2-(1H-indole-4-yl)methyl)isoindoline derivatives as factor B inhibitors

Abstract

The present invention relates to a compound (I) having an indole moiety linked to an isoindoline moiety, compounds having a similar core structure, and related salts, solvates, prodrugs, and pharmaceutical compositions. The present invention further relates to methods for synthesizing such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most specifically by inhibiting factor B. Typically, the compounds of the present invention contain one or fewer quaternary ammonium groups. More typically, the compounds of the present invention do not contain quaternary ammonium groups. JPEG2026522993000076.jpg78165

Description

[Technical Field]

[0001] The present invention relates to compounds having an indole moiety linked to an isoindoline moiety, compounds having a similar core structure, and related salts, solvates, prodrugs, and pharmaceutical compositions. The present invention further relates to methods for synthesizing such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most specifically by inhibiting factor B. [Background technology]

[0002] The complement system is an important part of the innate immune system, playing a role in helping the body fight infections caused by pathogens, ultimately leading to inflammation and the removal of pathogens or foreign substances through phagocytosis.

[0003] The complement system consists of several proteins, including zymogen, which are activated by proteolytic cleavage and promote further zymogen activation within the cascade. These proteins may be zymogen or proteins lacking enzymatic potential, whose binding sites to other components in the system are exposed through structural changes. Because these successive enzymatic cleavages lead to a greater amplification response, the system contains many regulatory components 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 induced by antigen-antibody complexes, linking the innate immune system to the adaptive immune system. The lectin pathway is directly induced by pathogens when mannan-binding lectins, collectins, or ficolins of serum proteins bind to bacterial or viral mannose-containing carbohydrates. The alternative pathway (also known as the alternate pathway) is initiated by the activation of C3, the central complement component, either through spontaneous hydrolysis or enzymatic cleavage. The alternative pathway also functions as a crucial amplification loop for all three pathways of complement activation.

[0005] Ultimately, all of these pathways generate C3 convertase, which further cleaves and activates C3 molecules, thereby 1) promoting opsonization of pathogens, allowing them to be phagocytosed by phagocytic cells that recognize key receptors; 2) promoting the recruitment of inflammatory cells by producing chemotactic inducers at the activation site; and 3) promoting the formation of C5 convertase, resulting in the production of C5a and C5b. The latter, C5b, assembles terminal complement components to induce direct killing of pathogens by forming membrane invasion complex (MAC) pores on the membranes of bacteria or other target cells (Janeway, CAJr. et al, (2001) The complement system and innate immunity, in Immunobiology: The Immune System in Health and Disease, Garland Science, New York).

[0006] Factor B, a trypsin-like serine protease, is an element of an alternative pathway in the complement cascade. It circulates in zymogenous form 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 forms C3(H2O). Factor B can bind to the active forms of C3:C3(H2O) and C3b, thereby generating the enzyme precursor C3bB (or C3(H2O)B), which is the target of activation by factor D. It is cleaved by factor D to produce two fragments, 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, I-Reds.), Academic Press). Ba is released, but Bb, which contains the serine protease domain, remains bound to C3(H2O) and C3b, forming the alternative C3 convertase pathway [C3(H2O)Bb and C3bBb]. These induce an amplification loop by converting C3 to C3a and then to C3b. When another C3b is added to the C3 convertase, a C5 convertase is produced (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 produce anaphylatoxins C5a and C5b, which function as a platform for the formation of membrane invasion complexes.

[0008] Dysregulation of alternative complement pathways, whether hereditary or due to the presence of autoantibodies, can lead to a wide variety of diseases. Therefore, inhibition of factor B is a key therapeutic target for regulating alternative pathways and, consequently, for treating many diseases, disorders, and conditions.

[0009] Iptacopan (LNP023), disclosed by Mainolfi et al. in J.Med.Chem., 2020, vol.63, pp.5697-5722, is a known factor B inhibitor having the following structure. [ka]

[0010] Iptacopan has been shown to have high selectivity for factor B and not inhibit factor D or the classical or lectin complement pathway. Furthermore, no significant effects have been observed in a broad panel of assays for receptors, ion channels, kinases, and proteases (Schubart, A. et al, Proc. Natl. Acad. Sci. USA 2019, 116, 7926-7931). This drug has recently shown success in a Phase III clinical trial in patients with paroxysmal nocturnal hemoglobinuria (PNH) (Novartis Press Release, “Novartis Phase III APPOINT-PNH trial shows investigational oral monotherapy iptacopan improves hemoglobin to near-normal levels, leading to transfusion independence in all treatment-naive PNH patients”, 26 April 2023). Further indole derivatives that have been reported to possess factor B inhibitory activity include WO2013 / 164802A1, US2013 / 0296377A1, WO2014 / 143638A1, WO2015 / 009616A1, WO2022 / 028507A1, WO2022 / 028527A1, WO2022 / 143940A1, and WO2022 / 143 It is disclosed in 845A1, WO2022 / 155294A1, WO2022 / 218429A1, WO2022 / 256586A2, WO2023 / 278698A1, WO2023 / 020566A1, WO2023 / 072197A1, WO2023 / 139534A1, WO2023 / 187715A1, and WO2024 / 049977A1. However, there is a need to provide further factor B inhibitors, particularly selective factor B inhibitors (e.g., those for inhibiting 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 compounds that provide useful substitutes for known compounds. [Prior art documents] [Patent Documents]

[0011] [Patent Document 1] International Publication No. 2013 / 164802 [Patent Document 2] U.S. Patent Application Publication No. 2013 / 0296377 [Patent Document 3] International Publication No. 2014 / 143638 [Patent Document 4] International Publication No. 2015 / 009616 [Patent Document 5] International Publication No. 2022 / 028507 [Patent Document 6] International Publication No. 2022 / 028527 [Patent Document 7] International Publication No. 2022 / 143940 [Patent Document 8] International Publication No. 2022 / 143845 [Patent Document 9] International Publication No. 2022 / 155294 [Patent Document 10] International Publication No. 2022 / 218429 [Patent Document 11] International Publication No. 2022 / 256586 [Patent Document 12] International Publication No. 2023 / 278698 [Non-patent literature]

[0012] [Non-Patent Document 1] Schubart,A.et al,Proc.Natl.Acad.Sci.USA2019,116,7926-7931 [Overview of the project] [Means for solving the problem]

[0013] A first aspect of the present invention provides a compound of formula (I): [ka] During the ceremony, R 1 is hydrogen; R 2 is selected from hydrogen or a halo group; R 3 The -S- moiety is selected from hydrogen or a halo, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 4 is selected from hydrogen or halo, -OH, -NH2, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain them, the hydrocarbyl group may be optionally substituted with one or more halo groups, the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo(=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 5 is selected from hydrogen or a halo group; R 6 is selected from hydrogen or halo, -R 60 or -OR 60 groups, where R 60 is selected from a C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl group; R 7 and R 8 are each independently selected from hydrogen or fluoro, or a C1-C 12 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain them, the hydrocarbyl group may be optionally substituted with one or more halo groups, the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo(=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 7 or R 8Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 3 and R 7 , or R 4 and R 7 These combine to form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched, or consist of one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which it is bonded is a carbon atom; X 10 is N or CR 10 and; X 11 is N or CR 11and; X 12 is N or CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 , and X 13 Two or fewer of these are N; Each R 10 , R 11 , R 12 , and R 13 This is hydrogen or halo, -OH, -SH, -NH2, -SO2NH2, or C1-C 12 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 18 and R 19 is hydrogen or fluoro, or C1-C 12 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining R is directly bonded to the molecule.18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and R 20 and R 21 is independently selected from hydrogen or fluoro groups, or R 20 and R 21 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0014] A second aspect of the present invention provides a compound of formula (II): [ka] During the ceremony, R 1 is hydrogen; R 4The hydrogen group is selected from hydrogen or a halo, -OH, -NH2, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 5 is selected from hydrogen or a halo group; R 6 is hydrogen or halo, -R 60 OR 60 Selected from the base, where R 60 This is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 is hydrogen or fluoro, or C1-C 12 A saturated or unsaturated hydrocarbyl group is independently selected, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining molecule is directly bonded to R 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; X 10 is N or CR 10 and; X 11 is N or CR 11 and; X 12 is N or CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 , and X 13 Two or fewer of these are N; Each R 10 , R 11 , R 12 , and R 13 This is hydrogen or halo, -OH, -SH, -NH2, -SO2NH2, or C1-C 12Independently selected from saturated or unsaturated hydrocarbyl groups, wherein said hydrocarbyl group is linear or branched, or one or more cyclic groups, or may contain them, said hydrocarbyl group may be optionally substituted with one or more halo groups, said hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo(=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; Each R 14 and R 15 is independently selected from hydrogen or a C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl group, or R 14 and R 15 together with the carbon atom to which they are attached form a 3- to 6-membered cyclic group, wherein said cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo(=O), methyl or ethyl groups, wherein any methyl or ethyl group may be optionally fluorine-substituted; R 16 is hydrogen or selected from fluoro, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, wherein said hydrocarbyl group is linear or branched, or one or more cyclic groups, or may contain them, said hydrocarbyl group may be optionally substituted with one or more halo groups, said hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo(=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 17is selected from hydrogen or a fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl group; Alternatively, R 16 and R 17 together with the carbon atom to which they are attached form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl or ethyl groups, where any methyl or ethyl group may be optionally fluoro-substituted; Alternatively, R 17 and R 7 or R 4 and R 7 together form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched or one or more cyclic groups or contain them, the hydrocarbylene group may be optionally substituted with one or more halo groups, the hydrocarbylene group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the atom of the hydrocarbylene group directly bonded to the carbon atom to which R 8 is attached is a carbon atom; R 18 and R 19 are hydrogen or fluoro, or C1-C 12A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining R is directly bonded to the molecule. 18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and R 20 and R 21 is independently selected from hydrogen or fluoro groups, or R 20 and R 21These, together with the carbon atoms to which they are bonded, form a C=O group. [Modes for carrying out the invention]

[0015] In the context of this specification, a "hydrocarbyl" substituent or hydrocarbyl moiety within a substituent contains only carbon and hydrogen atoms, but unless otherwise specified, its carbon skeleton does not contain any heteroatoms such as N, O, or S. Hydrocarbyl groups / molets may be saturated or unsaturated (including aromatic), and may be linear or branched, cyclic, or contain both, and unless otherwise specified, such cyclic groups do not contain any heteroatoms such as N, O, or S in their carbon skeleton. Examples of hydrocarbyl groups include alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl groups / molets, as well as all combinations of these groups / molets. Typically, a hydrocarbyl group is C1-C 20 It is a hydrocarbyl group. More typically, a hydrocarbyl group is C1-C 15 It is a hydrocarbyl group. More typically, a hydrocarbyl group is C1-C 10 It is a hydrocarbyl group. The "hydrocarbylene" group is defined in the same way as the divalent hydrocarbyl group.

[0016] The alkyl substituent or the alkyl moiety within the substituent can be linear (i.e., linear) or branched. Examples of alkyl groups / moieties include methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl, t-butyl, and n-pentyl groups / moieties. Unless otherwise specified, the term "alkyl" does not include "cycloalkyl". Typically, alkyl groups are C1-C 12 It is an alkyl group. More typically, alkyl groups are C1-C6 alkyl groups. The "alkylene" group is defined similarly to a divalent alkyl group.

[0017] An "alkenyl" substituent or alkenyl moiety within a substituent refers to an unsaturated alkyl group or moiety having one or more carbon-carbon double bonds. Examples of alkenyl groups / moies include ethenyl, propenyl, 1-butenyl, 2-butenyl, 1-pentenyl, 1-hexenyl, 1,3-butadienyl, 1,3-pentadienyl, 1,4-pentadienyl, and 1,4-hexadienyl groups / moies. Unless otherwise specified, the term "alkenyl" does not include "cycloalkenyl". Typically, an alkenyl group is C2-C 12 It is an alkenyl group. More typically, an alkenyl group is a C2-C6 alkenyl group. The "alkenylene" group is defined similarly to the divalent alkenyl group.

[0018] An "alkynyl" substituent or 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 / movies include ethynyl, propargyl, buta-1-inyl, and buta-2-inyl groups / movies. Typically, an alkynyl group is C2-C 12 It is an alkynyl group. More typically, an alkynyl group is a C2-C6 alkynyl group. The "alkynylene" group is defined similarly to the divalent alkynyl group.

[0019] A "cyclic" substituent or cyclic portion within a substituent refers to any hydrocarbyl ring, which may be saturated or unsaturated (including aromatic) and may contain one or more heteroatoms, e.g., N, O, or S, in its carbon skeleton. Examples of cyclic groups include cycloalkyl, cycloalkenyl, heterocyclic, aryl, and heteroaryl groups, as described later. Cyclic groups may be monocyclic, bicyclic (e.g., bridging, condensed, or spiro), or polycyclic. Typically, a cyclic group is a 3- to 12-membered cyclic group, meaning it contains 3 to 12 ring atoms. More typically, a cyclic group is a 3- to 7-membered monocyclic group, meaning it contains 3 to 7 ring atoms.

[0020] To avoid any ambiguity, when a bicyclic or polycyclic group or moiety is described as "saturated," it should be understood that all ring systems of the bicyclic or polycyclic group or moiety (excluding any substituent moiety or any ring systems formed by it) are saturated.

