2-(1h-indol-4-yl) methyl) 2h-indazole derivatives as factor b inhibitors

Abstract

The present invention relates to compounds of formula (I) having an indole moiety attached to an indazole moiety, compounds having core-like structures and related salts, solvates, prodrugs and pharmaceutical compositions. The invention also relates to methods of synthesizing such compounds and to the use of such compounds in the treatment and prophylaxis of medical conditions and diseases, most particularly by Factor B inhibition.

Description

Technical Field

[0001] This invention relates to compounds having an indole moiety linked to an indazole moiety, compounds having similar core structures, and related salts, solvates, prodrugs, and pharmaceutical compositions. The invention also relates to methods for synthesizing such compounds, and the use of such compounds, most particularly through factor B inhibition, in the treatment and prevention of medical conditions and diseases. Background Technology

[0002] The complement system is an important part of the innate immune system and helps the body fight pathogen infections, ultimately leading to inflammation and phagocytosis to remove pathogens or foreign particles.

[0003] The complement system comprises various proteins, including zymogens, which are activated through proteolytic cleavage and promote the activation of other zymogens in a cascade reaction. Proteins can be zymogens or proteins without potential enzymatic activity, whose conformational changes reveal binding sites for other components of the system. These successive enzymatic cleavages lead to large, amplified reactions, and numerous regulatory components exist within this system to prevent uncontrolled activation.

[0004] The complement system can be activated via three pathways: the classical pathway, the lectin pathway, and the alternative pathway. The classical pathway is triggered by antigen:antibody complexes and links the innate and adaptive immune systems. The lectin pathway is directly triggered by pathogens when serum protein mannan binds to lectins, collagen lectins, or ficolins that bind to mannan-containing carbohydrates in bacteria or viruses. The alternative pathway (also known as the alternative pathway) is initiated by the activation of the central complement component C3 through spontaneous hydrolysis or enzymatic cleavage. The alternative pathway also acts as a key amplifying loop for complement activation of all three pathways.

[0005] Ultimately, all these pathways lead to the generation of C3 convertases, which cleave and activate other C3 molecules to promote: 1) opsonization of pathogens so that they can be phagocytosed by phagocytes that recognize key receptors; 2) recruitment of inflammatory cells by generating chemical attractants at activation sites; and 3) the formation of C5 convertases, leading to the production of C5a and C5b, which induce direct killing of pathogens by assembling terminal complement components to form membrane attack complex (MAC) pores in the membranes of bacteria or other target cells (Janeway, CA Jr). et al., (2001) The complement system and innateimmunity, in Immunobiology: The Immune System in Health and Disease, GarlandScience, New York).

[0006] Factor B is a trypsin-like serine protease and an element of the alternative pathway in the complement cascade. It exists in its prozymogen form in the cycle until the pathway is activated (Schubart, A). et al. , Proc. Natl. Acad. Sci. USA 2019, 116, 7926-7931).

[0007] Spontaneous steady-state hydrolysis of C3 leads to the formation of C3(H2O). Factor B can bind to the active forms of C3: C3(H2O) and C3b, generating the proenzyme C3bB (or C3(H2O)B), which is a target of factor D activation. Upon cleavage by factor D, two fragments are generated: Ba and Bb (Schwaeble, WJ, Ali, YM and Sim, RB, (2020) Chapter 14 - The Roles and Contributions of the Complement System in the Pathophysiology of Autoimmune Diseases, in The Autoimmune Diseases (Sixth Edition) (Rose, NR and Mackay, IR eds.), Academic Press). Ba is released, and Bb, containing a serine protease domain, still binds to C3(H2O) and C3b, forming alternative pathway C3 convertases [C3(H2O)Bb and C3bBb]. These trigger the amplification loop by converting C3 to C3a and more C3b. Adding another C3b to the C3 convertase generates the C5 convertase (C3bBbC3b) (Laskowski, J., Thurman, JM (2018) Chapter 14 - Factor B, in The Complement Facts Book (Second Edition) (Barnum, S. and Schein, T. eds.), Academic Press). The C5 convertase cleaves C5 to generate anaphylatoxins C5a and C5b, which act as a platform for the formation of the membrane attack complex.

[0008] Dysregulation of the alternative complement pathway due to genetic factors or the presence of autoantibodies can cause a variety of diseases. Therefore, inhibitory factor B is a key therapeutic target for regulating the alternative pathway and thus for treating a wide range of diseases, conditions, and symptoms.

[0009] Iptacopan (LNP023) was disclosed on Mainolfi et al. In J. Med. Chem., 2020, Vol. 63, pp. 5697-5722, there is a known factor B inhibitor with the following structure: Iptacopan exhibits high selectivity for factor B and has no inhibitory effect on factor D, the classical complement pathway, or the lectin complement pathway. Furthermore, no significant effects were observed in a wide range of receptor, ion channel, kinase, and protease assays (Schubart, A). et al. (Proc. Natl. Acad. Sci. USA 2019, 116, 7926-7931). The drug recently underwent a successful Phase III clinical trial in patients with paroxysmal nocturnal hemoglobinuria (PNH) (Novartis Press Release, “Novartis Phase III APPOINT-PNH trialshows investigational oral monotherapy iptacopan improves hemoglobin to near-normal levels, leading to transfusion independence in all treatment-naïve PNH patients”, April 26, 2023).

[0010] Other indole derivatives allegedly possessing factor B inhibitory activity are disclosed in WO 2013 / 164802 A1, US 2013 / 0296377 A1, WO 2014 / 143638 A1, WO 2015 / 009616 A1, WO 2022 / 028507 A1, WO 2022 / 028527 A1, WO 2022 / 143940 A1, WO 2022 / 143845 A1, WO 2022 / 155294 A1, WO 2022 / 218429 A1, WO 2022 / 256586 A2, WO 2023 / 278698 A1, WO 2023 / 020566 A1, WO 2023 / 072197 A1, WO 2023 / 139534 A1, WO 2023 / 187715 A1 and WO 2024 / 049977 A1.

[0011] However, there is a need to provide other factor B inhibitors, particularly selective factor B inhibitors (e.g., compared to inhibitors of factor D, classical complement, and / or lectin complement activation). In particular, there is a need to provide compounds with improved pharmacological and / or physiological and / or physicochemical properties, and / or those that provide available alternatives to known compounds. Summary of the Invention

[0012] The first aspect of the present invention provides a compound of formula (I): Formula (I) in: R 1 It is hydrogen; R 2 Selected from hydrogen or halogen groups; R 3 Selected from hydrogen or halogen groups, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 4The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 5 Selected from hydrogen or halogen groups; R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; or R 3 and R 7 , or R 4 and R7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom; X 9 Is it N or CR? 9 ; R 9 It is a hydrogen or halogen group, -OH, -SH, -NH2, -SO2NH2, or C1-C. 12 Saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon groups may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon groups may optionally be substituted by one or more halogen groups, wherein the hydrocarbon groups may optionally contain one or more heteroatoms, each independently selected from N, O and S, in their carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; X 10 Is it N or CR? 10 ; X 11 Is it N or CR? 11 ; X 12 Is it N or CR? 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than two of them are N; and Each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

[0013] A second aspect of the present invention provides a compound of formula (II): Equation (II) in: R 1 It is hydrogen; R 4 The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 5 Selected from hydrogen or halogen groups; R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; X 9 Is it N or CR? 9 ; R 9 It is a hydrogen or halogen group, -OH, -SH, -NH2, -SO2NH2, or C1-C. 12 Saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon groups may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon groups may optionally be substituted by one or more halogen groups, wherein the hydrocarbon groups may optionally contain one or more heteroatoms, each independently selected from N, O and S, in their carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; X 10 Is it N or CR? 10 ; X 11 Is it N or CR? 11 ; X 12 Is it N or CR? 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than two of them are N; Each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12Saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon groups may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon groups may optionally be substituted by one or more halogen groups, wherein the hydrocarbon groups may optionally contain one or more heteroatoms, each independently selected from N, O and S, in their carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; Each R 14 and R 15 Independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted; R 16 Selected from hydrogen or fluorine, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl; or R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted; or R 17 and R 7 , or R 4 and R 7Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0014] In the context of this specification, a "hydrocarbon" substituent or the hydrocarbon moiety in a substituent comprises only carbon and hydrogen atoms, but does not contain any heteroatoms such as N, O, or S in its carbon skeleton unless otherwise stated. The hydrocarbon group / mole can be saturated or unsaturated (including aromatics), and can be linear or branched, or can be or include cyclic groups, wherein, unless otherwise stated, said cyclic groups do not contain any heteroatoms such as N, O, or S in their carbon skeleton. Examples of hydrocarbon groups include alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl groups / molecules, as well as combinations of all these groups / molecules. Typically, the hydrocarbon group is C1-C. 20 Hydrocarbon group. More typically, the hydrocarbon group is C1-C. 15 Hydrocarbon group. More typically, the hydrocarbon group is C1-C. 10 Hydrocarbon group. "Hydrocarbon group" is defined in a similar manner as a divalent hydrocarbon group.

[0015] The alkyl substituent or the alkyl moiety in a substituent can be linear (i.e., straight-chained) or branched. Examples of alkyl groups / molecular parts include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, and n-pentyl groups / molecular parts. Unless otherwise specified, the term "alkyl" does not include "cycloalkyl". Typically, alkyl is C1-C6. 12 Alkyl. More typically, alkyl is a C1-C6 alkyl. “Alkylene” is defined similarly as a divalent alkyl.

[0016] The term "alkenyl" or the alkenyl moiety in a substituent refers to an unsaturated alkyl group or moiety having one or more carbon-carbon double bonds. Examples of alkenyl groups / molecular parts include vinyl, propenyl, 1-butenyl, 2-butenyl, 1-pentenyl, 1-hexenyl, 1,3-butadienyl, 1,3-pentadienyl, 1,4-pentadienyl, and 1,4-hexadienyl groups / molecular parts. Unless otherwise specified, the term "alkenyl" does not include "cycloalkenyl". Typically, alkenyl groups are C2-C... 12Alkenyl. More typically, alkenyl groups are C2-C6 alkenyl groups. "Alkenyl" is defined in a similar manner as a divalent alkenyl group.

[0017] The term "alkynyl" in a substituent or the alkynyl moiety within a substituent refers to an unsaturated alkyl group or moiety having one or more carbon-carbon triple bonds. Examples of alkynyl groups / molecular parts include ethynyl, propynyl, buty-1-alkynyl, and buty-2-alkynyl groups / molecular parts. Typically, the alkynyl group is C2-C. 12 Alkynyl group. More commonly, the alkynyl group is a C2-C6 alkynyl group. "Idemynyl" is defined in a similar manner as a divalent alkynyl group.

[0018] A “cyclic” substituent, or the cyclic portion of a substituent, refers to any hydrocarbon ring, which may be saturated or unsaturated (including aromatic rings) and may include one or more heteroatoms, such as N, O, or S, in its carbon skeleton. Examples of cyclic groups include cycloalkyl, cycloalkenyl, heterocyclic, aryl, and heteroaryl groups, as discussed below. Cyclic groups can be monocyclic, bicyclic (e.g., bridged, fused, or spirocyclic), or polycyclic. Typically, cyclic groups are 3 to 12-membered cyclic groups, meaning they contain 3 to 12 ring atoms. More typically, cyclic groups are 3 to 7-membered monocyclic groups, meaning they contain 3 to 7 ring atoms.

[0019] To avoid ambiguity, when a bicyclic or polycyclic group or portion is described as “saturated,” it should be understood that all ring systems within the bicyclic or polycyclic group or portion (excluding any ring systems that are part of or formed by optional substituents) are saturated.

[0020] A "heterocyclic" substituent or heterocyclic portion of a substituent refers to a cyclic group or portion that contains one or more carbon atoms and one or more (such as one, two, three, or four) heteroatoms (e.g., N, O, or S) in a ring structure. Examples of heterocyclic groups include heteroaryl and non-aromatic heterocyclic groups discussed below, such as azirrobutyl, oxoheterobutyl, thioheterobutyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrazolyl, imidazoalkyl, dioxopentyl, oxothioheteropentyl, piperidinyl, tetrahydropyranyl, thianyl, piperazine, dioxane, morpholinyl, and thiomorpholinyl groups.

[0021] A “cycloalkyl” substituent or the cycloalkyl moiety in a substituent refers to a saturated hydrocarbon ring containing, for example, 3 to 7 carbon atoms, examples of which include cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. Unless otherwise stated, a cycloalkyl substituent or moiety may include a monocyclic, bicyclic, or polycyclic hydrocarbon ring.

[0022] A “cycloalkenyl” substituent or the cycloalkenyl moiety in a substituent refers to a non-aromatic unsaturated hydrocarbon ring having one or more carbon-carbon double bonds and containing, for example, 3 to 7 carbon atoms, examples of which include cyclopent-1-en-1-yl, cyclohex-1-en-1-yl, and cyclohex-1,3-dien-1-yl. Unless otherwise stated, a cycloalkenyl substituent or moiety may include a monocyclic, bicyclic, or polycyclic hydrocarbon ring.

[0023] The term "aryl" refers to an aromatic hydrocarbon ring, or the aryl portion of a substituent. The term "aryl" refers to both monocyclic and polycyclic aromatic hydrocarbons, where all fused-ring systems (excluding any ring system that is part of an optional substituent or formed by an optional substituent) are aromatic. Examples of aryl groups / parts include phenyl, naphthyl, anthracene, and phenanthrene. Unless otherwise stated, the term "aryl" does not include "heteroaryl".

[0024] The term "heteroaryl" refers to an aromatic heterocyclic group or part thereof. The term "heteroaryl" refers to both monocyclic and polycyclic fused-ring aromatic heterocycles, wherein all fused-ring systems (excluding any ring system that is part of an optional substituent or formed by an optional substituent) are aromatic. Examples of heteroaryl groups / parts include the following: Where G = O, S, or NH. Specific examples of 5- or 6-membered heteroaryl groups include furanyl, thiopheneyl, pyrroleyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, furazanyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and triazinyl.

[0025] Unless otherwise stated, when a bicyclic or polycyclic group or portion is described as aromatic (such as aryl or heteroaryl), it should be understood that all ring systems within the bicyclic or polycyclic group or portion (excluding any ring systems that are part of or formed by optional substituents) are aromatic. Similarly, when a bicyclic or polycyclic group or portion is described as non-aromatic (such as cycloalkyl, cycloalkenyl) or non-aromatic heterocyclic group, it should be understood that all ring systems within the bicyclic or polycyclic group or portion (excluding any ring systems that are part of or formed by optional substituents) are non-aromatic.

[0026] For the purposes of this specification, when a combination of multiple parts is referred to as a single group, such as arylalkyl, arylalenyl, arylynyl, alkylaryl, alkenylaryl, or ynylaryl, the last part mentioned contains an atom through which the group is attached to the remainder of the molecule. An example of an arylalkyl group is benzyl.

[0027] As should be understood, in the optional replacement section: - Each hydrogen atom may be optionally substituted by any specified monovalent substituent; - Any two hydrogen atoms attached to the same carbon or nitrogen atom may optionally be replaced by any designated π-bond substituent; - Any sulfur atom may optionally be substituted by one or two of any specified π-bonded substituents; and - Any two hydrogen atoms attached to the same or different atoms within the same optionally substituted group or portion may optionally be replaced by any designated divalent bridging substituent.

[0028] Typically, the substituted group contains 1, 2, 3 or 4 substituents, more usually 1, 2 or 3 substituents, more usually 1 or 2 substituents, and more usually 1 substituent.

[0029] Unless otherwise specified, optionally substituted groups or portions (e.g., R) 1 Any divalent bridging substituent (e.g., -O-, -S-, -NH-, -CH2-, -CH2-CH2-, etc.) must attach only to the specified group or part and may not attach to a second group or part (e.g., R). 2 ) Attachment, even if the second group or part itself may optionally be substituted.

[0030] The term "halogen" includes fluorine, chlorine, bromine, and iodine.

[0031] Unless otherwise stated, when a group is prefixed with the term "halogen," such as a haloalkyl or halomethyl group, it should be understood that the group in question is substituted by one or more halogen groups independently selected from fluorine, chlorine, bromine, and iodine. Generally, the maximum number of halogen substituents is limited only by the number of hydrogen atoms available for substitution on the corresponding group without the halogen prefix. For example, a halomethyl group may contain one, two, or three halogen substituents. A haloethyl or halophenyl group may contain one, two, three, four, or five halogen substituents. Similarly, unless otherwise stated, when a group is prefixed with a specific halogen group, it should be understood that the group in question is substituted by one or more of that specific halogen group. For example, the term "fluoromethyl" refers to a methyl group substituted by one, two, or three fluorine groups.

[0032] Similarly, unless otherwise stated, when a group is referred to as "halo-substituted," it should be understood that the group in question is substituted by one or more halogen groups independently selected from fluorine, chlorine, bromine, and iodine. Generally, the maximum number of halogen substituents is limited only by the number of hydrogen atoms that can be substituted on the group referred to as halo-substituted. For example, a halo-substituted methyl group may contain one, two, or three halogen substituents. A halo-substituted ethyl group or a halo-substituted phenyl group may contain one, two, three, four, or five halogen substituents.

[0033] Unless otherwise stated, any reference to an element shall be regarded as a reference to all isotopes of that element. Thus, for example, unless otherwise stated, any reference to hydrogen shall be regarded as covering all isotopes of hydrogen, including deuterium and tritium.

[0034] Unless otherwise stated, any reference to a compound or group shall be regarded as a reference to all tautomers of the compound or group.

