.78 mmol). The mixture was stirred at 65 ° C under nitrogen for 2 hours. After the starting material was consumed, the reaction was quenched with water (20 mL) and extracted three times with EA (50 mL). The combined organic layers were washed with saturated brine (50 mL), dried over anhydrous sodium sulfate, filtered and concentrated. The crude product was purified by column chromatography (EA / PE = 0 / 1 to 1 / 1, silica gel-CS 20 g, 30 mL / min, silica gel, UV 254) to give a white solid product (360 mg, 44% yield).

[0513] ESI-MS m / z calcd for [C 12 H 16 ClN3O3][M-56+H] + :230.1;found:230.1

[0514] 2.2 2-(Azetidine-3-oxy)-5-chloropyrimidine (02019-2)

[0515] To a solution of tert-butyl 3-((5-chloropyrimidin-2-yl)oxy)azetidine-1-carboxylate (360 mg, 1.26 mmol) in DCM (10 mL) was added TFA (1 mL). The mixture was stirred at room temperature under nitrogen for 3 hours. After the reaction was complete, the mixture was distilled under reduced pressure to remove the solvent to give the product as a white solid (212 mg, 91% yield).

[0516] ESI-MS m / z calcd for[C7H8ClN3O][M+H] + :186.0;found:186.3

[0517] 2.3(R)-2-(3-((5-chloropyrimidin-2-yl)oxy)azetidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02019)

[0518] To a solution of 2-(azetidine-3-oxy)-5-chloropyrimidine (100 mg, 0.54 mmol) in 1,4-dioxane (4 mL) was added (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (155 mg, 0.54 mmol) and DIEA (209 mg, 1.62 mmol). The mixture was stirred at 120°C under a nitrogen atmosphere for 25 minutes in a microwave oven. After completion of the reaction, the solvent was removed by distillation under reduced pressure, and the crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / LNH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to afford the product as a white solid (36.80 mg, 16% yield).

[0519] ESI-MS m / z calcd for [C 18 H 21 ClN6O3S][M+H] + :437.1; found:437.0

[0520] 1H NMR (400MHz, DMSO-d6) δ8.76(s,2H),7.49(s,1H),5.43–5.38(m,1H),4.86(t,J=5.6Hz,1H),4.42(dd,J=10.0,6.4Hz,2H),4.00(d,J=7.2Hz ,2H),3.73–3.66(m,2H),3.45–3.37(m,1H),3.25–3.17(m,1H),2.97– 2.85(m,2H),2.38–2.25(m,2H),2.14–2.10(m,2H),1.82–1.68(m,2H).

[0521] 1. Synthesis scheme:

[0522] 2. Experimental part:

[0523] 2.1

[0524] tert-Butyl 5-(5-chloropyrimidin-2-yl)-2,5-diazabicyclo[4.1.0]heptane-2-carboxylate (02020-1)

[0525] To a solution of tert-butyl 2,5-diazabicyclo[4.1.0]heptane-2-carboxylate (100 mg, 0.51 mmol) in DMF (3 mL) were added 2,5-dichloropyrimidine (76 mg, 0.51 mmol) and K2CO3 (211 mg, 1.53 mmol). The mixture was stirred at 100°C under nitrogen for 1 hour. Water (20 mL) was added to the mixture, and the mixture was extracted three times with EA (30 mL). The combined organic layers were washed with saturated brine (30 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0 / 1 to 1 / 1, silica gel-CS 20 g, 30 mL / min, silica gel, UV 254) to give the product as a white solid (140 mg, 90% yield).

[0526] ESI-MS m / z calcd for [C 14 H 19 ClN4O2][M-56+H] + :255.1; found:255.2

[0527] 2.2

[0528] 2-(5-chloropyrimidin-2-yl)-2,5-diazabicyclo[4.1.0]heptane (02020-2)

[0529] To a solution of tert-butyl 5-(5-chloropyrimidin-2-yl)-2,5-diazabicyclo[4.1.0]heptane-2-carboxylate (140 mg, 0.45 mmol) in DCM (5 mL) was added TFA (0.5 mL). The reaction mixture was stirred at room temperature under nitrogen for 3 hours. After the starting material was consumed, the mixture was concentrated to dryness by distillation under reduced pressure to give a white solid product (90 mg, 95% yield).

[0530] ESI-MS m / z calcd for [C9H 11 ClN4][M+H] + :211.1; found:211.3

[0531] 2.3

[0532] (5R)-2-(5-(5-chloropyrimidin-2-yl)-2,5-diazabicyclo[4.1.0]heptan-2-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02020)

[0533] To a solution of 2-(5-chloropyrimidin-2-yl)-2,5-diazabicyclo[4.1.0]heptane (90 mg, 0.43 mmol) in 1,4-dioxane (4 mL) was added (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (123 mg, 0.43 mmol) and DIEA (165 mg, 1.28 mmol). The mixture was stirred in a microwave oven at 120°C under nitrogen for 25 minutes. After the starting material was consumed, the solvent was removed by concentration under reduced pressure. The crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to afford the product as a white solid (19.09 mg, 10% yield).

[0534] ESI-MS m / z calcd for [C 20 H 24 ClN7O2S][M+H] + :462.1;found:462.0

[0535] 1H NMR(400MHz, DMSO-d6)δ8.51(s,2H),7.47–7.46(m,1H),4.84(t,J=6.0Hz,1H),3.98–3.53(m,7H),3.45–3.41(m,2H),3.26–3.19(m,1H) ,3.00–2.96(m,1H),2.91–2.86(m,1H),2.39–2.33(m,2H),2.18–2.17(m,2H),1.83–1.70(m,2H),1.16–1.15(m,1H),0.42–0.36(m,1H),.

[0536] 1. Synthesis scheme:

[0537] 2. Experimental part:

[0538] 2.1

[0539] Tert-Butyl 4-(5-chloropyrimidin-2-yl)-4,7-diazaspiro[2.5]octane-7-carboxylate (02021-1)

[0540] A mixture of 2,5-dichloropyrimidine (200 mg, 1.34 mmol), tert-butyl 4,7-diazaspiro[2.5]octane-7-carboxylate (711 mg, 3.35 mmol), and DIEA (1.1 mL, 6.7 mmol) in n-butanol (10 mL) was stirred at 150°C under argon protection in a microwave oven for 2 hours. After cooling, the solvent was removed by distillation under reduced pressure. The crude product was purified by column chromatography (EA / PE = 0-1 / 19, Silica Gel-CS 40 g, 40 mL / min, silica gel, UV 254) to afford the product as a colorless oil (71 mg, 16.3% yield).

[0541] ESI-MS m / z calcd for [C 15 H 21 ClN4O2][M-56+H] + :269.1; found:268.9

[0542] 2.2

[0543] (R)-2-(4-(5-chloropyrimidin-2-yl)-4,7-diazaspiro[2.5]octan-7-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02021)

[0544] A solution of tert-butyl 4-(5-chloropyrimidin-2-yl)-4,7-diazaspiro[2.5]octane-7-carboxylate (44 mg, 0.11 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (32 mg, 0.11 mmol) in HFP (3 mL) was stirred at 120° C. under microwave conditions for 2 hours. After the mixture was cooled, the solvent was distilled off under reduced pressure. The crude product was purified by reverse phase column (MeCN / H2O=0~12 / 13, C-18 column, 50mL / min, UV 214) to give a crude product (20 mg), and then the crude product was purified by preparative HPLC [MeCN / H2O (10mmol / L NH4HCO3), X-Select 10μm 19*250mm, 20mL / min, UV 254] to give a white solid product (11.48 mg, yield 17.8%).

[0545] ESI-MS m / z calcd for [C 21 H 26 ClN7O2S][M+H] + :476.2; found:475.8

[0546] 1 H NMR(400MHz, DMSO-d6)δ8.52(s,2H),7.41–7.38(m,1H),4.85(t,J=5.6Hz,1H),3.95–3.93(m,2H),3.83–3.66(m,6H) ,3.40–3.37(m,1H),3.24–3.16(m,1H),2.95–2.83(m,2H),2.33–2.12(m,4H),1.77–1.73(m,2H),0.95–0.89(m,4H).

[0547] 1. Synthesis scheme:

[0548] 2. Experimental part:

[0549] 2.1

[0550] 5-Iodo-1-(triisopropylsilyl)-1H-indole (02024-1)

[0551] A solution of 5-iodo-1H-indole (1.7 g, 6.99 mmol) in anhydrous THF (20 mL) was added dropwise to a solution of NaH (60%, 364 mg, 9.09 mmol) in THF (20 mL) at 0°C. The mixture was slowly warmed to room temperature over 30 minutes. Triisopropylsilyl chloride (1.75 g, 9.09 mmol) was then added dropwise over 5 minutes. The resulting mixture was slowly warmed to room temperature and stirred until the starting material was consumed as monitored by TLC. After completion, the reaction was quenched with saturated aqueous NH4Cl (20 mL) at 0°C and extracted three times with Et2O (15 mL). The combined organic phases were dried over anhydrous magnesium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0-10%, Silica Gel-CS 40 g, 50 mL / min, silica gel, UV 254) to afford the product as a colorless oil (2.1 g, 75.17% yield).

[0552] ESI-MS m / z calcd for [C 17 H 26 INSi]

[0553] 1 H NMR(400MHz,Chloroform-d)δ7.95(d,J=1.6Hz,1H),7.38(dd,J=8.4,1.6Hz,1H),7.29–7.26 (m,1H),7.20(d,J=3.2Hz,1H),6.54(d,J=2.8Hz,1H),1.71–1.63(m,3H),1.14–1.12(m,18H).

[0554] 2.2

[0555] Tert-Butyl 3-(1-(triisopropylsilyl)-1H-indol-5-yl)azetidine-1-carboxylate (02024-2)

[0556] Under nitrogen atmosphere, a solution of zinc powder (327 mg, 5.01 mmol) in DMA (1.6 mL) was vigorously stirred and heated to 65 ° C. Subsequently, TMSCl (65 mg, 0.6 mmol) and dibromoethane (113 mg, 0.6 mmol) were added, and the mixture was stirred for another 30 minutes at 65 ° C. At 65 ° C, a solution of tert-butyl 3-iodine azetidine-1-formate (851 mg, 3.0 mmol) in DMA (2 mL) was added dropwise to the solution prepared above, and the reaction mixture was then cooled to room temperature and a solution of 5-iodine-1-(triisopropylsilyl)-1H-indole (800 mg, 2.0 mmol) in DMA (4 mL) was added. Subsequently, Pd (dppf) Cl 2 (44 mg, 0.06 mmol) and CuI (23 mg, 0.12 mmol) were added. The reaction mixture was heated to 80° C. and stirred for 2 hours. The mixture was cooled to room temperature and quenched with water (150 mL). NH4Cl (2 g) was then added and the mixture was extracted twice with Et2O (150 mL). The combined organic layers were dried over anhydrous sodium sulfate, filtered and concentrated. The crude product was purified by column chromatography (EA / PE=0-10%, silica gel-CS 40 g, 50 mL / min, silica gel, UV 254) to give the product as a white solid (0.7 g, 81.52% yield).

[0557] ESI-MS m / z calcd for [C 25 H 40 N2O2Si][M+H] + :429.3; found:429.2

[0558] 2.3

[0559] Tert-Butyl 3-(1H-indol-5-yl)azetidine-1-carboxylate (02024-3)

[0560] To a solution of tert-butyl 3-(1-(triisopropylsilyl)-1H-indol-5-yl)azetidine-1-carboxylate (0.7 g, 1.64 mmol) in THF (10 mL) was added TBAF (1 M in THF, 3.27 mL). The mixture was stirred at room temperature for 2 hours, quenched with water (30 mL), and then extracted twice with EA (30 mL). The combined organic layers were dried over anhydrous magnesium sulfate, filtered and concentrated, and the crude product was purified by column chromatography (EA / PE = 0-30%, silica gel-CS25 g, 30 mL / min, silica gel, UV 254) to give the product as a white solid (401 mg, 90.03% yield).

[0561] ESI-MS m / z calcd for [C 16H 20 N2O2][M-56+H] + :217.2;found:217.2

[0562] 2.4

[0563] (R)-2-(3-(1H-indol-5-yl)azetidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02024)

[0564] A mixture of tert-butyl 3-(1H-indol-5-yl)azetidine-1-carboxylate (100 mg, 0.37 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (104 mg, 0.37 mmol) in HFP (3 mL) was stirred at 120° C. under microwave conditions for 2 hours. After completion of the reaction, the mixture was distilled under reduced pressure to remove the solvent, and the crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give the product as a white solid (58 mg, 37.3% yield).

[0565] ESI-MS m / z calcd for [C 22 H 25 N5O2S][M+H] + :424.2; found:424.0

[0566] 1 H NMR(400MHz,DMSO-d6)δ11.05(s,1H),7.50(s,1H),7.41–7.37(m,2H),7.32(t,J =2.8Hz,1H),7.09(d,J=8.4Hz,1H),6.39(s,1H),4.88(t,J=5.6Hz,1H),4.46–4.4 2(m,2H),4.03–3.94(m,3H),3.71–3.70(m,2H),3.44–3.38(m,1H),3.26–3.18(m, 1H),2.98–2.85(m,2H),2.39–2.31(m,2H),2.15–2.10(m,2H),1.80–1.70(m,2H).

[0567] 1. Synthesis scheme:

[0568] 2. Experimental part:

[0569] 2.1

[0570] (R)-tert-Butyl 3-((1H-indol-6-yl)oxy)pyrrolidine-1-carboxylate (02025-1)

[0571] To a solution of 1H-indol-6-ol (171 mg, 1.284 mmol) and tert-butyl (S)-3-hydroxypyrrolidine-1-carboxylate (200 mg, 1.07 mmol) in 1,4-dioxane (20 mL) was added CMBP (0.75 mL, 3.21 mmol). The mixture was stirred at 100°C under argon overnight. After cooling, the solvent was removed by distillation under reduced pressure. The crude product was purified by reverse phase column chromatography (MeCN / H2O = 1 / 9 to 11 / 9, C-18 column, 50 mL / min, UV 214) to obtain the product as a brown oil (322 mg, 99.7% yield).

[0572] ESI-MS m / z calcd for [C 17 H 22 N2O3][M-56+H] + :247.2;found:247.0

[0573] 2.2

[0574] (R)-6-(Pyrrolidin-3-oxy)-1H-indole (02025-2)

[0575] A solution of (R)-tert-butyl 3-((1H-indol-6-yl)oxy)pyrrolidine-1-carboxylate (200 mg, 0.66 mmol) in HFP (5 mL) was stirred at 120° C. under argon protection in a microwave oven for 10 hours. After the mixture was cooled, the solvent was removed by distillation under reduced pressure to obtain a brown oily crude product (133 mg, 99.4% yield), which was used directly in the next reaction.

[0576] ESI-MS m / z calcd for [C 12 H 14 N2O][M+H] + :203.1; found:203.2

[0577] 2.3

[0578] (R)-2-((R)-3-((1H-indol-6-yl)oxy)pyrrolidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02025)

[0579] To a solution of (R)-6-(pyrrolidin-3-oxy)-1H-indole (44 mg, 0.22 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (63 mg, 0.22 mmol) in DMF (10 mL) was added DIEA (0.18 mL, 1.1 mmol). The mixture was then stirred at 80°C overnight under argon. After cooling, the solvent was removed by distillation under reduced pressure. The crude product was purified by column chromatography (MeOH / DCM = 0-1 / 9, Silica Gel-CS 20 g, 20 mL / min, UV 254) to give a crude product (50 mg). The crude product was then purified by preparative HPLC [MeCN / H2O (10 mmol / LNH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give a white solid product (33.02 mg, yield 33.5%).