[0021] A "heterocyclic" substituent or heterocyclic portion within a substituent refers to a cyclic group or portion containing one or more carbon atoms and one or more (e.g., 1, 2, 3, or 4) heteroatoms, such as N, O, or S, in the ring structure. Examples of heterocyclic groups include heteroaryl groups and non-aromatic heterocyclic groups, such as azethinyl, azetidinyl, oxetanyl, thietanyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrazolidinyl, imidazolidinyl, dioxolanyl, oxathiolanyl, piperidinyl, tetrahydropyranyl, thianyl, piperazinyl, dioxanyl, morpholinyl, and thiomorpholinyl groups.

[0022] The "cycloalkyl" substituent or the cycloalkyl portion within the substituent refers to a saturated hydrocarbyl ring containing, for example, 3 to 7 carbon atoms, including cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. Unless otherwise specified, the cycloalkyl substituent or portion may include monocyclic, bicyclic, or polycyclic hydrocarbyl rings.

[0023] The "cycloalkenyl" substituent or cycloalkenyl moiety within the substituent refers to a non-aromatic unsaturated hydrocarbyl ring having one or more carbon-carbon double bonds, for example, containing 3 to 7 carbon atoms, including cyclopente-1-en-1-yl, cyclohexa-1-en-1-yl, and cyclohexa-1,3-dien-1-yl. Unless otherwise specified, the cycloalkenyl substituent or moiety may include monocyclic, bicyclic, or polycyclic hydrocarbyl rings.

[0024] The "aryl" substituent or the aryl portion within a substituent refers to an aromatic hydrocarbyl ring. The term "aryl" refers to monocyclic aromatic hydrocarbons and polycyclic fused-ring aromatic hydrocarbons, where all of the fused ring (except for any substituted portion or any ring system formed by them) is aromatic. Examples of aryl groups / parts include phenyl, naphthyl, anthracenyl, and phenantrenyl. Unless otherwise specified, the term "aryl" does not include "heteroaryl."

[0025] A heteroaryl substituent or heteroaryl moiety within a substituent refers to an aromatic heterocyclic group or moiety. The term "heteroaryl" refers to monocyclic and polycyclic fused aromatic heterocyclic rings, where all fused ring systems (except for any substituent moiety or any ring system formed by them) are aromatic. Examples of heteroaryl groups / moies include: [ka] In the formula, G = O, S, or NH. Specific examples of 5- or 6-membered heteroaryl groups include furanyl, thiophenyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, flazanyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, and triazinyl groups.

[0026] Unless otherwise specified, when a bicyclic or polycyclic group or part is described as aromatic, such as an aryl or heteroaryl group, it should be understood that the entire ring system of the bicyclic or polycyclic group or part (excluding any substituted part or any ring system formed by it) is aromatic. Similarly, when a bicyclic or polycyclic group or part is described as unaromatic, such as a cycloalkyl, cycloalkenyl, or non-aromatic heterocyclic group, it should be understood that the entire ring system of the bicyclic or polycyclic group or part (excluding any substituted part or any ring system formed by it) is unaromatic.

[0027] For the purposes of this specification, when a combination of parts is referred to as a single group, for example, arylalkyl, arylalkenyl, arylalkynyl, alkylaryl, alkenylaryl, or alkynylaryl, the last referred part includes the atoms of the remaining molecule to which the group is bonded. An example of an arylalkyl group is benzyl.

[0028] In the parts that have been optionally replaced, as can be understood: Each hydrogen atom may be optionally replaced by any given monovalent substituent; - Any two hydrogen atoms bonded to the same carbon or nitrogen atom may be optionally replaced by any given π-bond type substituent; - Any sulfur atom may be optionally substituted with one or two of any given π-bond type substituents; and - In the same optionally substituted group or moiety, any two hydrogen atoms bonded to the same or different atoms may be optionally replaced by any predetermined divalent bridging substituent.

[0029] Typically, substituents include one, two, three, or four substituents, more typically one, two, or three substituents, more typically one or two substituents, and more typically one substituent.

[0030] Unless otherwise specified, any divalent crosslinking substituent (e.g., -O-, -S-, -NH-, -CH2-, -CH2-CH2-CH2) of any selectively substituted group or moiety (e.g., R1) 2 - etc.) must bond only to the specified group or part, even if the second group or part itself can be optionally substituted, the second group or part (e.g., R 2 It cannot be joined to ).

[0031] The term "halo" includes fluoro, chloro, bromo, and iodine.

[0032] Unless otherwise stated, when a group is prefixed with the term "halo," such as a haloalkyl or halomethyl group, it should be understood that the group in question is substituted with one or more halo groups independently selected from fluoro, chloro, bromo, and iodine. Typically, the maximum number of halo substituents is limited only by the number of hydrogen atoms available for substitution in the corresponding group without the halo prefix. For example, a halomethyl group may contain one, two, or three halo substituents. A haloethyl or halophenyl group may contain one, two, three, four, or five halo substituents. Similarly, unless otherwise stated, when a group begins with a particular halo group, it should be understood that the group in question is substituted with one or more of those particular halo groups. For example, the term "fluoromethyl" refers to a methyl group substituted with one, two, or three fluoro groups.

[0033] Similarly, unless otherwise specified, in the case of a group said to be "halosubstituted," it should be understood that the group in question is substituted with one or more halo groups independently selected from fluoro, chloro, bromo, and iodo. Typically, the maximum number of halo substituents is limited only by the number of hydrogen atoms available for substitution in the group said to be halosubstituted. For example, a halosubstituted methyl group may contain one, two, or three halo substituents. A halosubstituted ethyl or halosubstituted phenyl group may contain one, two, three, four, or five halo substituents.

[0034] Unless otherwise specified, a reference to an element is assumed to refer to all isotopes of that element. Therefore, for example, unless otherwise stated, a reference to hydrogen is assumed to include all isotopes of hydrogen, including deuterium and tritium.

[0035] Unless otherwise specified, any reference to a compound or group shall be interpreted as a reference to all tautomers of that compound or group.

[0036] When referring to a hydrocarbyl or other group that contains one or more heteroatoms N, O, or S in its carbon skeleton, or when referring to a carbon atom of a hydrocarbyl or other group that is replaced by an N, O, or S atom, what is intended is: [ka] but [ka] Replaced by; [ka] but, [ka] Replaced by; -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, This means that CH≡ is replaced by N≡; However, this is conditional on the resulting group containing at least one carbon atom. For example, methoxy, dimethylamino, and aminoethyl groups are considered hydrocarbyl groups containing one or more heteroatoms N, O, or S in their carbon skeletons.

[0037] Typically, the compounds of the present invention contain one or fewer quaternary ammonium groups. More typically, the compounds of the present invention do not contain any quaternary ammonium groups.

[0038] In the context of this specification, unless otherwise specified, C x -C y A group is defined as a group containing x to y carbon atoms. For example, a C1-C4 alkyl group is defined as an alkyl group containing 1 to 4 carbon atoms. x -C y For the purpose of assigning x and y to the group, any substituent is not considered when calculating the total number of carbon atoms in the parent group substituted with any substituent. To avoid doubt, substituted heteroatoms, such as N, O, or S, are C x -C y When calculating the number of carbon atoms in a group, it is not counted as a carbon atom. For example, the morpholinyl group is considered a C4 heterocyclic group and not a C6 heterocyclic group.

[0039] For the purposes of this specification, where it is stated that a first atom or group is "directly bonded" 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 intervening atoms or groups. For example, in the group -(C=O)N(CH3)2, each carbon atom of the methyl group is directly bonded to the nitrogen atom, and each carbon atom of the carbonyl group is directly bonded to the nitrogen atom, but the carbon atoms of the carbonyl group are not directly bonded to either methyl group's carbon atoms.

[0040] As described in accordance with the first aspect of the present invention, R 2 R is selected from hydrogen or a halo group. In one embodiment, R 2 The group is selected from hydrogen, fluoro, chloro, or bromo groups. Most typically, R 2 It is hydrogen.

[0041] As described in accordance with the first aspect of the present invention, R 3is selected from hydrogen or halo, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, or R 3 and R 7 These combine to form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched, or consist of one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0042] In one embodiment, R 3The -S- moiety is selected from hydrogen or a halo, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety.

[0043] In one embodiment of such a configuration, R 3 is hydrogen or halo (e.g., fluoro, chloro, or bromo), -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Selected from the base, where R 30 This includes C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 31 Selected from the base, R 31 R is a 3-6 member monocyclic group, where the 3-6 member monocyclic group is one or more halo (e.g., fluoro, chloro, or bromo) groups and / or one or two groups R 32 It may be optionally replaced, and each R 32 The group R is independently selected from methyl or fluoromethyl groups, provided that the group R contains any substituent of either type. 3 The condition is that it contains 8 or fewer carbon atoms. Typically, in such embodiments, R 3 is hydrogen or fluoro, chloro, bromo, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Selected from the base, where R 30 This refers to C1-C4 alkyl, C1-C4 fluoroalkyl, or -R 31Selected from the base, where R 31 The group is selected from a C3-C6 cycloalkyl group, a 4-6 member saturated heterocyclic group, or a phenyl or 5 or 6 member heteroaryl group, where the C3-C6 cycloalkyl group and the 4-6 member saturated heterocyclic group are one or more fluoro groups and / or one or two groups R 32 The phenyl or the 5- or 6-membered heteroaryl group may be optionally substituted with one or more fluoro, chloro and / or bromo groups, and / or one or two R groups. 32 The group R may be optionally substituted, provided that any of the substituents are included. 3 The condition is that it contains 8 or fewer carbon atoms. More typically, in such embodiments, R 3 is hydrogen or fluoro, chloro, bromo, -R 30 , R 31 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Selected from the base, where R 30 is selected from a methyl or fluoromethyl group, and R 31 is a 5-membered heteroaryl group, where the 5-membered heteroaryl group is one or more fluoro, chloro and / or bromo groups and / or one or two groups R 32 It may be optionally replaced.

[0044] In another embodiment of such a configuration, R 3 is hydrogen or halo (e.g., fluoro, chloro, or bromo), -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Selected from the base, where R 30 R is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in such embodiments, R 3 is hydrogen or fluoro, chloro, bromo, -R 30 -CN, -CHO, -COR 30-CO2H or -CO2R 30 Selected from the base, where R 30 The group is selected from methyl or fluoromethyl groups.

[0045] In a further embodiment of such a configuration, R 3 R is selected from hydrogen or halo (e.g., fluoro, chloro, or bromo), -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in such embodiments, R 3 The group is selected from hydrogen, fluoro, chloro, bromo, -CN, or methyl groups, where the methyl group may be optionally substituted with a fluoro group.

[0046] More typically, R 3 The group is selected from hydrogen, fluoro, chloro, or bromo groups. Most typically, R 3 It is hydrogen.

[0047] In another embodiment of the first aspect of the present invention, R 3 and R 7 These combine to form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched, or consist of one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0048] Typically, R 3 and R 7When these atoms combine to form a hydrocarbylene group, the hydrocarbylene group containing any of the substituents contains four or fewer carbon atoms.

[0049] Typically, R 3 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any hydrocarbylene group (including any substituent) formed by is 3 or less. More typically, R 3 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any hydrocarbylene group (including any substituent) formed by this is 2 or less.

[0050] Typically, in such embodiments, R 3 and R 7 Together, they form a C1-C4 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear, branched, or cyclic, and may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0051] R 3 and R 7When these molecules combine to form a hydrocarbylene group, the hydrocarbylene group typically has a chain length of 1 to 3 atoms. More typically, the hydrocarbylene group has a chain length of 1 or 2 atoms. To be understood, the “chain length” of a hydrocarbylene group refers to the number of atoms in the hydrocarbylene group that are linked to each other in a continuous chain between the two bond points to which the hydrocarbylene group is attached to the rest of the molecule, when measured along 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.

[0052] [ka] More typically, R 3 and R 7 When these groups combine to form a hydrocarbylene group, the hydrocarbylene group is selected from -CH2-, -CH2-CH2-, -CH=CH-, -CH2-O-, or -O-CH2-, however, R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0053] Typically, R 3 and R 7 When they come together to form a hydrocarbylene group, R 8 R is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More typically, R 3 and R 7 When they come together to form a hydrocarbylene group, R 8 R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups. More typically, 3 and R 7 When they come together to form a hydrocarbylene group, R 8 It is hydrogen.

[0054] As described in both the first and second aspects of the present invention, R 4 is selected from hydrogen or halo, -OH, -NH2, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, or R 4 and R 7 These combine to form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched, or consist of one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0055] In one embodiment, R 4The group is selected from hydrogen or halo, -OH, -NH2, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety.

[0056] Typically, in such embodiments, R 4 This refers to hydrogen or fluoro, chloro, bromo, -OH, -NH2, -SO2NH2, -SO2-R 40 or -R 40 Selected from the base, where R 40 The group is selected from C1-C6 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and may optionally contain one, two, or three heteroatoms in its carbon skeleton, each independently selected from N and O.

[0057] More typically, in such embodiments, R 4 These are fluoro, chloro, bromo, -OH, and -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 , -L4 -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 Selected from the base, where R 41 is, -R 44 or -R 45 Selected from the basis; Each R 42 is hydrogen or -R 44 or -R 45 Either selected independently of the base, or any two R 42 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 4L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 4 It has a chain length of 1 to 4 atoms, and L 4 It consists of one or two oxo (=O) groups and / or one or more R groups. L4 It can be optionally replaced; Each R L4 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L4 and R 41 , or any R L4 and any R 42 These may, together with the atoms to which they are bonded, form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; R 43 is hydrogen or -R 44 Selected from the basis; Each R 44 is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, where the C1-C4 alkyl or C3-C6 cycloalkyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and Each R 45 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 45 Any methyl group may be optionally fluorosubstituted; However, R containing any of the substituents 4The condition is that it contains eight or fewer carbon atoms.