[0035] When referring to a hydrocarbon group or other group that contains one or more heteroatoms N, O, or S in its carbon skeleton, or when referring to a hydrocarbon group or other group whose carbon atoms are replaced by N, O, or S atoms, the intention is: quilt Substitute; quilt Substitute; -CH2- is replaced by -NH-, -O- or -S-; -CH3 is replaced by -NH2, -OH or -SH; -CH= is replaced by -N=; CH2= is replaced by NH=, O= or S=; or CH≡ is replaced by N≡; The prerequisite is that the resulting group contains at least one carbon atom. For example, methoxy, dimethylamino, and aminoethyl are considered hydrocarbon groups that contain one or more heteroatoms N, O, or S in their carbon skeleton.

[0036] Typically, the compounds of the present invention contain no more than one quaternary ammonium group. More typically, the compounds of the present invention do not contain any quaternary ammonium groups.

[0037] In the context of this specification, unless otherwise stated, C x -C y A group is defined as a group containing x to y carbon atoms. For example, C1-C4 alkyl groups are defined as alkyl groups containing 1 to 4 carbon atoms. (The last sentence appears to be incomplete and possibly refers to a different context.) x -C y The purpose of assigning x and y to the group is to exclude the optional substituents when calculating the total number of carbon atoms in the parent group substituted by the optional substituents. To avoid ambiguity, when calculating C... x -C y When determining the number of carbon atoms in a group, substituted heteroatoms (such as N, O, or S) are not counted as carbon atoms. For example, the morpholino group is considered a C4 heterocyclic group rather than a C6 heterocyclic group.

[0038] For the purposes of this specification, when a statement is made that a first atom or group is "directly attached" to a second atom or group, it should be understood that the first atom or group is covalently bonded to the second atom or group, and there are no one or more intermediary atoms or groups. Thus, for example, in the group (C=O)N(CH3)2, the carbon atom of each methyl group is directly attached to the nitrogen atom and the carbonyl group is directly attached to the nitrogen atom, but the carbonyl group carbon atom is not directly attached to the carbon atom of any methyl group.

[0039] As described in the first aspect of the invention, R 2 Selected from hydrogen or halogen groups. In one embodiment, R... 2 Selected from hydrogen, fluorine, chlorine, or bromine groups. Most commonly, R 2 It is hydrogen.

[0040] As described in the first aspect of the invention, R 3 Selected from hydrogen or halogen groups, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, or R 3 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0041] In one implementation, R 3The hydrocarbon group is selected from hydrogen or halogen, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

[0042] In one aspect of this implementation scheme, R 3 Selected from hydrogen or halogen groups (e.g., fluorine, chlorine, or bromine), -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 31 Group, wherein R 31 It is a 3- to 6-membered monocyclic group, wherein the 3- to 6-membered monocyclic group may optionally be replaced by one or more halogen groups (e.g., fluorine, chlorine, or bromine) and / or one or two R groups. 32 Replace, where each R 32 Independently selected from methyl or fluoromethyl groups, provided that the R group is present. 3 (Including any optional substituents) contains no more than 8 carbon atoms. Typically, in this embodiment, R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from C1-C4 alkyl, C1-C4 fluoroalkyl or -R 31 Group, wherein R 31 Selected from C3-C6 cycloalkyl, 4- to 6-membered saturated heterocyclic groups, or phenyl, or 5- or 6-membered heteroaryl groups, wherein the C3-C6 cycloalkyl and 4- to 6-membered saturated heterocyclic groups may optionally be converted by one or more fluorine groups and / or one or two R groups. 32 Substitution, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be replaced by one or more fluorine, chlorine, and / or bromine groups and / or one or two R groups. 32 Substitution, provided that the group R 3 (Including any optional substituents) contains no more than 8 carbon atoms. More typically, in this embodiment, R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -R 31-CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from methyl or fluoromethyl, wherein R 31 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 replace.

[0043] In another aspect of this implementation scheme, R 3 Selected from hydrogen or halogen groups (e.g., fluorine, chlorine, or bromine), -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 It is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in this embodiment, R... 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from methyl or fluoromethyl.

[0044] In another aspect of this implementation scheme, R 3 Selected from hydrogen or halogen (e.g., fluorine, chlorine, or bromine), -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in this embodiment, R... 3 It is selected from hydrogen or fluorine, chlorine, bromine, -CN or methyl, wherein the methyl group may optionally be fluorine-substituted.

[0045] More typically, R 3 Selected from hydrogen, fluorine, chlorine, or bromine groups. Most commonly, R 3 It is hydrogen.

[0046] In another embodiment of the first aspect of the invention, R 3 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R.8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0047] Typically, when R 3 and R 7 When they are combined to form an alkylene group, the alkylene group (including any optional substituents) contains no more than four carbon atoms.

[0048] Typically, by R 3 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any formed alkylene group (including any optional substituents) does not exceed three. More generally, it is formed by R 3 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any formed alkylene group (including any optional substituents) does not exceed two.

[0049] Typically, in this implementation scheme, R 3 and R 7 Together, they form a C1-C4 saturated or unsaturated alkylene group, wherein the alkylene group can be straight-chain or branched, or contain cyclic groups, wherein the alkylene group may optionally be substituted by one or more fluorine, chlorine, and / or bromine groups, and wherein the alkylene group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton, provided that they are directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0050] When R 3 and R 7 When they form alkylene groups, the alkylene groups typically have a chain length of 1 to 3 atoms. More commonly, they have a chain length of 1 or 2 atoms. As understood, the "chain length" of a hydrocarbon group refers to the number of hydrocarbon atoms bonded to each other in a continuous chain between the two bonding points of the hydrocarbon group and the rest of the molecule, measured by the shortest path. For example, structure (C) has a chain length of 3 atoms between A and B, while structure (D) has a chain length of 5 atoms between A and B. More typically, when R 3 and R 7 When they form a hydrocarbon group, the hydrocarbon group is selected from -CH2-, -CH2-CH2-, -CH=CH-, -CH2-O-, or -O-CH2-, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0051] Typically, when R 3 and R 7 When they form a hydrocarbon group together, R 8Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More generally, when R 3 and R 7 When they form a hydrocarbon group together, R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. More generally, when R... 3 and R 7 When they form a hydrocarbon group together, R 8 It is hydrogen.

[0052] As described in both the first and second aspects of the invention, R 4 The hydrocarbon group is selected from hydrogen or a halogen group, -OH, -NH2, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, or R 4 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0053] In one implementation, R 4 The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

[0054] Typically, in this implementation scheme, R4 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, -SO2NH2, -SO2-R 40 or -R 40 Group, wherein R 40 Selected from C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine and / or bromine groups, and wherein the hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0055] More typically, in this implementation, R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-SO2-L 4 -OH, -SO2-L 4 -OR 41 -SO2-L 4-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, wherein: R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R 45 Group, or any two R groups 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 replace; Each R L4 Independently selected from fluorine, methyl, or fluoromethyl; Or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; R 43 Selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and Each R 45 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 45Any methyl group may optionally be fluorinated; The premise is R 4 (Including any optional substituents) Contains no more than 8 carbon atoms.

[0056] In one aspect of this implementation scheme, R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group.

[0057] Another aspect of this implementation scheme: R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R)42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group; R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R 45 Group, or any two R groups 42 They can form 3- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 Replace, where each R L4 Independently selected from fluorine, methyl, or fluoromethyl; Or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 member saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 member saturated monocyclic heterocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups.

[0058] Therefore, for example, R 4 It can be a bromine or chlorine group, or -R 44 Groups such as methyl, -CF3 or cyclopropyl, or -OR 41 Groups such as -OMe, -OCD3, -OCHF2 or -OCH2CHF2, or -SO2-R 41 Groups such as -SO2Me or -SO2Et, or -OL 4 -N(R 42 )2 groups such as -OCH2CH2NHMe groups, or -L 4 -N(R 42 )2 Groups such as -CONHMe group.

[0059] Typically, R 4 (Including any optional substituents) Contains no more than 6 carbon atoms.

[0060] Typically, R 4 The total number of nitrogen, oxygen, and sulfur atoms in (including any optional substituents) does not exceed four. More generally, R 4 The total number of nitrogen, oxygen, and sulfur atoms in the sample (including any optional substituents) shall not exceed three.

[0061] In a more typical implementation, R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 44 -N(R) 42 )2、-COOH、-COOR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-OL 4 -OH, -OL 4 -OR 44 -OL 4 -N(R 42 )2、-NR43 -L 4 -OH, -NR 43 -L 4 -OR 44 -NR 43 -L 4 -N(R 42 )2 or -R 44 Group, wherein: Each R 42 Independently selected from hydrogen or -R 44 Group; R 43 Selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and L 4 It is a -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- group, wherein any -CH2-, -CHMe-, or -CMe2- group may optionally be fluorine-substituted.

[0062] Typically, in this implementation scheme, R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group. More typically, in this embodiment, R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group.

[0063] Typically, each R 44Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, wherein the C1-C4 alkyl or C3-C6 cycloalkyl groups may optionally be substituted with one or more fluorine groups. More generally, each R 44 It is independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

[0064] In one aspect of this implementation scheme, R 4 Selected from fluorine, chlorine, bromine, -OR 44 -SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-N(R 42 )2 or -R 44 Group. More generally, R 4 Selected from fluorine, chlorine, bromine, -R 44 or -OR 44 Group. Typically, in this embodiment, R 44 It is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

[0065] More typically, R 4 Selected from fluorine, chlorine, bromine, methyl (Me), or -OMe groups, wherein any methyl group may optionally be fluorine-substituted. More generally, R 4 It is selected from methyl (Me) or -OMe groups, wherein any methyl group may optionally be fluorinated.

[0066] In another embodiment of the first or second aspect of the invention, R 4 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0067] Typically, when R 4 and R 7 When they are combined to form an alkylene group, the alkylene group (including any optional substituents) contains no more than four carbon atoms.

[0068] Typically, by R 4 and R 7The total number of nitrogen, oxygen, and sulfur atoms in any formed alkylene group (including any optional substituents) does not exceed three. More generally, it is formed by R 4 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any formed alkylene group (including any optional substituents) does not exceed two.

[0069] Typically, in this implementation scheme, R 4 and R 7 Together, they form a C1-C4 saturated or unsaturated alkylene group, wherein the alkylene group can be straight-chain or branched, or contain cyclic groups, wherein the alkylene group may optionally be substituted by one or more fluorine, chlorine, and / or bromine groups, and wherein the alkylene group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton, provided that they are directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0070] When R 4 and R 7 When they form alkylene groups, the alkylene groups typically have a chain length of 2 to 4 atoms. More commonly, the alkylene groups have a chain length of 2 or 3 atoms.

[0071] More typically, when R 4 and R 7 When forming a hydrocarbon group, the hydrocarbon group is selected from -CH2-CH2-, -CH2-O-, -O-CH2-, -CH2-CH2-CH2-, -O-CH2-CH2-, -CH2-CH2-O-, or -CH2-O-CH2-, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0072] Typically, when R 4 and R 7 When they form a hydrocarbon group together, R 8 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More generally, when R 4 and R 7 When they form a hydrocarbon group together, R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. More generally, when R... 4 and R 7 When they form a hydrocarbon group together, R 8 It is hydrogen.

[0073] As described in both the first and second aspects of the invention, R 5 Selected from hydrogen or halogen groups. In one embodiment, R... 5 Selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R5 Selected from hydrogen or fluorine groups. Most commonly, R 5 It is hydrogen.

[0074] As described in both the first and second aspects of the invention, R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More generally, R 6 Selected from fluorine, chlorine, bromine, -R 60 or -OR 60 Group. More generally, R 6 Selected from chlorine, bromine, -R 60 or -OR 60 Group. More generally, R 6 Selected from -R 60 or -OR 60 Group.

[0075] In one implementation, R 60 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. For example, R 6 Optional from -R 60 or -OR 60 Group, and R 60 It can be selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

[0076] Typically, R 60 Selected from methyl, fluoromethyl, ethyl, or fluoroethyl. More commonly, R... 60 Selected from methyl or fluoromethyl.

[0077] In another implementation scheme, R 6 It is chlorinated, bromine, methyl, or fluoromethyl. Typically, in this embodiment, R... 6 It is methyl or fluoromethyl. More typically, R 6 It is a methyl group.

[0078] As illustrated, in one embodiment of both the first and second aspects of the invention, R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 Any hydrocarbon group whose atom is a carbon atom, or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0079] In one implementation, R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms. For example, R 7 It can be selected from hydrogen or fluorine or C1-C 12A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 Any hydrocarbon group in R is composed of carbon atoms, and R 8 It can be selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl.

[0080] In another implementation, R 7 and R 8 Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms. For example, R 7 The hydrocarbon group may be selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 Any hydrocarbon group in R is composed of carbon atoms, and R 8 It can be selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl.

[0081] In yet another implementation, R 7 and R 8Each group is independently selected from hydrogen or fluorine or C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine and / or bromine groups, and wherein the hydrocarbon group may optionally contain one, two or three heteroatoms independently selected from N and O in its carbon skeleton, provided that they are directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms. For example, R 7 The hydrocarbon group may be selected from hydrogen, fluorine, or C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine, and / or bromine groups, and wherein the hydrocarbon group may optionally contain one, two, or three heteroatoms, each independently selected from N and O, in its carbon skeleton, provided that they are directly attached to the R of the remaining part of the molecule. 7 Any hydrocarbon group in R is composed of carbon atoms, and R 8 It can be selected from hydrogen or fluorine, methyl or fluoromethyl.

[0082] In one implementation, R 7 and R 8 Each is independently selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -CO-N(R) 72 )2、-L 7 -COOH, -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, wherein: Each R 71 Independently selected from -R 73 or -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Each L 7 Independently selected from straight-chain alkylene or alkenylene groups, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 replace; Each R L7 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L7 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member monocyclic heterocyclic group, wherein the 3 to 6 member monocyclic heterocyclic group is saturated or monounsaturated, and wherein the 3 to 6 member monocyclic heterocyclic group may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Each R 73 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl, wherein the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and Each R 74Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 74 Any methyl group may optionally be fluorinated; The premise is that any R 7 or R 8 The group (including any optional substituents) contains no more than 12 carbon atoms and is directly attached to the R group of the remainder of the molecule. 7 or R 8 Each atom is a carbon atom, a hydrogen atom, or a fluorine atom.

[0083] Typically, in the above implementation scheme, any R 7 or R 8 The group (including any optional substituents) contains no more than 10 carbon atoms. In one aspect of this embodiment, R 7 and R 8 Each is independently selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that any R 7 or R 8 The group (including any optional substituents) contains no more than 8 carbon atoms and is directly attached to the R group of the remainder of the molecule. 7 or R 8 Each atom is a carbon atom, a hydrogen atom, or a fluorine atom.

[0084] More typically, R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -CO-N(R) 72 )2、-L 7 -COOH, -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OH, -L7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 12 carbon atoms, and directly attached to the R of the remainder of the molecule. 7 The atoms are carbon, hydrogen, or fluorine atoms, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0085] Therefore, for example, R 7 It can be hydrogen or -R 73 Groups such as methyl, -CF3, ethyl, isopropyl, or -CH2CH2CH=CH2 groups, or -COOH groups, or -L 7 -COOH groups such as -CMe2COOH, -CH2COOH, -CH2CH2COOH , or Group, or -L 7 -COOR 71 Groups such as -CMe2COOMe, -CH2CH2COOMe, or -CH2COOEt, or -L 7 -CO-N(R 72 )2 groups such as Group, or -L 7 -OH groups, such as -CMe2CH2OH, or Group, or -L 7 -OR 71 Groups such as -CH2OMe group, or -L 7 -N(R 72 )2 groups such as or Group.

[0086] Typically, in the above implementation scheme, R 7 (Including any optional substituents) contains no more than 10 carbon atoms. More generally, R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon, hydrogen, or fluorine atoms, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0087] For example, as will be understood, when R 7 It is selected from , or -L 7 When -COOH group, L 7 It can be seen as being controlled by two Rs L7 A straight-chain alkylene group substituted with two R groups. L7 Together they form -CH2CH2-, -CH2-, or -CF2- groups, respectively, making the two R groups... L7 Together with one or more carbon atoms to which they are attached, they form cyclopropyl or fluorocyclopropyl groups. Similarly, when R... 7 It is selected from or -L 7 -N(R 72 When )2 groups, L 7 It can be seen as being controlled by a single R L7 A linear alkylene group substituted with a group, wherein R L7 And an R 72 The groups together form -CH2CH2- or -CH2CH2CH2- groups, respectively, making R L7 and R 72 With the -L attached to them 7 -N(R 72 The atoms of the two groups together form a saturated 5- or 6-membered monocyclic heterocyclic group.

[0088] Typically, in the above implementation scheme, each L 7 Independently selected from straight-chain alkylene or alkenylene groups, wherein the straight-chain alkylene group optionally contains a single heteroatom selected from O and N in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L replace.

[0089] In one aspect of the above implementation scheme, each L7 Independently selected from straight-chain alkylene groups, wherein the straight-chain alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 Replace, where each R L7 Independently selected from fluorine, methyl, or fluoromethyl, or any two of these R L7 They can form 3- to 6-membered saturated monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered saturated monocyclic groups may optionally be substituted with one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups, or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member saturated monocyclic heterocyclic group, wherein the 3 to 6 member saturated monocyclic heterocyclic group may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0090] In another aspect of the above implementation plan: R 7 and R 8 Each is independently selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72They can form 3- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and Each L 7 Independently selected from straight-chain alkylene groups, wherein the straight-chain alkylene groups optionally contain one or two heteroatoms, each independently selected from O and N, in their carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 Replace, where each R L7 Independently selected from fluorine, methyl, or fluoromethyl; Or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member saturated monocyclic heterocyclic group, wherein the 3 to 6 member saturated monocyclic heterocyclic group may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; The premise is that any R 7 or R 8 The group (including any optional substituents) contains no more than 8 carbon atoms and is directly attached to the R group of the remainder of the molecule. 7 or R 8 Each atom is a carbon atom, a hydrogen atom, or a fluorine atom.