[0580] ESI-MS m / z calcd for [C 23 H 27 N5O3S][M+H] + :454.2; found:454.0

[0581] 1 H NMR (400MHz, DMSO-d6) δ10.88(s,1H),7.41(d,J=8.4Hz,1H),7.30(d,J=7.2Hz,1H) ,7.20(s,1H),6.91(s,1H),6.66(d,J=8.8Hz,1H),6.33(s,1H),5.08(s,1H),4.89– 4.84(m,1H),3.81–3.69(m,5H),3.60–3.51(m,1H),3.46–3.37(m,1H),3.25–3.15( m,1H),2.98–2.80(m,2H),2.41–2.29(m,2H),2.22–2.05(m,4H),1.81–1.66(m,2H).

[0582] 1. Synthesis scheme:

[0583] 2. Experimental part:

[0584] 2.1

[0585] tert-Butyl 5-(1-(tert-Butoxycarbonyl)-2,5-dihydro-1H-pyrrol-3-yl)-1H-indole-1-carboxylate (02026-1)

[0586] A reaction mixture of tert-butyl 5-bromo-1H-indole-1-carboxylate (1 g, 3.38 mmol), tert-butyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,5-dihydro-1H-pyrrole-1-carboxylate (1 g, 3.38 mmol), Pd(dppf)Cl2 (247 mg, 0.338 mmol), K2CO3 (1.4 g, 10.14 mmol), and water (16 mL) in 1,4-dioxane (80 mL) was stirred overnight at 100°C under argon protection. After cooling, the reaction mixture was distilled under reduced pressure to remove the solvent, and the crude product was purified by column chromatography (EA / PE = 0-1 / 9, silica gel-CS 40 g, 40 mL / min, silica gel, UV 254) to give the product as a white solid (960 mg, 73.9% yield).

[0587] ESI-MS m / z calcd for [C 22 H 28 N2O4][M-56+H] + :329.2; found:329.2

[0588] 2.2

[0589] tert-Butyl 5-(1-(tert-Butoxycarbonyl)pyrrolidin-3-yl)-1H-indole-1-carboxylate (02026-2)

[0590] To a solution of tert-butyl 5-(1-(tert-butoxycarbonyl)-2,5-dihydro-1H-pyrrol-3-yl)-1H-indole-1-carboxylate (300 mg, 0.34 mmol) in DCM (30 mL) and MeOH (75 mL) was added Pd(OH)2 (30 mg), and the mixture was stirred at room temperature for 12 minutes under a hydrogen atmosphere. After completion of the reaction, the mixture was filtered under reduced pressure, and the solvent was removed from the filtrate by distillation under reduced pressure. The crude product was purified by column chromatography (EA / PE = 0-1 / 9, silica gel-CS 20 g, 20 mL / min, silica gel, UV 254) to give the product as a colorless oil (260 mg, 86.2% yield).

[0591] ESI-MS m / z calcd for [C 22 H 30 N2O4][M-112+H] + :275.2;found:275.2

[0592] 2.3

[0593] 5-(Pyrrolidin-3-yl)-1H-indole (02026-3)

[0594] To a solution of tert-butyl 5-(1-(tert-butoxycarbonyl)pyrrolidin-3-yl)-1H-indole-1-carboxylate (248 mg, 0.64 mmol) in 1,4-dioxane (10 mL) was added a 4N (HCl) / 1,4-dioxane solution (10 mL) and stirred at room temperature overnight. After completion of the reaction, the mixture was distilled under reduced pressure to remove the solvent, and the crude product was neutralized with DIEA (10 mL) and concentrated by distillation under reduced pressure to yield a crude red solid (119 mg, 99.9% yield). This was used directly in the next reaction.

[0595] ESI-MS m / z calcd for [C 12 H 14 N2][M+H] + :187.1; found:187.4

[0596] 2.4

[0597] (5R)-2-(3-(1H-indol-5-yl)pyrrolidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02026)

[0598] To a solution of 5-(pyrrolidin-3-yl)-1H-indole (130 mg, 0.5 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (144 mg, 0.5 mmol) in 1,4-dioxane (10 mL) was added DIEA (0.41 mL, 2.5 mmol). The mixture was stirred at 120° C. under microwave conditions for 2 hours. After cooling, the mixture was distilled under reduced pressure to remove the solvent. The crude product was purified by column chromatography (MeOH / DCM=0-1 / 9, silica gel-CS20 g, 20 mL / min, UV 254) to give a crude product (50 mg). The crude product was then purified by preparative HPLC [MeCN / H2O (10 mmol / LNH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give a white solid product (4.69 mg, yield 2.1%).

[0599] ESI-MS m / z calcd for [C 23 H 27 N5O2S][M+H]+ :438.2; found:438.0

[0600] 1 H NMR (400MHz, DMSO-d6) δ11.03(s,1H),7.46(d,J=4.0Hz,1H),7.36–7.28(m,3H),7.05(d,J=8.4Hz,1H),6.37(s,1H),4.90–4.84(m,1H),4.05–3. 95(m,1H),3.82–3.67(m,3H),3.56–3.39(m,4H),3.24–3.17(m,1H),2.9 5–2.86(m,2H),2.46–2.27(m,3H),2.18–2.04(m,3H),1.79–1.66(m,2H).

[0601] 1. Synthesis scheme:

[0602] 2. Experimental part:

[0603] 2.1

[0604] 2-Chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one (02029-1)

[0605] To a solution of 2,4-dichloro-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one (23 mg, 0.105 mmol) in MeCN (4 mL) was added (1-aminocyclobutyl)methanol (11.7 mg, 0.115 mmol) and TEA (1 mL). The mixture was stirred at 70°C overnight and concentrated by distillation under reduced pressure. The crude product was purified by column chromatography (MeOH / DCM = 0-1 / 10, Silica Gel-CS 4 g, 20 mL / min, silica gel, UV 254) to give a yellow solid product (80% purity, 28.0 mg, 98.0% yield).

[0606] ESI-MS m / z calcd for [C 12 H 15 ClN4O2][M+H] + :283.1;found:283.1

[0607] 2.2

[0608] 2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one (MX02029)

[0609] A mixture of (2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one (purity 80%, 28.0 mg, 0.08 mmol) and tert-butyl 4-(5-chloropyrimidin-2-yl)piperidine-1-carboxylate (45 mg, 0.15 mmol) HFP (3 mL) was stirred at 120 ° C. for 2 hours under microwave conditions. The reaction mixture was concentrated by distillation under reduced pressure to remove the solvent, and the crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give a white solid product (2.0 mg, yield 4.55%).

[0610] ESI-MS m / z calcd for [C 21 H 26 ClN7O2][M+H] + :444.2; found:444.0

[0611] 1 H NMR (400MHz, DMSO-d6) δ9.07(s,1H),8.87(s,2H),7.43(s,1H),4.83(t,J=6.0Hz,1H),4.72(d,J=10.0Hz,2H),3.69(d,J=5.2Hz,2H),3.33–3.26(m, 2H),3.21–3.14(m,1H),3.05–2.99(m,2H),2.62(t,J=6.8Hz,2H),2.26–2 .11(m,4H),1.96(d,J=10.4Hz,2H),1.83–1.74(m,2H),1.67–1.59(m,2H),

[0612] 1. Synthesis scheme:

[0613] 2. Experimental part:

[0614] 2.1

[0615] (1-((2-chloropyrido[3,2-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (02035-1)

[0616] To a solution of (1-aminocyclobutyl)methanol (50.5 mg, 0.5 mmol) and DIEA (0.1 mL, 0.625 mmol) in THF (5 mL) was added dropwise a solution of 2,4-dichloropyrido[3,2-d]pyrimidine (100 mg, 0.5 mmol) in THF (15 mL) over 10 minutes. The resulting mixture was stirred at room temperature overnight under argon. After cooling, the reaction mixture was distilled under reduced pressure to remove the solvent. The crude product was purified by column chromatography (EA / PE = 0-1 / 1, silica gel-CS 20 g, 20 mL / min, silica gel, UV 254) to afford the product as a white solid (105 mg, 79.3% yield).

[0617] ESI-MS m / z calcd for [C 12 H 13 ClN4O][M+H] + :265.1;found:265.1

[0618] 2.2

[0619] (1-((2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)pyrido[3,2-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (MX02035)

[0620] To a solution of (1-((2-chloropyrido[3,2-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (68 mg, 0.32 mmol) and 5-chloro-2-(piperidin-4-yl)pyrimidine (92 mg, 0.32 mmol) in DMF (20 mL) was added DIEA (0.26 mL, 1.6 mmol), and the mixture was stirred at 80°C overnight under argon protection. After cooling, the mixture was distilled under reduced pressure to remove the solvent. The crude product was purified by column chromatography (MeOH / DCM=0-1 / 9, silica gel-CS20 g, 20 mL / min, UV 254) to give a crude product (100 mg). The crude product was then purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give a white solid product (73.60 mg, 49.6% yield).

[0621] ESI-MS m / z calcd for [C 21 H 24 ClN7O][M+H] + :426.2;found:426.0

[0622] 1H NMR (400MHz, DMSO-d6) δ8.86(s,2H),8.33(dd,J=4.4,1.6Hz,1H),7.65(dd,J=8.4,1.6Hz,1H),7.57–7.53(m,2H),4.99(t,J=5.6Hz,1H),4.83(d,J=12. 8Hz,2H),3.78(d,J=5.6Hz,2H),3.22–3.16(m,1H),3.10–3.04(m,2H),2.64 –2.56(m,2H),2.18–2.11(m,2H),1.99(d,J=10.4Hz,2H),1.88–1.65(m,4H).

[0623] 1. Synthesis scheme:

[0624] 2. Experimental part:

[0625] 2.1

[0626] tert-Butyl 2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (02036-1)

[0627] To a solution of tert-butyl 2,4-dichloro-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (660 mg, 2.17 mmol) in MeCN (15 mL) was added (1-aminocyclobutyl)methanol (219.5 mg, 2.17 mmol) and TEA (658.7 mg, 6.51 mmol). The mixture was heated to 70°C and stirred for 16 hours, cooled to room temperature and concentrated. The crude product was purified by column chromatography (EA / PE = 0-50%, silica gel-CS 40 g, 50 mL / min, silica gel, UV light 254) to give a white solid product (441 mg, 55.1% yield).

[0628] ESI-MS m / z calcd for [C 17 H 25 ClN4O3][M+H] + :369.2; found:369.0

[0629] 2.2

[0630] tert-Butyl 2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (02036-2)

[0631] To a solution of tert-butyl 2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (441 mg, 1.20 mmol) in DMF (15 mL) were added 5-chloro-2-(piperidin-4-yl)pyrimidine (378 mg, 1.91 mmol) and DIEA (309 mg, 2.39 mmol). The mixture was heated to 120°C and stirred for 16 hours, then cooled to room temperature and concentrated to dryness by distillation under reduced pressure. The crude product was purified by column chromatography (MeOH / DCM = 0-10%, silica gel-CS 25 g, 30 mL / min, UV 254) to give a white solid product (101 mg, 15.9% yield).

[0632] ESI-MS m / z calcd for [C 26 H 36 ClN7O3][M+H] + :530.3;found:530.0

[0633] 2.3

[0634] (1-((2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (MX02036)

[0635] A solution of tert-butyl 2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (20 mg, 0.04 mmol) in HFP (3 mL) was stirred at 120° C. under microwave conditions for 3.5 hours, then the mixture was cooled to room temperature and concentrated to dryness by distillation under reduced pressure. The crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / LNH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give the product as a white solid (3.6 mg, 18.0% yield).

[0636] ESI-MS m / z calcd for [C 21 H 28 ClN7O][M+H] + :430.2;found:430.0

[0637] 1H NMR (400MHz, DMSO-d6) δ8.85(s,2H),5.83(s,1H),4.78(t,J=5.6Hz,1H),4.61–4.58(m,2H),3.70(d,J=5.6Hz,2H),3.43(s,2H),3. 12–3.07(m,1H),2.90–2.85(m,4H),2.36–2.34(m,2H),2.25–2.10(m,5H),1.88–1.85(m,2H),1.77–1.74(m,2H),1.63–1.59(m,2H).

[0638] 1. Synthesis scheme:

[0639] 2. Experimental part:

[0640] 2.1

[0641] 1-(2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)prop-2-en-1-one (MX02037)

[0642] Acryloyl chloride (171 mg, 1.89 mmol) was added to a solution of (1-((2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (0.189 mmol, crude) in MeOH (5 mL). The mixture was stirred at room temperature for 16 hours and then concentrated to dryness by distillation under reduced pressure. The crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / LNH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give the product as a white solid (3.20 mg, 3.5% yield).

[0643] ESI-MS m / z calcd for [C 24 H 30 ClN7O2][M+H] + :484.2; found:484.0

[0644] 1H NMR(400MHz, DMSO-d6)δ8.85(s,2H),6.99–6.86(m,1H),6.34(d,J=11.6Hz,1H),6.17(dd,J =28.0,16.0Hz,1H),5.74(dd,J=24.8,11.2Hz,1H),4.78–4.73(m,1H),4.61(d,J=12.8Hz,2H ),4.34(d,J=14.4Hz,2H),3.75–3.72(m,4H),3.14–3.09(m,1H),2.90(t,J=12.0Hz,2H),2.5 9–2.57(m,1H),2.47–2.45(m,1H),2.33-2.17(m,4H),1.89–1.73(m,4H),1.64-1.56(m,2H).

[0645] 1. Synthesis scheme:

[0646] 2. Experimental part:

[0647] 2.1

[0648] tert-Butyl 2-(1-((Benzyloxy)carbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (02040-1)

[0649] A mixture of tert-butyl 2-chloro-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (300 mg, 1.11 mmol), benzyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate (381 mg, 1.11 mmol), Pd(dppf)Cl2 (81 mg, 0.111 mmol), K2CO3 (460 mg, 3.33 mmol) and water (0.8 mL) in 1,4-dioxane (4 mL) was stirred at 100 °C under argon protection overnight. After cooling, the reaction mixture was distilled under reduced pressure to remove the solvent, and the crude product was purified by column chromatography (EA / PE=0-1 / 3, silica gel-CS 40 g, 40 mL / min, silica gel, UV 254) to give a yellow oily product (501 mg, yield 99.9%).

[0650] ESI-MS m / z calcd for [C 25 H 30 N4O4][M-56+H] + :451.2; found:451.3

[0651] 2.2

[0652] tert-Butyl 2-(piperidin-4-yl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (02040-2)

[0653] To a solution of tert-butyl 2-(1-((benzyloxy)carbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (393 mg, 0.87 mmol) in EA (30 mL) was added Pd / C (80 mg). The mixture was stirred overnight under a hydrogen atmosphere at room temperature. After completion of the reaction, the mixture was filtered under reduced pressure, and the solvent was removed from the filtrate by distillation under reduced pressure. The crude product was purified by column chromatography (EA / PE = 0-1 / 3, silica gel-CS 40 g, 40 mL / min, silica gel, UV 254) to obtain the product as a colorless oil (277 mg, 99.7% yield).