[0058] In one embodiment of such a configuration, R 4 These are fluoro, chloro, bromo, -OH, and -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 Selected from the base.

[0059] In further embodiments of such a model, R 4 These are fluoro, chloro, bromo, -OH, and -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 Selected from the basis; Each R 42 is hydrogen or -R 44 or -R 45 Either selected independently of the base, or any two R 42 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and L 4L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 4 It has a chain length of 1 to 4 atoms, and L 4 It consists of one or two oxo (=O) groups and / or one or more R groups. L4 It can be optionally replaced, where each R L4 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L4 and R 41 , or any R L4 and any R 42 These may, together with the atoms to which they are bonded, form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups.

[0060] Therefore, for example, R 4 is a chloro group, or -R 44 A group (e.g., a cyclopropyl group), or -OR 41 It may be a single group (for example, -OMe or -OCHF2 groups).

[0061] Typically, R contains any of the substituents. 4 It contains six or fewer carbon atoms.

[0062] Typically, R contains any of the substituents. 4 The total number of nitrogen, oxygen, and sulfur atoms in is 4 or less. More typically, R contains any of the substituents. 4 The total number of nitrogen, oxygen, and sulfur atoms in is 3 or less.

[0063] In a more typical embodiment, R 4 These are fluoro, chloro, bromo, -OH, and -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, -NR 43 -L 4 -OH, -NR 43 -L 4 -OR 44 , -NR 43 -L 4 -N(R 42 )2, or -R 44 Selected from the base, where each R 42 is hydrogen or -R 44 Selected independently from the basis; R 43 is hydrogen or -R 44 Selected from the basis; Each R 44 is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, where the C1-C4 alkyl or C3-C6 cycloalkyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and L 4 The group is -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, or -CMe2-CMe2-, where any -CH2-, -CHMe-, or -CMe2- group may be optionally fluorosubstituted.

[0064] Typically, in such embodiments, R 4 Fluoro, chloro, bromo, -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 -R44 Selected from the base. More typically, in such embodiments, R 4 Fluoro, chloro, bromo, -OR 44 , -CON(R 42 )2, -SO2-R 44 , -O-CH2-CH2-OR 44 -O-CH2-CH2-N(R 42 )2, or -R 44 Selected from the base.

[0065] One embodiment, each R 44 R is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, where the C1-C4 alkyl or C3-C6 cycloalkyl group may be optionally substituted with one or more fluoro groups. More typically, each R 44 The group is independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups.

[0066] In one embodiment of such a configuration, R 4 Fluoro, chloro, bromo, -OR 44 -SO2-R 44 -SO2-N(R 42 )2,-O-CH2-CH2-N(R 42 )2, or -R 44 Selected from the base. More typically, R 4 Fluoro, chloro, bromo, -R 44 OR 44 Selected from the base. Typically, in such embodiments, R 44 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups.

[0067] Furthermore, more typically, R 4 The group is selected from fluoro, chloro, bromo, methyl (Me) or -OMe groups, where any methyl group may be optionally substituted with a fluoro group. More typically, R 4The group is selected from a methyl (Me) or -OMe group, where any methyl group may be optionally fluorosubstituted.

[0068] In another embodiment of the first or second aspect of the present invention, R 4 and R 7 These combine to form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched, or consist of one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0069] Typically, R 4 and R 7 When these atoms combine to form a hydrocarbylene group, the hydrocarbylene group containing any of the substituents contains four or fewer carbon atoms.

[0070] Typically, R 4 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any hydrocarbylene group (including any substituent) formed by is 3 or less. More typically, R 4 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any hydrocarbylene group (including any substituent) formed by this is 2 or less.

[0071] Typically, in such embodiments, R 4 and R 7Together, they form a C1-C4 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear, branched, or cyclic, and may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0072] R 4 and R 7 When these atoms combine to form a hydrocarbylene group, the hydrocarbylene group typically has a chain length of 2 to 4 atoms. More typically, the hydrocarbylene group has a chain length of 2 or 3 atoms.

[0073] More typically, R 4 and R 7 When these groups combine to form a hydrocarbylene group, the hydrocarbylene group is selected from -CH2-CH2-, -CH2-O-, -O-CH2-, -CH2-CH2-CH2-, -O-CH2-CH2-, -CH2-CH2-O-, or -CH2-O-CH2-, however, R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0074] Typically, R 4 and R 7 When they come together to form a hydrocarbylene group, R 8 R is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More typically, R 4 and R 7 When they come together to form a hydrocarbylene group, R 8R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups. More typically, 4 and R 7 When they come together to form a hydrocarbylene group, R 8 It is hydrogen.

[0075] As described in both the first and second aspects of the present invention, R 5 R is selected from hydrogen or a halo group. In one embodiment, R 5 The group is selected from hydrogen, fluoro, chloro, or bromo groups. More typically, R 5 The group is selected from hydrogen or fluoro groups. Most typically, R 5 It is hydrogen.

[0076] As described in both the first and second aspects of the present invention, R 6 is hydrogen or halo, -R 60 OR 60 Selected from the base, where R 60 The C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl group is selected from C1-C4 alkyl, C3-C4 cycloalkyl, or C3-C4 fluorocycloalkyl groups. More typically, R 6 Fluoro, chloro, bromo, -R 60 OR 60 Selected from the base. More typically, R 6 is chloro, bromo, -R 60 OR 60 Selected from the base. More typically, R 6 is, -R 60 OR 60 Selected from the base.

[0077] In one embodiment, R 60 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups. For example, R 6 is, -R 60 OR 60 It may be selected from the base, and R 60This group may be selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups.

[0078] Typically, R 60 The group is selected from methyl, fluoromethyl, ethyl, or fluoroethyl groups. More typically, R 60 The group is selected from methyl or fluoromethyl groups.

[0079] In further embodiments, R 6 is a chloro, bromo, methyl, or fluoromethyl group. Typically, in such embodiments, R 6 is a methyl or fluoromethyl group. More typically, R 6 This is a methyl group.

[0080] As described in one embodiment of both the first and second aspects of the present invention, R 7 and R 8 is hydrogen or fluoro, or C1-C 12 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining R is directly bonded to the molecule. 7 or R 8 The condition is that any atom in the hydrocarbyl group is a carbon atom, or R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton.

[0081] In one embodiment, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8 The condition is that any atom in the hydrocarbyl group is a carbon atom, or R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton.

[0082] In another embodiment, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or 8 The condition is that any atom in the hydrocarbyl group is a carbon atom. For example, R 7The R group may be selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 The condition is that any atom of the hydrocarbyl group is a carbon atom, and R 8 This may be selected from hydrogen, fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl.

[0083] In yet another embodiment, R 7 and R 8 The group is independently selected from hydrogen, fluoro, or C1-C6 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and may optionally contain one, two, or three heteroatoms independently selected from N and O in its carbon skeleton, provided that the remaining R is directly bonded to the molecule. 7 or R 8 The condition is that any atom in the hydrocarbyl group is a carbon atom. For example, R 7The R group may be selected from hydrogen, fluoro, or C1-C6 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl group may optionally contain one, two, or three heteroatoms independently selected from N and O in its carbon skeleton, provided that the R group is directly bonded to the rest of the molecule. 7 The condition is that any atom in the hydrocarbyl group is a carbon atom, and R 8 This may be selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0084] In one embodiment, R 7 and R 8 These are hydrogen or fluoro, -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 Each is independently selected from the base, where each R 71 is, -R 73 or -R 74 Selected independently from the basis; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Each L 7 L is independently selected from linear alkylene or alkenylene groups, wherein the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced; Each R L7 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L7 These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R L7 and R 71 , or any R L7 and any R 72 -L is where they are joined together. 7 -COOR 71 , -L 7 -CO-N(R 72 )2, -L 7 -OR 71 or L 7 -N(R 72) Together with two atoms, they may form a 3-6 member monocyclic heterocyclic group, where the 3-6 member monocyclic heterocyclic group is saturated or monounsaturated, and the 3-6 member monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Each R 73 is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and Each R 74 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 74 Any methyl group may be optionally fluorosubstituted; However, any R containing any of the substituents 7 or R 8 R contains 12 or fewer carbon atoms and is directly bonded to the rest of the molecule. 7 or R 8 Each atom must be a carbon, hydrogen, or fluorine atom.

[0085] Typically, in the above embodiments, any R containing any of the substituents is used. 7 or R 8 The group contains 10 or fewer carbon atoms. In one embodiment of such a configuration, R 7 and R 8 These are hydrogen or fluoro, -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 Each is independently selected from the group, however any R containing any substituent is available. 7 or R 8 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 or R 8 Each atom must be a carbon, hydrogen, or fluorine atom.

[0086] More typically, R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 12 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 The condition is that the atom is a carbon, hydrogen, or fluorine atom, and R 8 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0087] Therefore, for example, R 7 is hydrogen, or -R 73A group (e.g., methyl, -CF3, ethyl, isopropyl, or -CH2CH2CH=CH2 group), or a -COOH group, or -L 7 -COOH group (e.g., -CMe2COOH, -CH2COOH, -CH2CH2COOH, [ka] or -L 7 -COOR 71 A group (e.g., -CMe2COOMe, -CH2CH2COOMe, or -CH2COOEt group), or -L 7 -CO-N(R 72 ) 2 units (for example, [ka] or -L 7 -OH group (e.g., -CMe2CH2OH) [ka] or -L 7 -OR 71 A group (e.g., -CH2OMe group), or -L 7 -N(R 72 ) 2 units (for example, [ka] That's fine.

[0088] Typically, in the above embodiments, R includes any of the substituents. 7 It contains 10 or fewer carbon atoms. More typically, R 7 These are hydrogen or fluoro, -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 -L7 -R 74 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 The condition is that the atom is a carbon, hydrogen, or fluorine atom, and R 8 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0089] For example, as can be understood, R 7 but, [ka] Selected from -L 7 -If it is a COOH group, L 7 This is two R's L7 It can be considered as a linear alkylene group substituted with a group, where the two R L7 They combine to form -CH2CH2-, -CH2-, or -CF2- groups, respectively, in which case two R L7 And the carbon atoms (or more) to which they are bonded together form a cyclopropyl or fluorocyclopropyl group. Similarly, R 7 but, [ka] Selected from -L 7 -N(R 72 ) If there are two units, L 7 This is a single R L7 It can be considered as a linear alkylene group substituted with a group, where R L7 and one R 72 The groups combine to form either a -CH2CH2- or -CH2CH2CH2- group, in which case R L7 and R 72 -L is where they are joined together. 7 -N(R 72 ) Together with two atoms, they form a saturated 5- or 6-membered monocyclic or heterocyclic group.

[0090] Typically, in the above embodiment, each L 7 L is independently selected from linear alkylene or alkenylene groups, wherein the linear alkylene group optionally contains a single heteroatom selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L It may be optionally replaced.

[0091] In one embodiment of the above-described model, each L 7 L is independently selected from a linear alkylene group, wherein the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced, where each R L7 The group is independently selected from fluoro, methyl, or fluoromethyl groups, or any two R groups. L7 However, together with the atom(s) to which they are bonded, they form a 3-6 member saturated monocyclic group, where the 3-6 member saturated monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups, or any R L7 and R 71 , or any R L7 and any R 72 However, they are combined -L 7 -COOR 71 , -L 7 -OR 71 or -L 7 -N(R 72) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups.

[0092] In another embodiment of the above-described model, R 7 and R 8 These are hydrogen or fluoro, -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 Each is independently selected from the base; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each L 7 L is independently selected from a linear alkylene group, wherein the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced, where each R L7 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L7 and R 71 , or any R L7 and any R 72 -L is where they are joined together. 7 -COOR 71 , -L 7 -OR 71 or -L 7 -N(R 72 ) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; However, any R containing any of the substituents 7 or R 8 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 or R 8 Each atom must be a carbon, hydrogen, or fluorine atom.

[0093] In yet another embodiment of the above-described model, R 7 and R 8 These are hydrogen or fluoro, -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 Each is independently selected from the base; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each L 7L is independently selected from a linear alkylene group, wherein the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced, where each R L7 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L7 and R 71 , or any R L7 and any R 72 -L is where they are joined together. 7 -OR 71 or -L 7 -N(R 72 ) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and Each R 73 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, where the C1-C4 alkyl or C3-C6 cycloalkyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; However, any R containing any of the substituents 7 or R 8 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 or R 8 Each atom must be a carbon, hydrogen, or fluorine atom.

[0094] Typically, in such an embodiment, R 7 These are hydrogen or fluoro, -CN, -COOH, -L 7 -COOH, -L 7 -OH, -L 7 -OR 71 , -L7 -N(R 72 )2, -R 73 ,-R 74 or -L 7 -R 74 Selected from the base, and R 8 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0095] Typically, in the above embodiments, any R containing any of the substituents is used. 7 or R 8 The group contains six or fewer carbon atoms.

[0096] Typically, any R containing any of the substituents 7 or R 8 The total number of nitrogen, oxygen, and sulfur atoms in is 4 or less. More typically, any R containing any of the substituents. 7 or R 8 The total number of nitrogen, oxygen, and sulfur atoms in is 3 or less.