[0091] In another aspect of the above implementation plan, R 7 and R 8 Each is independently selected from hydrogen or fluorine, -CN, -COOH, -L 7 -COOH, -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74Group, or any two R groups 72 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; Each L 7 Independently selected from straight-chain alkylene groups, wherein the straight-chain alkylene groups optionally contain one or two heteroatoms, each independently selected from O and N, in their carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 replace; Each R L7 Independently selected from fluorine, methyl, or fluoromethyl, or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -OR 71 or -L 7 -N(R 72 The atoms of the two groups together form a 3- to 6-membered saturated monocyclic heterocyclic group, wherein the 3- to 6-membered saturated monocyclic heterocyclic group may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and Each R 73 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; The premise is that any R 7 or R 8 The group (including any optional substituents) contains no more than 8 carbon atoms and is directly attached to the R group of the remainder of the molecule. 7 or R 8 Each atom is a carbon atom, a hydrogen atom, or a fluorine atom.

[0092] Typically, in this respect, R 7 Selected from hydrogen or fluorine, -CN, -COOH, -L 7 -COOH, -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, and R8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0093] Typically, in the above implementation scheme, any R 7 or R 8 The group (including any optional substituents) contains no more than 6 carbon atoms.

[0094] Typically, any R 7 or R 8 The total number of nitrogen, oxygen, and sulfur atoms in any group (including any optional substituents) does not exceed four. More generally, any R 7 or R 8 The total number of nitrogen, oxygen, and sulfur atoms in the group (including any optional substituents) shall not exceed three.

[0095] In another implementation scheme, R 7 and R 8 Each is independently selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group, wherein: Each -L 71 - All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75 They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, such as aziridine, pyrrolidinyl, piperidinyl, morpholinyl or piperazine, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; The premise is that any R 7 or R 8 The group (including any optional substituents) contains no more than 12 carbon atoms.

[0096] Typically, in this implementation scheme, R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. More generally, R 8 It is hydrogen.

[0097] Typically, when R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 When the group is R 7 (Including any optional substituents) Contains no more than 10 carbon atoms.

[0098] In another implementation scheme, R 7 and R 8 Each is independently selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group, wherein: Each -L 71 -Selected independently , -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 It is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl.

[0099] Typically, in this implementation scheme, R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0100] In one aspect of this implementation scheme, each -L 71 - Independently selected from -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- groups, wherein any -CH2-, -CHMe-, or -CMe2- group may optionally be fluorinated. More generally, each -L 71 - Independently selected from -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, or -CMe2-CH2- groups, wherein any -CH2-, -CHMe-, or -CMe2- group may optionally be fluorine-substituted.

[0101] Typically, in this implementation scheme, R 7 (Including any optional substituents) contains no more than 6 carbon atoms, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. More generally, R 7 (Including any optional substituents) contains no more than 5 carbon atoms, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0102] In another implementation, R 7 and R 8 Each is independently selected from hydrogen or fluorine, -L 71 -COOH, -L 71 -COOR 75 -L71 -OH, -L 71 -OR 75 or -R 75 Group, wherein: Each -L 71 - Independently selected from -CH2-, -CHMe-, or -CMe2- groups, wherein any -CH2-, -CHMe-, or -CMe2- group may optionally be fluorine-substituted; and Each R 75 It is independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

[0103] Typically, in this implementation scheme, R 7 Selected from hydrogen or fluorine, -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group, and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0104] In one implementation, R 7 yes: or ;and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. Typically, in this embodiment, R 8 It is hydrogen.

[0105] In another implementation, R 7 yes: or ;and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. Typically, in this embodiment, R 8 It is hydrogen.

[0106] In another implementation scheme, R 7 yes: ;and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. Typically, in this embodiment, R 8 It is hydrogen.

[0107] In another implementation, R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; The premise is R 7 It contains no more than 8 carbon atoms; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl.

[0108] Typically, in this implementation scheme, R 8 It is hydrogen.

[0109] Typically, in this implementation scheme, R 7 It contains no more than 6 carbon atoms. More typically, R 7 It contains no more than 5 carbon atoms.

[0110] In yet another implementation, R 7 and R 8 Each is independently selected from hydrogen or fluorine, methyl or fluoromethyl. For example, R 7 It can be selected from hydrogen or fluorine, methyl or fluoromethyl, and R 8 It can be a hydrogen or fluorine group.

[0111] In one implementation, R 7 and R 8 At least one of them is hydrogen. Typically, R... 8 It is hydrogen.

[0112] In another implementation scheme, R 7 and R 8 They're all hydrogen.

[0113] In another embodiment of the first or second aspect of the invention, R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0114] Typically, in this implementation scheme, R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 6-membered saturated monocyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the saturated monocyclic group to which the attached carbon atom is attached is a cyclic carbon atom, wherein the saturated monocyclic group may optionally be substituted by one or more fluorine groups and / or one or two substituents each independently selected from oxo (=O), -CN or C1-C3 saturated hydrocarbon groups, wherein the saturated hydrocarbon groups may be straight-chain or branched, wherein the saturated hydrocarbon groups may optionally be substituted by one or more fluorine groups, and wherein the saturated hydrocarbon groups may optionally contain a single heteroatom selected from N and O in their carbon skeleton.

[0115] For example, R 7 and R 8 They can form the group -L together 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group in the substituent may optionally be fluorinated.

[0116] As described in both the first and second aspects of the invention, X 9 Is it N or CR? 9 .

[0117] In one implementation, X 9 It is N.

[0118] In another implementation scheme, X 9 It is CR 9 .

[0119] When X 9 It is CR 9 At that time, R 9 Selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

[0120] In one implementation, R 9 The hydrocarbon group is selected from hydrogen or a halogen group, -OH, -NH2, or a C1-C8 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two, or three heteroatoms, each independently selected from N and O, in its carbon skeleton. Typically, in this embodiment, R... 9 The hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2 or C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine and / or bromine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0121] For example, R 9 The following can be selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, -R 91 -OR 91 -N(R) 92 )2、-L 9 -OH, -L 9 -OR 91 -L 9 -N(R 92 )2、-OL 9 -OH, -OL 9 -OR 91 -OL 9 -N(R 92 )2、-NR 93 -L 9 -OH, -NR 93 -L 9 -OR 91 or -NR 93 -L 9 -N(R 92 )2 groups, wherein: Each R 91Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 92 Independently selected from hydrogen or -R 91 Group; R 93 Selected from hydrogen or -R 91 Group; L 9 It is a straight-chain alkylene or alkenylene group, wherein L 9 Chains with lengths of 1 to 4 atoms, where L 9 Optionally, it may be oxidized (=O) group and / or one or more R groups. L9 replace; Each R L9 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L9 , or any R L9 and R 91 , or any two R 91 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by a single oxo (=O) group and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 9 (Including any optional substituents) contains no more than six carbon atoms, and R 9 The total number of nitrogen and oxygen atoms in it does not exceed two.

[0122] For example, R 9 It can be -L 9 -N(R 92 )2 groups, such as As will be understood, in this implementation scheme, L 9 It can be viewed as a straight-chain subalkenyl group, one of which is R L9 And an R 92 Together they form a -CH2CH2- group, which makes R L9 and R 92 With the -L attached to them 9 -N(R 92 The atoms of the two groups together form a 6-membered monocyclic monounsaturated heterocyclic group.

[0123] In another implementation, R 9The hydrocarbon group is selected from hydrogen or a halogen group, -OH, -NH2 or C1-C4 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight or branched, or contain a cyclic group, wherein the hydrocarbon group can optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group can optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0124] In yet another implementation, R 9 The saturated hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine, -CN, -OH, -NH2 or C1-C3 saturated hydrocarbon groups, wherein the saturated hydrocarbon group may be straight-chain or branched, wherein the saturated hydrocarbon group may optionally be substituted by one or more halogen groups and / or a single oxo (=O) group, and wherein the saturated hydrocarbon group may optionally contain a single heteroatom selected from N and O in its carbon skeleton.

[0125] In another implementation scheme, R 9 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 9 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated. For example, R 9 It can be selected from hydrogen or fluorine, chlorine, bromine or -OH groups.

[0126] In one implementation, R 9 It is -OH.

[0127] In another implementation, R 9 It is hydrogen.

[0128] As described in both the first and second aspects of the invention, X 10 Is it N or CR? 10 X 11 Is it N or CR? 11 X 12 Is it N or CR? 12 And X 13 Is it N or CR? 13 , making X 10 X 11 X 12 and X 13 No more than two of them are N. Typically, X 10 X 11 X 12 and X 13 No more than one of them is N.

[0129] Typically, X 11 It is CR 11 And X 12 It is CR 12, or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 More typically, X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is N and X 12 It is CR 12 .

[0130] In one implementation, X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 Is it N or CR? 13 Typically, in this implementation scheme, X 10 and X 13 No more than one of them is N.

[0131] In one implementation, X 10 It is CR 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 It is N.

[0132] In another implementation scheme, X 10 It is CR 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 It is CR 13 .

[0133] As explained, if it exists, each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

[0134] In one implementation, if present, each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or a halogen group (e.g., fluorine, chlorine, or bromine), -OH, -SH, -NH2, -SO2NH2, or C1-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted with one or more halogen groups (e.g., fluorine, chlorine and / or bromine), wherein the hydrocarbon group may optionally contain one, two, three, four, five or six (more often, one, two, three or four) heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted with one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs.

[0135] In another implementation, if present, each R 10 R 11 R 12 and R 13 The saturated hydrocarbon group is independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2, -CN or C1-C8 saturated hydrocarbon group, wherein the saturated hydrocarbon group may be straight-chain or branched, or may contain a single cyclic group, wherein the saturated hydrocarbon group may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups, and wherein the saturated hydrocarbon group may optionally contain one, two or three heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein one of the -S- moieties may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties.

[0136] In another implementation, if present, each R 10 R 11 R 12 and R 13The hydrocarbon group is independently selected from hydrogen or a halogen group, -OH, -NH2, or a C1-C8 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two, or three heteroatoms, each independently selected from N and O, in its carbon skeleton. In one aspect of this embodiment, R 9 The hydrocarbon group is selected from hydrogen or a halogen group, -OH, -NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0137] In one implementation, if present, each R 10 R 11 R 12 and R 13 The hydrocarbon group is independently selected from hydrogen or a halogen group, -OH, -NH2, or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. In one aspect of this embodiment, R 9 The hydrocarbon group is selected from hydrogen or a halogen group, -OH, -NH2 or C1-C4 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight or branched, or contain a cyclic group, wherein the hydrocarbon group can optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group can optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0138] In one implementation, if present, each R 10 R 11 R 12 and R 13 The saturated hydrocarbon group is independently selected from hydrogen or fluorine, chlorine, bromine, -CN, -OH, -NH2 or C1-C3 saturated hydrocarbon groups, wherein the saturated hydrocarbon group can be straight-chain or branched, wherein the saturated hydrocarbon group can optionally be substituted by one or more halogen groups and / or a single oxo (=O) group, and wherein the saturated hydrocarbon group can optionally contain a single heteroatom selected from N and O in its carbon skeleton.

[0139] In another implementation scheme, X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X11 It is N and X 12 It is CR 12 The premise is: (i) X 11 Is it N or X? 12 It is N; and / or (ii) R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups.

[0140] Typically, in this implementation scheme, R 11 and R 12 One of them is present and selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. In one aspect of this embodiment, R 11 and R 12 One of them is present and selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. More generally, in this embodiment, R 11 and R 12 One of them is present and selected from chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN groups. More generally, R 11 and R 12 One of them is present and is selected from chlorine, bromine, methoxy, fluoromethoxy, or -CN groups. Or, R 11 and R 12 One of them can be present and is selected from -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. Most commonly, X 11 Is it C-CN or X? 12 It is C-CN. Typically, in such implementations, a remaining R... 10 R 11 R 12 or R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, and if present, each additional residual R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups. For example, a remaining R 10 R 11 R 12 or R 13 It can be independently selected from hydrogen or fluorine, chlorine or bromine groups, or -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR131 -SL 13 -N(R 132 )2、-SL 13 -SO2-R 131 -SL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein said groups (including any optional substituents) contain no more than 12 carbon atoms, and if present, each additional remaining R 10 R 11 R 12 or R 13 It can be independently selected from hydrogen or fluorine, chlorine or bromine groups, wherein: Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups.

[0141] When any two R L13 , or any R L13 And any R 131 , or any two R 131 Together with one or more atoms to which they are attached, they form 3 to 7-membered monocyclic groups, which may be saturated or unsaturated.

[0142] For example, any two R L13 They can form C3-C7 cycloalkyl or 3- to 7-membered saturated monocyclic heterocyclic groups together with one or more atoms to which they are attached, wherein the C3-C7 cycloalkyl or 3- to 7-membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups. Similarly, any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered saturated monocyclic heterocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups.

[0143] Or, any two R L13They can form phenyl or 5- or 6-membered heteroaryl groups together with one or more atoms to which they are attached, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted with one or two -OH groups and / or one or more fluorine, methyl, and / or fluoromethyl groups. Similarly, any R L13 And any R 131 , or any two R 131 They can form a 5-membered heteroaryl group together with one or more atoms to which they are attached, wherein the 5-membered heteroaryl group may optionally be substituted with one or two -OH groups and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0144] When any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 When forming a 6- to 10-membered bicyclic heterocyclic group together with the atoms to which they are attached, the 6- to 10-membered bicyclic heterocyclic group can be saturated or unsaturated. Similarly, the 6- to 10-membered bicyclic heterocyclic group can be a fused 6- to 10-membered bicyclic heterocyclic group, a spirocyclic 6- to 10-membered bicyclic heterocyclic group, or a bridged 6- to 10-membered bicyclic heterocyclic group.

[0145] For example, any two R L13 And any R 131 They can form saturated fused 8- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated fused 8- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups. Alternatively, any two R L13 And any R 131 They can form fused 8- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 8- to 10-membered bicyclic heterocyclic group comprises a first ring system fused with a second ring system, wherein the first ring system is aromatic and the second ring system is non-aromatic, and wherein the fused 8- to 10-membered bicyclic heterocyclic group may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups. Alternatively, any two R... L13 And any R 131 They can form fused 8- to 10-membered bicyclic heteroaryl groups together with the atoms to which they are attached, wherein the fused 8- to 10-membered bicyclic heteroaryl groups may optionally be substituted with one or two -OH groups and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0146] In another instance, any two R L13 And any R 131They can form saturated bridging 6- to 8-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated bridging 6- to 8-membered bicyclic heterocyclic groups may optionally be replaced by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0147] In another instance, any three R L13 And any R 131 They can form saturated fused 8- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated fused 8- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups. Alternatively, any three R L13 And any R 131 They can form fused 8- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 8- to 10-membered bicyclic heterocyclic group comprises a first ring system fused with a second ring system, wherein the first ring system is aromatic and the second ring system is non-aromatic, and wherein the fused 8- to 10-membered bicyclic heterocyclic group may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups. Alternatively, any three R... L13 And any R 131 They can form fused 8- to 10-membered bicyclic heteroaryl groups together with the atoms to which they are attached, wherein the fused 8- to 10-membered bicyclic heteroaryl groups may optionally be substituted with one or two -OH groups and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0148] In one instance, any three R L13 And any R 131 They can form saturated spirocyclic 7- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated spirocyclic 7- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups.

[0149] In another instance, any three R L13 And any R 131 They can form saturated bridging 6- to 8-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated bridging 6- to 8-membered bicyclic heterocyclic groups may optionally be replaced by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0150] In one instance, any two R atoms attached to the same nitrogen atom 131 And any two R L13They can form saturated fused 8- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated fused 8- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups.

[0151] In another instance, any two R atoms attached to the same nitrogen atom 131 And any two R L13 They can form saturated bridging 6- to 8-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the saturated bridging 6- to 8-membered bicyclic heterocyclic groups may optionally be replaced by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0152] In any of the above implementation schemes, one aspect is: L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131 , or any two R 131 They can form 3 to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3 to 7-membered monocyclic groups are saturated or monounsaturated, and wherein the 3 to 7-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 and R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups are saturated or monounsaturated, and wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0153] More typically, in such implementations, a remaining R 10 R 11 R 12 or R 13Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine and / or bromine groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six (more commonly, one, two, three or four) heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs, and if present, each additional residual R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups. More generally, in such embodiments, R 10 and R 13 One of them is present and selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2, -CN or C1-C8 saturated hydrocarbon groups, wherein the saturated hydrocarbon group can be straight-chain or branched, or contains a single cyclic group, wherein the saturated hydrocarbon group may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups, and wherein the saturated hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs, and if present, each additional remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0154] Typically, when a remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups, or -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L13 -OR 131 、 -L 13 -SR 131 、 -L 13 -N(R 132 )2、 -L 13 -SO2-R 131 、 -L 13 -SO2-N(R 132 )2、 -O-L 13 -OH、 -O-L 13 -SH、 -O-L 13 -OR 131 、 -O-L 13 -SR 131 、 -O-L 13 -N(R 132 )2、 -O-L 13 -SO2-R 131 、 -O-L 13 -SO2-N(R 132 )2、 -S-L 13 -OH、 -S-L 13 -SH、 -S-L 13 -OR 131 、 -S-L 13 -SR 131 、 -S-L[[ID= 56]] 13 -N(R 132 )2、 -S-L 13 -SO2-R 131 、 -S-L 13 -SO2-N(R 132 )2、 -NR 133 -L 13 -OH、 -NR 133 -L 13 -SH、 -NR 133 -L 13 -OR 131 、 -NR 133 -L 13 -SR 131 、 -NR 133 -L 13 -N(R 132 )2、 -NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132When the group (including any optional substituents) contains 2 groups, the group (including any optional substituents) contains no more than 10 carbon atoms. More typically, the group (including any optional substituents) contains no more than 8 carbon atoms. Typically, the total number of nitrogen, oxygen, and sulfur atoms in the group (including any optional substituents) does not exceed six. More typically, the total number of nitrogen, oxygen, and sulfur atoms in the group (including any optional substituents) does not exceed four, or does not exceed three.