[0654] ESI-MS m / z calcd for [C 17 H 26 N4O2][M+H] + :319.2; found:319.2

[0655] 2.3

[0656] (R)-tert-Butyl 2-(1-(4-((1-(hydroxymethyl)cyclobutyl)amino)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperidin-4-yl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (02040-3)

[0657] To a mixture of tert-butyl 2-(piperidin-4-yl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (277 mg, 0.87 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (280 mg, 0.87 mmol) in 1,4-dioxane (10 mL) was added DIEA (0.43 mL, 2.61 mmol), and the mixture was stirred under argon protection at 120°C in a microwave oven for 1 hour. After cooling, the mixture was distilled under reduced pressure to remove the solvent. The crude product was purified by column chromatography (MeOH / DCM = 0-1 / 9, Silica Gel-CS 20 g, 20 mL / min, UV 254) to afford the product as a yellow solid (495 mg, 99.9% yield).

[0658] ESI-MS m / z calcd for [C 28 H 39 N7O4S][M+H] + :570.3; found:569.8

[0659] 2.4

[0660] (R)-4-((1-(Hydroxymethyl)cyclobutyl)amino)-2-(4-(5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-yl)piperidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02040)

[0661] A mixture of (R)-tert-butyl 2-(1-(4-((1-(hydroxymethyl)cyclobutyl)amino)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperidin-4-yl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (150 mg, 0.26 mmol) in HFP (10 mL) was stirred under argon protection at 120°C under microwave conditions for 2 hours. After cooling, the mixture was distilled under reduced pressure to remove the solvent. The crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give the product as a white solid (49.00 mg, 39.6% yield).

[0662] ESI-MS m / z calcd for [C 23 H 31 N7O2S][M+H] + :470.2;found:470.0

[0663] 1 H NMR (400MHz, DMSO-d6) δ8.36 (s, 1H), 7.36 (s, 1H), 4.85 (t, J = 5.6Hz, 1H), 4. 71(d,J=12.4Hz,2H),3.79(s,2H),3.73–3.71(m,2H),3.45–3.37(m,1H),3.2 4–3.17(m,1H),3.09–2.83(m,8H),2.69(t,J=6.0Hz,2H),2.39–2.25(m,2H), 2.18–2.12(m,2H),1.91–1.88(m,2H),1.79–1.73(m,2H),1.65–1.61(m,2H).

[0664] 1. Synthesis scheme:

[0665] 2. Experimental part:

[0666] 2.1

[0667] (1-((2-Chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (02043-1)

[0668] To a solution of 2,4-dichloro-6,7-dihydrothieno[3,2-d]pyrimidine (6.641 g, 32.07 mmol) in MeCN (50 mL) were added (1-aminocyclobutyl)methanol (3.244 g, 32.07 mmol) and TEA (20 mL). The mixture was stirred at 75°C for 16 hours, and then the solvent was removed by distillation under reduced pressure. The crude product was purified by column chromatography (EA / DCM = 0-60%, Silica Gel-CS 120 g, 50 mL / min, silica gel, UV 254) to give the product as a yellow solid (4.01 g, 46.1% yield).

[0669] ESI-MS m / z calcd for [C 11 H 14 ClN3OS][M+H] + :272.1;found:272.1

[0670] 2.2

[0671] (R)-2-Chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (02043-2)

[0672] To a solution of (1-((2-chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (3.5 g, 12.88 mmol) and S-1,1'-bi-2-naphthol (369.0 mg, 1.288 mmol) in DCM (60 mL) were added titanium tetraisopropoxide (182.0 mg, 0.64 mmol) and water (232.0 mg, 12.88 mmol). After the mixture was stirred at room temperature for 1 hour, 70% aqueous tert-butyl hydroperoxide solution (2 g, 14.17 mmol) was added in one portion. The mixture was then stirred at room temperature for 2 hours, after which water (50 mL) was added and the mixture was extracted three times with DCM (60 mL). The combined organic layers were dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. The crude product was purified by column chromatography (DCM / MeOH=1 / 0-10 / 1, Silica-CS 80 g, 50 mL / min, silica gel, UV 254) to give a yellow solid product (3.50 g, yield 94.6%).

[0673] ESI-MS m / z calcd for [C 11 H 14 ClN3O2S][M+H] + :288.0;found:288.0

[0674] 1 H NMR(400MHz, DMSO-d6)δ8.62(s,1H),4.89(t,J=5.6Hz,1H),3.74–3.66(m,2H),3.61–3.52(m,1H) ,3.38–3.30(m,1H),3.16–3.12(m,1H),3.05–2.99(m,1H),2.32–2.17(m,4H),1.81–1.71(m,2H).

[0675] 2.3

[0676] (R)-2-(4,5-dihydro-2H-pyrazolo[3,4-c]pyridin-6(7H)-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02043)

[0677] To a solution of (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (57 mg, 0.2 mmol) in DMF (5 mL) was added 4,5,6,7-tetrahydro-2-hydro-pyrazolo[3,4-c]pyridine hydrochloride (38 mg, 0.24 mmol) and DIEA (1.5 mL). The reaction mixture was stirred at 80°C for 4 hours, and the solvent was removed by distillation under reduced pressure. The crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give the product as a white solid (20.0 mg, 26.9% yield).

[0678] ESI-MS m / z calcd for [C 17 H 22 N6O2S][M+H] + :375.2; found:375.0

[0679] 1 H NMR(400MHz,DMSO-d6)δ12.49(s,1H),7.47(s,1H),7.41(s,1H),4.88–4.83(m,3H),3.96(br,2H),3.78–3.71(m,2H),3.46–3.38(m,1H),3.24–3.1 6(m,1H),2.94(dd,J=16.8,8.0Hz,1H),2.86(dd,J=14.4,7.2Hz,1H),2.6 7–2.61(m,2H),2.40–2.27(m,2H),2.21–2.17(m,2H),1.82–1.74(m,2H).

[0680] 1. Synthesis scheme:

[0681] 2. Experimental part:

[0682] 2.1

[0683] tert-Butyl 2-chloro-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (02044-1)

[0684] To a solution of tert-butyl 2,4-dihydro-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (300 mg, 1.03 mmol) in MeOH (10 mL) and AcOH (1 mL) was added Zn powder (338 mg, 5.17 mmol). The mixture was then stirred at 50°C overnight, the solvent was distilled off under reduced pressure, water (20 mL) was added, and the mixture was extracted three times with DCM (20 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0 / 1 to 1 / 1, silica gel-CS 20 g, 40 mL / min, silica gel, UV 254) to give a yellow oily product (202.0 mg, yield 84.8%).

[0685] ESI-MS m / z calcd for [C 11 H 14 ClN3O2][M+H] + :256.1; found:256.2

[0686] 2.2

[0687] tert-Butyl 2-(1-((Benzyloxy)carbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (02044-2)

[0688] To a solution of tert-butyl 2-chloro-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (200 mg, 0.782 mmol) in 1,4-dioxane (5 mL) and water (1 mL) was added benzyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate (322 mg, 0.94 mmol), K2CO3 (324 mg, 2.35 mmol), and Pd(dppf)Cl2 (32 mg, 0.04 mmol). The mixture was stirred at 100°C under nitrogen overnight. After completion of the reaction, the solvent was removed by distillation under reduced pressure, water (20 mL) was added, and the mixture was extracted three times with DCM (20 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE=0 / 1-1 / 1, silica gel-CS 20 g, 40 mL / min, UV 254) to give an off-white solid product (255.0 mg, yield 74.6%).

[0689] ESI-MS m / z calcd for [C 24 H 28N4O4][M+H] + :437.2; found:437.2

[0690] 2.3

[0691] tert-Butyl 2-(piperidin-4-yl)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (MX02044-3)

[0692] To a solution of tert-butyl 2-(1-((benzyloxy)carbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (255 mg, 0.584 mmol) in MeOH / THF (v / v=1:1, 10 mL) was added Pd / C (50 mg, 0.256 mmol). The mixture was stirred under a hydrogen atmosphere at room temperature overnight, filtered, and concentrated to give the product as a yellow solid (200 mg, 0.584 mmol, 100% yield).

[0693] ESI-MS m / z calcd for [C 16 H 24 N4O2][M+H] + :305.2; found:305.2

[0694] 2.4

[0695] (R)-tert-Butyl-2-(1-(4-((1-(hydroxymethyl)cyclobutyl)amino)-5-oxo-6,7-dihydrothiophene[3,2-d]pyrimidin-2-yl)piperidin-4-yl)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (02044-4)

[0696] To a solution of (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (90 mg, 0.313 mmol) in DMF (5 mL) and DIEA (1 mL) was added tert-butyl 2-(piperidin-4-yl)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (200 mg, 0.584 mmol). The reaction mixture was stirred at 115°C for 3 hours. The reaction mixture was concentrated by distillation under reduced pressure, and the crude product was purified by column chromatography (MeOH / DCM = 0 / 1 to 1 / 10, Silica Gel-CS 40 g, 40 mL / min, silica gel, UV 254) to give the product as a yellow solid (165.0 mg, 95.0% yield).

[0697] ESI-MS m / z calcd for [C27 H 37 N7O4S][M+H] + :556.3; found:556.2

[0698] 2.5

[0699] (R)-2-(4-(6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-2-yl)piperidin-1-yl)-4-((1-

[0700] (Hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine-5-oxide (MX02044)

[0701] A mixed solution of (R)-tert-butyl-2-(1-(4-((1-(hydroxymethyl)cyclobutyl)amino)-5-oxo-6,7-dihydrothiophene[3,2-d]pyrimidin-2-yl)piperidin-4-yl)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (50 mg, 0.09 mmol) in HFP (2 mL) was stirred at 120°C for 2 hours under microwave conditions. The solvent was evaporated under reduced pressure, and the crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give the product as a white solid (10.05 mg, 24.4% yield).

[0702] ESI-MS m / z calcd for [C 22 H 29 N7O2S][M+H] + :456.2;found:456.0

[0703] 1 H NMR (400MHz, DMSO-d6) δ8.58(s,1H),7.39(s,1H),4.86(t,J=5.6Hz,1H),4.71( d,J=12.0Hz,2H),4.58–4.51(m,1H),4.08(s,2H),3.98(s,2H),3.70–3.68(m,2 H),3.45–3.37(m,1H),3.24–3.12(m,2H),3.07–2.98(m,2H),2.96–2.28(m,2H) ,2.38–2.25(m,2H),2.18–2.13(m,2H),1.94–1.91(m,2H),,1.82–1.60(m,4H).

[0704] 1. Synthesis scheme:

[0705] 2. Experimental part:

[0706] 2.1

[0707] 4,4-Dimethyl-2-oxocyclohexanecarboxaldehyde (02053-1)

[0708] To a solution of NaH (60%, 349 mg, 8.72 mmol) in THF (10 mL) was added 3,3-dimethylcyclohexanone (1 g, 7.92 mmol) at 30°C, and the mixture was stirred for 1 hour. Ethyl formate (1.2 g, 16.24 mol) was then added to the reaction solution at 35°C, and stirred at 40°C overnight. The mixture was acidified to pH 3 with 1N aqueous HCl solution and then extracted twice with EA (50 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated to give the product as a yellow oil (990 mg, 81.1% yield).

[0709] ESI-MS m / z calcd for [C9H 14 O2][M+H] + :155.1; found:155.4

[0710] 2.2

[0711] 6,6-Dimethyl-4,5,6,7-tetrahydro-1H-indazole (02053-2)

[0712] To a solution of 4,4-dimethyl-2-oxocyclohexanecarboxaldehyde (250 mg, 1.62 mmol) in MeOH (10 mL) was added dropwise a solution of hydrazine hydrate (82 mg, 1.64 mmol) in MeOH (5 mL). The mixture was heated under reflux for 15 minutes. After cooling, the solvent was distilled off under reduced pressure, water (20 mL) was added, and the mixture was extracted with EA (20 mL). The organic layer was washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated to give a yellow oily compound (135 mg, 55.4% yield).

[0713] ESI-MS m / z calcd for [C9H 14 N2][M+H] + :151.1; found:151.4

[0714] 2.3

[0715] 3-Iodo-6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazole (02053-3)

[0716] To a solution of 6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazole (523 mg, 3.48 mmol) in DMF (10 mL) was added I2 (3.68 g, 8.7 mmol) and KOH (967 mg, 17.23 mmol) at room temperature, and the mixture was stirred at room temperature for 4 hours. The reaction was cooled in an ice bath, and an aqueous solution of NaHSO3 (2 g in 20 mL of water) was added dropwise. More water (100 mL) was then added, and a precipitate formed. The product was filtered to give a yellow solid (400 mg, 41% yield).

[0717] ESI-MS m / z calcd for [C9H 13 IN2][M+H] + :277.0;found:277.1

[0718] 2.4

[0719] Benzyl 4-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate (02053-4)

[0720] To a solution of 3-iodo-6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazole (229 mg, 0.83 mmol) and 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylic acid benzyl ester (285 mg, 0.83 mmol) in 1,4-dioxane / water (12 mL, v / v 3:1) was added Pd(dppf)Cl2 (18 mg, 0.02 mmol) and K2CO3 (344 mg, 2.49 mmol). The mixture was stirred at 60°C under nitrogen for 3 hours. Water (20 mL) was then added and extracted with EA (20 mL). The organic phase was dried over anhydrous sodium sulfate, filtered and concentrated. The crude product was purified by column chromatography (PE / EA=0-1, silica gel-CS 20 g, 30 mL / min, silica gel, UV 254) to give a white solid product (164 mg, yield 54.0%).

[0721] ESI-MS m / z calcd for [C 23 H 28 N2O2][M+H] + :365.2; found:366.2

[0722] 2.5

[0723] 6,6-Dimethyl-3-(piperidin-4-yl)-4,5,6,7-tetrahydro-1H-indazole (02053-5)

[0724] To a solution of benzyl 4-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate (210 mg, 0.57 mmol) in MeOH (3 mL) was added Pd / C (20 mg). The reaction mixture was stirred at room temperature overnight under a hydrogen atmosphere, then filtered through Celite to remove the Pd / C. The filtrate was concentrated by distillation under reduced pressure to afford the product as a colorless oil (120 mg, 89.5% yield).

[0725] ESI-MS m / z calcd for [C 14 H 23 N3][M+H] + :234.2; found:234.4

[0726] 2.6

[0727] (R)-2-(4-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02053)

[0728] To a solution of (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (60 mg, 0.41 mmol) in DMF (7 mL) was added 6,6-dimethyl-3-(piperidin-4-yl)-4,5,6,7-tetrahydro-1H-indazole (120 mg, 0.51 mmol) and DIEA (131 mg, 1.03 mmol). The mixture was then stirred at 70°C for 3 hours. After completion of the reaction, the solvent was removed by distillation under reduced pressure. The crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give the product as a white solid (20.75 mg, 8.33% yield).

[0729] ESI-MS m / z calcd for [C 25 H 36 N6O2S][M+H] + :485.3; found:485.0

[0730] 1 H NMR(400MHz,DMSO-d6)δ11.95–11.82(m,1H),7.38–7.30(m,1H),4.84(t, J=5.6Hz,1H),4.81–4.62(m,2H),3.75–3.68(m,2H),3.45–3.36(m,1H),3. 24–3.16(m,1H),3.01–2.82(m,5H),2.39–2.27(m,6H),2.19–2.10(m,2H), 1.86–1.70(m,4H),1.60–1.48(m,2H),1.43(t,J=6.4Hz,2H),0.93(s,6H).