[0097] In further embodiments, R 7 and R 8 is hydrogen or fluoro, -COOH, -COOR 75 -CONH2, -CONHR 75 , -CON(R 75 )2, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -CONH2, -L 71 -CON editing 75 , -L 71 -CON(R 75 )2, -L 71 -OH, -L 71 -OR 75 or -R 75 Each element is independently selected from the base, and in the formula, Each-L 71 - is -CH2-, -CHMe-, -CMe2-, [ka] -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe-, -CMe2-CMe2-, [ka] -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-, [ka] Selected independently from the base, where any -L 71 -The portion may be optionally substituted with fluoropolymers; and Each R 75 This is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl groups, or any two R groups bonded to the same nitrogen atom. 75However, together with the nitrogen atom to which they are bonded, they may form a 4-6 member saturated monocyclic heterocyclic group, such as an azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, or piperazinyl group, where the 4-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two methyl groups, where the aforementioned methyl groups may be optionally fluorosubstituted; However, any R containing any of the substituents 7 or R 8 The condition is that the group contains 12 or fewer carbon atoms.

[0098] Typically, in such embodiments, R 7 is hydrogen or fluoro, -COOH, -COOR 75 -CONH2, -CONHR 75 , -CON(R 75 )2, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -CONH2, -L 71 -CON editing 75 , -L 71 -CON(R 75 )2, -L 71 -OH, -L 71 -OR 75 or -R 75 Selected from the base, and R 8 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups. More typically, R 8 It is hydrogen.

[0099] Typically, R 7 is hydrogen or fluoro, -COOH, -COOR 75 -CONH2, -CONHR 75 , -CON(R 75 )2, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -CONH2, -L 71 -CON editing 75 , -L71 -CON(R 75 )2, -L 71 -OH, -L 71 -OR 75 or -R 75 If selected from the base, R 7 (including any of the substituents) contains 10 or fewer carbon atoms.

[0100] In further embodiments, R 7 and R 8 is hydrogen or fluoro, -COOH, -COOR 75 , -L 71 -COOH, -L 71 -COOR 75 , -L 71 -OH, -L 71 -OR 75 or -R 75 Each is independently selected from the base, and here, Each-L 71 -teeth, [ka] -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe- or -CMe2-CMe2- groups are independently selected, where any -L 71 -The portion may be optionally substituted with fluoropolymers; and Each R 75 The group is independently selected from C1-C4 alkyl, C2-C4 alkenyl, cyclopropyl, cyclobutyl, C1-C4 fluoroalkyl, C2-C4 fluoroalkenyl, fluorocyclopropyl, or fluorocyclobutyl groups.

[0101] Typically, in such embodiments, R 7 is hydrogen or fluoro, -COOH, -COOR 75 , -L 71 -COOH, -L 71 -COOR 75 , -L71 -OH, -L 71 -OR 75 or -R 75 Selected from the base, and R 8 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0102] In one embodiment of such a configuration, each -L 71 - is independently selected from the -CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe-, -CHMe-CMe2-, -CMe2-CH2-, -CMe2-CHMe- or -CMe2-CMe2- groups, where any -CH2-, -CHMe- or -CMe2- group may be optionally fluorosubstituted. More typically, each -L 71 - is independently selected from the CH2-, -CHMe-, -CMe2-, -CH2-CH2-, -CH2-CHMe-, -CH2-CMe2-, -CHMe-CH2-, -CHMe-CHMe- or -CMe2-CH2- groups, where any -CH2-, -CHMe- or -CMe2- group may be optionally fluorosubstituted.

[0103] Typically, in such embodiments, R includes any of the substituents. 7 It contains 6 or fewer carbon atoms, and R 8 R is selected from hydrogen or fluoro, methyl or fluoromethyl groups. More typically, R contains any of these substituents. 7 It contains 5 or fewer carbon atoms, and R 8 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0104] In another embodiment, R 7 and R 8 is hydrogen or fluoro, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -OH, -L 71 -OR 75or -R 75 Each is independently selected from the base, and here, Each-L 71 - is independently selected from the -CH2-, -CHMe-, or -CMe2- group, where any -CH2-, -CHMe-, or -CMe2- group may be optionally fluorosubstituted; and Each R 75 The group is independently selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups.

[0105] Typically, in such embodiments, R 7 is hydrogen or fluoro, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -OH, -L 71 -OR 75 or -R 75 Selected from the base, and R 8 is selected from hydrogen or fluoro, methyl or fluoromethyl groups. More typically, in such embodiments, R 7 is hydrogen, or -L 71 -COOH, -L 71 -COOR 75 Or -R 75 Selected from the base, and R 8 It is hydrogen.

[0106] In another embodiment, R 7 and R 8 R is independently selected from hydrogen, fluoro, methyl, or fluoromethyl groups. For example, R 7 R may be selected from hydrogen, fluoro, methyl, or fluoromethyl groups, and 8 This may be a hydrogen atom or a fluoro group.

[0107] In one embodiment, R 7 and R 8 At least one of them is hydrogen. Typically, R 8 It is hydrogen.

[0108] In a further embodiment, R 7 and R 8 are both hydrogen.

[0109] In another embodiment of either the first or second aspect of the present invention, R 7 and R 8 together with the carbon atom to which they are attached form a 3- to 10-membered cyclic group, where each ring atom of the cyclic group directly attached to the carbon atom to which R 7 and R 8 are attached is a ring carbon atom, where the cyclic group may be optionally substituted with one or more substituents each independently selected from halo, oxo (=O), -OH, -NH2, or a C-C saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched or cyclic or may contain it, the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms each independently selected from N and O in its carbon skeleton.

[0110] Typically, in such embodiments, R 7 and R 8 together with the carbon atom to which they are attached form a 3- to 6-membered saturated monocyclic group, where each ring atom of the saturated monocyclic group directly attached to the carbon atom to which R 7 and R 8 are attached is a ring carbon atom, where the saturated monocyclic group may be optionally substituted with one or more fluoro groups and / or one or two substituents each independently selected from oxo (=O), -CN, or a C-C saturated hydrocarbyl group, where the saturated hydrocarbyl group may be linear or branched, the saturated hydrocarbyl group may be optionally substituted with one or more fluoro groups, and the saturated hydrocarbyl group may optionally contain a single heteroatom selected from N and O in its carbon skeleton.

[0111] For example, R 7 and R 8 may combine together to form a group -L 78 -, where -L 78 - is selected from the groups -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-, where -L 78 - may be optionally substituted with one or two substituents independently selected from one or more fluoro groups and / or oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, where -L 78 - any methyl group of the substituents may be optionally fluoro-substituted.

[0112] As described according to both the first and second aspects of the present invention, X 10 is N or CR 10 and X 11 is N or CR 11 and X 12 is N or CR 12 and X 13 is N or CR 13 and in that case, no more than two of X 10 X 11 X 12 and X 13 are N. Typically, no more than one of X 10 X 11 X 12 and X 13 is N.

[0113] Typically, X 11 is CR 11 and X 12 is CR 12 or X 11 is CR 11 and X 12 is N or X 11 is N and X12 is CR 12 More typically, X 11 is CR 11 and X 12 is CR 12 or X 11 is N and X 12 is CR 12 is.

[0114] In one embodiment, X 10 is N or CR 10 and X 11 is CR 11 and X 12 is CR 12 and X 13 is N or CR 13 is. Typically, in such embodiments, one or fewer of X 10 and X 13 is N.

[0115] In one embodiment, X 10 is N, X 11 is CR 11 and X 12 is CR 12 and X 13 is CR 13 is.

[0116] In a further embodiment, X 10 is CR 10 and X 11 is CR 11 and X 12 is CR 12 and X 13 is CR 13 is.

[0117] As noted, when present, each R 10 , R 11 , R 12 , and R 13 is hydrogen or halo, -OH, -SH, -NH2, -SO2NH2, or C1-C 12A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety.

[0118] In one embodiment, if present, each R 10 , R 11 , R 12 , and R 13 This can be hydrogen or a halo (e.g., fluoro, chloro, or bromo), -OH, -SH, -NH2, -SO2NH2, or C1-C 10 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo (e.g., fluoro, chloro, and / or bromo) groups, and the hydrocarbyl group may optionally contain one, two, three, four, five, or six (more typically one, two, three, or four) heteroatoms independently selected from N, O, and S in its carbon skeleton, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety.

[0119] Further embodiments, if any, each R 10 , R 11 , R 12 , and R 13The group is independently selected from hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, -CN, or C1-C8 saturated hydrocarbyl groups, where the saturated hydrocarbyl group may be linear or branched, or a single cyclic group or contain thereof, and the saturated hydrocarbyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups, and the saturated hydrocarbyl group may optionally contain one, two or three heteroatoms independently selected from N, O, and S in its carbon skeleton, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety.

[0120] In another embodiment, if present, each R 10 , R 11 , R 12 , and R 13 R is independently selected from hydrogen or halo, -OH, -NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one, two or three heteroatoms independently selected from N and O in its carbon skeleton. In one embodiment of such a configuration, R 18 and R 19The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 or R 19 The condition is that any atom in the hydrocarbyl group is a carbon atom, or R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton, or R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0121] In one embodiment, if present, each R 10 , R 11 , R 12 , and R 13The group is independently selected from hydrogen, halo, -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear, branched, or cyclic, and may be optionally substituted with one or more halo groups, and may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton.

[0122] In another embodiment, if present, each R 10 , R 11 , R 12 , and R 13 The group is independently selected from hydrogen or a fluoro, chloro, bromo, -CN, -OH, -NH2, or C1-C3 saturated hydrocarbyl group, where the saturated hydrocarbyl group may be linear or branched, and may be optionally substituted with one or more halo groups and / or a single oxo (=O) group, and may optionally contain a single heteroatom selected from N and O in its carbon skeleton.

[0123] In further embodiments, X 11 CR 11 and X 12 CR 12 is or X 11 CR 11 and X 12 is N, or X 11 is N and X 12 CR 12 And, R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. In one embodiment of such a configuration, R 11 and R 12One of the following is present and selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups. Typically, in such embodiments, R 11 and R 12 One of the following is present, and selected from chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN groups. More typically, R 11 and R 12 One of the following is present and selected from chloro, bromo, methoxy, fluoromethoxy, or -CN groups. Alternatively, R 11 and R 12 One of these is present and can be selected from -CN, -COOH, -CONH2, or -C(=NH)NH2 groups. Most typically, X 11 Is it C-CN or X 12 C-CN is typically one of the remaining R 10 , R 11 , R 12 or R 13 This is hydrogen or halo, -OH, -SH, -NH2, -SO2NH2, or C1-C 12 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally 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 present, further remaining R 10 , R 11 , R 12 , or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups. For example, one of the remaining R 10 , R 11 , R12 or R 13 is a hydrogen or fluoro, chloro or bromo group, 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 ) may be independently selected from two groups, where any of the aforementioned groups containing any substituents contain 12 or fewer carbon atoms, and if present, further remaining R 10 , R 11 , R 12 or R 13 Each of these may be independently selected from hydrogen or a fluoro, chloro, or bromo group, in the formula, Each R 131 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 132 is hydrogen or -R 131 Selected independently from the basis; R 133 is hydrogen or -R 131 Selected from the basis; L 13 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains 1, 2, or 3 heteroatoms independently selected from O and N in its carbon skeleton, where L 13 It has a chain length of 1 to 8 atoms, and L 13 R is one or two groups independently selected from oxo (=O) and -OH, and / or one or more groups R L13 It can be optionally replaced; Each R L13 This is independently selected from fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe, or -CH2O-fluoromethyl groups; Alternatively, any two R L13 , or any R L13 and any R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered monocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups; Alternatively, 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 These may, together with the atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0124] Any two R L13 , or any R L13 and any R 131 , or any two R 131 When these atoms, together with the atom(s) to which they are bonded, form a monocyclic group of 3 to 7 members, the monocyclic group may be saturated or unsaturated.

[0125] For example, any two R L13 These may, together with the atom(s) to which they are bonded, form a C3-C7 cycloalkyl group or a 3-7 member saturated monocyclic heterocyclic group, where the C3-C7 cycloalkyl group or the 3-7 member saturated monocyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups. Similarly, any R L13and any R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered saturated monocyclic heterocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0126] Alternatively, any two R L13 These may, together with the atom(s) to which they are bonded, form a phenyl group or a 5- or 6-membered heteroaryl group, where the phenyl group or the 5- or 6-membered heteroaryl group may be optionally substituted with one or two -OH groups and / or one or more fluoro, methyl and / or fluoromethyl groups. Similarly, any R L13 and any R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a five-membered heteroaryl group, which may be optionally substituted with one or two -OH groups and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0127] 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 These atoms may, together with the atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, where the 6-10 membered bicyclic heterocyclic group may be saturated or unsaturated. Similarly, the 6-10 membered bicyclic heterocyclic group may be a fused 6-10 membered bicyclic heterocyclic group, a spiro 6-10 membered bicyclic heterocyclic group, or a bridging 6-10 membered bicyclic heterocyclic group.