[0155] In a typical implementation, when R 11 and R 12 When one of the following groups is present and selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2, X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12 X 13 Is it N or CR? 13 And X 10 and X 13 No more than one of them is N. Typically, in this implementation, R... 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, where R 11 or R 12 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated. More typically, in this embodiment, R 11 and R 12 One of them is selected from chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN groups, and R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R 11 and R 12 One of them is selected from chlorine, bromine, methoxy, fluoromethoxy, or -CN groups, and R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R... 11 and R 12 One of them is a -CN group, and R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. Typically, in such embodiments, R... 10 and R 13One of them is selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine, and / or bromine groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five, or six (more commonly, one, two, three, or four) heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- motif, and if present, R 10 and R 13 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. More typically, in such embodiments, R 10 and R 13 One of them is selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2, -CN, or C1-C8 saturated hydrocarbon groups, wherein the saturated hydrocarbon group can be straight-chain or branched, or contain a single cyclic group, wherein the saturated hydrocarbon group may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups, and wherein the saturated hydrocarbon group may optionally contain one, two, or three heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- motifs, and if present, R 10 and R 13 The other group is selected from hydrogen, fluorine, chlorine, or bromine.

[0156] In one implementation, when R 11 and R 12 If one of the following is present and selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, then each remaining R 10 R 11 R 12 and R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 R 11 R 12 or R 13Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated. More typically, if present, a remaining R group... 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 R 11 R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated, and each additional residual R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups. For example, when R 11 and R 12 If one of the following is present and selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, then R 10 or R 13 One of them can be selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated, and each remaining R group... 10 R 11 R 12 or R 13 It can be independently selected from hydrogen or fluorine, chlorine or bromine groups. More generally, when R... 11 and R 12 If one of the following is present and selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, then each remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0157] In yet another implementation, X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12And X 13 Is it N or CR? 13 X 10 and X 13 No more than one of them is N, R 11 and R 12 One of them is selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 group, R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 groups, and if present, R 10 and R 13 Each is independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 R 11 R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated. Typically, in this embodiment, R... 11 and R 12 One of them is selected from -CN, -COOH, -CONH2 or -C(=NH)NH2 group, and R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R 11 and R 12 One of them is a -CN group, and R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. Typically, in this embodiment, R... 10 and R 13 One of them is selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated, and if present, R 10 and R 13 The other group is selected from hydrogen or fluorine, chlorine or bromine groups. More generally, in this embodiment, if present, each R 10 and R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0158] In one aspect of this implementation plan, X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 Is it N or CR? 13 X 10 and X 13 If at most one of them is N, then R 10 Selected from hydrogen or fluorine, chlorine or bromine groups, R 11 and R 12 One of them is selected from -CN, -COOH, -CONH2 or -C(=NH)NH2 group, R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups, and if present, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 groups. Generally, in this respect, if present, R 10 Selected from hydrogen or fluorine, chlorine or bromine groups, R 11 and R 12 One of them is the -CN group, R 11 and R 12 The other group is selected from hydrogen or fluorine, chlorine or bromine groups, and if present, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -NH2, methyl (Me), -NHMe, or -NMe2 groups. Typically, in this respect, X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 It is CR 13 .

[0159] In another implementation, X 10 It is CR 10 X 11 It is CR 11 X 12 It is N and X 13 It is CR 13 Typically, in this implementation scheme, X 9 It is CR 9 In one aspect of this implementation scheme, X 9 It is CH, CF, C-Cl or C-Br, X 10 It is CH, CF, C-Cl or C-Br, X11 It is CH, CF, C-Cl or C-Br, X 12 It is N, and X 13 It is CH, CF, C-Cl, or C-Br. For example, in one case, X 9 It is CH, X 10 It is CH, X 11 It is CH, X 12 It is N and X 13 It is CH.

[0160] In one implementation, when X 9 It is CR 9 And R 9 When it is -OH, X 11 It is CR 11 And R 11 The group is selected from chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN groups. In another embodiment, when X... 9 It is CR 9 And R 9 When it is -OH, X 11 It is CR 11 And R 11 Selected from -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. Typically, in such embodiments, R... 11 Yes -CN. Typically, in such implementations, X 10 Is it N or CR? 10 X 12 It is CR 12 And X 13 Is it N or CR? 13 And X 10 and X 13 No more than one of them is N. For example, the compound can be a compound of formula (Ia): Formula (Ia) Where X 10 Is it N or CR? 10 X 13 Is it N or CR? 13 X 10 and X 13 No more than one of them is N, and R 1 To R 8 R 10 R 12 and R 13 As defined by formula (I). Similarly, a compound can be a compound of formula (IIa): Formula (IIa) Where X 10 Is it N or CR? 10 X 13 Is it N or CR? 13 X 10 and X 13 No more than one of them is N, and R 1 R 4 To R 8 R 10 R 12 and R 13 To R 17 As defined by equation (II).

[0161] Typically, when X 9 It is CR 9 R 9 It is -OH, X 11 It is CR 11 And R 11 When selected from chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN groups, or selected from -CN, -COOH, -CONH2, or -C(=NH)NH2 groups, X 10 Is it N or CR? 10 X 12 It is CR 12 And X 13 It is CR 13 More typically, in this implementation, X 10 It is CR 10 X 12 It is CR 12 And X 13 It is CR 13 In one aspect of this implementation scheme, if it exists, R 10 R 12 and R 13 Each is independently selected from hydrogen or fluorine, chlorine or bromine groups. More generally, in this respect, if present, R 10 R 12 and R 13 Each is hydrogen.

[0162] Typically, when the compound is a compound of formula (Ia) or (IIa), if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six (more often, one, two, three or four) heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs. More generally, when the compound is a compound of formula (Ia) or (IIa), if present, R 10 The saturated hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or C1-C8 saturated hydrocarbon group, wherein the saturated hydrocarbon group may be straight-chain or branched, or may contain a single cyclic group, wherein the saturated hydrocarbon group may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups, and wherein the saturated hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs.

[0163] In one implementation, for example when the compound is a compound of formula (Ia) or (IIa), if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR 131 -SL 13 -N(R 132 )2、-SL 13 -SO2-R 131 -SL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein: Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 10 (Including any optional substituents) Contains no more than 12 carbon atoms.

[0164] Typically, in this implementation scheme, R 10 (Including any optional substituents) contains no more than 10 carbon atoms. More generally, R 10 (Including any optional substituents) Contains no more than 8 carbon atoms.

[0165] Typically, in this implementation scheme, R 10 The total number of nitrogen, oxygen, and sulfur atoms in (including any optional substituents) does not exceed six. More generally, R 10 The total number of nitrogen, oxygen, and sulfur atoms in the (including any optional substituents) group shall not exceed four, or three.

[0166] Typically, in this implementation scheme, if R exists, 10 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 group. More typically, in this embodiment, if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -OR 131 -L 13 -N(R 132 )2、-OL 13 -OH, -OL 13 -OR 131 -OL 13 -SR131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 or -NR 133 -L 13 -N(R 132 )2 group.

[0167] More generally, when the compound is a compound of formula (Ia) or (IIa), if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine or C1-C4 saturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. More generally, when the compound is a compound of formula (Ia) or (IIa), if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine, methyl or fluoromethyl.

[0168] Typically, when the compound is a compound of formula (Ia) or formula (IIa), R 12 Selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R 12 It is hydrogen.

[0169] Typically, when the compound is a compound of formula (Ia) or (IIa), if present, R 13 Selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R 13 It is hydrogen.

[0170] In one implementation, when X 9 Is it N or CR? 9 When, and when it exists, R 9 It is a hydrogen or halogen group (e.g., fluorine, chlorine, or bromine) or a C1-C6 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine, and / or bromine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. 12 It is CR 12 And R 12 The group is selected from chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN groups. In another embodiment, when X...9 Is it N or CR? 9 When, and when it exists, R 9 It is hydrogen or a halogen group, X 12 It is CR 12 And R 12 Selected from -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. Typically, in such embodiments, R... 12 Yes -CN. Typically, in such implementations, X 10 Is it N or CR? 10 X 11 It is CR 12 And X 13 Is it N or CR? 13 And X 10 and X 13 No more than one of them is N. Typically, in such implementations, X 9 It is CR 9 For example, the compound can be a compound of formula (Ib): Formula (Ib) in: R 9 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, -CH2OH, or -CN groups; X 10 Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; and R 1 To R 8 R 10 R 11 and R 13 As defined by equation (I).

[0171] Similarly, the compound can be a compound of formula (IIb): Equation (IIb) in: R 9 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, -CH2OH, or -CN groups; X 10Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; and R 1 R 4 To R 8 R 10 R 11 and R 13 To R 17 As defined by equation (II).

[0172] Typically, when X 9 Is it N or CR? 9 When, R exists 9 It is hydrogen or a halogen group, X 12 It is CR 12 And R 12 Selected from -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, X 10 It is CR 10 X 11 It is CR 11 And X 13 Is it N or CR? 13 More typically, in this implementation, X 10 It is CR 10 X 11 It is CR 11 And X 13 It is CR 13 In one aspect of this implementation scheme, if it exists, R 10 and R 11 Each is independently selected from hydrogen or fluorine, chlorine or bromine groups, and if present, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -NH2, methyl (Me), -NHMe or -NMe2 groups.

[0173] Typically, when the compound is of formula (Ib) or formula (IIb), if present, R 10 Selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R 10 It is hydrogen.

[0174] Typically, when the compound is of formula (Ib) or formula (IIb), R 11 Selected from hydrogen or fluorine, chlorine or bromine groups. More generally, R 11 It is hydrogen.

[0175] Typically, when the compound is of formula (Ib) or formula (IIb), R12 Selected from chlorine, bromine, methoxy, fluoromethoxy, or -CN groups. More generally, when the compound is of formula (Ib) or (IIb), R 12 It is a -CN group.

[0176] Typically, when the compound is of formula (Ib) or formula (IIb), if present, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six (more often, one, two, three or four) heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs. More generally, when the compound is a compound of formula (Ib) or (IIb), if present, R 13 The saturated hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or C1-C8 saturated hydrocarbon group, wherein the saturated hydrocarbon group may be straight-chain or branched, or may contain a single cyclic group, wherein the saturated hydrocarbon group may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups, and wherein the saturated hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- motifs may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- motifs.

[0177] In one implementation, for example when the compound is a compound of formula (Ib) or (IIb), if present, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR 131 -SL 13 -N(R 132 )2、-SL 13 -SO2-R 131 -SL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein: Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 13 (Including any optional substituents) Contains no more than 12 carbon atoms.

[0178] One aspect of this implementation plan: L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groupsL13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131 , or any two R 131 They can form 3 to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3 to 7-membered monocyclic groups are saturated or monounsaturated, and wherein the 3 to 7-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 and R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups are saturated or monounsaturated, and wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups.

[0179] Typically, in this implementation scheme, R 13 (Including any optional substituents) contains no more than 10 carbon atoms. More generally, R 13 (Including any optional substituents) Contains no more than 8 carbon atoms.

[0180] Typically, in this implementation scheme, R 13 The total number of nitrogen, oxygen, and sulfur atoms in (including any optional substituents) does not exceed six. More generally, R 13 The total number of nitrogen, oxygen, and sulfur atoms in the (including any optional substituents) group shall not exceed four, or three.

[0181] Typically, in this implementation scheme, if R exists, 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13-OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 group.

[0182] For example, R 13 It can be a hydrogen, fluorine, or chlorine group, or -R 131 Groups (such as methyl), or -OR 131 Groups (such as -OMe or (group), or -N(R) 132 )2 groups (such as -NH2, -NHMe or -NMe2 groups), or -L 13 -OH groups (such as -CH2COOH groups), or -L 13 -OR 131 Groups (such as -CH2COOEt group), or -L 13 -N(R 132 )2 groups (such as -CH2CONMe2 groups), or -OL 13 -OH groups (such as...) , , , , , , , , , , , , , , or (group), or -OL 13 -OR 131 Groups (such as -OCH2COOMe, , , , , , , , , , , or (group), or -OL 13 -SR 131 Groups (such as) (group), or -OL 13 -N(R 132 )2 groups (such as , , , , , , , , , , , , , , , , , , , , , , , , , or (group), or -OL 13 -SO2-R 131 Groups (such as) or (group), or -NR 133 -L 13 -OH groups (such as -NHCH2COOH, ...) or (group), or -NR 133 -L 13 -OR 131Groups (such as -NHCH2COOMe, , , or (group), or -NR 133 -L 13 -N(R 132 )2 groups (such as -NHCH2CH2NMe2, -NHCH2CONHMe, , , , , , , , , , or (group).

[0183] As will be understood through examples, when R 13 For example When the group is R 13 Can be regarded as OL 13 -OH group, of which L 13 It is a straight-chain alkylene group with a chain length of 5 atoms, wherein the straight-chain alkylene group contains a single nitrogen atom in its carbon skeleton, wherein the straight-chain alkylene group is surrounded by a single oxo (=O) group and two R groups. L13 Group substitution, wherein the two R groups are... L13 The groups together form a -CH2- group, such that the two R groups... L13 The groups, together with the atoms to which they are attached, form saturated 4-membered monocyclic heterocyclic groups.

[0184] In a similar example, when R 13 For example When the group is R 13 Can be considered as -OL 13 -N(R 132 )2 groups, wherein L 13 It is a straight-chain alkylene group with a chain length of 3 atoms, wherein the straight-chain alkylene group is separated by two R... L13 Replace, one of the R 132 The group is R 131 Groups, such that two R L13 Groups and R 131 The groups, together with the atoms to which they are attached, form a saturated 7-membered bridged bicyclic heterocyclic group, and one of the R groups... 132 The group is R 131 Groups that make R 131 The group is an ethyl group that has been replaced by a single oxo (=O) group.

[0185] Similarly, when R13 For example When the group is R 13 Can be considered as -OL 13 -N(R 132 )2 groups, wherein L 13 It is a straight-chain subalkenyl group with a chain length of 6 atoms, wherein the straight-chain subalkenyl group contains two nitrogen atoms in its carbon skeleton, and the straight-chain subalkenyl group is separated by three R atoms. L13 Group substitution (to obtain -CH(R)) L13 )-CH2-N(R L13 )-CH2-C(R L13 )=N-group), where two R L13 The groups together form a -CH2- group, which makes the two R groups... L13 The groups, together with the atoms to which they are attached, form a saturated 4-membered monocyclic heterocyclic group, one of which is R. 132 The group is R 131 Groups, making the remaining R L13 Groups and R 131 The groups together form -N=N- groups, thus obtaining the remaining R. L13 Groups and R 131 The groups, together with the atoms to which they are attached, form a 5-membered monocyclic heteroaryl group, and one of the R groups... 132 The radical is hydrogen.

[0186] More typically, in such implementations: Each R 131 Independently selected from C1-C3 alkyl, cyclopropyl, or fluorocyclopropyl groups, wherein the C1-C3 alkyl group may optionally be substituted with one or more fluorine groups and / or a single oxo (=O) group; and L 13 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains a single heteroatom selected from O and N in its carbon skeleton, wherein L 13 Chains with lengths of 2 to 7 atoms, and where L 13 Optionally can be replaced by a single oxo (=O) group and / or one or more R groups. L13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131 , or any two R 131 They can form 3- to 6-membered saturated monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered saturated monocyclic groups may optionally be substituted by one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13and R 131 They can form 7 to 9 member saturated bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 7 to 9 member saturated bicyclic heterocyclic groups may optionally be substituted by one or more fluorine, methyl and / or fluoromethyl groups.

[0187] In another implementation scheme, X 10 It is N, CH, CF, C-Cl or C-Br, X 11 It is CH, CF, C-Cl or C-Br, X 12 It is C-CN and X 13 It is N, CH, CF, C-Cl, or C-Br, provided that X is present. 10 and X 13 No more than one of them is N.

[0188] In the alternative implementation plan, X 10 It is N, CH, CF, C-Cl or C-Br, X 11 It's C-CN, X 12 It is CH, CF, C-Cl or C-Br and X 13 It is N, CH, CF, C-Cl, or C-Br, provided that X is present. 10 and X 13 No more than one of them is N.

[0189] As described in the second aspect of the invention, each R 14 and R 15 Independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted.

[0190] In one implementation scheme, each R 14 and R 15 Independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. For example, R 14 It can be hydrogen, and R 15 It can be selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in this embodiment, each R... 14 and R 15 Independently selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. For example, R 14It can be hydrogen and R 15 It can be selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. More typically, in this embodiment, each R 14 and R 15 Independently selected from hydrogen, methyl, or fluoromethyl. For example, R 14 It can be hydrogen and R 15 It can be selected from hydrogen, methyl, or fluoromethyl.

[0191] In one implementation, R 14 and R 15 They're all hydrogen.

[0192] In another implementation, R 14 and R 15 Together with the carbon atoms to which they are attached, they form 3- to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl, or ethyl, wherein any methyl or ethyl group may optionally be fluorine-substituted. Typically, in this embodiment, R 14 and R 15 Together with the carbon atoms to which they are attached, they form 3- to 5-membered saturated monocyclic groups, wherein the saturated monocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O) or methyl or fluoromethyl. For example, R 14 and R 15 Together with the carbon atoms to which they are attached, they can form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups.