[0731] 1. Synthesis scheme:

[0732] 2. Experimental part:

[0733] 2.1

[0734] 5-(Benzyloxy)-1-(triisopropylsilyl)-1H-indole (02058-1)

[0735] To a solution of 5-(benzyloxy)-1H-indole (3 g, 13.45 mmol) in anhydrous THF (20 mL) at 0°C was added dropwise a solution of NaH (60%, 699 mg, 17.48 mmol) in THF (20 mL). The mixture was slowly warmed to room temperature over 30 minutes, and then chlorotriisopropylsilane (3.37 g, 17.48 mmol) was added dropwise at 0°C over 5 minutes. The reaction solution was slowly warmed to room temperature and stirred for 4 hours. The reaction was then quenched with saturated aqueous NH4Cl (20 mL) at 0°C and extracted three times with Et2O (15 mL). The combined organic phases were dried over anhydrous magnesium sulfate and concentrated to remove the solvent. The crude product was purified by column chromatography (EA / PE = 0-10%, Silica Gel-CS 40 g, 40 mL / min, silica gel, UV 254) to give the product as a white solid (3.2 g, 62.69% yield).

[0736] ESI-MS m / z calcd for [C9H 10 FNO2],NO MS was found

[0737] 2.2

[0738] 1-(Triisopropylsilyl)-1H-indol-5-ol (02058-2)

[0739] To a solution of 5-(benzyloxy)-1-(triisopropylsilyl)-1H-indole (3.2 g, 8.43 mmol) in EtOH (40 mL) was added Pd / C (120 mg) at room temperature. The mixture was stirred overnight under a hydrogen atmosphere, filtered through celite, and the filtrate was distilled under reduced pressure to give the product as a colorless oil (2.3 g, 94.3%).

[0740] ESI-MS m / z calcd for [C 17 H 27 NOSi][M+H] + :290.2;found:290.2

[0741] 2.3

[0742] Tert-Butyl 3-((1H-indol-5-yl)oxy)azetidine-1-carboxylate (02058-3)

[0743] To a solution of 1-(triisopropylsilyl)-1H-indole-5-ol (2.67 g, 9.22 mmol) and Cs2CO3 (9.0 g, 27.67 mmol) in DMF (50 mL) was added tert-butyl 3-iodoazetidine-1-carboxylate (3.1 g, 11.07 mmol). The reaction mixture was stirred at 140 ° C for 3 hours, and then the mixture was distilled under reduced pressure to remove the solvent. Water (150 mL) was added and extracted twice with EA (75 mL). The combined organic layer was washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered and concentrated. The crude product was purified by column chromatography (EA / PE = 0-50%, silica gel-CS 40 g, 50 mL / min, silica gel, UV 254) to give a yellow solid product (480 mg, yield 81.5%).

[0744] ESI-MS m / z calcd for [C 16 H 20 N2O3][M+H] + :289.2; found:289.1

[0745] 2.4

[0746] (R)-2-(3-((1H-indol-5-yl)oxy)azetidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02058)

[0747] A solution of tert-butyl 3-((1H-indol-5-yl)oxy)azetidine-1-carboxylate (50 mg, 0.17 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (49 mg, 0.17 mmol) in HFP (2 mL) was stirred at 120° C. under microwave conditions for 2 hours. After completion of the reaction, the mixture was distilled under reduced pressure to remove the solvent, and the crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give the product as a white solid (23.54 mg, 30.89% yield).

[0748] ESI-MS m / z calcd for [C 22 H 25 N5O3S][M+H] + :440.2;found:440.0

[0749] 1 H NMR (400MHz, DMSO-d6) δ10.97(s,1H),7.46(s,1H),7.32–7.30(m,2H),6.93(d,J=2.4Hz,1H) ,6.72(dd,J=8.8,2.4Hz,1H),6.35(t,J=2.0Hz,1H),5.11–5.06(m,1H),4.85(t,J=5.6Hz,1H ),4.45(dd,J=9.6,6.4Hz,2H),3.95–3.92(m,2H),3.73–3.66(m,2H),3.45–3.37(m,1H),3.2 5–3.17(m,1H),2.97–2.84(m,2H),2.38–2.25(m,2H),2.14–2.10(m,2H),1.82–1.65(m,2H).

[0750] 1. Synthesis scheme:

[0751] 2. Experimental part:

[0752] 2.1

[0753] tert-Butyl 4-(5-chloropyrimidin-2-yl)piperidine-1-carboxylate (A-3)

[0754] To a solution of 4-cyanopiperidine hydrochloride (3.1 g, 21.2 mmol) in 4N HCl / 1,4-dioxane (10.6 mL, 42.4 mmol) was added MeOH (2.57 mL, 63.6 mmol) while maintaining the temperature below 10°C. The mixture was cooled to 5°C, and a 25% solution of NaOMe in MeOH (13.74 g, 63.6 mmol) was added while maintaining the temperature below 15°C. To this mixture was added 7N NH3 / MeOH (4.54 mL, 31.8 mmol), and the mixture was stirred at room temperature for 2 hours. The mixture was then concentrated under reduced pressure at 60°C to provide a solution of the crude product in 1,4-dioxane (this solution was not isolated).

[0755] A solution of the intermediate compound in 1,4-dioxane was cooled to 0°C, and a 25% NaOMe solution in MeOH (11.45 g, 53.0 mmol) was added. The mixture was then stirred for 30 minutes. Compound (Z)-N-(2-chloro-3-(dimethylamino)allylidene)-N-methylmethanium hexafluorophosphate (5.52 g, 18.02 mmol) was added to the mixture in two portions over 10 minutes at room temperature, followed by stirring at room temperature for 6 hours. The mixture was concentrated by distillation under reduced pressure, and the crude product was dispersed in DCM (100 mL). TEA (10 mL, 71.8 mmol) and (Boc)2O (9.24 g, 42.4 mmol) were added. The mixture was then stirred at room temperature for 3 hours, followed by addition of water (100 mL), and extraction with DCM (150 mL) twice. The combined organic phases were washed with saturated brine (150 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE=0 / 1-1 / 3, silica gel-CS 80 g, 50 mL / min, silica gel, UV 254) to give a yellow oily product (2.50 g, yield 39.7%).

[0756] ESI-MS m / z calcd for [C 14 H 20 ClN3O2][M-56+H] + :298.1; found:242.3

[0757] 2.2

[0758] 5-Chloro-2-(piperidin-4-yl)pyrimidine (A-4)

[0759] To a solution of tert-butyl 4-(5-chloropyrimidin-2-yl)piperidine-1-carboxylate (100 mg, 0.335 mmol) in DCM (5.0 mL) was added TFA (0.5 mL). The mixture was stirred at room temperature overnight, and the pH of the solution was adjusted to 8 with TEA. The solvent was concentrated under reduced pressure to give a yellow oily crude product (135 mg, 100% yield) which was used directly in the next step.

[0760] ESI-MS m / z calcd for [C9H 12 ClN3][M+H] + :198.1; found:198.3

[0761] 2.3

[0762] tert-Butyl 2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (02060-1)

[0763] To a solution of tert-butyl 2,4-dichloro-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (345 mg, 1.19 mmol) in MeCN (10 mL) and TEA (3 mL) was added (1-aminocyclobutyl)methanol (120 mg, 1.19 mmol). The mixture was then stirred at 70°C for 16 hours, the solvent was removed by distillation under reduced pressure, water (20 mL) was added, and the mixture was extracted three times with DCM (20 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0 / 1 to 1 / 0, silica gel-CS 20 g, 40 mL / min, UV 254) to give a yellow solid product (150.0 mg, yield 35.6%).

[0764] ESI-MS m / z calcd for [C 16 H 23 ClN4O3][M+H] + :355.1; found:355.2

[0765] 2.4

[0766] tert-Butyl 2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (02060-2)

[0767] To a solution of tert-butyl 2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (60 mg, 0.17 mmol) in DMF (4 mL) and DIEA (1 mL) was added 5-chloro-2-(piperidin-4-yl)pyrimidine (135 mg, 0.335 mmol). The mixture was then stirred at 120° C. overnight. The reaction mixture was concentrated under reduced pressure, and the crude product was purified by column chromatography (EA / PE=0 / 1 to 1 / 0, silica gel-CS 20 g, 40 mL / min, silica gel, UV 254) to give the product as a yellow solid (40.0 mg, 45.6% yield).

[0768] ESI-MS m / z calcd for [C 25 H 34 ClN7O3][M+H] + :516.2;found:516.0

[0769] 2.5

[0770] (1-((2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-4-yl)amino)cyclobutyl)methanol (MX02060)

[0771] To a solution of tert-butyl 2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-[(1-(hydroxymethyl)cyclobutyl)amino]-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (40 mg, 0.078 mmol) in DCM (3 mL) was added TFA (0.3 mL), and the mixture was stirred at room temperature overnight. The pH of the reaction solution was adjusted to 7 with 1N NaHCO3 aqueous solution. The solvent was distilled off under reduced pressure, and the crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give a white solid product (19.05 mg, 59.0% yield).

[0772] ESI-MS m / z calcd for [C 20 H 26 ClN7O][M+H] + :416.2;found:416.0

[0773] 1H NMR (400MHz, DMSO-d6) δ8.85(s,2H),6.47(s,1H),4.79(t,J=5.6Hz,1H),4.61(d,J=12.8Hz,2H),4.27–4.21(m,1H),3.80–3. 67(m,6H),3.15–3.09(m,1H),2.95–2.89(m,2H),2.25–2.11(m,4H),1.89–1.86(m,2H),1.80–1.73(m,2H),1.67–1.57(m,2H).

[0774] 1. Synthesis scheme:

[0775] 2. Experimental part:

[0776] 2.1

[0777] Tert-Butyl (1-(5-chloropyrimidin-2-yl)piperidin-4-yl)carbamate (02063-1)

[0778] To a solution of tert-butyl piperidin-4-ylcarbamate (664 mg, 3.32 mmol) in 1,4-dioxane (8 mL) at room temperature were added 2,5-dichloropyrimidine (450 mg, 3.02 mmol) and Cs2CO3 (1.97 g, 6.04 mmol). The mixture was stirred at 100°C for 3 hours, then water (30 mL) was added and extracted three times with EA (30 mL). The combined organic layers were dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0-50%, Silica-CS20 g, 20 mL / min, silica gel, UV 254) to give a yellow solid product (800 mg, 84.6% yield).

[0779] ESI-MS m / z calcd for [C 14 H 21 ClN4O2][M+H] + :313.1; found:313.2

[0780] 2.2

[0781] 1-(5-Chloropyrimidin-2-yl)piperidin-4-amine (02063-2)

[0782] To a solution of tert-butyl (1-(5-chloropyrimidin-2-yl)piperidin-4-yl)carbamate (210 mg, 0.67 mmol) in DCM (5 mL) was added TFA (0.5 mL). The reaction mixture was stirred at room temperature overnight, and the solvent was concentrated by distillation under reduced pressure to give a crude yellow oil (230 mg, 100% yield) which was used directly in the next reaction.

[0783] ESI-MS m / z calcd for [C9H 13 ClN4][M+H] + :213.1; found:213.2

[0784] 2.3

[0785] (R)-2-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)amino)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02063)

[0786] To a solution of 1-(5-chloropyrimidin-2-yl)piperidin-4-amine (230 mg, 0.67 mmol) in DMF (5 mL) and DIEA (1 mL) was added (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (100 mg, 0.347 mmol). The reaction mixture was stirred at 80°C for 16 hours. The mixture was concentrated by distillation under reduced pressure, and the crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give the product as a white solid (12 mg, 7.5% yield).

[0787] ESI-MS m / z calcd for [C 20 H 26 ClN7O2S][M+H] + :464.2;found:464.0

[0788] 1H NMR (400MHz, DMSO-d6) δ8.41(s,2H),7.31–7.24(m,2H),4.87(t,J=5.6Hz,1H),4.49(d,J=13.2Hz,2H),3.94–3.90(m,1H),3.72(d,J=5.2Hz ,2H),3.39–3.31(m,1H),3.22–3.04(m,3H),2.88–2.81(m,2H),2.41– 2.30(m,2H),2.17–2.12(m,2H),1.88–1.71(m,4H),1.44–1.36(m,2H).

[0789] 1. Synthesis scheme:

[0790] 2. Experimental part:

[0791] 2.1

[0792] 1-Benzyl-N-((1R,2R)-2-hydroxycyclohexyl)piperidine-4-carboxamide (02069-1)

[0793] To a solution of 1-benzylpiperidine-4-carboxylic acid (512 mg, 2.34 mmol) in DCM (8 mL) was added (COCl) 2 (358 mg, 2.82 mmol). The mixture was stirred at room temperature for 1 hour under nitrogen protection, and the solvent was removed by distillation under reduced pressure. The resulting crude product was added with DCM (8 mL), (1R, 2R)-2-aminocyclohexanol (270 mg, 2.34 mmol) and TEA (709 mg, 7.02 mmol), and the mixture was stirred at room temperature overnight. After the reaction was complete, water (50 mL) was added and extracted three times with EA (50 mL). The combined organic layers were washed with saturated brine (30 mL), dried over anhydrous sodium sulfate, filtered and concentrated to give a white solid product (602 mg, 81% yield).

[0794] ESI-MS m / z calcd for [C 19 H 28 N2O2][M+H] + :317.2; found:317.3

[0795] 2.2

[0796] (R)-1-Benzyl-N-(2-oxocyclohexyl)piperidine-4-carboxamide (02069-2)

[0797] To a solution of 1-benzyl-N-((1R,2R)-2-hydroxycyclohexyl)piperidine-4-carboxamide (602 mg, 1.90 mmol) in DCM (15 mL) was added PCC (1.23 g, 5.71 mmol). The resulting reaction mixture was stirred at room temperature overnight. The solvent was removed by distillation under reduced pressure, water (15 mL) was added, and the mixture was extracted three times with EA (50 mL). The combined organic layers were washed with saturated brine (30 mL), dried over anhydrous sodium sulfate, filtered, and concentrated to afford the product as a white solid (340 mg, 56% yield).

[0798] ESI-MS m / z calcd for [C 19 H 26 N2O2][M+H] + :315.2; found:315.2

[0799] 2.3

[0800] 2-(1-Benzylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-benzo[d]imidazole (02069-3)

[0801] To a solution of (R)-1-benzyl-N-(2-oxocyclohexyl)piperidine-4-carboxamide (140 mg, 0.44 mmol) in HOAc (5 mL) was added CH3COONH4 (338 mg, 4.4 mmol). The mixture was stirred at 150°C under nitrogen for 20 minutes. After the starting material was consumed, the reaction mixture was concentrated and the crude product was purified by reverse phase column chromatography (MeCN / H2O=1 / 20 to 1 / 1, C-18 column, 20 mL / min, UV 254) to give the product as a yellow solid (72 mg, 55% yield).

[0802] ESI-MS m / z calcd for [C 19 H 25 N3][M+H] + :296.2;found:296.2

[0803] 2.4

[0804] 2-(Piperidin-4-yl)-4,5,6,7-tetrahydro-1H-benzo[d]imidazole (02069-4)

[0805] To a solution of 2-(1-benzylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-benzo[d]imidazole (72 mg, 0.24 mmol) in MeOH (3 mL) was added Pd / C (24 mg). The mixture was stirred at room temperature under a hydrogen atmosphere overnight. After the starting material was consumed, the mixture was filtered and the filtrate was concentrated to give the product as a colorless oil (40 mg, 80% yield).