[0128] For example, any two R L13and any R 131 These may, together with the atoms to which they are bonded, form a saturated condensed 8-10 member bicyclic heterocyclic group, where the saturated condensed 8-10 member bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups. Alternatively, any two R L13 and any R 131 These may, together with the atoms to which they are bonded, form a fused 8-10 member bicyclic heterocyclic group, where the 8-10 member bicyclic heterocyclic group comprises a first ring system fused to a second ring system, where the first ring system is aromatic and the second ring system is non-aromatic, and the fused 8-10 member bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups. Alternatively, any two R L13 and any R 131 These may, together with the atoms to which they are bonded, form a condensed 8-10 membered bicyclic heteroaryl group, which may be optionally substituted with one or two -OH groups and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0129] In another example, any two R L13 and any R 131 These may, together with the atoms to which they are bonded, form a saturated bridged 6-8 member bicyclic heterocyclic group, where the saturated bridged 6-8 member bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0130] In further examples, any three R L13 and any R 131These may, together with the atoms to which they are bonded, form a saturated condensed 8-10 member bicyclic heterocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups. Alternatively, any three R L13 and any R 131 These may, together with the atoms to which they are bonded, form a fused 8-10 member bicyclic heterocyclic group, where the 8-10 member bicyclic heterocyclic group comprises a first ring system fused to a second ring system, where the first ring system is aromatic and the second ring system is non-aromatic, and the fused 8-10 member bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups. Alternatively, any three R L13 and any R 131 These may, together with the atoms to which they are bonded, form a condensed 8-10 membered bicyclic heteroaryl group, which may be optionally substituted with one or two -OH groups and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0131] For example, any three R L13 and any R 131 These may, together with the atoms to which they are bonded, form a saturated spiro 7-10 membered bicyclic heterocyclic group, where the saturated spiro 7-10 membered bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0132] In another example, any three R L13 and any R 131These may, together with the atoms to which they are bonded, form a saturated bridged 6-8 member bicyclic heterocyclic group, where the saturated bridged 6-8 member bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0133] For example, any two R atoms bonded to the same nitrogen atom 131 and any two R L13 These may, together with the atoms to which they are bonded, form a saturated condensed 8-10 member bicyclic heterocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0134] In another example, any two R atoms bonded to the same nitrogen atom 131 and any two R L13 These may, together with the atoms to which they are bonded, form a saturated bridged 6-8 member bicyclic heterocyclic group, where the saturated bridged 6-8 member bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups.

[0135] In any one embodiment of the above-described embodiment, L 13 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 13 It has a chain length of 1 to 8 atoms, and L 13 It consists of one or two oxo (=O) groups and / or one or more R groups. L13 It can be optionally replaced; Each R L13This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L13 , or any R L13 and R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered monocyclic group, where the 3- to 7-membered monocyclic group is saturated or monounsaturated, and the 3- to 7-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any two R L13 and R 131 These may, together with multiple atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, where the 6-10 membered bicyclic heterocyclic group is saturated or monounsaturated, and the 6-10 membered bicyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups.

[0136] More typically, in such embodiments, one remaining R 10 , R 11 , R 12 or R 13 This is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, or C1-C 10A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl group may optionally contain 1, 2, 3, 4, 5, or 6 (more typically 1, 2, 3, or 4) heteroatoms in its carbon skeleton, which are independently selected from N, O, and S, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, and if present, further remaining R 10 , R 11 , R 12 , or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups. More typically, in such embodiments, R 10 and R 13 One of the following is present, and selected from hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, -CN, or C1-C8 saturated hydrocarbyl groups, where the saturated hydrocarbyl group may be linear or branched, or a single cyclic group or contain thereof, and the saturated hydrocarbyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups, and the saturated hydrocarbyl group may optionally contain one, two or three heteroatoms in its carbon skeleton that are independently selected from N, O, and S, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, respectively, to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, and if present, further remaining R 10 , R 11 , R 12 , or R 13Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups.

[0137] Typically, one remaining R 10 , R 11 , R 12 or R 13 However, hydrogen or fluoro, chloro or bromo group, 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, -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 When selected independently from two groups, the aforementioned group containing any of the substituents contains 10 or fewer carbon atoms. More typically, the aforementioned group containing any of the substituents contains 8 or fewer carbon atoms. Typically, the total number of nitrogen, oxygen, and sulfur atoms in the aforementioned group containing any of the substituents is 6 or less. More typically, the total number of nitrogen, oxygen, and sulfur atoms in the aforementioned group containing any of the substituents is 4 or less, or 3 or less.

[0138] In a typical embodiment, R 11 and R 12 If one of the following is present and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups, then X 10 is N or CR 10 X 11 CR 11 X 12 CR 12 X 13 is N or CR 13 and X 10 and X 13 One or fewer of these is N. Typically, in such embodiments, R 11 and R 12 The other of these is selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, where R11 or R 12 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted. More typically, in such embodiments, R 11 and R 12 One of them is selected from chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, or -CN group, and R 11 and R 12 The other of these is selected from hydrogen, fluoro, chloro, or bromo groups. More typically, R 11 and R 12 One of them is selected from chloro, bromo, methoxy, fluoromethoxy, or -CN groups, and R 11 and R 12 The other of these is selected from hydrogen, fluoro, chloro, or bromo groups. More typically, R 11 and R 12 One of them is a -CN group, and R 11 and R 12 The other of these is selected from hydrogen or a fluoro, chloro, or bromo group. Typically, in such embodiments, R 10 and R 13 One of them is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, or C1-C 10 Selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, and may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and may optionally contain 1, 2, 3, 4, 5, or 6 (more typically 1, 2, 3, or 4) heteroatoms in its carbon skeleton, independently selected from N, O, and S, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, and if present, R 10and R 13 The other of these is selected from hydrogen or a fluoro, chloro, or bromo group. More typically, in such embodiments, R 10 and R 13 One of these is selected from hydrogen or a fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, -CN, or C1-C8 saturated hydrocarbyl group, where the saturated hydrocarbyl group may be linear or branched, or a single cyclic group or contain thereof, and the saturated hydrocarbyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups, and the saturated hydrocarbyl group may optionally contain one, two or three heteroatoms in its carbon skeleton that are independently selected from N, O, and S, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, and if present, R 10 and R 13 The other of these is selected from hydrogen, fluoro, chloro, or bromo groups.

[0139] In one embodiment, R 11 and R 12 If one of the following is present and selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, then the remaining R 10 , R 11 , R 12 and R 13 Each of these is independently selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, where R 10 , R 11 , R 12 or R 13Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted. More typically, if present, one of the remaining R groups is fluorosubstituted. 10 , R 11 , R 12 or R 13 R is independently selected from hydrogen or fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 groups, where R 10 , R 11 , R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted, and further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups. For example, R 11 and R 12 If one of the following is present and selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, then R 10 or R 13 If present, one of these may be selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, where R 10 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH) 2- The ) group may be optionally fluorosubstituted, and the remaining R 10 , R 11 , R 12 or R 13 Each of these may be independently selected from hydrogen or fluoro, chloro, or bromo groups. More typically, R 11 and R 12If one of the following is present and selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2 or -C(=NH)NH2 groups, then the remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups.

[0140] In yet another embodiment, X 10 is N or CR 10 X 11 CR 11 X 12 CR 12 and X 13 is N or CR 13 X 10 and X 13 One or fewer of these is N, and R 11 and R 12 One of these is selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups, R 11 and R 12 The other of these is selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, and if present, R 10 and R 13 R is independently selected from hydrogen or fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 groups, where R 10 , R 11 , R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted. Typically, in such embodiments, R 11 and R 12 One of them is selected from -CN, -COOH, -CONH2, or -C(=NH)NH2 groups, and R 11 and R12 The other of these is selected from hydrogen, fluoro, chloro, or bromo groups. More typically, R 11 and R 12 One of them is a -CN group, and R 11 and R 12 The other of these is selected from hydrogen or a fluoro, chloro, or bromo group. Typically, in such embodiments, R 10 and R 13 One of these is selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, where R 10 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted, and if present, R 10 and R 13 The other of these is selected from hydrogen or fluoro, chloro or bromo groups. More typically, in such embodiments, if present, each R 10 and R 13 The group is independently selected from hydrogen, fluoro, chloro, or bromo groups.

[0141] In a typical embodiment, X 10 is N or CR 10 X 11 CR 11 X 12 CR 12 and X 13 is N or CR 13 X 10 and X 13 One or fewer of these is N, and R 10 R is selected from hydrogen or a fluoro, chloro, bromo, or fluoromethyl group. 11 However, the group is selected from chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH or -CN, R 12 is selected from hydrogen, fluoro, chloro, or bromo groups, and R 13X is selected from hydrogen or a fluoro, chloro, bromo, methyl or fluoromethyl group. Typically, in such embodiments, X 10 is N or CR 10 X 11 CR 11 X 12 CR 12 Yes, and X 13 CR 13 Typically, in such embodiments, R 11 The group is selected from chloro, bromo, methoxy, fluoromethoxy, -CH2OH, or -CN groups. More typically, R 11 The group is selected from chloro, bromo, methoxy, fluoromethoxy, or -CN groups. Most typically, R 11 is a -CN group, that is, X 11 It is C-CN. Typically, X 10 , X 12 and X 13 At least one of them is CH. More typically, X 10 , X 12 and X 13 At least two of them are CH.

[0142] In further embodiments, X 10 is N, CH, CF, C-Cl or C-Br, and X 11 These are CH, CF, C-Cl or C-Br, and X 12 is C-CN and X 13 is N, CH, CF, C-Cl or C-Br, however X 10 and X 13 The condition is that at least one of them is N.

[0143] In an alternative embodiment, X 10 is N, CH, CF, C-Cl or C-Br, and X 11 C-CN and X 12 is CH, CF, C-Cl or C-Br, and X 13 is N, CH, CF, C-Cl or C-Br, however X10 and X 13 The condition is that at least one of them is N.

[0144] As described in accordance with a second aspect of the present invention, each R 14 and R 15 is independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl, or R 14 and R 15 These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally substituted with a fluoro substituent.

[0145] One embodiment, each R 14 and R 15 R is independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. For example, R 14 may be hydrogen, and R 15 R may be selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in such embodiments, each R 14 and R 15 R is independently selected from hydrogen or a C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl group. For example, R 14 may be hydrogen, and R 15 R may be selected from hydrogen or a C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl group. More typically, in such embodiments, each R 14 and R 15 R is independently selected from hydrogen, methyl, or fluoromethyl groups. For example, R 14may be hydrogen, and R 15 This may be selected from hydrogen, methyl, or fluoromethyl groups.

[0146] In one embodiment, R 14 and R 15 Both are hydrogen.

[0147] In another embodiment, R 14 and R 15 These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted. Typically, in such embodiments, R 14 and R 15 These, together with the carbon atoms to which they are bonded, form a 3-5 membered saturated monocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O) or methyl or fluoromethyl groups. For example, R 14 and R 15 These may, together with the carbon atoms to which they are bonded, form a cyclopropyl or cyclobutyl group, which may be optionally substituted with one or more fluoro groups.

[0148] As described in one embodiment of the second aspect of the present invention, R 16The group is selected from hydrogen, fluoro, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, and R 17 is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, or R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted.

[0149] In one embodiment, R 16 The group is selected from hydrogen, fluoro, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, and R 17This is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl.

[0150] In one embodiment of such a configuration, R 16 is hydrogen or fluoro, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Selected from the base, where R 160 This refers to C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl, or -R 161 Selected from the base, where R 161 R is a 3-6 member monocyclic group, where the 3-6 member monocyclic group is one or more halo (e.g., fluoro, chloro, or bromo) groups and / or one or two groups R 162 It can be optionally replaced, where each R 162 The group R is independently selected from methyl or fluoromethyl groups, provided that the group R contains any substituent of either type. 16 The condition is that it contains 8 or fewer carbon atoms. Typically, in such embodiments, R 16 is hydrogen or fluoro, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Selected from the base, where R 160 This refers to C1-C4 alkyl, C1-C4 fluoroalkyl, or -R 161 Selected from the base, where R 161 The group is selected from a C3-C6 cycloalkyl group, a 4-6 member saturated heterocyclic group, or a phenyl or 5 or 6 member heteroaryl group, where the C3-C6 cycloalkyl group and the 4-6 member saturated heterocyclic group are one or more fluoro groups and / or one or two groups R 162 The phenyl or the 5- or 6-membered heteroaryl group may be optionally substituted with one or more fluoro, chloro and / or bromo groups, and / or one or two R groups. 162The group R may be optionally substituted, provided that any of the substituents are included. 16 The condition is that it contains 8 or fewer carbon atoms. More typically, in such embodiments, R 16 is hydrogen or fluoro, -R 160 ,-R 161 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Selected from the base, where R 160 is selected from a methyl or fluoromethyl group, and R 161 is a 5-membered heteroaryl group, where the 5-membered heteroaryl group is one or more fluoro, chloro and / or bromo groups and / or one or two groups R 162 It may be optionally replaced.

[0151] Typically, in the above embodiment, R 17 R is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More typically, R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups. Most typically, R 17 It is hydrogen.

[0152] In one embodiment of such a configuration, R 16 is hydrogen or fluoro, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Selected from the base, where R 160 is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl, and R 17 R is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. Typically, in such embodiments, R 17The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups. For example, R 16 is hydrogen or fluoro, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 It may be selected from the base, and R 17 R may be hydrogen. Typically, in such a configuration, 160 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups. More typically, in such embodiments, R 160 The group is selected from methyl or fluoromethyl groups.