[0193] As illustrated, in one embodiment of the second aspect of the invention, R 16 Selected from hydrogen or fluorine, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, and R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, or R 16 and R 17Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted.

[0194] In one implementation, R 16 Selected from hydrogen or fluorine, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, and R 17 It is selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl.

[0195] In one aspect of this implementation scheme, R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, wherein R 160 Selected from C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 161 Group, wherein R 161 It is a 3- to 6-membered monocyclic group, wherein the 3- to 6-membered monocyclic group may optionally be replaced by one or more halogen groups (e.g., fluorine, chlorine, or bromine) and / or one or two R groups. 162 Replace, where each R 162 Independently selected from methyl or fluoromethyl groups, provided that the R group is present. 16 (Including any optional substituents) contains no more than 8 carbon atoms. Typically, in this embodiment, R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, wherein R 160 Selected from C1-C4 alkyl, C1-C4 fluoroalkyl or -R 161 Group, wherein R 161 Selected from C3-C6 cycloalkyl, 4- to 6-membered saturated heterocyclic groups, or phenyl, or 5- or 6-membered heteroaryl groups, wherein the C3-C6 cycloalkyl and 4- to 6-membered saturated heterocyclic groups may optionally be converted by one or more fluorine groups and / or one or two R groups.162 Substitution, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be replaced by one or more fluorine, chlorine, and / or bromine groups and / or one or two R groups. 162 Substitution, provided that the group R 16 (Including any optional substituents) contains no more than 8 carbon atoms. More typically, in this embodiment, R 16 Selected from hydrogen or fluorine, -R 160 -R 161 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, wherein R 160 Selected from methyl or fluoromethyl, wherein R 161 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 162 replace.

[0196] Typically, in the above aspects, R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More generally, R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. Most commonly, R 17 It is hydrogen.

[0197] In one aspect of this implementation scheme, R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, wherein R 160 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl, and R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in this respect, R... 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. For example, R 16 Selectable from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, and R 17 It can be hydrogen. Typically, in this respect, R... 160 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. More generally, in this respect, R 160 Selected from methyl or fluoromethyl.

[0198] In another aspect of this implementation scheme, R 16 Selected from hydrogen or fluorine, -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl, and R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. For example, R 16 It can be selected from hydrogen or fluorine, -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl, and R 17 It can be hydrogen. Typically, in this implementation, R 16 Selected from hydrogen or fluorine, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl, and R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. For example, R 16 It can be selected from hydrogen or fluorine, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl, and R 17 It can be hydrogen. More typically, in this implementation, each R 16 and R 17 Independently selected from hydrogen, methyl, or fluoromethyl. For example, R 16 It can be selected from hydrogen, methyl, or fluoromethyl, and R 17 It could be hydrogen.

[0199] In one implementation, R 16 and R 17 They're all hydrogen.

[0200] In another implementation, R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3- to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl, or ethyl, wherein any methyl or ethyl group may optionally be fluorine-substituted. Typically, in this embodiment, R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3- to 5-membered saturated monocyclic groups, wherein the saturated monocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O) or methyl or fluoromethyl. For example, R 16 and R 17 Together with the carbon atoms to which they are attached, they can form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups.

[0201] In one embodiment of the second aspect of the invention: R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, wherein R 160 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; and R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; or R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3 to 5 member saturated monocyclic groups, wherein the saturated monocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O) or methyl or fluoromethyl.

[0202] In another embodiment of the second aspect of the invention: R 16 Selected from hydrogen or fluorine, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; and R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; or R 16 and R 17 Together with the carbon atoms to which they are attached, they form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups.

[0203] In another embodiment of the second aspect of the invention, R 17 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0204] Typically, when R 17 and R 7When they are combined to form an alkylene group, the alkylene group (including any optional substituents) contains no more than four carbon atoms.

[0205] Typically, by R 17 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any formed alkylene group (including any optional substituents) does not exceed three. More generally, it is formed by R 17 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any formed hydrocarbon group (including any optional substituents) does not exceed two.

[0206] Typically, in this implementation scheme, R 17 and R 7 Together, they form a C1-C4 saturated or unsaturated alkylene group, wherein the alkylene group can be straight-chain or branched, or contain a cyclic group, wherein the alkylene group may optionally be substituted by one or more halogen groups, and wherein the alkylene group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0207] When R 17 and R 7 When they form alkylene groups, the alkylene groups typically have a chain length of 1 to 3 atoms. More commonly, the alkylene groups have a chain length of 1 or 2 atoms.

[0208] More typically, when R 17 and R 7 When they form a hydrocarbon group, the hydrocarbon group is selected from -CH2-, -CH2-CH2-, -CH=CH-, -CH2-O-, or -O-CH2-, provided that it is directly attached to R. 8 The atom of the hydrocarbon group attached to the carbon atom is a carbon atom.

[0209] Typically, when R 17 and R 7 When they form a hydrocarbon group together, R 8 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More generally, when R 17 and R 7 When they form a hydrocarbon group together, R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl. More generally, when R... 17 and R 7 When they form a hydrocarbon group together, R 8 It is hydrogen.

[0210] Typically, when R 17 and R 7When they form a hydrocarbon group together, R 16 Selected from hydrogen or fluorine, -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More generally, R... 17 and R 7 Together they form a hydrocarbon group, R 16 Selected from hydrogen or fluorine, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl. More generally, when R... 17 and R 7 When they form a hydrocarbon group together, R 16 Selected from hydrogen, methyl, or fluoromethyl. More typically, when R... 17 and R 7 When they form a hydrocarbon group together, R 16 It is hydrogen.

[0211] As will be understood, in practice, embodiments for one substituent or part (such as a given R or X group) can be read in conjunction with embodiments for different substituents or parts.

[0212] For example, in a first exemplary embodiment, a compound of formula (I) as defined above is provided, wherein: R 1 It is hydrogen; R 2 Selected from hydrogen or halogen groups; R 3 Selected from hydrogen or halogen groups, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 4 The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 5 Selected from hydrogen or halogen groups; R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; X 9 Is it N or CR? 9 ; R 9 It is a hydrogen or halogen group, -OH, -SH, -NH2, -SO2NH2, or C1-C. 12 Saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon groups may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon groups may optionally be substituted by one or more halogen groups, wherein the hydrocarbon groups may optionally contain one or more heteroatoms, each independently selected from N, O and S, in their carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; X 10 Is it N or CR? 10 ; X 11 Is it N or CR? 11 ; X 12 Is it N or CR? 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than two of them are N; and Each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

[0213] Typically, in this exemplary implementation: R 7 and R 8 Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0214] In one aspect of the first exemplary implementation: R 7 and R 8 Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; R 9 It is a hydrogen or halogen group, -OH, -NH2, or a C1-C8 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two, or three heteroatoms, each independently selected from N and O, in its carbon skeleton; and Each R 10 R 11 R 12 and R 13The hydrocarbon group is independently selected from hydrogen or a halogen group, -OH, -NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0215] In another aspect of the first exemplary implementation: R 7 and R 8 Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; R 9 It is a hydrogen or halogen group, -OH, -NH2, or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; and Each R 10 R 11 R 12 and R 13The hydrocarbon group is independently selected from hydrogen or a halogen group, -OH, -NH2 or C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight or branched, or contain a cyclic group, wherein the hydrocarbon group can optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group can optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0216] In the corresponding second exemplary embodiment, a compound of formula (II) as defined above is provided, wherein: R 1 It is hydrogen; R 4 The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 5 Selected from hydrogen or halogen groups; R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; X 9 Is it N or CR? 9 ; R 9 It is a hydrogen or halogen group, -OH, -SH, -NH2, -SO2NH2, or C1-C. 12 Saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon groups may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon groups may optionally be substituted by one or more halogen groups, wherein the hydrocarbon groups may optionally contain one or more heteroatoms, each independently selected from N, O and S, in their carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; X 10 Is it N or CR? 10 ; X 11 Is it N or CR? 11 ; X 12 Is it N or CR? 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than two of them are N; Each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12Saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon groups may be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon groups may optionally be substituted by one or more halogen groups, wherein the hydrocarbon groups may optionally contain one or more heteroatoms, each independently selected from N, O and S, in their carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; Each R 14 and R 15 Independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted; R 16 The hydrocarbon group is selected from hydrogen or fluorine, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; and R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl; or R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted.

[0217] Typically, in this exemplary implementation: R 7 and R 8Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0218] In one aspect of the second exemplary implementation: R 7 and R 8 Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; R 9 It is a hydrogen or halogen group, -OH, -NH2, or a C1-C8 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two, or three heteroatoms, each independently selected from N and O, in its carbon skeleton; and Each R 10 R 11 R 12 and R 13 The hydrocarbon group is independently selected from hydrogen or a halogen group, -OH, -NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one, two or three heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0219] In another aspect of the second exemplary implementation: R 7 and R 8 Each group is independently selected from hydrogen or fluorine or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 or R 8 The atoms of any hydrocarbon group are carbon atoms; or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; R 9 It is a hydrogen or halogen group, -OH, -NH2, or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight-chain or branched, or contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; and Each R 10 R 11 R 12 and R 13 The hydrocarbon group is independently selected from hydrogen or a halogen group, -OH, -NH2 or C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group can be straight or branched, or contain a cyclic group, wherein the hydrocarbon group can optionally be substituted by one or more halogen groups, and wherein the hydrocarbon group can optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0220] In a third exemplary embodiment, a compound of formula (I) as defined above is provided, wherein: R 1 It is hydrogen; R 2 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, provided that R 3 (Including any optional substituents) Contains no more than 8 carbon atoms; R 30 Selected from C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 31 Group; R 31 It is a 3- to 6-membered monocyclic group, wherein the 3- to 6-membered monocyclic group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 replace; Each R 32 Independently selected from methyl or fluoromethyl; R4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-SO2-L 4 -OH, -SO2-L 4 -OR 41 -SO2-L 4 -N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R45 Group, or any two R groups 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 replace; Each R L4 Independently selected from fluorine, methyl, or fluoromethyl; Or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; R 43 Selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 45 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 45 Any methyl group may optionally be fluorinated; R 5 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 6 Selected from chlorine, bromine, -R 60 or -OR 60 Group; R 60 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 7Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -CO-N(R) 72 )2、-L 7 -COOH, -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 10 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; R 71 Selected from -R 73 or -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 7 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 replace; Each R L7 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L7 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any R L7 and R71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member monocyclic heterocyclic group, wherein the 3 to 6 member saturated monocyclic heterocyclic group is saturated or monounsaturated, and wherein the 3 to 6 member monocyclic heterocyclic group may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Each R 73 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl, wherein the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 74 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 74 Any methyl group may optionally be fluorinated; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; X 9 Is it N or CR? 9 ; R 9 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2 or C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than one of them is N; The premise is: (i) X 11 Is it N or X? 12 It is N; and / or (ii) R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six heteroatoms independently selected from N, O and S in its carbon skeleton, and one of the -S- moieties may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties; and If it exists, each additional remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0221] In one aspect of the third exemplary implementation: R 30 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon, hydrogen, or fluorine atoms; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; R 11 and R 12One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three or four heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and one of the -S- moieties may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties; and If it exists, each additional remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0222] In another aspect of the third exemplary embodiment: R 9 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, -R 91 -OR 91 -N(R) 92 )2、-L 9 -OH, -L 9 -OR 91 -L 9 -N(R 92 )2、-OL 9 -OH, -OL 9 -OR 91 -OL 9 -N(R 92 )2、-NR 93 -L 9 -OH, -NR 93 -L 9 -OR 91 or -NR 93 -L 9 -N(R 92 )2 groups, provided that R 9 (Including any optional substituents) contains no more than six carbon atoms, and R 9The total number of nitrogen and oxygen atoms in the mixture does not exceed two. Each R 91 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 92 Independently selected from hydrogen or -R 91 Group; R 93 Selected from hydrogen or -R 91 Group; L 9 It is a straight-chain alkylene or alkenylene group, wherein L 9 Chains with lengths of 1 to 4 atoms, where L 9 Optionally, it may be oxidized (=O) group and / or one or more R groups. L9 replace; Each R L9 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L9 , or any R L9 and R 91 , or any two R 91 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by a single oxo (=O) group and / or one or more fluorine, methyl and / or fluoromethyl groups; X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than one of them is N; The premise is: (i) X 11 Is it N or X? 12 It is N; and / or (ii) R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups, or -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR 131 -SL 13 -N(R 132 )2、-SL 13 -SO2-R 131 -SL 13 -SO2-N(R 132 )2、-NR 133-L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein the groups (including any optional substituents) contain no more than 10 carbon atoms, and the total number of nitrogen atoms, oxygen atoms and sulfur atoms in the groups (including any optional substituents) does not exceed six; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups; and If it exists, each additional remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0223] In one implementation of this other aspect: R 30 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon, hydrogen, or fluorine atoms; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78-Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups, or -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR 131 -SL13 -N(R 132 )2、-SL 13 -SO2-R 131 -SL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein the groups (including any optional substituents) contain no more than 10 carbon atoms, and the total number of nitrogen atoms, oxygen atoms and sulfur atoms in the groups (including any optional substituents) does not exceed four; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131 , or any two R131 They can form 3 to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3 to 7-membered monocyclic groups are saturated or monounsaturated, and wherein the 3 to 7-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 and R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups are saturated or monounsaturated, and wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; and If it exists, each additional remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0224] In the corresponding fourth exemplary embodiment, a compound of formula (II) as defined above is provided, wherein: R 1 It is hydrogen; R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43-L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-SO2-L 4 -OH, -SO2-L 4 -OR 41 -SO2-L 4 -N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R 45 Group, or any two R groups 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 replace; Each R L4 Independently selected from fluorine, methyl, or fluoromethyl; Or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; R 43 Selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 45 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 45 Any methyl group may optionally be fluorinated; R 5 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 6 Selected from chlorine, bromine, -R 60 or -OR 60 Group; R 60 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -CO-N(R) 72 )2、-L 7 -COOH, -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 10 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; R 71 Selected from -R 73 or -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 7 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 replace; Each R L7 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L7 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member monocyclic heterocyclic group, wherein the 3 to 6 member monocyclic heterocyclic group is saturated or monounsaturated, and wherein the 3 to 6 member monocyclic heterocyclic group may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Each R 73 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl, wherein the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 74Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 74 Any methyl group may optionally be fluorinated; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; X 9 Is it N or CR? 9 ; R 9 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2 or C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than one of them is N; The premise is: (i) X 11 Is it N or X? 12 It is N; and / or (ii) R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein one of the -S- moieties may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties; If it exists, each additional remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups; Each R 14 and R 15 Independently selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups; R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, provided that R 16 (Including any optional substituents) Contains no more than 8 carbon atoms; R 160Selected from C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 161 Group; R 161 It is a 3- to 6-membered monocyclic group, wherein the 3- to 6-membered monocyclic group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 162 replace; Each R 162 Independently selected from methyl or fluoromethyl; and R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; or R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3 to 5 member saturated monocyclic groups, wherein the saturated monocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O) or methyl or fluoromethyl.

[0225] In one aspect of the fourth exemplary embodiment: R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42)2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon, hydrogen, or fluorine atoms; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; R 11 and R12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three or four heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein one of the -S- moieties may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties; If it exists, each additional remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups; and R 160 It is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

[0226] In another aspect of the fourth exemplary embodiment: R 9 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, -R 91 -OR 91 -N(R) 92 )2、-L 9 -OH, -L 9 -OR 91 -L 9 -N(R 92 )2、-OL 9 -OH, -OL 9 -OR 91 -OL 9 -N(R 92 )2、-NR 93 -L 9 -OH, -NR 93 -L 9 -OR 91 or -NR 93 -L 9 -N(R 92)2 groups, provided that R 9 (Including any optional substituents) contains no more than six carbon atoms, and R 9 The total number of nitrogen and oxygen atoms in the mixture does not exceed two. Each R 91 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 92 Independently selected from hydrogen or -R 91 Group; R 93 Selected from hydrogen or -R 91 Group; L 9 It is a straight-chain alkylene or alkenylene group, wherein L 9 Chains with lengths of 1 to 4 atoms, where L 9 Optionally, it may be oxidized (=O) group and / or one or more R groups. L9 replace; Each R L9 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L9 , or any R L9 and R 91 , or any two R 91 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by a single oxo (=O) group and / or one or more fluorine, methyl and / or fluoromethyl groups; X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than one of them is N; The premise is: (i) X 11 Is it N or X? 12 It is N; and / or (ii) R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups, or -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR 131 -SL 13 -N(R 132 )2、-SL 13 -SO2-R 131-SL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein the groups (including any optional substituents) contain no more than 10 carbon atoms, and the total number of nitrogen atoms, oxygen atoms and sulfur atoms in the groups (including any optional substituents) does not exceed six; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more fluorine, methyl, and / or fluoromethyl groups; and If it exists, each additional remaining R 10 R 11 R 12 or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

[0227] In one implementation of this other aspect: R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon, hydrogen, or fluorine atoms; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups, or -R 131 -OH, -SH, -OR 131 -SR 131 -N(R) 132 )2、-SO2-R 131 -SO2-N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-SL 13 -OH, -SL 13 -SH, -SL 13 -OR 131 -SL 13 -SR 131 -SL 13 -N(R 132 )2、-SL 13 -SO2-R 131 -SL 13 -SO2-N(R 132 )2、-NR 133 -L13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein the groups (including any optional substituents) contain no more than 10 carbon atoms, and the total number of nitrogen atoms, oxygen atoms and sulfur atoms in the groups (including any optional substituents) does not exceed four; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131 , or any two R 131 They can form 3 to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3 to 7-membered monocyclic groups are saturated or monounsaturated, and wherein the 3 to 7-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two RL13 and R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups are saturated or monounsaturated, and wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; and If it exists, each additional remaining R 10 R 11 R 12 or R 13 Independently selected from hydrogen or fluorine, chlorine or bromine groups; and R 160 It is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

[0228] In a fifth exemplary embodiment, a compound of formula (I) as defined above is provided, wherein: R 1 It is hydrogen; R 2 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4-SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R 45 Group, or any two R groups 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 Replace, where each R L4 Independently selected from fluorine, methyl, or fluoromethyl, or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; R 43 Selected from hydrogen or -R 44 Group; Each R44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 45 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 45 Any methyl group may optionally be fluorinated; R 5 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 6 Selected from -R 60 or -OR 60 Group; R 60 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71 -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; R 71 Selected from -R 73 or -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; L 7 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 Replace, where each R L7 Independently selected from fluorine, methyl, or fluoromethyl, or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member saturated monocyclic heterocyclic group, wherein the 3 to 6 member saturated monocyclic heterocyclic group may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 73 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl, wherein the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 74 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 74 Any methyl group may optionally be fluorinated; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; X 9 Is it N or CR? 9 ; R 9 Selected from hydrogen or fluorine, chlorine, bromine, -CN, -OH, -NH2 or C1-C3 saturated hydrocarbon groups, wherein the saturated hydrocarbon group may be straight-chain or branched, wherein the saturated hydrocarbon group may optionally be substituted by one or more halogen groups and / or a single oxo (=O) group, and wherein the saturated hydrocarbon group may optionally contain a single heteroatom selected from N and O in its carbon skeleton. X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than one of them is N; R 11 and R 12 One of them is present and selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups; and If it exists, each remaining R 10 R 11 R 12 and R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 R 11 R 12 or R 13Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated.