[0806] ESI-MS m / z calcd for [C 12 H 19 N3][M+H] + :206.2; found:206.4

[0807] 2.5

[0808] (R)-4-((1-(Hydroxymethyl)cyclobutyl)amino)-2-(4-(4,5,6,7-tetrahydro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02069)

[0809] To a solution of 2-(piperidin-4-yl)-4,5,6,7-tetrahydro-1H-benzo[d]imidazole (40 mg, 0.20 mmol) in 1,4-dioxane (4 mL) was added (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (57 mg, 0.20 mmol) and DIEA (77 mg, 0.60 mmol). The mixture was stirred at 110°C under nitrogen for 2 hours. After the starting material was consumed, the reaction mixture was concentrated. The crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / LNH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to afford the product as a white solid (8.55 mg, 9% yield).

[0810] ESI-MS m / z calcd for [C 23 H 32 N6O2S][M+H] + :457.2; found:457.0

[0811] 1H NMR (400MHz, DMSO-d6) δ11.19(s,1H),7.37(s,1H),4.86(t,J=5.6Hz,1H),4.62(d,J=11.6Hz,2H),3.72–3.69(m,2H),3.45–3.36(m,1H) ,3.23–3.16(m,1H),3.03–2.83(m,5H),2.41–2.26(m,6H),2.19–2.13(m,2H),1.85–1.73(m,4H),1.68–1.66(m,4H),1.58–1.54(m,2H),.

[0812] 1. Synthesis scheme:

[0813] 2. Experimental part:

[0814] 2.1

[0815] Methyl 2-(4-(((2-chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)phenyl)acetate (02075-1)

[0816] To a solution of 2,4-dichloro-6,7-dihydrothieno[3,2-d]pyrimidine (3 g, 14.48 mmol) and DIEA (5.61 g, 43.44 mmol) in DMF (50 mL) at room temperature was added methyl 2-(4-aminophenyl)acetate (2.39 g, 14.48 mmol). The mixture was stirred at 100°C overnight, after which water (50 mL) was added to the reaction mixture and extracted twice with DCM (70 mL). The combined organic layers were washed with saturated brine (30 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0 / 1 to 1 / 2, silica gel-CS 80 g, 50 mL / min, UV 254) to afford the product as an orange solid (3.11 g, 63.9% yield).

[0817] ESI-MS m / z calcd for [C 15 H 14 ClN3O2S][M+H] + :336.1;found:336.0

[0818] 2. Methyl 2-(4-((2-chloro-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)phenyl)acetate (02075-2)

[0819] To a solution of methyl 2-(4-((2-chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)-2-fluorophenyl)acetate (420 mg, 1.25 mmol) and S-1,1'-bin-2-naphthol (37.2 mg, 0.13 mmol) in DCM (10 mL) were added titanium tetraisopropoxide (17.8 mg, 0.06 mmol) and water (22.5 mg, 1.25 mmol). The mixture was stirred at room temperature under nitrogen for 16 hours, and then a 70% aqueous solution of tert-butyl hydroperoxide (123.9 mg, 1.37 mmol) was added in one portion. The mixture was then stirred at room temperature for 2 hours, and then water (20 mL) was added, and the mixture was extracted three times with DCM (60 mL). The combined organic layers were dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (DCM / MeOH=1 / 0-20 / 1, Silica Gel-CS 40 g, 50 mL / min, silica gel, UV 254) to give a white solid product (367 mg, yield 83.4%).

[0820] ESI-MS m / z calcd for [C 15 H 14 ClN3O3S][M+H]+:352.0; found:352.0

[0821] 2.3

[0822] (R)-2-(4-((2-(4,5-dihydro-1H-pyrazolo[3,4-c]pyridin-6(7H)-yl)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)phenyl)acetate (02075-3)

[0823] To methyl (R)-2-(4-((2-chloro-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)phenyl)acetate (30 mg, 0.08 mmol) and DIEA (31 mg, 0.24 mmol) in DMF (5 mL) was added 4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine (9.8 mg, 0.08 mmol). The mixture was then stirred at 90° C. for 1 hour. After the starting material was consumed, the reaction mixture was concentrated. The crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give the product as a white solid (27 mg, 72.2% yield).

[0824] ESI-MS m / z calcd for [C 21 H22 FN6O3S][M+H] + :439.2; found:439.0

[0825] 2.4

[0826] (R)-2-(4-((2-(4,5-dihydro-1H-pyrazolo[3,4-c]pyridin-6(7H)-yl)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)phenyl)acetic acid (MX02075)

[0827] To a solution of methyl (R)-2-(4-((2-(4,5-dihydro-1H-pyrazolo[3,4-c]pyridin-6(7H)-yl)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino)phenyl)acetate (27 mg, 0.06 mmol) in EtOH (3 mL) was added 1N aqueous LiOH solution (0.6 mL, 0.6 mmol). The mixture was then stirred at 50° C. for 1 hour, and the pH of the reaction solution was adjusted to 6 with 1N aqueous HCl. The solvent was removed by distillation under reduced pressure, and the crude product was purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give a white solid product (11.57 mg, 35.1% yield).

[0828] ESI-MS m / z calcd for [C 20 H 20 N6O3S][M+H] + :425.1; found:425.0

[0829] 1 H NMR (400MHz, DMSO-d6+D2O) δ7.61(d,J=8.0Hz,2H),7.47(s,1H),7.28(d,J=8.8Hz,2H),4.89–4.87(m ,2H),4.02–4.00(m,2H),3.59–3.54(m,3H),3.35–3.32(m,1H),3.14–3.02(m,2H),2.65–2.63(m,2H).

[0830] 1. Synthesis scheme:

[0831] 2. Experimental part:

[0832] 2.1

[0833] Tert-Butyl 4-(5-chloropyrimidin-2-yl)-1,4-diazepane-1-carboxylate (02077-1)

[0834] A mixture of 2,5-dichloropyrimidine (500 mg, 3.36 mmol), tert-butyl 1,4-diazepane-1-carboxylate (673 mg, 3.36 mmol), and DIEA (2.8 mL, 16.8 mmol) in DMF (20 mL) was stirred at 80°C overnight under argon. After cooling, the reaction mixture was evaporated under reduced pressure to remove the solvent. The crude product was purified by column chromatography (EA / PE = 0-1 / 9, silica gel-CS 40 g, 40 mL / min, UV 254) to give the product as a white solid (981 mg, 93.4% yield).

[0835] ESI-MS m / z calcd for [C 14 H 21 ClN4O2][M+H] + :313.1; found:313.2

[0836] 2.2

[0837] 1-(5-chloropyrimidin-2-yl)-1,4-diazepane(02077-2)

[0838] To a solution of tert-butyl 4-(5-chloropyrimidin-2-yl)-1,4-diazepane-1-carboxylate (200 mg, 0.64 mmol) in DCM (20 mL) was added TFA (4 mL). The mixture was stirred at 35° C. under argon protection for 2 hours, and then the reaction mixture was concentrated to dryness to give a pale yellow oily crude product (136 mg, 99.9% yield).

[0839] ESI-MS m / z calcd for [C9H 13 ClN4][M+H] + :213.1; found:213.2

[0840] 2.3

[0841] (R)-2-(4-(5-chloropyrimidin-2-yl)-1,4-diazepan-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02077)

[0842] To a solution of 1-(5-chloropyrimidin-2-yl)-1,4-diazepane (68 mg, 0.32 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (92 mg, 0.32 mmol) in DMF (20 mL) was added DIEA (0.26 mL, 1.6 mmol). The mixture was stirred at 80° C. under argon protection overnight, and then the solvent was distilled off under reduced pressure. The crude product was purified by column chromatography (MeOH / DCM=0-1 / 9, silica gel-CS20 g, 20 mL / min, UV 254) to give a crude product (90 mg). The crude product was then purified by preparative HPLC [MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254] to give a white solid product (73.60 mg, 49.6% yield).

[0843] ESI-MS m / z calcd for [C 20 H 26 ClN7O2S][M+H] + :464.2; found:463.9

[0844] 1 H NMR (400MHz, DMSO-d6) δ8.40–8.38(m,2H),7.30(s,1H),4.85(t,J=5.6Hz,1H),3.95–3.78(m,4H),3.74–3.57(m,6H) ,3.42–3.36(m,1H),3.23–3.15(m,1H),2.94–2.81(m,2H),2.36–2.28(m,2H),2.16–2.14(m,2H),1.86–1.72(m,4H).

[0845] 1. Synthesis scheme:

[0846] 2. Experimental part:

[0847] 2.1

[0848] tert-Butyl 3-ethoxy-2,5,6,7-tetrahydro-1H-1,4-diazepine-1-carboxylate (02078-1)

[0849] To a solution of tert-butyl 3-oxo-1,4-diazepane-1-carboxylate (500 mg, 2.34 mmol) in DCM (10 mL) was added triethoxyammonium tetrafluoroborate (613 mg, 3.50 mmol). The mixture was stirred at room temperature overnight under nitrogen protection. After the starting material was consumed, the reaction mixture was quenched with saturated NaHCO3 aqueous solution (50 mL) and extracted three times with EA (50 mL). The combined organic layer was washed with saturated brine (50 mL), dried over anhydrous sodium sulfate, filtered and concentrated to give a yellow oily product (525 mg, 93% yield).

[0850] ESI-MS m / z calcd for [C 12 H 22 N2O3][M+H] + :243.2; found:243.3

[0851] 2.2

[0852] tert-Butyl 3-(2-(methoxycarbonyl)hydrazino)-2,5,6,7-tetrahydro-1H-1,4-diazepine-1-carboxylate (02078-2)

[0853] To a solution of tert-butyl 3-ethoxy-2,5,6,7-tetrahydro-1H-1,4-diazepine-1-carboxylate (525 mg, 2.17 mmol) in MeOH (5 mL) was added methyl carbazate (195 mg, 2.17 mmol). The mixture was stirred at room temperature under nitrogen for 16 hours. After the starting material was consumed, the reaction mixture was concentrated. The crude product was purified by column chromatography (MeCN / H2O = 1 / 20 to 1 / 1, C-18 column, 30 mL / min, UV 254) to give the product as a colorless oil (126 mg, 20% yield).

[0854] ESI-MS m / z calcd for [C 12 H 22 N4O4][M+H] + :287.2; found:287.1

[0855] 2.3

[0856] tert-Butyl 3-oxo-5,6,7,9-tetrahydro-2H-[1,2,4]triazolo[4,3-a][1,4]diazepine-8(3H)-carboxylate (02078-3)

[0857] To a solution of tert-butyl 3-(2-(methoxycarbonyl)hydrazinyl)-2,5,6,7-tetrahydro-1H-1,4-diazepine-1-carboxylate (126 mg, 0.44 mmol) in EtOH (3 mL) was added NaOMe (24 mg, 0.44 mmol). The mixture was stirred at 75°C under nitrogen for 4 hours. After the starting material was consumed, the reaction mixture was concentrated. The crude product was purified by reverse phase column chromatography (MeCN / H2O = 1 / 20 to 1 / 1, C-18 column, 20 mL / min, UV 254) to give a white solid product (61 mg, 55% yield).

[0858] ESI-MS m / z calcd for [C 11 H 18 N4O3][M+H] + :255.1; found:255.2

[0859] 2.4

[0860] 6,7,8,9-Tetrahydro-2H-[1,2,4]triazolo[4,3-a][1,4]diazepin-3(5H)-one (02078-4)

[0861] To a solution of tert-butyl 3-oxo-5,6,7,9-tetrahydro-2H-[1,2,4]triazolo[4,3-a][1,4]diazepine-8(3H)-carboxylate (61 mg, 0.24 mmol) in DCM (2 mL) was added TFA (0.2 mL). The mixture was stirred at room temperature under nitrogen for 3 hours. After the starting material was consumed, the mixture was concentrated to give the product as a colorless oil (33 mg, 89% yield).

[0862] ESI-MS m / z calcd for [C 12 H 22 N4O4][M+H] + :155.1; found:155.3

[0863] 2.5

[0864] (R)-8-(4-((1-(Hydroxymethyl)cyclobutyl)amino)-5-oxido-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)-6,7,8,9-tetrahydro-2H-[1,2,4]triazolo[4,3-a][1,4]diazepin-3(5H)-one (MX02078)

[0865] To a solution of 6,7,8,9-tetrahydro-2H-[1,2,4]triazolo[4,3-a][1,4]diazepin-3(5H)-one (33 mg, 0.21 mmol) in DMF (3 mL) was added (R)-2-chloro-4-[(1-(hydroxymethyl)cyclobutyl)amino]-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (60 mg, 0.21 mmol) and DIEA (81 mg, 0.63 mmol). The mixture was stirred at 100°C under nitrogen for 2 hours. After the starting material was consumed, the reaction mixture was concentrated. The crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to afford the product as a white solid (7.13 mg, 8% yield).

[0866] ESI-MS m / z calcd for [C 17 H 23 N7O3S][M+H] + :406.2;found:406.2

[0867] 1 H NMR(400MHz,DMSO-d6)δ11.47(s,1H),7.52–7.38(m,1H),4.83–4.72(m,3H),4.04–3.94(m,2H),3.80–3.7 0(m,4H),3.44–3.36(m,1H),3.23–3.16(m,1H),2.95–2.83(m,2H),2.37–2.14(m,4H),1.77–1.71(m,4H).

[0868] 1. Synthesis scheme:

[0869] 2. Experimental part:

[0870] 2.1

[0871] (R)-2-(2-chloro-7,8-dihydro-1,6-naphthyridin-6(5H)-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02089)

[0872] A solution of tert-butyl 2-chloro-7,8-dihydro-1,6-naphthyridine-6(5H)-carboxylate (40 mg, 0.148 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (40 mg, 0.138 mmol) in HFP (3 mL) was stirred at 120°C under microwave conditions for 2 hours. After completion of the reaction, water (10 mL) was added to the reaction solution, and the mixture was extracted twice with DCM (10 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give a white solid product (16.6 mg, yield 19.1%).

[0873] ESI-MS m / z calcd for [C 19 H 22 ClN5O2S][M+H] + :420.12;found:420.0

[0874] 1 H NMR (400MHz, DMSO-d6) δ7.76(d,J=8.4Hz,1H),7.52(s,1H),7.35(d,J=8.4Hz,1H),4.90–4.86(m,3H),4.06–4.04(m,2H),3.75–3.74(m,2 H),3.43–3.39(m,1H),3.22–3.19(m,1H),2.99–2.94(m,1H),2.90–2.86(m,3H),2.42–2.29(m,2H),2.21–2.19(m,2H),1.80–1.78(m,2H).

[0875] 1. Synthesis scheme:

[0876] 2. Experimental part:

[0877] 2.1

[0878] tert-Butyl 2-cyano-7,8-dihydro-1,6-naphthyridine-6(5H)-carboxylate (02090-1)

[0879] To a solution of tert-butyl 2-chloro-7,8-dihydro-1,6-naphthyridine-6(5H)-carboxylate (230 mg, 0.86 mmol) in DMF (15 mL) were added Zn powder (562.4 mg, 8.6 mmol), Zn(CN)2 (1.01 g, 8.6 mmol), Pd2(dba)3 (238.1 mg, 0.26 mmol), and dppf (144.1 mg, 0.26 mmol). The reaction mixture was then heated to 120°C and stirred for 6 hours before being cooled to room temperature and concentrated. Water (10 mL) was added, and the mixture was extracted twice with DCM (10 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE=0-1 / 2, silica gel-CS 12 g, 30 mL / min, silica gel, UV 254) to give a white solid product (167 mg, yield 75.2%).