[0153] In another embodiment of such a configuration, R 16 is selected from hydrogen or fluoro, -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, and R 17 R is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. For example, R 16 R may be selected from hydrogen or fluoro, -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl or C3-C4 fluorocycloalkyl, and R 17 R may be hydrogen. Typically, in such embodiments, R 16 is selected from hydrogen or fluoro, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl groups, and R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups. For example, R 16 R may be selected from hydrogen, fluoro, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups, and R17 R may be hydrogen. More typically, in such an embodiment, each R 16 and R 17 R is independently selected from hydrogen, methyl, or fluoromethyl groups. For example, R 16 R may be selected from hydrogen, methyl, or fluoromethyl groups, and 17 It can be hydrogen.

[0154] In one embodiment, R 16 and R 17 Both are hydrogen.

[0155] In another embodiment, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted. Typically, in such embodiments, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3-5 membered saturated monocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O) or methyl or fluoromethyl groups. For example, R 16 and R 17 These may, together with the carbon atoms to which they are bonded, form a cyclopropyl or cyclobutyl group, which may be optionally substituted with one or more fluoro groups.

[0156] In one embodiment of a second aspect of the present invention, R 16 is hydrogen or fluoro, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Selected from the base, where R 160is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl groups; and R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; Alternatively, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3-5 member saturated monocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O) or methyl or fluoromethyl groups.

[0157] In another embodiment of a second aspect of the present invention, R 16 is selected from hydrogen or fluoro, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; and R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; Alternatively, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a cyclopropyl or cyclobutyl group, which may be optionally substituted with one or more fluoro groups.

[0158] In another embodiment of a second aspect of the present invention, R 17 and R 7These combine to form a C1-C6 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear or branched, or consist of one or more cyclic groups, and may be optionally substituted with one or more halo groups, and may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0159] Typically, R 17 and R 7 When these atoms combine to form a hydrocarbylene group, the hydrocarbylene group containing any of the substituents contains four or fewer carbon atoms.

[0160] Typically, R 17 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any hydrocarbylene group (including any substituent) formed by is 3 or less. More typically, R 17 and R 7 The total number of nitrogen, oxygen, and sulfur atoms in any hydrocarbylene group (including any substituent) formed by this is 2 or less.

[0161] Typically, in such embodiments, R 17 and R 7Together, they form a C1-C4 saturated or unsaturated hydrocarbylene group, where the hydrocarbylene group may be linear, branched, or cyclic, and may be optionally substituted with one or more halo groups, and may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton, provided that R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0162] R 17 and R 7 When these atoms combine to form a hydrocarbylene group, the hydrocarbylene group typically has a chain length of 1 to 3 atoms. More typically, the hydrocarbylene group has a chain length of 1 or 2 atoms.

[0163] More typically, R 17 and R 7 When these groups combine to form a hydrocarbylene group, the hydrocarbylene group is selected from -CH2-, -CH2-CH2-, -CH=CH-, -CH2-O-, or -O-CH2-, however, R 8 The condition is that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is attached is a carbon atom.

[0164] Typically, R 17 and R 7 When they come together to form a hydrocarbylene group, R 8 R is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More typically, R 17 and R 7 When they come together to form a hydrocarbylene group, R 8 R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups. More typically, 17 and R 7When they come together to form a hydrocarbylene group, R 8 It is hydrogen.

[0165] Typically, R 17 and R 7 When they come together to form a hydrocarbylene group, R 16 R is selected from hydrogen or fluoro, -CN, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl. More typically, 17 and R 7 When they come together to form a hydrocarbylene group, R 16 The group is selected from hydrogen or fluoro, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups. More typically, R 17 and R 7 When they come together to form a hydrocarbylene group, R 16 R is selected from hydrogen, methyl, or fluoromethyl groups. More typically, 17 and R 7 When they come together to form a hydrocarbylene group, R 16 It is hydrogen.

[0166] As described in both the first and second aspects of the present invention, R 18 and R 19 is hydrogen or fluoro, or C1-C 12A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining R is directly bonded to the molecule. 18 or R 19 The condition is that any atom in the hydrocarbyl group is a carbon atom, or R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton, or R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0167] More typically, R 18 and R 19The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 or R 19 The condition is that any atom in the hydrocarbyl group is a carbon atom, or R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton, or R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0168] In one embodiment, R 18 and R 19 is hydrogen or fluoro, or C1-C 12(More typically, C1-C8) Saturated or unsaturated hydrocarbyl groups are independently selected, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the remaining R is directly bonded to the molecule. 18 or R 19 The condition is that any atom in the hydrocarbyl group is a carbon atom. For example, R 18 is hydrogen or fluoro, or C1-C 12 The hydrocarbyl group may be selected from (more typically C1-C8) saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 The condition is that any atom of the hydrocarbyl group is a carbon atom, and R 19 This may be selected from hydrogen, fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl.

[0169] In another embodiment, R 18 and R 19The group is independently selected from hydrogen, fluoro, or C1-C7 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and may optionally contain one, two, or three heteroatoms independently selected from N and O in its carbon skeleton, provided that the remaining R is directly bonded to the molecule. 18 or R 19 The condition is that any atom in the hydrocarbyl group is a carbon atom. For example, R 18 The R group may be selected from hydrogen, fluoro, or C1-C7 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl group may optionally contain one, two, or three heteroatoms independently selected from N and O in its carbon skeleton, provided that the R group is directly bonded to the rest of the molecule. 18 The condition is that any atom in the hydrocarbyl group is a carbon atom, and R 19 This may be selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0170] In one embodiment, R 18 and R 19 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 ,-CO-N(R 182 )2, -L 18 -COOH, -L 18 -COOR 181 , -L 18 -CO-N(R 182 )2, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R183 ,-R 184 or -L 18 -R 184 Each is independently selected from the base, where each R 181 is, -R 183 or -R 184 Selected independently from the basis; Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Each L 18 The linear alkylene, alkenylene, or alkynylene group is independently selected from linear alkylene, alkenylene, or alkynylene groups, wherein the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced; Each R L18 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L18 These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R L18 and R 181 , or any R L18 and any R 182-L is where they are joined together. 18 -COOR 181 , -L 18 -CO-N(R 182 )2, -L 18 -OR 181 or -L 18 -N(R 182 ) Together with two atoms, they may form a 3-6 member monocyclic heterocyclic group, where the 3-6 member monocyclic heterocyclic group is saturated or monounsaturated, and the 3-6 member monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Or, L 18 is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; Each R 183 is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and Each R 184 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 184 The methyl group may be optionally fluorosubstituted; However, any R containing any of the substituents 18 or R 19R contains 12 or fewer carbon atoms and is directly bonded to the rest of the molecule. 18 or R 19 Each atom must be a carbon, hydrogen, or fluorine atom.

[0171] Typically, in the above embodiments, any R containing any of the substituents is used. 18 or R 19 The group contains 10 or fewer carbon atoms. In one embodiment of such a configuration, R 18 and R 19 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 18 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Each is independently selected from the group, however any R containing any substituent is available. 18 or R 19 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 or R 19 Each atom must be a carbon, hydrogen, or fluorine atom.

[0172] More typically, R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 ,-CO-N(R 182 )2, -L 18 -COOH, -L 18 -COOR 181 , -L 18 -CO-N(R 182 )2, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 12 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom, and R 19 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0173] Typically, in the above embodiments, R includes any of the substituents. 18 It contains 10 or fewer carbon atoms. More typically, R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 18 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom, and R 19 The group is selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0174] In one embodiment of such a configuration, R 18 and R 19 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 18 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Each is independently selected from the base; Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each L 18 The linear alkylene, alkenylene, or alkynylene group is independently selected from linear alkylene, alkenylene, or alkynylene groups, wherein the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced, where each R L18 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L18 and R 181 , or any R L18 and any R 182 -L is where they are joined together. 18 -COOR 181 , -L 18 -OR 181 or -L 18 -N(R 182 ) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Or, L 18is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; However, any R containing any of the substituents 18 or R 19 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 or R 19 Each atom must be a carbon, hydrogen, or fluorine atom.

[0175] In another embodiment of such a configuration, R 18 and R 19 These are hydrogen or fluoro, -CN, -COOH, -L 18 -COOH, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Each is independently selected from the base, and each R 183 R is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, where the C1-C4 alkyl or C3-C6 cycloalkyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups, provided that any R containing any of the substituents is selected. 18 or R 19 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 or R 19 Each atom is a carbon, hydrogen, or fluorine atom. Typically, in such embodiments, R 18 These are hydrogen or fluoro, -CN, -COOH, -L 18 -COOH, -L 18 -OH, -L 18 -OR 181 , -L18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Selected from the base, and R 19 is selected from hydrogen or fluoro, methyl or fluoromethyl groups. Typically, in such embodiments, Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each L 18 The linear alkylene, alkenylene, or alkynylene group is independently selected from linear alkylene, alkenylene, or alkynylene groups, wherein the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced, where each R L18 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L18 and R 181 , or any R L18 and any R 182 -L is where they are joined together. 18 -COOR 181 , -L 18 -OR 181 or -L 18 -N(R 182) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Or, L 18 is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl.

[0176] Typically, in the above embodiments, any R containing any of the substituents is used. 18 or R 19 The group contains seven or fewer carbon atoms.

[0177] Typically, any R containing any of the substituents 18 or R 19 The total number of nitrogen, oxygen, and sulfur atoms in is 4 or less. More typically, any R containing any of the substituents. 18 or R 19 The total number of nitrogen, oxygen, and sulfur atoms in is 3 or less.

[0178] In one embodiment of the above-described model, R 18 and R 19 is hydrogen or fluoro or -R 183 Each is selected independently from the base. Typically, in such an embodiment, each R 183 R is independently selected from C1-C4 alkyl, C3-C6 cycloalkyl, C1-C4 fluoroalkyl, or C3-C6 fluorocycloalkyl. More typically, 18 and R 19 The group is independently selected from hydrogen, fluoro, methyl, or fluoromethyl groups.

[0179] In one embodiment, R 18 and R 19At least one of them is hydrogen.

[0180] In further embodiments, R 18 and R 19 Both are hydrogen.

[0181] In another embodiment, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton.

[0182] Typically, in such embodiments, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a saturated monocyclic group of 3 to 6 members, in which case R 18 and R 19 Each ring atom of the saturated monocyclic group directly bonded to the carbon atom to which is bonded is a ring carbon atom, where the saturated monocyclic group may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O), -CN, or C1-C3 saturated hydrocarbyl groups, where the saturated hydrocarbyl group may be linear or branched, and the saturated hydrocarbyl group may optionally contain a single heteroatom selected from N and O in its carbon skeleton.

[0183] For example, R 18 and R 19 They come together, base-L 89 - may be formed, where -L 89 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 89 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH2, -NHMe, or -NMe2 groups, where -L 89 Any methyl group of the substituent may be optionally fluorosubstituted.

[0184] In further embodiments, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0185] As described in both the first and second aspects of the present invention, R 20 and R 21 is independently selected from hydrogen or fluoro groups, or R 20 and R 21 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0186] In one embodiment, R 20 and R 21 The group is independently selected from either a hydrogen or a fluoro group.

[0187] In one embodiment, R 20 and R 21 Both are hydrogen.

[0188] In one embodiment of the first aspect of the present invention, the compound of formula (I) is [ka] isn't it.

[0189] To the extent that it is understandable, embodiments relating to a particular substituent or part (such as a given R or X group) may be read in conjunction with embodiments relating to a different substituent or part, insofar as they are practical.

[0190] For example, in the first exemplary embodiment, a compound of formula (I) as defined above is provided, where, R 1 is hydrogen; R 2 is selected from hydrogen or a halo group; R 3 The -S- moiety is selected from hydrogen or a halo, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form a -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 4The hydrogen group is selected from hydrogen or a halo, -OH, -NH2, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 5 is selected from hydrogen or a halo group; R 6 is hydrogen or halo, -R 60 OR 60 Selected from the base, where R 60 This is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 is hydrogen or fluoro, or C1-C 12 A saturated or unsaturated hydrocarbyl group is independently selected, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining molecule is directly bonded to R 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; X 10 is N or CR 10 and; X 11 is N or CR 11 and; X 12 is N or CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 , and X 13 Two or fewer of these are N; Each R 10 , R 11 , R 12 , and R 13 This is hydrogen or halo, -OH, -SH, -NH2, -SO2NH2, or C1-C 12A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 18 and R 19 is hydrogen or fluoro, or C1-C 12 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining R is directly bonded to the molecule. 18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and R 20 and R 21 is independently selected from hydrogen or fluoro groups, or R 20 and R 21 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0191] Typically, in such exemplary embodiments, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton.