[0229] In one aspect of the fifth exemplary embodiment: R 3 It is selected from hydrogen or fluorine, chlorine, bromine, -CN or methyl, wherein the methyl group may optionally be fluorine-substituted; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -L 7 -COOH, -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; Each R 73 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group in the substituent may optionally be fluorinated.

[0230] In the corresponding sixth exemplary embodiment, a compound of formula (II) as defined above is provided, wherein: R 1 It is hydrogen; R 4 Selected from fluorine, chlorine, bromine, -OH, -OR 41 -N(R) 42 )2、-SO2-R 41 -SO2-N(R) 42 )2、-L 4 -OH, -L 4 -OR 41 -L 4 -N(R 42 )2、-L 4 -SO2-R 41 -L 4 -SO2-N(R 42 )2、-OL 4 -OH, -OL 4 -OR 41 -OL 4 -N(R 42 )2、-OL 4 -SO2-R 41 -OL 4 -SO2-N(R 42 )2、-NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 -NR 43 -L 4 -N(R 42 )2、-NR 43 -L 4 -SO2-R 41 -NR 43 -L 4 -SO2-N(R 42 )2、-R 44 -R 45 or -L 4 -R 45 Group, provided that R 4 (Including any optional substituents) Contains no more than 8 carbon atoms; R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R 45 Group, or any two R groups 42They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 Replace, where each R L4 Independently selected from fluorine, methyl, or fluoromethyl, or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; R 43 Selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 45 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 45 Any methyl group may optionally be fluorinated; R 5 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 6 Selected from -R 60 or -OR 60 Group; R 60 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -L 7 -COOH, -L 7 -COOR 71-L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; R 71 Selected from -R 73 or -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; L 7 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 Replace, where each R L7 Independently selected from fluorine, methyl, or fluoromethyl, or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member saturated monocyclic heterocyclic group, wherein the 3 to 6 member saturated monocyclic heterocyclic group may optionally be replaced by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 73Independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl, wherein the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 74 Independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine, and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, wherein R 74 Any methyl group may optionally be fluorinated; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; X 9 Is it N or CR? 9 ; R 9 Selected from hydrogen or fluorine, chlorine, bromine, -CN, -OH, -NH2 or C1-C3 saturated hydrocarbon groups, wherein the saturated hydrocarbon group may be straight-chain or branched, wherein the saturated hydrocarbon group may optionally be substituted by one or more halogen groups and / or a single oxo (=O) group, and wherein the saturated hydrocarbon group may optionally contain a single heteroatom selected from N and O in its carbon skeleton. X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than one of them is N; R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups; If it exists, each remaining R 10 R 11 R 12 and R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 10 R 11 R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated; Each R 14 and R 15 Independently selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups; R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group, wherein R 160 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; and R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; or R 16 and R 17Together with the carbon atoms to which they are attached, they form 3 to 5 member saturated monocyclic groups, wherein the saturated monocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O) or methyl or fluoromethyl.

[0231] In one aspect of the sixth exemplary embodiment: R 7 Selected from hydrogen or fluorine, -CN, -COOH, -L 7 -COOH, -L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Group, provided that R 7 (Including any optional substituents) Containing no more than 8 carbon atoms and directly attached to the R of the remainder of the molecule 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; Each R 73 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group of the substituent may optionally be fluorinated; R 16 Selected from hydrogen or fluorine, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; and R17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; or R 16 and R 17 Together with the carbon atoms to which they are attached, they form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups.

[0232] In a seventh exemplary embodiment, a compound of formula (I) as defined above is provided, wherein: R 1 It is hydrogen; R 2 It is hydrogen; R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from methyl or fluoromethyl; R 4 Selected from fluorine, chlorine, bromine, -R 44 or -OR 44 Group; R 44 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is hydrogen; R 6 It is methyl or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group, provided that R 7 (Including any optional substituents) Contains no more than 6 carbon atoms; -L 71 - Selected from -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe- or -CMe2-CH2- groups, wherein any -CH2-, -CHMe- or -CMe2- group may optionally be fluorine-substituted; R 75Selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; X 9 It is CR 9 ; R 9 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 9 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated; X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 Is it N or CR? 13 ; If it exists, R 10 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 11 and R 12 One of them is the -CN group, R 11 and R 12 The other group is selected from hydrogen, fluorine, chlorine, or bromine groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -NH2, methyl (Me), -NHMe or -NMe2 groups; and X 10 and X 13 No more than one of them is N.

[0233] In one aspect of the seventh exemplary embodiment: R 3 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 7 and R 8 Each is independently selected from hydrogen or fluorine, methyl or fluoromethyl; X 10 It is N, CH, CF, C-Cl, or C-Br; X 11 It is C-CN and X 12 It is CH, CF, C-Cl or C-Br, or X 12 It is C-CN and X 11It is CH, CF, C-Cl, or C-Br; X 13 It is N, CH, CF, C-Cl, or C-Br; and X 10 and X 13 No more than one of them is N.

[0234] In the corresponding eighth exemplary embodiment, a compound of formula (II) as defined above is provided, wherein: R 1 It is hydrogen; R 4 Selected from fluorine, chlorine, bromine, -R 44 or -OR 44 Group; R 44 Selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is hydrogen; R 6 It is methyl or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group, provided that R 7 (Including any optional substituents) Contains no more than 6 carbon atoms; -L 71 - Selected from -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe- or -CMe2-CH2- groups, wherein any -CH2-, -CHMe- or -CMe2- group may optionally be fluorine-substituted; R 75 Selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; X 9 It is CR 9 ; R 9Selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH or -CH2NH2 groups, wherein R 9 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may optionally be fluorinated; X 10 Is it N or CR? 10 X 11 It is CR 11 X 12 It is CR 12 And X 13 Is it N or CR? 13 ; If it exists, R 10 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 11 and R 12 One of them is the -CN group, R 11 and R 12 The other group is selected from hydrogen, fluorine, chlorine, or bromine groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -NH2, methyl (Me), -NHMe or -NMe2 groups; X 10 and X 13 No more than one of them is N; R 14 and R 15 They are all hydrogen; and R 16 and R 17 They're all hydrogen.

[0235] In one aspect of the eighth exemplary embodiment: R 7 and R 8 Each is independently selected from hydrogen or fluorine, methyl or fluoromethyl; X 10 It is N, CH, CF, C-Cl, or C-Br; X 11 It is C-CN and X 12 It is CH, CF, C-Cl or C-Br, or X 12 It is C-CN and X 11 It is CH, CF, C-Cl, or C-Br; X 13 It is N, CH, CF, C-Cl, or C-Br; and X 10 and X 13 No more than one of them is N.

[0236] In the ninth exemplary embodiment, a compound of formula (Ia) as defined above is provided, wherein: R 1 It is hydrogen; R 2 It is hydrogen; R 3 Selected from hydrogen or fluorine, chlorine or bromine, -R 30 -R 31 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group; R 30 Selected from methyl or fluoromethyl; R 31 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 replace; Each R 32 Independently selected from methyl or fluoromethyl; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; Each R 42 Independently selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is a hydrogen, fluorine, chlorine, or bromine group; R 6 It is chlorine, bromine, methyl, or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 - All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 10 carbon atoms; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; X 10 Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; If it exists, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein one of the -S- moieties may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties; R 12 Selected from hydrogen or fluorine, chlorine or bromine groups; and If it exists, R 13 Selected from hydrogen, fluorine, chlorine, or bromine groups.

[0237] In one aspect of the ninth exemplary embodiment, if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13-OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein: Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 10 (Including any optional substituents) Contains no more than 10 carbon atoms.

[0238] Typically, in this respect, R 10 The total number of nitrogen, oxygen, and sulfur atoms in the sample (including any optional substituents) shall not exceed six.

[0239] In another aspect of the ninth exemplary embodiment: R 3 Selected from hydrogen or fluorine, chlorine or bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42)2、-SO2-R 44 -O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; R 5 It is hydrogen; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 -Selected independently , -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 It is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 8 carbon atoms; and If it exists, R 10 The hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine or C1-C4 saturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

[0240] In the corresponding tenth exemplary embodiment, a compound of formula (IIa) as defined above is provided, wherein: R 1 It is hydrogen; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; Each R 42 Independently selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is a hydrogen, fluorine, chlorine, or bromine group; R 6 It is chlorine, bromine, methyl, or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 - All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75 They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 10 carbon atoms; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; X 10 Is it N or CR?10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; If it exists, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five or six heteroatoms independently selected from N, O and S in its carbon skeleton, and wherein one of the -S- moieties may optionally be substituted by one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moieties; R 12 Selected from hydrogen, fluorine, chlorine, or bromine groups; If it exists, R 13 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 14 and R 15 They are all hydrogen; R 16 Selected from hydrogen or fluorine, -R 160 -R 161 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group; R 160 Selected from methyl or fluoromethyl; R 161 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 162 replace; Each R 162 Independently selected from methyl or fluoromethyl; and R 17 It is hydrogen.

[0241] In one aspect of the tenth exemplary embodiment, if present, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, wherein: Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 10 (Including any optional substituents) Contains no more than 10 carbon atoms.

[0242] Typically, in this respect, R 10 The total number of nitrogen, oxygen, and sulfur atoms in the sample (including any optional substituents) shall not exceed six.

[0243] In another aspect of the tenth exemplary embodiment: R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; R 5 It is hydrogen; R 7 Selected from hydrogen or fluorine, -COOH, -COOR75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 -Selected independently , -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 It is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 8 carbon atoms; If it exists, R 10 The hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine, or C1-C4 saturated hydrocarbon groups, wherein the hydrocarbon group can be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton; and R 16 It is hydrogen.

[0244] In the eleventh exemplary embodiment, a compound of formula (Ib) as defined above is provided, wherein: R 1 It is hydrogen; R 2 It is hydrogen; R 3Selected from hydrogen or fluorine, chlorine or bromine, -R 30 -R 31 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group; R 30 Selected from methyl or fluoromethyl; R 31 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 replace; Each R 32 Independently selected from methyl or fluoromethyl; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; Each R 42 Independently selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is a hydrogen, fluorine, chlorine, or bromine group; R 6 It is chlorine, bromine, methyl, or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71- All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75 They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 10 carbon atoms; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; R 9 Selected from hydrogen, fluorine, chlorine, or bromine groups; X 10 Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; If it exists, R 10 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 11 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, -CH2OH, or -CN groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two RL13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 13 (Including any optional substituents) Contains no more than 10 carbon atoms.

[0245] Typically, in this implementation scheme, R 13 The total number of nitrogen, oxygen, and sulfur atoms in the sample (including any optional substituents) shall not exceed six.

[0246] One aspect of the eleventh exemplary implementation: R 3 Selected from hydrogen or fluorine, chlorine or bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; R 5 It is hydrogen; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR 75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 -Selected independently , -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 It is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 8 carbon atoms; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, or -CN groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups; Each R 131 Independently selected from C1-C3 alkyl, cyclopropyl, or fluorocyclopropyl, wherein the C1-C3 alkyl may optionally be substituted by one or more fluorine groups and / or a single oxo (=O) group; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains a single heteroatom selected from O and N in its carbon skeleton, wherein L 13 Chains with lengths of 2 to 7 atoms, and where L 13 Optionally can be replaced by a single oxo (=O) group and / or one or more R groups. L13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131 , or any two R 131 They can form 3- to 6-membered saturated monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered saturated monocyclic groups may optionally be substituted by one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 and R 131They can form 7 to 9 membered saturated bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 7 to 9 membered saturated bicyclic heterocyclic groups may optionally be substituted by one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 13 (Including any optional substituents) Contains no more than 8 carbon atoms.

[0247] In the corresponding twelfth exemplary embodiment, a compound of formula (IIb) as defined above is provided, wherein: R 1 It is hydrogen; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; Each R 42 Independently selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is a hydrogen, fluorine, chlorine, or bromine group; R 6 It is chlorine, bromine, methyl, or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 - All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75 They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 10 carbon atoms; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; R 9 Selected from hydrogen, fluorine, chlorine, or bromine groups; X 10 Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; If it exists, R 10 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 11 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, -CH2OH, or -CN groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three RL13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 13 (Including any optional substituents) Contains no more than 10 carbon atoms; R 14 and R 15 They are all hydrogen; and R 16 Selected from hydrogen or fluorine, -R 160 -R 161 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Group; R 160 Selected from methyl or fluoromethyl; R 161 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be surrounded by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 162 replace; Each R 162 Independently selected from methyl or fluoromethyl; and R 17 It is hydrogen.

[0248] Typically, in this implementation scheme, R 13 The total number of nitrogen, oxygen, and sulfur atoms in the sample (including any optional substituents) shall not exceed six.

[0249] One aspect of the twelfth exemplary implementation: R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group; R 5 It is hydrogen; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -L 71 -COOH, -L 71 -COOR75 -L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 -Selected independently , -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2- groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 It is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl or fluorocyclobutyl; or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 8 carbon atoms; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, or -CN groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups; Each R 131 Independently selected from C1-C3 alkyl, cyclopropyl, or fluorocyclopropyl, wherein the C1-C3 alkyl may optionally be substituted by one or more fluorine groups and / or a single oxo (=O) group; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains a single heteroatom selected from O and N in its carbon skeleton, wherein L 13 Chains with lengths of 2 to 7 atoms, and where L 13 Optionally can be replaced by a single oxo (=O) group and / or one or more R groups. L13 replace; Each R L13 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L13 , or any R L13 and R 131, or any two R 131 They can form 3- to 6-membered saturated monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered saturated monocyclic groups may optionally be substituted by one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 and R 131 They can form 7 to 9 membered saturated bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 7 to 9 membered saturated bicyclic heterocyclic groups may optionally be substituted by one or more fluorine, methyl and / or fluoromethyl groups; The premise is R 13 (Including any optional substituents) Contains no more than 8 carbon atoms; and R 16 It is hydrogen.

[0250] In any of the above embodiments, the compound of the first or second aspect of the invention has a molecular weight of 247 to 750 Da. Typically, the compound of the first or second aspect of the invention has a molecular weight of 260 to 600 Da, or 260 to 500 Da. More typically, the compound of the first or second aspect of the invention has a molecular weight of 270 to 580 Da, or 270 to 550 Da, or 270 to 450 Da. Still more typically, the compound of the first or second aspect of the invention has a molecular weight of 280 to 575 Da, or 280 to 520 Da, or 280 to 400 Da.

[0251] A third aspect of the present invention provides a compound selected from the group consisting of: , , , , , , , , , , , , , , , , , , , , , , , , , , , 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , and .

[0252] The fourth aspect of the invention provides pharmaceutically acceptable salts and / or solvates and / or prodrugs of any compound of the first, second or third aspects of the invention.

[0253] In one embodiment, the fourth aspect of the invention provides a pharmaceutically acceptable salt and / or solvate of any compound of the first, second, or third aspect of the invention. For example, the fourth aspect of the invention may provide (i) a pharmaceutically acceptable salt of any compound of the first, second, or third aspect of the invention, or (ii) a pharmaceutically acceptable solvate of any compound of the first, second, or third aspect of the invention, or (iii) a pharmaceutically acceptable solvate of a pharmaceutically acceptable salt of any compound of the first, second, or third aspect of the invention.

[0254] The compounds of the present invention can be used in their free base form and their acid addition salt form. For the purposes of this invention, the term "salt" in the compounds of the present invention includes acid addition salts. The acid addition salt is preferably a pharmaceutically acceptable, non-toxic addition salt of a suitable acid, including but not limited to inorganic acids such as hydrohalic acids (e.g., hydrofluoric acid, hydrochloric acid, hydrobromic acid, or hydroiodic acid) or other inorganic acids (e.g., nitric acid, perchloric acid, sulfuric acid, or phosphoric acid); or organic acids such as organic carboxylic acids (e.g., propionic acid, butyric acid, glycolic acid, lactic acid, mandelic acid, citric acid, acetic acid, benzoic acid, salicylic acid, succinic acid, malic acid or hydroxysuccinic acid, tartaric acid, fumaric acid, maleic acid, hydroxymaleic acid, viscous acid or galactopic acid, gluconic acid, pantothenic acid, or pyruvic acid), organic sulfonic acids (e.g., methanesulfonic acid, trifluoromethanesulfonic acid, ethanesulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, naphthalene-2-sulfonic acid, or camphorsulfonic acid) or amino acids (e.g., ornithine, glutamic acid, or aspartic acid). The acid addition salt can be a monoacid, diacid, triacid, or polyacid addition salt. The preferred salt is an addition salt of hydrohalic acid, sulfuric acid, phosphoric acid, or organic acid. The preferred salt is an addition salt of hydrochloric acid.