[0880] ESI-MS m / z calcd for [C 14 H 17 N3O2][M+H] + :260.1;found:260.2

[0881] 2.2

[0882] (R)-6-(4-((1-(Hydroxymethyl)cyclobutyl)amino)-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridine-2-carbonitrile (MX02090)

[0883] A solution of tert-butyl 2-cyano-7,8-dihydro-1,6-naphthyridine-6(5H)-carboxylate (147 mg, 0.57 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (164 mg, 0.57 mmol) in HFP (3.0 mL) was stirred at 120°C for 2 hours under microwave conditions, then cooled to room temperature and concentrated. Water (10 mL) was added, and the mixture was extracted twice with DCM (10 mL). The combined organic layers were washed with saturated brine (20 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by preparative HPLC (MeCN / H2O (10 mmol / L NH4HCO3), X-Select 10 μm 19*250 mm, 20 mL / min, UV 254) to give a white solid product (16.0 mg, yield 6.9%).

[0884] ESI-MS m / z calcd for [C20 H 22 N6O2S][M+H] + :411.2; found:411.0

[0885] 1 H NMR (400MHz, DMSO-d6) δ7.97(d,J=8.0Hz,1H),7.88(d,J=7.6Hz,1H),7.55(s,1H),5.01(s,2H),4.86(t,J=5.6Hz,1H),4.09(t,J =5.2Hz,2H),3.78–3.73(m,2H),3.47–3.39(m,1H),3.25–3.17(m,1H),2.99–2.85(m,4H),2.39–2.20(m,4H),1.86–1.71(m,2H).

[0886] 1. Synthesis scheme:

[0887] 2. Experimental part:

[0888] 2.1

[0889] 5-Benzyl-1-oxa-5-azaspiro[2.4]heptane (02096-1)

[0890] To a solution of NaH (60%, 300 mg, 7.41 mmol) in DMSO (10 mL) at 0°C was added trimethylsulfonium iodide (1.38 g, 6.27 mmol) portionwise. The mixture was stirred at 25°C under argon for 1 hour, followed by the addition of a solution of 1-benzylpyrrolidin-3-one (1.0 g, 5.7 mmol) in DMSO (11 mL). The mixture was then stirred at 25°C for 2 hours. The reaction was quenched with saturated aqueous NH4Cl (20 mL) and extracted four times with EA (50 mL). The combined organic layers were washed with saturated brine (50 mL), dried over anhydrous sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography (EA / PE = 0-1 / 1, silica gel-CS 40 g, 40 mL / min, silica gel, UV 254) to give the product as a yellow oil (326 mg, 30.2% yield).

[0891] ESI-MS m / z calcd for [C 12 H 15 NO][M+H] + :190.1;found:190.1

[0892] 2.2

[0893] 3-((1H-Benzo[d]imidazol-1-yl)methyl)-1-benzylpyrrolidin-3-ol (02096-2)

[0894] To a solution of NaH (60%, 96 mg, 2.4 mmol) in THF (6 mL) at 0°C was added 1H-benzo[d]imidazole (142 mg, 1.2 mmol) in portions and the reaction was stirred at 0°C under argon for 1 hour. A solution of 5-benzyl-1-oxa-5-azaspiro[2.4]heptane (226 mg, 1.2 mmol) in THF (4 mL) was then added and stirred at 40°C for 24 hours. The reaction was quenched with water (20 mL) and extracted three times with EA (50 mL). The combined organic layers were washed with saturated brine (50 mL), dried over anhydrous sodium sulfate, filtered and concentrated. The crude product was purified by column chromatography (MeOH / DCM = 0-1 / 9, silica gel-CS 40 g, 40 mL / min, UV 254) to give the product as a colorless oil (245 mg, 66.7% yield).

[0895] ESI-MS m / z calcd for [C 19 H 21 N3O][M+H] + :308.2; found:308.2

[0896] 2.3

[0897] 3-((1H-Benzo[d]imidazol-1-yl)methyl)pyrrolidin-3-ol (02096-3)

[0898] To a solution of 3-((1H-benzo[d]imidazol-1-yl)methyl)-1-benzylpyrrolidin-3-ol (100 mg, 0.33 mmol) and HCOONH4 (250 mg, 3.96 mmol) in MeOH (20 mL) was added Pd / C (30 mg), and the mixture was stirred at 70°C under a hydrogen atmosphere for 3 hours. After cooling, the reaction mixture was filtered under reduced pressure, and the filtrate was distilled under reduced pressure to remove the solvent. The crude product was purified by reverse phase column chromatography (MeCN / H2O = 0-3 / 17, C-18 column, 50 mL / min, UV 214) to give the product as a pale yellow solid (40 mg, 56.6% yield).

[0899] ESI-MS m / z calcd for [C 12 H 15 N3O][M+H] + :218.1;found:218.1

[0900] 2.4

[0901] (5R)-2-(3-((1H-benzo[d]imidazol-1-yl)methyl)-3-hydroxypyrrolidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (MX02096)

[0902] To a solution of 3-((1H-benzo[d]imidazol-1-yl)methyl)pyrrolidin-3-ol (10 mg, 0.05 mmol) and (R)-2-chloro-4-((1-(hydroxymethyl)cyclobutyl)amino)-...

Claims

1. A compound represented by the following formula H, its racemate, stereoisomer, tautomer, isotope-labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug: in: X1 represents chemical bond, C 1-20 Alkylene, O, S, NR q , S(=O), S(=O)2 or C(=O); R q selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6- 20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 ); L represents chemical bond, C 2-20 Alkynyl or Cy; wherein L can be at any position with X1 or R c connect; Cy represents a 3-20 membered heterocyclic group, C 6-20 Aryl, 5-20 membered heteroaryl, wherein the 3-20 membered heterocyclic group, C 6-20 The aryl group and the 5-20 membered heteroaryl group may be optionally fused with a 4-7 membered cycloalkyl group, provided that when the heterocyclic group contains a N atom, the heterocyclic group may be bonded to the carbon atom at the 2-position of the pyrimidine ring in formula H through its N atom or C atom; W represents a chemical bond, CH, O, S, N, -S(O)-, -S(O)2-, -C(O), sub-C 1-6 Alkyl, C 2-6 Alkenyl or C 2- 6-alkynyl; R2 is selected from absent, H, unsubstituted or optionally replaced by 1, 2 or more R d1 Substituted with the following groups: C 6-20 Aryl, 5-20 membered heteroaryl; R 2’ represents absence, H, halogen, OH, CN, unsubstituted or optionally replaced by 1, 2 or more R d2 Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2; The condition is that R2 and R 2’ Not at the same time "does not exist"; Alternatively, R2, R 2’ It may be taken together with the atoms to which it is attached to form an unsubstituted or optionally substituted group consisting of 1, 2 or more R d3 Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, 6-20 membered aryl; R a represents H or -X-R3; X represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-; R3 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d4 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2; R b represents H or -Y-R4; Y represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-; R4 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d5 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2; The condition is R a 、R b Not at the same time H; Or, R a 、R b Together with the atoms to which it is attached, it forms an unsubstituted or optionally substituted group consisting of 1, 2 or more R d6 Substituted with the following groups: C 5-20 Cycloalkenyl, 3-20 membered heterocyclyl, 5-20 membered heteroaryl, 6-20 membered aryl; Every R d1 、R d2 、R d3 、R d4 、R d5 、R d6 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), SO, SO2, unsubstituted or optionally substituted by 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-CH2-C(O)R 31 、-C(O)OR 32 、-CH2C(O)OR 32 、-C(O)NHR 32 、-CH2C(O)NHR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); Alternatively, when there are two or more selected from R d1 、R d2 、R d3 、R d4 、R d5 、R d6 When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R e Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6-20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, 3-20 membered heterocyclyl, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); m is an integer selected from 1 to 10; Every R e the same or different, independently selected from H, halogen, OH, CN, NO2, NH2, oxo (=O), thio (=S), O-CONH2, O-CONHR f , unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 ); Alternatively, when there are two or more selected from R e When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R f Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3- 20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R f the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R g Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 51 、-C(O)OR 52 、-OC(O)R 53 、-S(O)2R 54 、-S(O)2OR 55 、-OS(O)2R 56 、-P(O)(OR 57 )(OR 58 ); Alternatively, when there are two or more selected from R f When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R g Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R g the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2; Every R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2; The 3-20 membered heterocyclyl represents a saturated or unsaturated non-aromatic ring or ring system, such as a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, such as 1, 2, 3, 4, 5 or more heteroatoms independently selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2-; The C 6-20 Aryl represents a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, or spirocyclic) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which may be a single aromatic ring or multiple aromatic rings fused together; The 5-20 membered heteroaryl group represents a monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring system having 5 to 20 ring atoms and containing 1, 2, 3, 4, 5 or more heteroatoms independently selected from N, O and S. For example, a compound represented by the following formula G, its racemate, stereoisomer, tautomer, isotope-labeled substance, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug: in: Cy represents a chemical bond, a 3-20 membered heterocyclic group, C 6-20 Aryl, 5-20 membered heteroaryl, provided that when the heterocyclic group contains a N atom, the heterocyclic group can be bonded to the carbon atom at the 2-position of the pyrimidine ring in formula G through its N atom or C atom; W represents a chemical bond, CH, O, S, N, -S(O)-, -S(O)2-, -C(O), sub-C 1-6 Alkyl, C 2-6 Alkenyl or C 2- 6-alkynyl; R2 is selected from absent, H, unsubstituted or optionally replaced by 1, 2 or more R d1 Substituted with the following groups: C 6-20 Aryl, 5-20 membered heteroaryl; R 2’ represents absence, H, halogen, OH, CN, unsubstituted or optionally replaced by 1, 2 or more R d2 Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkyl sulfide Base, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2; The condition is that R2 and R 2’ Not at the same time "does not exist"; Alternatively, R2, R 2’ It may be taken together with the atoms to which it is attached to form an unsubstituted or optionally substituted group consisting of 1, 2 or more R d3 Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, 6-20 membered aryl; R a represents H or -X-R3; X represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-; R3 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d4 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2; R b represents H or -Y-R4; Y represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-; R4 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d5 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2; The condition is R a 、R b Not at the same time H; Or, R a 、R b Together with the atoms to which it is attached, it forms an unsubstituted or optionally substituted group consisting of 1, 2 or more R d6 Substituted with the following groups: C 5-20 Cycloalkenyl, 3-20 membered heterocyclyl, 5-20 membered heteroaryl, 6-20 membered aryl; Every R d1 、R d2 、R d3 、R d4 、R d5 、R d6 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-CH2-C(O)R 31 、-C(O)OR 32 、-CH2C(O)OR 32 、-C(O)NHR 32 、-CH2C(O)NHR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); Alternatively, when there are two or more selected from R d1 、R d2 、R d3 、R d4 、R d5 、R d6 When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R e Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); m is an integer selected from 1 to 10; Every R e the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、- OS(O)2R 46 、-P(O)(OR 47 )(OR 48 ); Alternatively, when there are two or more selected from R e When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R f Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3- 20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R f the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R g Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 51 、-C(O)OR 52 、-OC(O)R 53 、-S(O)2R 54 、-S(O)2OR 55 、-OS(O)2R 56 、-P(O)(OR 57 )(OR 58 ); Alternatively, when there are two or more selected from R f When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R g Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R g the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2; Every R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2; The 3-20 membered heterocyclyl represents a saturated or unsaturated non-aromatic ring or ring system, such as a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, such as 1, 2, 3, 4, 5 or more heteroatoms independently selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2-; The C 6-20 Aryl represents a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, or spirocyclic) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which may be a single aromatic ring or multiple aromatic rings fused together; The 5-20 membered heteroaryl group represents a monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring system having 5 to 20 ring atoms and containing 1, 2, 3, 4, 5 or more heteroatoms independently selected from N, O and S; Preferably, the cycloalkyl group may be saturated or partially saturated; Preferably, the compound does not contain compounds selected from the following compounds and / or their stereoisomers and / or their racemates:

2. The compound of formula G according to claim 1, its racemate, stereoisomer, tautomer, isotope-labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula G is selected from the compounds represented by the following formulas I, II, III, IV, V, VI, VII or VIII:

3. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula I has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in; Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; The heteroaryl ring is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substituted with an aryl substituent, R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or R2 represents hydrogen, a mono- or polycyclic C 6-20- Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in . Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted with a substituent, or R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4- 11-membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or bridged heterocyclic ring, which is unsubstituted or optionally substituted in the ortho, para or meta position by 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; R3 represents H, C 1-6 -alkyl, F, chlorine, bromine, hydroxyl, -CN, -CH2CN, -CH2COOR, -COOR, -CO-NH(CH3)C 1-3 -fluoroalkyl, (C 1-6 -alkyl)-OH, (C 1-6 -alkyl)-OCH3, (C 1-6 -alkyl)-NH2, (C 1-6 -alkyl)-N(C 1-3 -alkyl) or (C 1-6 -alkyl)-NH; R 3’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-20- Aryl, C 6-20- Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- Alkyl groups are substituted. Alternatively, R3 and R 3’ Together they represent oxo, methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 -alkyl) is substituted with a substituent; R4 represents H, C 1-6 -alkyl, F, chlorine, bromine, hydroxyl, -CN, -CH2CN, -CH2COOR, -COOR, -CO-NH(CH3)C 1-3 -fluoroalkyl, (C 1-6 -alkyl)-OH, (C 1-6 -alkyl)-OCH3, (C 1-6 -alkyl)-NH2, (C 1-6 -alkyl)-N(C 1-3 -alkyl) or (C 1-6 -alkyl)-NH; R 4’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-20- Aryl, C 6-20- Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- Alkyl groups are substituted. Alternatively, R4 and R 4’ Together they represent oxo, methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3- alkyl) is substituted by a substituent; R5 and R6 independently represent H, F, or C 1-6 -alkyl, C 1-3 -fluoroalkyl, C 1-6 -alkyl-OH, C 1-6 -Alkenyl-OCH3, C 1-6 -alkyl-NH2, C 1-6 -alkynyl-NH(C 1-3 -alkyl) and C 1-6 -alkyl-N(C 1-3 -alkyl)2; Alternatively, R1 and R3 together with the C- and N-atoms of piperidine form a saturated or partially saturated 5- or 7-membered heterocyclic group containing two or three nitrogen atoms, which may be optionally selected from -CH3, -CH2CH3, -CH2CH2CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3- alkyl) group, Alternatively, R3 and R6 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution; Alternatively, R3 and R5 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution; Alternatively, R3 and R4 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution; Alternatively, R4 and R6 together form a bridged ring of methylene, ethylene and propylene, which may optionally be selected from -CH3, -OH, -F, -CF3, -CHF2, -CH2F, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2 and O-(C 1-3 alkyl) group substitution; Alternatively, R4 and R7 together with the carbon atom to which they are attached form a double bond. For example, examples of R1 can be selected from the following groups: For example, -W-R2R 2’ Examples of can be selected from the following groups:

4. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula II has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 5-10 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocyclic ring, heteroaromatic ring, CO-NH2, CO-NH-CH3, -CO-N(CH3)2, SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 Substituents substituted; R2 represents hydrogen, a mono- or polycyclic C 6-20- Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in; Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1- 3-Alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 5-10 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-20- Aryl, C 6-20- Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. or, R2 and R 2’ together form a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, R3 represents a group selected from aryl and heteroaryl, which is independently optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or is independently optionally substituted by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 , CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; R4 represents a group selected from aryl and heteroaryl, which is independently optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or is independently optionally substituted by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; A ring represents a chemical bond, a mono- or polycyclic C 6-20- Aryl may be optionally substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or, Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20- aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of can be selected from the following groups: For example, examples of -X-R3 substituents may be selected from the following groups:

5. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula III has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted with a substituent, or R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 2.2 R 2.3 substituted by a substituent in Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20 Aryl, C 1-6 -alkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally associated heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic CC 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted with a substituent, or R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20 Aryl and NR 1.2 R 1.3 Substituents in substituted; Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20 Aryl, C 1-6 -alkyl, CC 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclic ring Base-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20 Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of can be selected from the following groups:

6. The compound of formula G according to claim 2, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula IV has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); V represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20 Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20 Aryl and NR 1.2 R 1.3 substituted by a substituent in Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 20 Aryl, C 1-6 -alkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 20 Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 or R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6- 10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 2.1 substituted with a substituent, or R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; A ring represents a chemical bond, a mono- or polycyclic C 6-20 Aryl may be optionally substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or, Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of can be selected from the following groups:

7. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotope-labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula V has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); V represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in; or, R1 represents a group selected from heterocyclic and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1- 6-alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; where R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6- 20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6- 20 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in or, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1- 6-alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; where R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6- 20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent, R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted with a substituent, or R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. or, R2 and R 2’ together form a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or, Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 Aryl, R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of substituents may be selected from the following groups:

8. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotopically labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula VI has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in or, R1 represents a group selected from heterocyclic and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1- 6-alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted with a substituent, or R2 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in; Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5- 20-membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 Substituents substituted; R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; A ring represents a chemical bond, a mono- or polycyclic C 6-20 Aryl may be optionally substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 or Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20 Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of substituents may be selected from the following groups:

9. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotopically labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula VII has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in; Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 Substituents substituted; R2 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1- 3-Alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted with a substituent, or R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 or Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of groups may be selected from the following groups:

10. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotopically labeled product, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula VIII has the following definition: in: W represents CH, O, S, N, S(O), S(O)2 or C(O), C 1-2 - alkyl, vinyl or ethynyl; X represents CH2, O, S, NH, S(O), S(O)2 or C(O); Y represents CH2, O, S, NH, S(O), S(O)2 or C(O); Z represents CH2, O, S, NH, S(O), S(O)2 or C(O); R1 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by a substituent in; Alternatively, R1 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 Substituents substituted; R2 represents hydrogen, a mono- or polycyclic C 6-20 -aryl, which may be optionally replaced by one at the ortho, para or meta position, Two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or 1, 2 or more substituents selected from OR 2.1 ,COOR 2.1 CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by a substituent in Alternatively, R2 represents a group selected from heterocycle and heteroaryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 2.2 R 2.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 substituted with an aryl substituent; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 Substituents substituted; R 2’ Indicates H, F, Me, C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 -Aryl-C 1-6 -alkyl, C 6-20 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 6-20 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3- 10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; R4 represents a group selected from aryl and heteroaryl, which is independently optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or independently optionally substituted at the ortho, para or meta positions by one, two or more halogen, OH, oxo, CF3, CHF2 and CH2F groups. Selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6- 10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by 1, 2 or more substituents; A ring represents a chemical bond, a mono- or polycyclic C 6-20 - aryl, which may be substituted at the ortho, para or meta positions by one, two or three independent fluorine, chlorine, bromine, hydroxyl, CN or NH2 groups, or by one, two or more groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1- 3-alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-10 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 or Ring A represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-10 -aryl, C 1-6 -alkyl, C 6-10 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 -aryl), 3-20 membered heterocyclyl-C 6-20 -aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20 -aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20 aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20 Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20 Aryl, 3-20 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent. For example, examples of Ring A may be selected from the following groups: For example, -W-R2R 2’ Examples of groups may be selected from the following groups:

11. The compound according to claim 2, its racemate, stereoisomer, tautomer, isotopically labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein the compound of formula IX has the following definition: in: X1 represents chemical bond, C 1-20 Alkylene, O, S, NR q , S(=O), S(=O)2 or C(=O); U stands for -(CH2) t -, O, S, NR q , S(=O), S(=O)2 or C(=O), wherein t represents 0, 1, 2 or 3; R q selected from H, halogen, OH, CN, NO2, NH2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 ); v represents 0, 1, 2, 3, 4, or 5; L represents chemical bond, C 2-20 Alkynyl or Cy; wherein L can be at any position with X1 or R c connect; Cy represents a chemical bond, a 3-20 membered heterocyclic group, C 6-20 Aryl, 5-20 membered heteroaryl, wherein the 3-20 membered heterocyclic group, C 6-20 The aryl group and the 5-20 membered heteroaryl group may be optionally fused with a 4-7 membered cycloalkyl group, provided that when the heterocyclic group contains a N atom, the heterocyclic group may be bonded to the carbon atom at the 2-position of the pyrimidine ring in formula IX through its N atom or C atom; R a represents H or -X-R3; X represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-; R3 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d4 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2; R b represents H or -Y-R4; Y represents CH2, O, S, NH, -S(O)-, -S(O)2- or -C(O)-; R4 represents H, halogen, OH, CN, -CH2CF3, -NHR d4 , unsubstituted or optionally substituted with 1, 2 or more R d5 Substituted with the following groups: C 1-20 Alkyl, -C(O)R 61 、-C(O)OR 62 、-OC(O)R 63 , NH2; The condition is R a 、R b Not at the same time H; Or, R a 、R b Together with the atoms to which it is attached, it forms an unsubstituted or optionally substituted group consisting of 1, 2 or more R d6 Substituted with the following groups: C 5-20 Cycloalkenyl, 3-20 membered heterocyclyl, 5-20 membered heteroaryl, 6-20 membered aryl; Every R d2 、R d4 、R d5 、R d6 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), SO, SO2, unsubstituted or optionally substituted by 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-CH2-C(O)R 31 、-C(O)OR 32 、-CH2C(O)OR 32 、-C(O)NHR 32 、-CH2C(O)NHR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); Alternatively, when there are two or more selected from R d2 、R d4 、R d5 、R d6 When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R e Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6-20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, 3-20 membered heterocyclyl, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); For example, the 4-10 membered heterocycloalkyl or 4-10 membered heterocycloalkenyl group may be: 1-methylpyrrolidinyl, 1-ethylpyrrolidinyl, 1-cyclopropylpyrrolidinyl, 1-cyclopropylmethylpyrrolidinyl, 5-methyl-4,5-dihydropyridazin-3(2H)-onyl, 1-methylazetidinyl, 1-methylpiperidinyl; m is an integer selected from 1 to 10; Every R e the same or different, independently selected from H, halogen, OH, CN, NO2, NH2, oxo (=O), thio (=S), O-CONH2, O-CONHR f , unsubstituted or optionally substituted with 1, 2 or more R f Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, C 1-8 -heteroalkyl C 6-20- Aryl-, C 1-8 -heteroalkyl-C 6-20- Aryl-, NH2, -C(O)R 41 、-C(O)OR 42 、-OC(O)R 43 、-S(O)2R 44 、-S(O)2OR 45 、-OS(O)2R 46 、-P(O)(OR 47 )(OR 48 ); Alternatively, when there are two or more selected from R e When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R f Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3- 20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R f the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R g Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 51 、-C(O)OR 52 、-OC(O)R 53 、-S(O)2R 54 、-S(O)2OR 55 、-OS(O)2R 56 、-P(O)(OR 57 )(OR 58 ); Alternatively, when there are two or more selected from R f When the substituents are substituted, the two substituents may be taken together with the atoms to which they are attached to form an unsubstituted or optionally substituted group with 1, 2 or more R g Substituted with the following groups: C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl; Every R g the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2; Every R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclyl, NH2; The 3-20 membered heterocyclyl represents a saturated or unsaturated non-aromatic ring or ring system, such as a 4-, 5-, 6- or 7-membered monocyclic ring, a 7-, 8-, 9-, 10-, 11- or 12-membered bicyclic ring (such as a fused ring, a bridged ring, a spirocyclic ring) or a 10-, 11-, 12-, 13-, 14- or 15-membered tricyclic ring system, and contains at least one, such as 1, 2, 3, 4, 5 or more heteroatoms independently selected from O, S and N, wherein N and S may also be optionally oxidized to various oxidation states to form nitrogen oxides, -S(O)- or -S(O)2-; The C 6-20 Aryl represents a monovalent aromatic or partially aromatic monocyclic, bicyclic (such as fused, bridged, or spirocyclic) or tricyclic hydrocarbon ring having 6 to 20 carbon atoms, which may be a single aromatic ring or multiple aromatic rings fused together; The 5-20 membered heteroaryl group represents a monovalent monocyclic, bicyclic (e.g., fused, bridged, spiro) or tricyclic aromatic ring system having 5 to 20 ring atoms and containing 1, 2, 3, 4, 5 or more heteroatoms independently selected from N, O and S. According to an embodiment of the present disclosure, L represents an alkynyl group; a mono- or polycyclic C 6-20- Aryl or a mono- or polycyclic C 6-20 - aryl and 4-7 membered cycloalkyl, which may be independently substituted at the ortho, para or meta positions by one, two, or three independent fluorine, chlorine, bromine, hydroxyl, CN, NH2 groups, or by one, two or more substituted groups selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 , CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-10- Aryl and NR 1.2 R 1.3 The substituents in substituted, or, L represents a group selected from heterocyclic or heteroaryl, which is optionally substituted at the ortho, para or meta positions by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more substituted groups selected from OR 1.1 、C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 , mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally selected from OH, OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; Heteroaryl is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; in some embodiments, L is selected from a 5-membered monocyclic heteroaryl, a 5-membered heteroarylacene ring, a 5-membered heteroaryl and 5-10 membered heteroaryl, a 5-membered heteroaryl and 4-7 membered cycloalkyl, a 5-membered heteroaryl and 4-7 membered heterocycloalkyl, a 6-membered heteroarylacene ring, a 6-membered heteroaryl and 5-10 membered heteroaryl, a 6-membered heteroaryl and 6-membered heteroaryl, a 6-membered heteroaryl and 4-7 membered cycloalkyl, and a 6-membered heteroaryl and 4-7 membered heterocycloalkyl; Cycloalkyl groups may be saturated or partially saturated; R 1.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, C 3-11 -mono- or biheterocyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1- 10- Alkyl and C 6-20- aryl; R 1.2 and R 1.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20- Aryl, 3-10 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 1.1 and COOR 1.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 1.1 substituted by a substituent. According to an embodiment of the present disclosure, examples of L may be selected from the following groups: According to an embodiment of the present disclosure, each R d2 The same or different, independently of each other, represent hydrogen, halogen, cyano, hydroxyl, CF3, C 1-6 -alkyl, C 1-3 -Fluoroalkyl, CHF2, CH2F, SO2-CH3, SO2-CH2CH3, SO2-NR 1.2 R 1.3 , C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2 or C 1-3 -alkyl-NHR 1.1 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, OR 1.1 , oxo, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in; According to an embodiment of the present disclosure, R e Can be selected from OH; Every R d6 The same or different, independently represent H, F, Me, C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 , C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, a mono- or polycyclic C 6- 20- Aryl or a mono- or polycyclic C 6-20 -aryl and 4-7 membered cycloalkyl, a mono- or polycyclic C6-20-heteroaryl and 4-7 membered cycloalkyl, C 6-10 -Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1-6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent; or Every R d6 The same or different, independently represent H, F, Me, C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 1.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 1.1 , C 1-6- Alkyl, C 2-6- Alkenyl, C 2-6- Alkynyl, C 6-10- Aryl, C 6-10 - Aryl-C 1-6 -alkyl, C 5-10 -heteroaryl-C 1-6 -alkyl, C 3-10 -heterocyclic and C 5-10 -heterocycle, -NR'R", fluorine, C 1-6- Fluoroalkyl and C 1- 6- Fluoroalkoxy, wherein R' and R" are independently selected from H and C 1-6- Alkyl; said group may in each case be optionally substituted by 1, 2 or more selected from OH, oxo, halogen, C 1-6- Alkyl and OC 1-6- substituted by an alkyl substituent. Or, two and R d6 together with the atoms to which it is attached, form a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged cycloalkyl, or a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 ; R 2.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally selected from OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 6-20- aryl; R 2.2 and R 2.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkylene, mono- or bicyclic C 6-20- Aryl, 3-10 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 2.1 and COOR 2.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 2.1 substituted by a substituent. Every R c the same or different, independently of each other, represents hydrogen, a mono- or polycyclic C 6-20 -aryl or a mono- or polycyclic C 6-20 - aryl and 4-7 membered cycloalkyl, such as C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6- 20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, or selected from 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, the above groups may be substituted at the ortho, para or meta positions by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2 substituents, or by one, two or more substituents selected from OR 4.1 ,COOR 4.1 CH2COOR 4.1 ,CH2CH2COOR 4.1 ,CH=CHCOOR 4.1 ,CO-NR 4.1 CH2CO-NR 4.1 ,CH2CH2CO-NR 4.1 ,CH=CHCO-NR 4.1 ,NR 4.2 R 4.3 ,CH2-NR 4.2 R 4.3 ,CH2CH2-NR 4.2 R 4.3 ,C 1-3 -alkyl-CN, C 1-3 -alkyl-OH, C 1-3 -alkyl-OR 4.1 、C 1-3 -alkyl-NH2, C 1-3 -alkyl-NHR 4.1 , C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 4.2 R 4.3 Substituents substituted, Or, each R c are identical or different and independently represent a group selected from heterocycle and heteroaryl, which may be optionally substituted in the ortho, para or meta position by one, two or three halogen, OH, oxo, CF3, CHF2 and CH2F groups, or by one, two or more groups selected from OR 4.1 、C 1-3 -alkyl-OR 4.1 SR 4.1 、C 1-3 -alkyl-SR 4.1 ,SO-R 4.1 ,C 1-3 -alkyl-SOR 4.1 ,SO2-R 4.1 ,C 1-3 -alkyl-SO2R 4.1 ,COOR 4.1 ,CH2COOR 4.1 ,CH2CH2COOR 4.1 ,CH=CHCOOR 4.1 ,CO-NR 4.1 CH2CO-NR 4.1 ,CH2CH2CO-NR 4.1 ,CH=CHCO-NR 4.1 ,COR 4.1 ,CH2COR 4.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-10 membered heterocyclyl-C 6-20- Aryl, 3-10 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 4.1 and NR 4.2 R 4.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 4.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 4.2 R 4.3 substituted by 1, 2 or more substituents; Heterocycle represents a 3-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused or optionally bridged ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; The heteroaryl ring is a 5-10 membered, monocyclic or bicyclic, optionally fused heteroaryl group including 1, 2, 3 or 4 heteroatoms independently selected from N, S or O; in some embodiments R4 is selected from a 5-membered monocyclic heteroaryl, a 5-membered heteroarylacene ring, a 5-membered heteroaryl and 5-10 membered heteroaryl, a 5-membered heteroaryl and 4-7 membered cycloalkyl, a 5-membered heteroaryl and 4-7 membered heterocycloalkyl, a 6-membered heteroarylacene ring, a 6-membered heteroaryl and 5-10 membered heteroaryl, a 6-membered heteroaryl and 6-membered heteroaryl, a 6-membered heteroaryl and 4-7 membered cycloalkyl, and a 6-membered heteroaryl and 4-7 membered heterocycloalkyl; Cycloalkyl groups may be saturated or partially saturated; R 4.1 Is H or selected from C 1-6- Alkyl, C 1-6- Alkyl alcohol, C 1-3 -haloalkyl, mono- or bicyclic, -C 3-10 -cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 -alkyl, 3-10 membered heterocyclic-C 1-6 -alkyl, C 3-10 -cycloalkyl-C 1-6 -alkyl, mono- or bicyclic C 6-20- Aryl, 5-20 membered heteroaryl and heterocyclic ring, which may be optionally substituted by OH, O-(C 1-3 -alkyl), halogen, C 1-10- Alkyl and C 5-10 substituted with an aryl substituent; R 4.2 and R 4.3 independently represent H or selected from C 1-6- Alkyl, mono- or bicyclic C 3-10- Cycloalkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, mono- or bicyclic C 6-20- Aryl, 3-10 membered heterocycle, heteroaromatic ring, CO-NH2, CO-NH - CH3、-CO-N(CH3)2、SO2-(C 1-3 -alkyl), CO-R 4.1 and COOR 4.1 A group, which may be optionally substituted by 1, 2 or more selected from OH, halogen, C 1-6 -alkyl, C 6-20- Aryl and COOR 4.1 Substituents substituted; For example, the 4-10 membered heterocyclic group or 4-10 membered heterocycloalkenyl group can be: 1-methylpyrrolidinyl, 1-ethylpyrrolidinyl, 1-cyclopropylpyrrolidinyl, 1-cyclopropylmethylpyrrolidinyl, 5-methyl-4,5-dihydropyridazin-3(2H)-one, 1-methylazetidinyl, 1-methylpiperidinyl.