[0192] In one embodiment of the first exemplary embodiment, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Each R 10 , R 11 , R 12 , and R 13 is independently selected from hydrogen or halo, -OH, -NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one, two, or three heteroatoms independently selected from N and O in its carbon skeleton; and R 18 and R 19The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0193] In another aspect of the first exemplary embodiment, R 7 and R 8The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Each R 10 , R 11 , R 12 , and R 13is independently selected from hydrogen or halo, -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or may contain such a group, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; and R 18 and R 19 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0194] In a corresponding second exemplary embodiment, a compound of formula (II) as defined above is provided, where, R 1 is hydrogen; R 4 The hydrogen group is selected from hydrogen or a halo, -OH, -NH2, -SO2NH2, or a C1-C8 saturated or unsaturated hydrocarbyl group, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; R 5 is selected from hydrogen or a halo group; R 6 is hydrogen or halo, -R 60 OR 60 Selected from the base, where R 60This is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 7 and R 8 is hydrogen or fluoro, or C1-C 12 A saturated or unsaturated hydrocarbyl group is independently selected, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining molecule is directly bonded to R 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; X 10 is N or CR 10 and; X11 is N or CR 11 and; X 12 is N or CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 , and X 13 Two or fewer of these are N; Each R 10 , R 11 , R 12 , and R 13 This is hydrogen or halo, -OH, -SH, -NH2, -SO2NH2, or C1-C 12 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; Each R 14 and R 15 is independently selected from hydrogen or C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl, or R 14 and R 15 These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted; R 16The group is selected from hydrogen, fluoro, -SO2NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties; R 17 This is selected from hydrogen or fluoro, C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; Alternatively, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted; R 18 and R 19 is hydrogen or fluoro, or C1-C 12A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety, provided that the remaining R is directly bonded to the molecule. 18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and R 20 and R 21 is independently selected from hydrogen or fluoro groups, or R 20 and R 21These, together with the carbon atoms to which they are bonded, form a C=O group.

[0195] Typically, in such exemplary embodiments, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton.

[0196] In one embodiment of the second exemplary embodiment, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Each R 10 , R 11 , R 12 , and R 13is independently selected from hydrogen or halo, -OH, -NH2, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one, two, or three heteroatoms independently selected from N and O in its carbon skeleton; and R 18 and R 19 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 or R 19 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0197] In another aspect of the second exemplary embodiment, R 7 and R 8 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 7 or R 8 Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 7 and R 8 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 7 and R 8Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Each R 10 , R 11 , R 12 , and R 13 is independently selected from hydrogen or halo, -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or may contain such a group, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; and R 18 and R 19 The R group is independently selected from hydrogen, fluoro, or C1-C8 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moieties, provided that the R group is directly bonded to the rest of the molecule. 18 or R 19Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R 18 and R 19 Each ring atom of the cyclic group directly bonded to the carbon atom to which is bonded is a cyclic carbon atom, where the cyclic group may be optionally substituted with one or more substituents independently selected from halo, oxo (=O), -OH, -NH2, or C1-C4 saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or a cyclic group, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0198] In a third exemplary embodiment, a compound of formula (I) as defined above is provided, wherein, R 1 is hydrogen; R 2 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 3 is hydrogen or fluoro, chloro, bromo, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 The group is selected from the group, but R contains any of the substituents. 3 Provided that it contains 8 or fewer carbon atoms; R 30 This includes C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 31 Selected from the basis; R31 R is a 3-6 member monocyclic group, where the 3-6 member monocyclic group is one or more fluoro, chloro, and / or bromo groups, and / or one or two groups R 32 It can be optionally replaced; Each R 32 The group is independently selected from methyl or fluoromethyl groups; R 4 These are fluoro, chloro, bromo, -OH, and -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 -L4 -R 45 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 41 is, -R 44 or -R 45 Selected from the basis; Each R 42 is hydrogen or -R 44 or -R 45 Either selected independently of the base, or any two R 42 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 4 L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 4 It has a chain length of 1 to 4 atoms, and L 4 It consists of one or two oxo (=O) groups and / or one or more R groups. L4 It can be optionally replaced; Each R L4 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L4 and R 41 , or any R L4 and any R 42 These may, together with the atoms to which they are bonded, form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; R 43 is hydrogen or -R 44 Selected from the basis; Each R 44The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 45 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 45 Any methyl group may be optionally fluorosubstituted; R 5 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 6 is chloro, bromo, -R 60 OR 60 Selected from the basis; R 60 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7R contains 10 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 Provided that the atom is a carbon, hydrogen, or fluorine atom; R 71 is, -R 73 or -R 74 Selected from the basis; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 7 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced; Each R L7 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L7 These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R L7 and R 71 , or any R L7 and any R 72 -L is where they are joined together. 7 -COOR71 , -L 7 -CO-N(R 72 )2, -L 7 -OR 71 or L 7 -N(R 72 ) Together with two atoms, they may form a 3-6 member monocyclic heterocyclic group, where the 3-6 member monocyclic heterocyclic group is saturated or monounsaturated, and the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Each R 73 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 74 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 74 Any methyl group may be optionally fluorosubstituted; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78- is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; X 10 is N or CR 10 and; X 11 CR 11 and X 12 CR 12 is or X 11 CR 11 and X 12 is N, or X 11 is N and X 12 CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 and X 13 One or fewer of these is N; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 This is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, or C1-C 10A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, or contain them, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl group may optionally contain in its carbon skeleton one, two, three, four, five, or six heteroatoms independently selected from N, O, and S, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 ,-CO-N(R 182 )2, -L 18 -COOH, -L 18 -COOR 181 , -L 18 -CO-N(R 182 )2, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 10 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 19 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 18 and R19 These, together with the carbon atoms to which they are bonded, form a C=O group; R 181 is, -R 183 or -R 184 Selected from the basis; Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 18 is a linear alkylene, alkenylene, or alkynylene group, where the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced; Each R L18 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L18 These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R L18 and R 181 , or any R L18 and any R 182 -L is where they are joined together. 18 -COOR181 , -L 18 -CO-N(R 182 )2, -L 18 -OR 181 or -L 18 -N(R 182 ) Together with two atoms, they may form a 3-6 member monocyclic heterocyclic group, where the 3-6 member monocyclic heterocyclic group is saturated or monounsaturated, and the 3-6 member monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Or, L 18 is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; Each R 183 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 184 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 184 The methyl group may be optionally fluorosubstituted; and R 20 and R 21 The group is independently selected from either a hydrogen or a fluoro group.

[0199] In one embodiment of the third exemplary embodiment, R 30 This is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 4 These are fluoro, chloro, bromo, -OH, and -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 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12or R 13 This is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, or C1-C 10 A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, or contain them, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl group may optionally contain one, two, three, or four heteroatoms independently selected from N, O, and S in its carbon skeleton, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 18 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 19 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 18and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0200] In a further embodiment of the third exemplary embodiment, R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 is a hydrogen or fluoro, chloro or bromo group, 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 ) independently selected from two groups, wherein the aforementioned group containing any of the substituents contains 10 or fewer carbon atoms, and the total number of nitrogen, oxygen, and sulfur atoms in the aforementioned group containing any of the substituents is 6 or less; Each R 131 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 132 is hydrogen or -R 131 Selected independently from the basis; R 133 is hydrogen or -R 131 Selected from the basis; L 13 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains 1, 2, or 3 heteroatoms independently selected from O and N in its carbon skeleton, where L 13 It has a chain length of 1 to 8 atoms, and L 13R is one or two groups independently selected from oxo (=O) and -OH, and / or one or more groups R L13 It can be optionally replaced; Each R L13 This is independently selected from fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe, or -CH2O-fluoromethyl groups; Alternatively, any two R L13 , or any R L13 and any R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered monocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups; Alternatively, 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 These may, together with the atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, where the 6-10 membered bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups; and If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups.

[0201] In one embodiment of such further aspects, R 30This is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 4 These are fluoro, chloro, bromo, -OH, and -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 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 7 These are hydrogen or fluoro, -CN, -COOH, -COOR 71 , -L 7 -COOH, -L 7 -COOR71 , -L 7 -OH, -L 7 -OR 71 , -L 7 -N(R 72 )2, -R 73 ,-R 74 or -L 7 -R 74 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 is a hydrogen or fluoro, chloro or bromo group, or -R131 、-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、-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 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、-NR133 -L 13 -SO2-R 131 or -NR 133 -L 13 -SO2-N(R 132 ) independently selected from two groups, wherein the aforementioned group containing any of the substituents contains 10 or fewer carbon atoms, and the total number of nitrogen, oxygen, and sulfur atoms in the aforementioned group containing any of the substituents is 4 or less; Each R 131 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 132 is hydrogen or -R 131 Selected independently from the basis; R 133 is hydrogen or -R 131 Selected from the basis; L 13 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 13 It has a chain length of 1 to 8 atoms, and L 13 It consists of one or two oxo (=O) groups and / or one or more R groups. L13 It can be optionally replaced; Each R L13 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L13 , or any R L13 and R 131 , or any two R 131These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered monocyclic group, where the 3- to 7-membered monocyclic group is saturated or monounsaturated, and the 3- to 7-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any two R L13 and R 131 These may, together with multiple atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, where the 6-10 membered bicyclic heterocyclic group is saturated or monounsaturated, and the 6-10 membered bicyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; and If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 18 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 19 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 18 and R 19These, together with the carbon atoms to which they are bonded, form a C=O group.

[0202] In the corresponding fourth exemplary embodiment, a compound of formula (II) as defined above is provided, where, R 1 is hydrogen; R 4 These are fluoro, chloro, bromo, -OH, and -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 -R45 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 41 is, -R 44 or -R 45 Selected from the basis; Each R 42 is hydrogen or -R 44 or -R 45 Either selected independently of the base, or any two R 42 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 4 L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 4 It has a chain length of 1 to 4 atoms, and L 4 It consists of one or two oxo (=O) groups and / or one or more R groups. L4 It can be optionally replaced; Each R L4 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R L4 and R 41 , or any R L4 and any R 42 These may, together with the atoms to which they are bonded, form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; R 43 is hydrogen or -R 44 Selected from the basis; Each R 44The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 45 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 45 Any methyl group may be optionally fluorosubstituted; R 5 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 6 is chloro, bromo, -R 60 OR 60 Selected from the basis; R 60 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7R contains 10 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 Provided that the atom is a carbon, hydrogen, or fluorine atom; R 71 is, -R 73 or -R 74 Selected from the basis; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 7 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced; Each R L7 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L7 These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R L7 and R 71 , or any R L7 and any R 72 -L is where they are joined together. 7 -COOR71 , -L 7 -CO-N(R 72 )2, -L 7 -OR 71 or L 7 -N(R 72 ) Together with two atoms, they may form a 3-6 member monocyclic heterocyclic group, where the 3-6 member monocyclic heterocyclic group is saturated or monounsaturated, and the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Each R 73 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 74 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 74 Any methyl group may be optionally fluorosubstituted; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78- is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; X 10 is N or CR 10 and; X 11 CR 11 and X 12 CR 12 is or X 11 CR 11 and X 12 is N, or X 11 is N and X 12 CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 and X 13 One or fewer of these is N; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 This is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, or C1-C 10A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, or contain them, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl 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 -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups; Each R 14 and R 15 is independently selected from hydrogen or a C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl group, or R 14 and R 15 These, together with the carbon atoms to which they are bonded, form a cyclopropyl or cyclobutyl group, which may be optionally substituted with one or more fluoro groups; R 16 is hydrogen or fluoro, -R 160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 The group is selected from the group, but R contains any of the substituents. 16 Provided that it contains 8 or fewer carbon atoms; R 160 This includes C1-C6 alkyl, C1-C6 fluoroalkyl, C2-C6 alkenyl, C2-C6 fluoroalkenyl or -R 161 Selected from the basis; R 161R is a 3-6 member monocyclic group, where the 3-6 member monocyclic group is one or more fluoro, chloro, and / or bromo groups, and / or one or two groups R 162 It can be optionally replaced; Each R 162 is independently selected from methyl or fluoromethyl groups; and R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; Alternatively, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3-5 membered saturated monocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O) or methyl or fluoromethyl groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 ,-CO-N(R 182 )2, -L 18 -COOH, -L 18 -COOR 181 , -L 18 -CO-N(R 182 )2, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 10 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 19 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 18 and R 19These, together with the carbon atoms to which they are bonded, form a C=O group; R 181 is, -R 183 or -R 184 Selected from the basis; Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L 18 is a linear alkylene, alkenylene, or alkynylene group, where the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced; Each R L18 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L18 These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R L18 and R 181 , or any R L18 and any R 182 -L is where they are joined together. 18 -COOR 181 , -L18 -CO-N(R 182 )2, -L 18 -OR 181 or -L 18 -N(R 182 ) Together with two atoms, they may form a 3-6 member monocyclic heterocyclic group, where the 3-6 member monocyclic heterocyclic group is saturated or monounsaturated, and the 3-6 member monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Or, L 18 is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; Each R 183 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 184 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 184 The methyl group may be optionally fluorosubstituted; and R 20 and R 21 The group is independently selected from either a hydrogen or a fluoro group.

[0203] In one aspect of the fourth exemplary embodiment, R 4 These are fluoro, chloro, bromo, -OH, and -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 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 This is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH2, -SO2NH2, or C1-C 10A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, or contain them, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl group may optionally contain one, two, three, or four heteroatoms independently selected from N, O, and S in its carbon skeleton, and one -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH to form an -SO-, -SO2-, -S(=NH)-, or -SO(=NH)- moiety; If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups; R 160 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 18 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 The group is selected from the group, but R contains any of the substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 19 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group.