[0255] When the compounds of this invention include a quaternary ammonium group, the compounds are typically used in their salt form. The counterion of the quaternary ammonium group can be any pharmaceutically acceptable, non-toxic counterion. Examples of suitable counterions include the conjugate base of a protic acid associated with acid addition salts as discussed above.

[0256] The compounds of the present invention can also be used in their free acid form and their salt form. For the purposes of this invention, a "salt" of the compounds of the present invention includes a salt formed between a protic acid functional group (such as a carboxylic acid group) of the compound of the present invention and a suitable cation. Suitable cations include, but are not limited to, lithium, sodium, potassium, magnesium, calcium, and ammonium. The salt can be a monosalt, disalt, trisalt, or multisalt. Preferably, the salt is a monolithium salt, monosodium salt, monopotassium salt, monomagnesium salt, monocalcium salt, or monoammonium salt, or a dilithium salt, disodium salt, dipotassium salt, dimagnesium salt, dicalcium salt, or diammonium salt. More preferably, the salt is a monosodium salt or a monopotassium salt.

[0257] Preferably, any salt is a pharmaceutically acceptable, non-toxic salt. However, in addition to pharmaceutically acceptable salts, other salts are also included in this invention because they can be used as intermediates for purifying or preparing other (e.g.) pharmaceutically acceptable salts, or for identifying, characterizing, or purifying free acids or bases.

[0258] The compounds and / or salts of the present invention may be anhydrous or in hydrate (e.g., hemihydrate, monohydrate, dihydrate, or trihydrate) or other solvate forms. Such other solvates may be formed using common organic solvents, including but not limited to alcohol solvents such as methanol, ethanol, or isopropanol.

[0259] In one embodiment, the fourth aspect of the invention provides a prodrug of any compound of the first, second, or third aspect of the invention. Similarly, the fourth aspect of the invention provides a pharmaceutically acceptable salt and / or solvate of such a prodrug. For example, the fourth aspect of the invention provides (i) a pharmaceutically acceptable salt of a prodrug, or (ii) a pharmaceutically acceptable solvate of a prodrug, or (iii) a solvate of a pharmaceutically acceptable salt of a pharmaceutically acceptable prodrug.

[0260] In some embodiments of the invention, a therapeutically inactive prodrug is provided. A prodrug is a compound that is wholly or partially converted into a compound of the invention upon administration to a subject (e.g., a human). In most embodiments, the prodrug is a pharmacologically inert chemical derivative that can be converted in vivo into an active drug molecule to exert a therapeutic effect. Any compound described herein may be administered as a prodrug to increase the activity, bioavailability, or stability of the compound or otherwise alter its properties. Typical examples of prodrugs include compounds having a biologically unstable protecting group on the functional portion of an active compound. Prodrugs include, but are not limited to, compounds that can be oxidized, reduced, amination, deamination, hydroxylation, dehydroxylation, hydrolysis, dehydrolysis, alkylation, dealkylation, acylation, deacylation, phosphorylation, and / or dephosphorylation to produce an active compound. The invention also covers salts and solvates of such prodrugs as described above.

[0261] The compounds, salts, solvates, and prodrugs of the present invention can be obtained at various purity levels, for example by conventional techniques such as recrystallization and / or column chromatography.

[0262] For example, the compounds, salts, solvates, and prodrugs of the present invention may be at least 90% pure, at least 95% pure, at least 99% pure, at least 99.5% pure, or at least 99.9% pure, as determined by HPLC.

[0263] Alternatively, the compounds, salts, solvates, and prodrugs of the present invention may be at least 90% pure, at least 95% pure, at least 99% pure, at least 99.5% pure, or at least 99.9% pure, as determined by LCMS.

[0264] Alternatively, the compounds, salts, solvates, and prodrugs of the present invention may be at least 90% pure, at least 95% pure, at least 99% pure, at least 99.5% pure, or at least 99.9% pure, as described above. 1 H NMR determination.

[0265] The compounds, salts, solvates, and prodrugs of the present invention may contain at least one chiral center. Therefore, the compounds, salts, solvates, and prodrugs may exist in at least two isomeric forms. The present invention covers racemic mixtures of the compounds, salts, solvates, and prodrugs of the present invention, as well as enantiomerically enriched and substantially enantiomerically pure isomers. For the purposes of the present invention, a "substantially enantiomerically pure" isomer of a compound comprises less than 5%, more typically less than 2%, and most typically less than 0.5% by weight of other isomers of the same compound.

[0266] The compounds, salts, solvates, and prodrugs of this invention may contain any stable isotopes, including but not limited to... 12 C 13 C 1 H, 2 H (D), 14 N、 15 N、 16 O、 17 O、 18 O、 19 F and 127 I, and any radioactive isotope, including but not limited to 11 C 14 C 3 H (T), 13 N、 15 O、 18 F, 123 I, 124 I, 125 I and 131 I.

[0267] The compounds, salts, solvates, and prodrugs of the present invention may be in any polymorphic or amorphous form.

[0268] A fifth aspect of the present invention provides a pharmaceutical composition comprising a compound of the first, second, or third aspect of the present invention, or a pharmaceutically acceptable salt and / or solvate and / or prodrug of the fourth aspect of the present invention, and a pharmaceutically acceptable excipient.

[0269] The routine procedures for selecting and preparing suitable pharmaceutical formulations are described, for example, in “Aulton’s Pharmaceuticals - The Design and Manufacture of Medicines”, ME Aulton and KMG Taylor, Churchill Livingstone Elsevier, 4th edition, 2013.

[0270] Pharmaceutically acceptable excipients (including adjuvants, diluents, or carriers) that can be used in the pharmaceutical compositions of the present invention are those adjuvants, diluents, or carriers conventionally used in the field of pharmaceutical formulations, and include, but are not limited to, sugars, sugar alcohols, starches, ion exchangers, alumina, aluminum stearate, lecithin, serum proteins (such as human serum albumin), buffering substances (such as phosphates), glycine, sorbic acid, potassium sorbate, mixtures of saturated vegetable fatty acid metaglycerides, water, salts or electrolytes (such as protamine sulfate), disodium hydrogen phosphate, potassium hydrogen phosphate, sodium chloride, zinc salts, colloidal silica, magnesium trisilicate, polyvinylpyrrolidone, cellulose-based substances, polyethylene glycol, sodium carboxymethyl cellulose, polyacrylates, waxes, polyethylene-polyoxypropylene block polymers, polyethylene glycol, and lanolin.

[0271] A sixth aspect of the invention provides compounds of the first, second, or third aspects of the invention, or pharmaceutically acceptable salts, solvates, or prodrugs of the fourth aspect of the invention, or pharmaceutical compositions of the fifth aspect of the invention, wherein the compounds, the pharmaceutically acceptable salts, solvates, or prodrugs, or the pharmaceutical compositions are used as pharmaceuticals, and / or for the treatment or prevention of diseases, symptoms, or ailments. Typically, the use includes administering the compound, salt, solvate, prodrug, or pharmaceutical composition to a subject.

[0272] As used herein, the term “treatment” equally refers to curative and palliative therapies. The term includes achieving a beneficial or desired physiological outcome, which may or may not be clinically determined. Beneficial or desired clinical outcomes include, but are not limited to, detectable or undetectable symptom relief, symptom prevention, reduction of disease severity, disease stabilization (i.e., no exacerbation), delay or slowing of disease / symptom progression / exacerbation, and improvement or remission of disease / symptoms (whether partial or complete). As used herein, the term “remission” and variations thereof mean a reduction in the severity and / or undesirable manifestations of a physiological disorder or symptom and / or a slowing or prolonging of its progression compared to the absence of the compounds, salts, solvates, prodrugs, or pharmaceutical compositions of the present invention. As used herein, the term “prevention” in relation to disease, condition, or disorder refers to prophylactic or preventative therapy and therapies that reduce the risk of developing a disease, condition, or disorder. The term “prevention” includes both avoiding the occurrence of a disease, condition, or disorder and delaying its onset. Any statistically significant (p≤0.05) occurrence avoidance, delayed onset, or reduced risk as measured by controlled clinical trials can be considered prevention of a disease, condition, or disorder. Suitable subjects for prevention include those identified as having a higher risk of disease, condition, or disorder by genetic or biochemical markers. Typically, genetic or biochemical markers are appropriate for the disease, condition, or disorder under consideration, and may include, in inflammatory cases, inflammatory biomarkers such as C-reactive protein (CRP) and monocyte chemoattractant protein 1 (MCP-1), and complement system-related biomarkers such as C5a, terminal complement complex, factor B, fragments Ba and Bb, complement C3 fragments C3a and C3b, and downstream degradation products iC3b, C3c, and C3d(g).

[0273] A seventh aspect of the invention provides the use of the compounds of the first, second, or third aspects, or the pharmaceutically effective salts, solvates, or prodrugs of the fourth aspect, in the manufacture of a medicament for treating or preventing a disease, symptom, or ailment. Typically, treatment or prevention involves administering the compound, salt, solvate, prodrug, or medicament to a subject.

[0274] An eighth aspect of the invention provides a method for treating or preventing a disease, symptom, or disorder, the method comprising the steps of: administering an effective amount of a compound of the first, second, or third aspect, or a pharmaceutically acceptable salt, solvate, or prodrug of the fourth aspect, or a pharmaceutical composition of the fifth aspect, to thereby treat or prevent the disease, symptom, or disorder. Typically, the administration is directed to a subject in need.

[0275] Dysregulation of the alternative complement pathway, caused by genetic factors or the presence of autoantibodies, can lead to a variety of diseases. Common polymorphisms or rare mutations in complement proteins can result in complement system dysfunction or dysregulation, due to overactivation or imbalance. Autoantibodies can bind to the body's own cells and drive the complement system, overburdening the protective capacity of natural regulators. In some cases, the cell's natural defense mechanisms, such as the shedding of active complexes, can lead to symptoms due to...

Claims

1. A compound of formula (I): Formula (I) Or its pharmaceutically acceptable salts and / or solvates and / or prodrugs; in: R 1 It is hydrogen; R 2 Selected from hydrogen or halogen groups; R 3 Selected from hydrogen or halogen groups, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 4 The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms each independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups each independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 5 Selected from hydrogen or halogen groups; R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted with one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted with one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 Or R 8 The atoms of any hydrocarbon group are carbon atoms; Or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. Or R 3 and R 7 , or R 4 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the alkylene group attached to the carbon atom is a carbon atom; X 9 Is it N or CR? 9 ; R 9 It is a hydrogen or halogen group, -OH, -SH, -NH2, -SO2NH2, or C1-C. 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; X 10 Is it N or CR? 10 ; X 11 Is it N or CR? 11 ; X 12 Is it N or CR? 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than two of them are N; and Each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted with one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted with one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety.

2. The compound of claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein R 2 Selected from hydrogen, fluorine, chlorine, or bromine groups.

3. The compound of claim 1 or claim 2, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group, wherein R 30 Selected from C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 31 Group, wherein R 31 It is a 3- to 6-membered monocyclic group, wherein the 3- to 6-membered monocyclic group may optionally be replaced by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 Replace, where each R 32 The group R is independently selected from methyl or fluoromethyl, provided that it includes any optional substituents. 3 It contains no more than 8 carbon atoms.

4. A compound of formula (II): Equation (II) Or its pharmaceutically acceptable salts and / or solvates and / or prodrugs; in: R 1 It is hydrogen; R 4 The hydrocarbon group is selected from hydrogen or halogen, -OH, -NH2, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms each independently selected from N, O and S in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups each independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 5 Selected from hydrogen or halogen groups; R 6 Selected from hydrogen or halogen groups, -R 60 or -OR 60 Group, wherein R 60 Selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 Each is independently selected from hydrogen or fluorine or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted with one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O, and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted with one or two groups, each independently selected from oxo (=O) and =NH, to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to the R of the remaining part of the molecule. 7 Or R 8 The atoms of any hydrocarbon group are carbon atoms; Or R 7 and R 8 Together with the carbon atoms to which they are attached, they form 3 to 10-membered cyclic groups, allowing direct attachment to R... 7 and R 8 Each ring atom of the cyclic group of the attached carbon atom is a cyclic carbon atom, wherein the cyclic group may optionally be substituted by one or more substituents, each independently selected from a halogen, an oxo (=O), -OH, -NH2 or a C1-C4 saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain a cyclic group, wherein the hydrocarbon group may optionally be substituted by one or more halogens, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton. X 9 Is it N or CR? 9 ; R 9 It is a hydrogen or halogen group, -OH, -SH, -NH2, -SO2NH2, or C1-C. 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; X 10 Is it N or CR? 10 ; X 11 Is it N or CR? 11 ; X 12 Is it N or CR? 12 ; X 13 Is it N or CR? 13 ; X 10 X 11 X 12 and X 13 No more than two of them are N; Each R 10 R 11 R 12 and R 13 Independently selected from hydrogen or halogen groups, -OH, -SH, -NH2, -SO2NH2, or C1-C 12 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; Each R 14 and R 15 Independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted; R 16 Selected from hydrogen or fluorine, -SO2NH2 or C1-C8 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or more cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more halogen groups, wherein the hydrocarbon group may optionally contain one or more heteroatoms, each independently selected from N, O and S, in its carbon skeleton, and wherein any -S- moiety may optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)- or -SO(=NH)- moiety; R 17 Selected from hydrogen or fluorine, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl; Or R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3 to 6-membered cyclic groups, wherein the cyclic groups may optionally be substituted by one or more substituents, each independently selected from fluorine, -OH, oxo (=O), methyl or ethyl, wherein any methyl or ethyl may optionally be fluorine-substituted; Or R 17 and R 7 , or R 4 and R 7 Together, they form C1-C6 saturated or unsaturated alkylene groups, wherein the alkylene groups can be straight-chain or branched, or contain one or more cyclic groups, wherein the alkylene groups can optionally be substituted by one or more halogen groups, wherein the alkylene groups can optionally contain one or more heteroatoms, each independently selected from N, O, and S, in their carbon skeleton, and wherein any -S- moiety can optionally be substituted by one or two groups, each independently selected from oxo (=O) and =NH, to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that it is directly attached to R. 8 The atom of the alkylene group attached to the carbon atom is a carbon atom.

5. The compound of claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein each R 14 and R 15 Independently selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl, or R 14 and R 15 Together with the carbon atoms to which they are attached, they form cyclopropyl or cyclobutyl groups, wherein the cyclopropyl or cyclobutyl groups may optionally be substituted with one or more fluorine groups.

6. The compound of claim 4 or claim 5, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein: R 16 Selected from hydrogen or fluorine, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Groups, provided that the R group includes any optional substituents. 16 It contains no more than 8 carbon atoms; R 160 Selected from C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 161 Group; R 161 It is a 3- to 6-membered monocyclic group, wherein the 3- to 6-membered monocyclic group may optionally be replaced by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 162 replace; Each R 162 Independently selected from methyl or fluoromethyl; and R 17 Selected from hydrogen or fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; Or R 16 and R 17 Together with the carbon atoms to which they are attached, they form 3 to 5 member saturated monocyclic groups, wherein the saturated monocyclic groups may optionally be substituted by one or more fluorine groups and / or one or two substituents each independently selected from oxo (=O) or methyl or fluoromethyl.

7. The compound of any one of claims 1 to 6, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein: R 4 selected from fluorine, chlorine, bromine, -OH, -OR 41 , -N(R 42 )2, -SO2-R 41 , -SO2-N(R 42 )2, -L 4 -OH, -L 4 -OR 41 , -L 4 -N(R 42 )2, -L 4 -SO2-R 41 , -L 4 -SO2-N(R 42 )2, -O-L 4 -OH, -O-L 4 -OR 41 , -O-L 4 -N(R 42 )2, -O-L 4 -SO2-R 41 , -O-L 4 -SO2-N(R 42 )2, -NR 43 -L 4 -OH, -NR 43 -L 4 -OR 41 , -NR 43 -L 4 -N(R 42 )2, -NR 43 -L 4 -SO2-R 41 , -NR 43 -L 4 -SO2-N(R 42 )2, -SO2-L 4 -OH, -SO2-L 4 -OR 41 , -SO2-L 4 -N(R 42 )2, -R 44 , -R 45 or -L 4 -R 45 group; R 41 Selected from -R 44 or -R 45 Group; Each R 42 Independently selected from hydrogen or -R 44 or -R 45 Group, or any two R groups 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted with one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 4 It is a straight-chain alkylene group, wherein the straight-chain alkylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 4 Chains with lengths of 1 to 4 atoms, where L 4 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L4 replace; Each R L4 Independently selected from fluorine, methyl, or fluoromethyl; Or any R L4 and R 41 , or any R L4 And any R 42 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted with one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; R 43 Selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, wherein the C1-C4 alkyl or C3-C6 cycloalkyl groups may optionally be substituted with one or more fluorine groups and / or one or two oxo (=O) groups; and Each R 45 The group is independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or the 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe and -NMe2, wherein R 45 Any methyl group may optionally be fluorinated; The premise is that R includes any optional substituents. 4 It contains no more than 8 carbon atoms.