12. The compound according to any one of claims 1 to 11, its racemate, stereoisomer, tautomer, isotope-labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt or prodrug, wherein: R1 represents hydrogen, a mono- or polycyclic C 6-20 Aryl, which may be optionally substituted at the ortho, para or meta positions by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO - NHOH, -CO - NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, CN, NO2, NH2, or substituted by 1, 2 or more substituents selected from OR 1.1 ,COOR 1.1 CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,NR 1.2 R 1.3 ,CH2-NR 1.2 R 1.3 ,CH2CH2-NR 1.2 R 1.3 ,C 3-10 -cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20- Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-20- Aryl, SO2-CH3, SO2-CH2CH3 and SO2-NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO - NHOH, -CO - NHOH, -C 1-3- Alkyl-NH - CO - NR 1.2 R 1.3 、-NR 1.1 CN, -CHO,, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 、-OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in; wherein R 1.1 、R 1.2 、R 1.3 has the meaning given above; Alternatively, R1 represents a group selected from heterocyclic and heteroaryl groups, which may be optionally substituted in the ortho, para or meta positions by one, two or three halogens, OH, CN, NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO - NHOH, -CO - NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, nitro, oxo, CF3, CHF2 and CH2F, or substituted by 1, 2 or more selected from OR 1.1 、C 1-3 -alkyl-OR 1.1 SR 1.1 、C 1-3 -alkyl-SR 1.1 ,SO-R 1.1 ,C 1-3 -alkyl-SOR 1.1 ,SO2-R 1.1 ,C 1-3 -alkyl-SO2R 1.1 ,COOR 1.1 ,CH2COOR 1.1 ,CH2CH2COOR 1.1 ,CH=CHCOOR 1.1 ,CO-NR 1.1 CH2CO-NR 1.1 ,CH2CH2CO-NR 1.1 ,CH=CHCO-NR 1.1 ,COR 1.1 ,CH2COR 1.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 1.1 and NR 1.2 R 1.3 substituted by a substituent, each of which may be optionally substituted by OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO - NHOH, -CO-NHOH, -C 1-3- Alkyl-NH - CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 , OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by one, two or more substituents; wherein R 1.1 、R 1.2 、R 1.3 has the meaning given above; Alternatively, R2 represents hydrogen, a mono- or polycyclic C 6-20 Aryl may be substituted at the ortho, para or meta position by one, two or three fluorine, chlorine, bromine, iodine, hydroxyl, CN, NO2, NH2, or by one, two or more substituents selected from OR 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,C(CH3)2COOR 2.1 ,CF2COOR 2.1 ,CHFCOOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 ,CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,NR 2.2 R 2.3 ,CH2-NR 2.2 R 2.3 ,CH2CH2-NR 2.2 R 2.3 ,C 3-10 -cycloalkyl, COOR 2.1 -C 3-8- Cycloalkyl, CO-NR 2.1 -C 3-8- Cycloalkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, C 1-6 -alkyl, C 1-3 -fluoroalkyl, CF3, CHF2, CH2F, C 6-20 Aryl-C 1-6 -alkyl, 3-20 membered heterocyclic-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6- Alkyl, C 6-10 -aryl, C 1-3 -alkyl-SOR 2.1 、C 1-3 -alkyl-SO2R 2.1 , SO2-CH3, SO2-CH2CH3 and SO2-NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by 1, 2 or more substituents selected from OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3 -alkyl-CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 , OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 2.2 R 2.3 Substituted by the substituent in CCOOR 2.1 ; Among them, R 2.1 、R 2.2 、R 2.3 has the meaning given above; Alternatively, R2 represents a group selected from heterocyclic and heteroaryl groups, which may be optionally substituted in the ortho, para or meta positions by one, two or three halogens, OH, CN, NH2, -NHOH, -C 1-3 -alkyl-NHOH, -C 1-3 -alkyl-CO - NHOH, -CO-NHOH, -C 1-3 -alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, nitro, oxo, CF3, CHF2 and CH2F, or substituted by 1, 2 or more selected from OR 2.1 、C 1-3 -alkyl-OR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,COOR 2.1 -C 3-8 -cycloalkyl, CO-NR 2.1 -C 3-8 -cycloalkyl, CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20 Aryl, C 1-6 -alkyl, C 6-20 -Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6- 20 aryl), 3-20 membered heterocyclyl-C 6-20 Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 and NR 2.2 R 2.3 substituted by a substituent, each of which may be optionally substituted by OH, OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-20- Aryl and NR 2.2 R 2.3 substituted by one, two or more substituents; wherein R 2.1 、R 2.2 、R 2.3 has the meaning given above; Alternatively, R2 and R 2’ Together with the atoms to which it is attached, it forms a 4-11 membered, monocyclic or bicyclic, saturated or partially saturated, optionally fused combination or optionally bridged heterocyclic ring containing 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, said heterocyclic ring being unsubstituted or optionally substituted in the ortho, para or meta position with 1, 2 or more substituents selected from the group consisting of halogen, OH, oxo, CF3, CHF2, CH2F, OR 2.1 、C 1-3 -alkyl-OR 2.1 、C 1-3 -alkyl-OC 1-3 -alkyl-COOH, C 1-3 -alkyl-OC 1-3 -alkyl-CONR 2.1 、C 1-3 -alkyl-phosphoric acid, C 1-3 -alkyl-OC(O)-OR 2.1 、C 1-3 -alkyl-OC(O)-NR 2.1 、C 1-3 -alkyl-OC(=O)-C 1-3 -alkyl-(OC 1-3 -alkyl)v, C 1-3 -alkyl-OC(=O)-C 1-6 -alkyl-COOR 2.1 、C 1-3 -alkyl-NC(=O)-C 1-6 -alkyl-COOR 2.1 、C 1-3 -alkyl-NC(=O)-OC 1-6 -alkyl-COOR 2.1 、C 1-3 -alkyl-NC(=O)-NC 1-6 -alkyl-COOR 2.1 SR 2.1 、C 1-3 -alkyl-SR 2.1 ,SO-R 2.1 ,C 1-3 -alkyl-SOR 2.1 ,SO2-R 2.1 ,C 1-3 -alkyl-SO2R 2.1 ,COOR 2.1 ,CH2COOR 2.1 ,CH2CH2COOR 2.1 ,CH=CHCOOR 2.1 ,CO-NR 2.1 ,CH2CO-NR 2.1 ,CH2CH2CO-NR 2.1 ,CH=CHCO-NR 2.1 ,COR 2.1 ,CH2COR 2.1 ,C 1-6 -alkyl alcohol, mono- or bicyclic C 3-10 -cycloalkyl, C 6-20- Aryl, C 1-6 -alkyl, C 6-20- Aryl-C 1-6 -alkyl, 5-20 membered heteroaryl-C 1-6 Alkyl, C 1-3 -alkyl-(monocyclic or polycyclic-C 6-20- aryl), 3-20 membered heterocyclyl-C 6-20- Aryl, 3-20 membered heterocyclic ring, 5-20 membered heteroaryl C 1-3 -alkyl-OR 2.1 NR 2.2 R 2.3 、C 6-20- Aryl and NR 2.2 R 2.3 Each of the substituents may be optionally replaced by one, two or more substituents selected from OH, CN, C 1-3 -alkyl-CN, C 1-3 -alkyl-NH2, -SH, -NH2, -NHOH, -C 1-3- Alkyl-NHOH, -C 1-3- Alkyl-CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO - NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 、 CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 、-OR 1.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6 -alkyl, C 6-20- Aryl and NR 1.2 R 1.3 substituted by a substituent in which R 2.1 、R 1.2 、R 1.3 , v has the meaning given above; Or, each R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 、R 41 、R 42 、R 43 、R 44 、R 45 、R 46 、R 47 、R 48 、R 51 、R 52 、R 53 、R 54 、R 55 、R 56 、R 57 、R 58 the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, 5-20 membered heteroaryl, 3-20 membered heterocyclic group, NH2; each of the above groups may be optionally replaced by OH, CN, C 1-3 -alkyl-CN, -SH, -NH2, -NHOH, -C 1-3 -alkyl-NHOH, -C 1-3 -alkyl-CO-NHOH, -CO-NHOH, -C 1-3- Alkyl-NH-CO-NR 1.2 R 1.3 、-NR 1.1 CN, -CHO, C 2-6 -alkenyl, -OC 3-8 -cycloalkyl, COOR 1.1 、C 1-3 -alkyl-COOR 1.1 , CONHR 1.1 、C 1-3 -alkyl-CONHR 1.1 , OR 2.1 , oxo, halogen, CF3, CHF2, CH2F, C 1-6- Alkyl, C 6-10- Aryl and NR 1.2 R 2.3 substituted by one, two or more substituents; wherein R 1.1 、R 1.2 、R 2.1 、R 2.3 has the meaning given above; Or, each R c the same or different, independently selected from H, halogen, OH, CN, NO2, oxo (=O), thio (=S), unsubstituted or optionally substituted with 1, 2 or more R e Substituted with the following groups: C 1-20 Alkyl, C 2-20 Alkenyl, C 2-20 Alkynyl, C 3-20 Cycloalkyl, C 3-20 Cycloalkenyl, C 3-20 Cycloalkynyl, C 6-20 Aryl, C 1-6 Alkyl-C 4-10 Heterocycloalkyl, C 1-6 Alkyl-C 4-10 Heterocycloalkenyl, C 1-6 Alkyl-C 6-20 Aryl, C 1-6 Alkyl-C 5-20 Heteroaryl, 5-20 membered heteroaryl-OC 6-20 Aryl-, 5-20 membered heteroaryl-NC 6-20 Aryl-, 5-20 membered heteroaryl-SC 6-20 Aryl-, 5-20 membered heteroaryl-CH2-C 6-20 Aryl-, C 4-10 Cycloalkyl C 6-20 Aryl-, 4-10 membered heterocycloalkyl and C 6-20 Aryl-, 4-10 membered heterocycloalkenyl and C 6-20 Aryl-, C 4-10 Cycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkyl-C 6-20 Aryl-, 4-10 membered heterocycloalkenyl-C 6-20 Aryl-, 5-20 membered heteroaryl, C 4-10 Cycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl and 5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl and 5-20 membered heteroaryl-, C 4-10 Cycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkyl-5-20 membered heteroaryl-, 4-10 membered heterocycloalkenyl-5-20 membered heteroaryl-, 3-20 membered heterocyclyl, C 1-20 Alkyloxy, C 2-20 Alkenyloxy, C 2-20 Alkynyloxy, C 3-20 Cycloalkyloxy, C 3-20 Cycloalkenyloxy, C 3-20 Cycloalkynyloxy, C 6-20 Aryloxy, 5-20 membered heteroaryloxy, 3-20 membered heterocyclyloxy, C 1-20 Alkylthio, C 2-20 Alkenylthio, C 2-20 Alkynylthio, C 3-20 Cycloalkylthio, C 3-20 Cycloalkenylthio, C 3-20 Cycloalkynylthio, C 6-20 Arylthio, 5-20 membered heteroarylthio, 3-20 membered heterocyclylthio, NH2, -C(O)R 31 、-C(O)OR 32 、-OC(O)R 33 、-S(O)2R 34 、-S(O)2OR 35 、-OS(O)2R 36 、-P(O)(OR 37 )(OR 38 ); where R 31 、R 32 、R 33 、R 34 、R 35 、R 36 、R 37 、R 38 has the meaning given above; Alternatively, the compound is selected from the following compounds:

13. A method for preparing the compound according to any one of claims 1 to 12, its racemate, stereoisomer, tautomer, isotopically labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt, or prodrug, wherein the method comprises reacting a compound of formula A1 with a compound of formula B1 to obtain a compound of formula H: and optionally, derivatizing the compound of formula G into a stereoisomer, tautomer, isotopically labeled form, solvate, polymorph, metabolite, pharmaceutically acceptable salt, or prodrug thereof; in, LG is a leaving group, for example, Cl, Br or I; X1, L, W, R a 、R b 、R c , R2, R 2’ , m independently have the definitions in any one of claims 1-11.

14. A pharmaceutical composition comprising a therapeutically effective amount of at least one of the compound of any one of claims 1 to 12 (e.g., any one of the compounds of Formulae I to IX), its racemate, stereoisomer, tautomer, isotopically labeled form, solvate, polymorph, pharmaceutically acceptable salt, or prodrug compound thereof.

15. A method for preventing or treating a disease, comprising administering to a patient in need thereof at least one of the compound of any one of claims 1 to 12 (e.g., one of the compounds of Formulae I to IX), its racemate, stereoisomer, tautomer, isotope-labeled form, solvate, polymorph, pharmaceutically acceptable salt, or prodrug thereof; The disease may be a PDE4B-mediated disease, or a disease mediated at least by PDE4; Preferably, the disease includes but is not limited to respiratory inflammatory diseases, inflammatory bowel diseases, arthritic diseases, skin inflammatory diseases, eye inflammatory diseases and diseases of the peripheral or central nervous system, degenerative diseases of the central nervous system, Alzheimer's Disease (AD), non-alcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) or pulmonary hypertension associated therewith, chronic obstructive pulmonary disease (COPD) or pulmonary hypertension associated therewith, hepatic fibrosis (HF), renal fibrosis, benign prostatic hyperplasia (BPH), gastroesophageal reflux disease. Gastroesophageal Reflux disease, obstructive sleep apnea, and coronary artery disease or cancer; Preferably, the cancer includes but is not limited to one selected from the group consisting of: stomach cancer, bladder cancer, blood cancer, bone cancer, brain cancer, breast cancer, central nervous system cancer, cervical cancer, colon cancer, endometrial cancer, esophageal cancer, gallbladder cancer, gastrointestinal cancer, external genital cancer, urogenital tract cancer, head cancer, kidney cancer, laryngeal cancer, liver cancer, lung cancer, muscle tissue cancer, cervical cancer, oral or nasal mucosal cancer, ovarian cancer, pancreatic cancer, prostate cancer, skin cancer, spleen cancer, small intestine cancer, large intestine cancer, testicular cancer and / or thyroid cancer; Preferably, the lesions of the disease include the respiratory system, digestive system, excretory system and / or reproductive system, such as the lungs, liver, kidneys and / or prostate.

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