8. The compound of any one of claims 1 to 7, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein R 5 Selected from hydrogen, fluorine, chlorine, or bromine groups.

9. The compound of any one of claims 1 to 8, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein: R 6 Selected from chlorine, bromine, -R 60 or -OR 60 Group; and R 60 It is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl.

10. The compound of any one of claims 1 to 9, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein: R 7 Selected from hydrogen or fluorine, -CN, -COOH, -COOR 71 -CO-N(R) 72 )2、-L 7 -COOH, -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OH, -L 7 -OR 71 -L 7 -N(R 72 )2、-R 73 -R 74 or -L 7 -R 74 Groups, provided that the R group includes any optional substituents. 7 R contains no more than 12 carbon atoms and is directly attached to the remainder of the molecule. 7 The atoms are carbon atoms, hydrogen atoms, or fluorine atoms; R 71 Selected from -R 73 or -R 74 Group; Each R 72 Independently selected from hydrogen or -R 73 or -R 74 Group, or any two R groups 72 They can form 3 to 6 membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 3 to 6 membered saturated monocyclic heterocyclic groups may optionally be substituted with one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups; L 7 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one or two heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 7 Chains with lengths of 1 to 4 atoms, where L 7 Optionally can be occupied by one or two oxo (=O) groups and / or one or more R groups L7 replace; Each R L7 Independently selected from fluorine, methyl, or fluoromethyl; Or any two R L7 They can form 3- to 6-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 6-membered monocyclic groups are saturated or monounsaturated, and wherein the 3- to 6-membered monocyclic groups may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups. Or any R L7 and R 71 , or any R L7 And any R 72 Can be attached to them -L 7 -COOR 71 -L 7 -CO-N(R 72 )2、-L 7 -OR 71 or -L 7 -N(R 72 The atoms of the 2 groups together form a 3 to 6 member monocyclic heterocyclic group, wherein the 3 to 6 member monocyclic heterocyclic group is saturated or monounsaturated, and wherein the 3 to 6 member monocyclic heterocyclic group may optionally be substituted by one or two oxo (=O) groups and / or one or more fluorine, methyl and / or fluoromethyl groups. Each R 73 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl, wherein the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl or C5-C6 cycloalkenyl may optionally be substituted by one or more fluorine groups and / or one or two oxo (=O) groups; Each R 74 The group is independently selected from phenyl or 5- or 6-membered heteroaryl groups, wherein the phenyl or the 5- or 6-membered heteroaryl group may optionally be substituted by one or more groups each independently selected from fluorine, chlorine and bromine and / or one or two groups each independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe and -NMe2, wherein R 74 Any methyl group may optionally be fluorinated; and R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; Or R 7 and R 8 Together they form the group -L 78 -, where -L 78 - Selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-O-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-O-CH2-, -CH2-NH-CH2-CH2-, or -CH2-O-CH2-CH2- groups, wherein -L 78 -Optionally may be substituted with one or more fluorine groups and / or one or two substituents, each independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, wherein -L 78 - Any methyl group in the substituent may optionally be fluorinated.

11. The compound of any one of claims 1 to 10, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein X 9 It is CR 9 .

12. The compound of any one of claims 1 to 11, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein R 9 The hydrocarbon group is selected from hydrogen or fluorine, chlorine, bromine, -OH, -NH2 or C1-C6 saturated or unsaturated hydrocarbon groups, wherein the hydrocarbon group may be straight-chain or branched, or contain cyclic groups, wherein the hydrocarbon group may optionally be substituted by one or more fluorine, chlorine and / or bromine groups, and wherein the hydrocarbon group may optionally contain one or two heteroatoms, each independently selected from N and O, in its carbon skeleton.

13. The compound of any one of claims 1 to 12, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein: X 10 Is it N or CR? 10 ; X 11 It is CR 11 And X 12 It is CR 12 , or X 11 It is CR 11 And X 12 It is N, or X 11 It is N and X 12 It is CR 12 ; X 13 Is it N or CR? 13 ;and X 10 X 11 X 12 and X 13 No more than one of them is N.

14. The compound of any one of claims 1 to 13, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein: R 11 and R 12 One of them is present and is selected from fluorine, chlorine, bromine, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2 or -C(=NH)NH2 group; A remaining R 10 R 11 R 12 Or R 13 Independently selected from hydrogen or fluorine, chlorine, bromine, -OH, -SH, -NH2, -SO2NH2 or Cl-C 10 A saturated or unsaturated hydrocarbon group, wherein the hydrocarbon group may be straight-chain or branched, or may contain one or two cyclic groups, wherein the hydrocarbon group may optionally be substituted with one or more fluorine, chlorine, and / or bromine groups, wherein the hydrocarbon group may optionally contain one, two, three, four, five, or six heteroatoms independently selected from N, O, and S in its carbon skeleton, and one of the -S- moieties may optionally be substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties; and If it exists, each additional remaining R 10 R 11 R 12 Or R 13 It is independently selected from hydrogen or fluorine, chlorine or bromine groups.

15. The compound of claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein the compound is a compound of formula (Ia): Formula (Ia) in: R 1 It is hydrogen; R 2 It is hydrogen; R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -R 31 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group; R 30 Selected from methyl or fluoromethyl; R 31 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be converted by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 replace; Each R 32 Independently selected from methyl or fluoromethyl; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group, Each R 42 Independently selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is a hydrogen, fluorine, chlorine, or bromine group; R 6 It is chlorine, bromine, methyl, or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 - All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75 They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; Or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 10 carbon atoms; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; X 10 Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; If it exists, R 10 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups, provided that the R group includes any optional substituents 10 It contains no more than 10 carbon atoms, of which: Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted with one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups can optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; R 12 Selected from hydrogen or fluorine, chlorine or bromine groups; and If it exists, R 13 Selected from hydrogen, fluorine, chlorine, or bromine groups.

16. The compound of claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein the compound is a compound of formula (Ib): Formula (Ib) in: R 1 It is hydrogen; R 2 It is hydrogen; R 3 Selected from hydrogen or fluorine, chlorine, bromine, -R 30 -R 31 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Group; R 30 Selected from methyl or fluoromethyl; R 31 It is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group may optionally be converted by one or more fluorine, chlorine and / or bromine groups and / or one or two R groups. 32 replace; Each R 32 Independently selected from methyl or fluoromethyl; R 4 Selected from fluorine, chlorine, bromine, -OR 44 -CON(R) 42 )2、-SO2-R 44 -SO2-N(R) 42 )2、-O-CH2-CH2-OR 44 -O-CH2-CH2-N(R) 42 )2 or -R 44 Group, Each R 42 Independently selected from hydrogen or -R 44 Group; Each R 44 Independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl; R 5 It is a hydrogen, fluorine, chlorine, or bromine group; R 6 It is chlorine, bromine, methyl, or fluoromethyl; R 7 Selected from hydrogen or fluorine, -COOH, -COOR 75 -CONH2, -CONHR 75 -CON(R) 75 )2、-L 71 -COOH, -L 71 -COOR 75 -L 71 -CONH2, -L 71 -CONHR 75 -L 71 -CON(R 75 )2、-L 71 -OH, -L 71 -OR 75 or -R 75 Group; Each -L 71 - All are independently selected from -CH2-, -CHMe-, -CMe2-, , -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, , , , -CH2-CH2-CH2-, -CHMe-CH2-CH2-, -CH2-CHMe-CH2-, -CH2-CH2-CHMe-, -CMe2-CH2-CH2-, -CHMe-CHMe-CH2-, -CHMe-CH2-CHMe-, -CH2-CMe2-CH2-, -CH2-CHMe-CHMe-, -CH2-CH2-CMe2-, -CMe2-CHMe-CH2-, -CMe2-CH2-CHMe -, -CHMe-CHMe2-CH2-, -CHMe-CHMe-CHMe-, -CHMe-CH2-CMe2-, -CH2-CMe2-CHMe-, -CH2-CHMe-CMe2-, -CMe2-C Me2-CH2-, -CMe2-CHMe-CHMe-, -CMe2-CH2-CMe2-, -CHMe-CMe2-CHMe-, -CHMe-CHMe-CMe2-, -CH2-CMe2-CMe2-, , , , or Groups, wherein any -L 71 -Optionally fluorinated; and Each R 75 Independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl, or any two R atoms attached to the same nitrogen atom. 75 They can form 4- to 6-membered saturated monocyclic heterocyclic groups together with the nitrogen atoms to which they are attached, wherein the 4- to 6-membered saturated monocyclic heterocyclic groups may optionally be substituted with one or more fluorine groups and / or one or two methyl groups, wherein the methyl groups may optionally be fluorine-substituted; Or R 7 yes: in: m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4 or 5; 2≤m+n≤5; and R 76 Selected from hydrogen or C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl; R 7 It contains no more than 10 carbon atoms; R 8 Selected from hydrogen or fluorine, methyl or fluoromethyl; R 9 Selected from hydrogen, fluorine, chlorine, or bromine groups; X 10 Is it N or CR? 10 ; X 13 Is it N or CR? 13 ; X 10 and X 13 No more than one of them is N; If it exists, R 10 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 11 Selected from hydrogen, fluorine, chlorine, or bromine groups; R 12 Selected from chlorine, bromine, methoxy, fluoromethoxy, -CH2OH, or -CN groups; If it exists, R 13 Selected from hydrogen or fluorine, chlorine, bromine, -R 131 -OR 131 -N(R) 132 )2、-L 13 -OH, -L 13 -SH、-L 13 -OR 131 -L 13 -SR 131 -L 13 -N(R 132 )2、-L 13 -SO2-R 131 -L 13 -SO2-N(R 132 )2、-OL 13 -OH, -OL 13 -SH、-OL 13 -OR 131 -OL 13 -SR 131 -OL 13 -N(R 132 )2、-OL 13 -SO2-R 131 -OL 13 -SO2-N(R 132 )2、-NR 133 -L 13 -OH, -NR 133 -L 13 -SH、-NR 133 -L 13 -OR 131 -NR 133 -L 13 -SR 131 -NR 133 -L 13 -N(R 132 )2、-NR 133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 )2 groups; Each R 131 Independently selected from C1-C4 alkyl or C3-C6 cycloalkyl, wherein the C1-C4 alkyl or C3-C6 cycloalkyl may optionally be substituted with one or more fluorine groups and / or one or two oxo (=O) groups; Each R 132 Independently selected from hydrogen or -R 131 Group; R 133 Selected from hydrogen or -R 131 Group; L 13 It is a straight-chain alkylene or alkenylene group, wherein the straight-chain alkylene or alkenylene group optionally contains one, two, or three heteroatoms, each independently selected from O and N, in its carbon skeleton, wherein L 13 Chains with lengths ranging from 1 to 8 atoms, where L 13 Optionally, it may be composed of one or two groups, each independently selected from oxo (=O) and -OH, and / or one or more groups R. L13 replace; Each R L13 It is independently selected from fluorine, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe or -CH2O-fluoromethyl; Or any two R L13 , or any R L13 And any R 131 , or any two R 131 They can form 3- to 7-membered monocyclic groups together with one or more atoms to which they are attached, wherein the 3- to 7-membered monocyclic groups can optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; Or any two R L13 And any R 131 , or any three R L13 And any R 131 , or any two R L13 And any two R 131 They can form 6- to 10-membered bicyclic heterocyclic groups together with the atoms to which they are attached, wherein the 6- to 10-membered bicyclic heterocyclic groups may optionally be substituted by one or two groups each independently selected from oxo (=O) and -OH and / or one or more fluorine, methyl and / or fluoromethyl groups; The premise is that R includes any optional substituents. 13 It contains no more than 10 carbon atoms.

17. A compound, said compound being selected from the group consisting of: 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 , , , , , , , , , , and ; Or a pharmaceutically acceptable salt and / or solvate and / or prodrug of the selected compound.

18. A pharmaceutical composition comprising the compound of any one of claims 1 to 17 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, and a pharmaceutically acceptable excipient.

19. The compound of any one of claims 1 to 17, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, or the pharmaceutical composition of claim 18, for use as a medicament.

20. The compound of any one of claims 1 to 17 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, or the pharmaceutical composition of claim 18, for the treatment or prevention of a disease, condition or disorder, wherein the disease, condition or disorder is responsive to factor B inhibition.

21. The compound of claim 19 or claim 20, or a pharmaceutically acceptable salt and / or solvate and / or prodrug, or pharmaceutical composition thereof, for the treatment or prevention of a disease, condition, or ailment, wherein said disease, condition, or ailment is selected from: (i) Eye disease, condition or disorder; (ii) Blood disorders, ailments, or ailments; (iii) Kidney disease, condition, or disorder; (iv) Respiratory diseases, symptoms or ailments; (v) Diseases, symptoms or disorders of the central nervous system; (vi) Cardiovascular disease, condition or illness; (vii) Reproductive diseases, symptoms, or ailments; (viii) Metabolic diseases, symptoms, or disorders; (ix) Cancer; (x) Autoimmune diseases, conditions, or disorders; (xi) Musculoskeletal diseases, conditions or disorders; (xii) Antiphospholipid syndrome; (xiii) Skin diseases, symptoms, or ailments; (xiv) Hemodialysis; or (xv) Any disease in which an individual has been identified as carrying a germline or somatic non-silent mutation of factor B.

22. The compound of claim 19 or claim 20, or a pharmaceutically acceptable salt and / or solvate and / or prodrug, or pharmaceutical composition thereof, for the treatment or prevention of a disease, condition, or ailment, wherein said disease, condition, or ailment is selected from: (i) Acute kidney injury; (ii) Age-related macular degeneration; (iii) Airway hyperresponsiveness with inflammation; (iv) Alzheimer's disease; (v) Amyotrophic lateral sclerosis (ALS); (vi) ANCA vasculitis; (vii) Antiphospholipid syndrome; (viii) Aortic stenosis; (ix) Atypical hemolytic uremic syndrome; (x) Acquired partial lipodystrophy; (xi) Acquired thrombotic thrombocytopenic purpura; (xii) Bullous pemphigoid; (xiii) C3 glomerulonephropathy; (xiv) Immune complex-mediated membranoproliferative glomerulonephritis (IC-MPGN) (xv) Myocardial ischemia-reperfusion; (xvi) Cardiac remodeling; (xvii) Cardiovascular and metabolic diseases; (xviii) Celiac diarrhea; (xix) Cold agglutinin disease; (xx) Respiratory symptoms caused by SARs Cov-2; (xxi) Diabetic nephropathy; (xxii) Diabetic retinopathy; (xxiii) Doyne’s honeycomb retinal dystrophy, also known as familial dominant drusen (DHRD / ML); (xxiv) Focal segmental glomerulosclerosis (FSGS); (xxv) Glomerulosclerosis; (xxvi) Guillain-Barré syndrome; (xxvii) Heart failure; (xxviii) Hemodialysis; (xxix) Idiopathic thrombocytopenic purpura (ITP); (xxx) Idiopathic pulmonary fibrosis; (xxxi) IgA nephropathy; (xxxii) Ischemic stroke; (xxxiii) Systemic lupus erythematosus; (xxxiv) Lupus nephritis (xxxv) Lupus encephalitis; (xxxvi) Malignant nephrosclerosis; (xxxvii) Multiple sclerosis; (xxxviii) Myasthenia gravis; (xxxix) Neuromyelitis optica; (xl) Non-infectious uveitis; (xli) Osteoarthritis; (xlii) Pancreatic cancer; (xliii) Paroxysmal nocturnal hemoglobinuria (PNH); (xliv) photocarcinogenic effects; (xlv) Post-infectious glomerulonephritis; (xlvi) Preeclampsia; (xlvii) membranous nephropathy; (xlviii) Kidney allogeneic transplantation; (xlix) Retinal detachment; (l) Retinal ischemia-reperfusion; (li) Rheumatoid arthritis; (lii) Schizophrenia; (liii) Delayed hemolytic transfusion reaction (DHTR) in individuals with sickle cell disease; (liv) Vascular occlusive crisis in sickle cell disease; (lv) Spinal cord injury; (lvi) squamous cell carcinoma; (lvii) Thrombotic microangiopathy (TMA)-mediated acute kidney injury (AKI); (lviii) Transplant-related thrombotic microangiopathy; or (lix) Traumatic brain injury.

23. A method for inhibiting factor B, the method comprising using a compound of any one of claims 1 to 17 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, or a pharmaceutical composition of claim 18 to inhibit factor B.

24. A method for synthesizing the compound of claim 1 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, the method comprising the following steps: (i) Reacting compound (SM-1) with compound (SM-2) to produce intermediate (It-1): as well as (ii) Deprotecting the intermediate of formula (It-1) to produce a compound of formula (I), or a pharmaceutically acceptable salt and / or solvate thereof: in: R P It is a nitrogen-protecting group; R L It is a leaving group; and R 1 To R 8 and X 9 To X 13 As defined in claim 1.

25. A method for synthesizing the compound of claim 4 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, the method comprising the following steps: (i) Reacting the compound of formula (SM-3) with the compound of formula (SM-2) to produce the intermediate of formula (It-2): as well as (ii) Deprotecting the intermediate of formula (It-2) to produce a compound of formula (II), or a pharmaceutically acceptable salt and / or solvate thereof: in: R P It is a nitrogen-protecting group; R L It is a leaving group; and R 1 R 4 To R 8 X 9 To X 13 and R 14 To R 17 As defined in claim 4.

26. A method for synthesizing the compound of claim 4 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, the method comprising the following steps: (i) Reduction of compound (P-1) to compound (P-2), or its pharmaceutically acceptable salt and / or solvate: in: R X Selected from hydrogen or R P ; R P It is a nitrogen-protecting group; R 4 To R 8 X 9 To X 13 and R 14 To R 17 As defined in claim 4; and R 2 and R 3 As defined in claim 1.

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