[0204] In a further embodiment of the fourth exemplary embodiment, R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 is a hydrogen or fluoro, chloro or bromo group, 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 -SL13 -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 ) independently selected from two groups, wherein the aforementioned group containing any of the substituents contains 10 or fewer carbon atoms, and the total number of nitrogen, oxygen, and sulfur atoms in the aforementioned group containing any of the substituents is 6 or less; Each R 131 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 132 is hydrogen or -R 131 Selected independently from the basis; R 133 is hydrogen or -R 131 Selected from the basis; L 13 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains 1, 2, or 3 heteroatoms independently selected from O and N in its carbon skeleton, where L 13 It has a chain length of 1 to 8 atoms, and L13 R is one or two groups independently selected from oxo (=O) and -OH, and / or one or more groups R L13 It can be optionally replaced; Each R L13 This is independently selected from fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, fluorocyclopropyl, -CH2OH, -CH2OMe, or -CH2O-fluoromethyl groups; Alternatively, any two R L13 , or any R L13 and any R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered monocyclic group, which may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups; Alternatively, 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 These may, together with the atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, where the 6-10 membered bicyclic heterocyclic group may be optionally substituted with one or two groups independently selected from oxo (=O) and -OH, and / or one or more fluoro, methyl and / or fluoromethyl groups; and If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups.

[0205] In one embodiment of such further aspects, R 4 These are fluoro, chloro, bromo, -OH, and -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 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH2OH, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; One remaining R 10 , R 11 , R 12 or R 13 is a hydrogen or fluoro, chloro or bromo group, or -R 131 -OH, -SH, -OR 131 , -SR 131 , -N(R 132 )2, -SO2-R 131 -SO2-N(R132 )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、-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 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 または-NR 133 -L 13 -SO2-N(R 132) independently selected from two groups, wherein the aforementioned group containing any of the substituents contains 10 or fewer carbon atoms, and the total number of nitrogen, oxygen, and sulfur atoms in the aforementioned group containing any of the substituents is 4 or less; Each R 131 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 132 is hydrogen or -R 131 Selected independently from the basis; R 133 is hydrogen or -R 131 Selected from the basis; L 13 L is a linear alkylene or alkenylene group, wherein the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 13 It has a chain length of 1 to 8 atoms, and L 13 It consists of one or two oxo (=O) groups and / or one or more R groups. L13 It can be optionally replaced; Each R L13 This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R L13 , or any R L13 and R 131 , or any two R 131 These may, together with the atom(s) to which they are bonded, form a 3- to 7-membered monocyclic group, where the 3- to 7-membered monocyclic group is saturated or monounsaturated, and the 3- to 7-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any two R L13 and R 131These may, together with multiple atoms to which they are bonded, form a 6-10 membered bicyclic heterocyclic group, where the 6-10 membered bicyclic heterocyclic group is saturated or monounsaturated, and the 6-10 membered bicyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; and If any, further remaining R 10 , R 11 , R 12 or R 13 Each of these is independently selected from hydrogen, fluoro, chloro, or bromo groups.

[0206] A fifth exemplary embodiment provides a compound of formula (I) as defined above, wherein, R 1 is hydrogen; R 2 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 3 is hydrogen or fluoro, chloro, bromo, -R 30 -CN, -CHO, -COR 30 -CO2H or -CO2R 30 Selected from the base, where R 30 This is selected from C1-C4 alkyl, C3-C4 cycloalkyl, C1-C4 fluoroalkyl, or C3-C4 fluorocycloalkyl; R 4 These are fluoro, chloro, bromo, -OH, and -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 The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 41 is, -R 44 or -R 45 Selected from the basis; Each R 42 is hydrogen or -R 44 or -R 45 Either selected independently of the base, or any two R 42 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; L 4 L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 4 It has a chain length of 1 to 4 atoms, and L 4 It consists of one or two oxo (=O) groups and / or one or more R groups. L4It can be optionally replaced, where each R L4 is independently selected from fluoro, methyl, or fluoromethyl groups, or any R L4 and R 41 , or any R L4 and any R 42 However, together with the atoms to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; R 43 is hydrogen or -R 44 Selected from the basis; Each R 44 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 45 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 45 Any methyl group may be optionally fluorosubstituted; R 5 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 6 is, -R 60 OR 60 Selected from the basis; R 60 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 Provided that the atom is a carbon, hydrogen, or fluorine atom; R 71 is, -R 73 or -R 74 Selected from the basis; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; L 7 L is a linear alkylene group, wherein the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced, where each R L7 is independently selected from fluoro, methyl, or fluoromethyl groups, or any R L7 and R 71 , or any R L7 and any R 72 However, they are combined -L 7 -COOR71 , -L 7 -OR 71 or -L 7 -N(R 72 ) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 73 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 74 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 74 Any methyl group may be optionally fluorosubstituted; R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78- may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; X 10 is N or CR 10 and; X 11 CR 11 and X 12 CR 12 is or X 11 CR 11 and X 12 is N, or X 11 is N and X 12 CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 and X 13 One or fewer of these is N; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; If present, the remaining R 10 , R 11 , R 12 and R 13 Each of these is independently selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, where R 10 , R 11 , R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted; R 18These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 7 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Selected from the base, and R 19 R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups, however, R may contain any of these substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 Provided that the atom is a carbon, hydrogen, or fluorine atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group; R 181 is, -R 183 or -R 184 Selected from the basis; Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; L 18is a linear alkylene, alkenylene, or alkynylene group, where the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced, where each R L18 is independently selected from fluoro, methyl, or fluoromethyl groups, or any R L18 and R 181 , or any R L18 and any R 182 -L is where they are joined together. 7 -COOR 181 , -L 18 -OR 181 or -L 18 -N(R 182 ) Together with two atoms, they form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups, or L 18 is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; Each R 183 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 184R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 184 The methyl group may be optionally fluorosubstituted; and R 20 and R 21 The group is independently selected from either a hydrogen or a fluoro group.

[0207] In one embodiment of the fifth exemplary embodiment, R 3 This group is selected from hydrogen, fluoro, chloro, bromo, -CN, or methyl groups, where the methyl group may be optionally fluorosubstituted; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 Provided that the atom is a carbon, hydrogen, or fluorine atom; Each R 73 is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, where the C1-C4 alkyl or C3-C6 cycloalkyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; R 18 These are hydrogen or fluoro, -CN, -COOH, -L 18 -COOH, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Selected from the base, and R 19 R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups, however, R may contain any of these substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 Provided that the atom is a carbon, hydrogen, or fluorine atom; Alternatively, R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and Each R 183The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups.

[0208] In the corresponding sixth exemplary embodiment, a compound of formula (II) as defined above is provided, where, R 1 is hydrogen; R 4 These are fluoro, chloro, bromo, -OH, and -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 45The group is selected from the group, but R contains any of the substituents. 4 Provided that it contains 8 or fewer carbon atoms; R 41 is, -R 44 or -R 45 Selected from the basis; Each R 42 is hydrogen or -R 44 or -R 45 Either selected independently of the base, or any two R 42 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; L 4 L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 4 It has a chain length of 1 to 4 atoms, and L 4 It consists of one or two oxo (=O) groups and / or one or more R groups. L4 It can be optionally replaced, where each R L4 is independently selected from fluoro, methyl, or fluoromethyl groups, or any R L4 and R 41 , or any R L4 and any R 42 However, together with the atoms to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; R 43 is hydrogen or -R 44 Selected from the basis; Each R 44The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 45 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 45 Any methyl group may be optionally fluorosubstituted; R 5 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 6 is, -R 60 OR 60 Selected from the basis; R 60 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 Provided that the atom is a carbon, hydrogen, or fluorine atom; R71 is, -R 73 or -R 74 Selected from the basis; Each R 72 is hydrogen or -R 73 or -R 74 Either selected independently of the base, or any two R 72 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; L 7 L is a linear alkylene group, wherein the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L 7 It has a chain length of 1 to 4 atoms, and L 7 It consists of one or two oxo (=O) groups and / or one or more R groups. L7 It can be optionally replaced, where each R L7 is independently selected from fluoro, methyl, or fluoromethyl groups, or any R L7 and R 71 , or any R L7 and any R 72 However, they are combined -L 7 -COOR 71 , -L 7 -OR 71 or -L 7 -N(R 72 ) Together with two atoms, they may form a 3-6 member saturated monocyclic heterocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 73The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 74 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 74 Any methyl group may be optionally fluorosubstituted; R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; X 10 is N or CR 10 and; X 11 CR11 and X 12 CR 12 is or X 11 CR 11 and X 12 is N, or X 11 is N and X 12 CR 12 and; X 13 is N or CR 13 and; X 10 , X 11 , X 12 and X 13 One or fewer of these is N; R 11 and R 12 One of the following is present, and selected from fluoro, chloro, bromo, fluoromethyl, -CN, -COOH, -CONH2, or -C(=NH)NH2 groups; If present, the remaining R 10 , R 11 , R 12 and R 13 Each of these is independently selected from hydrogen or a fluoro, chloro, bromo, -OH, -NH2, methyl (Me), ethyl (Et), -OMe, -NHMe, -NMe2, -CH2OH, or -CH2NH2 group, where R 10 , R 11 , R 12 or R 13 Any methyl (Me), ethyl (Et), or methylene (-CH2-) group may be optionally fluorosubstituted; Each R 14 and R 15 is independently selected from hydrogen or a C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl or fluorocyclopropyl group, or R 14 and R 15 These, together with the carbon atoms to which they are bonded, form a cyclopropyl or cyclobutyl group, which may be optionally substituted with one or more fluoro groups; R 16 is hydrogen or fluoro, -R160 -CN, -CHO, -COR 160 -CO2H or -CO2R 160 Selected from the basis; R 160 is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; and R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; Alternatively, R 16 and R 17 These, together with the carbon atoms to which they are bonded, form a 3-5 membered saturated monocyclic group, which may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo (=O) or methyl or fluoromethyl groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -COOR 181 , -L 18 -COOH, -L 7 -COOR 181 , -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Selected from the base, and R 19 R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups, however, R may contain any of these substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 Provided that the atom is a carbon, hydrogen, or fluorine atom; Alternatively, R 18 and R 19 These, together with the carbon atoms to which they are bonded, form a C=O group; R 181 is, -R 183or -R 184 Selected from the basis; Each R 182 is hydrogen or -R 183 or -R 184 Either selected independently of the base, or any two R 182 However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; L 18 is a linear alkylene, alkenylene, or alkynylene group, where the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more R groups. L18 It can be optionally replaced, where each R L18 is independently selected from fluoro, methyl, or fluoromethyl groups, or any R L18 and R 181 , or any R L18 and any R 182 -L is where they are joined together. 7 -COOR 181 , -L 18 -OR 181 or -L 18 -N(R 182 ) Together with two atoms, they form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups, or L 18is a divalent phenyl or a divalent 5 or 6-membered heteroaryl group, where the divalent phenyl or the divalent 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; Each R 183 The group is independently selected from a C1-C4 alkyl or C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group, where the C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, or C5-C6 cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R 184 R is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, and bromo, and / or one or two groups independently selected from methyl (Me), -CN, -OH, -OMe, -NH2, -NHMe, and -NMe2, where R 184 The methyl group may be optionally fluorosubstituted; and R 20 and R 21 The group is independently selected from either a hydrogen or a fluoro group.

[0209] In one embodiment of the sixth exemplary embodiment, R 7 These are hydrogen or fluoro, -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 The group is selected from the group, but R contains any of the substituents. 7R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 7 Provided that the atom is a carbon, hydrogen, or fluorine atom; Each R 73 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R 7 and R 8 They come together, base-L 78 -forms, where -L 78 - is selected from -CH2-CH2-, -CH2-CH2-CH2-, -CH2-NH-CH2-, -CH2-G-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-NH-CH2-, -CH2-CH2-G-CH2-, -CH2-NH-CH2-CH2- or -CH2-G-CH2-CH2-base, where -L 78 - may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O), -CN, methyl(Me), -OH, -OMe, -NH2, -NHMe or -NMe2 groups, and -L 78 - Any methyl group of the substituent may be optionally fluorosubstituted; R 16 is selected from hydrogen or fluoro, -CN, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; and R 17 The group is selected from hydrogen, fluoro, C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; Alternatively, R 16 and R 17These, together with the carbon atoms to which they are bonded, form a cyclopropyl or cyclobutyl group, which may be optionally substituted with one or more fluoro groups; R 18 These are hydrogen or fluoro, -CN, -COOH, -L 18 -COOH, -L 18 -OH, -L 18 -OR 181 , -L 18 -N(R 182 )2, -R 183 ,-R 184 or -L 18 -R 184 Selected from the base, and R 19 R is selected from hydrogen, fluoro, methyl, or fluoromethyl groups, however, R may contain any of these substituents. 18 R contains 8 or fewer carbon atoms and is directly bonded to the remaining molecule. 18 Provided that the atom is a carbon, hydrogen, or fluorine atom; Alternatively, R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and Each R 183 The C1-C4 alkyl or C3-C6 cycloalkyl group is independently selected from C1-C4 alkyl or C3-C6 cycloalkyl groups, which may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups.

[0210] A seventh exemplary embodiment provides a compound of formula (I) as defined above, wherein, R 1 is hydrogen; R 2 is hydrogen; R 3 The group is selected from hydrogen, fluoro, chloro, or bromo groups; R 4 Fluoro, chloro, bromo, -R 44 OR 44 Selected from the basis; R 44 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 5 is hydrogen; R 6 This is a methyl or fluoromethyl group; R 7 is hydrogen or fluoro, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -OH, -L 71 -OR 75 or -R 75 Selected from the basis; -L 71 - is selected from -CH2-, -CHMe-, or -CMe2- groups, where any -CH2-, -CHMe-, or -CMe2- group may be optionally fluorosubstituted; R 75 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; X 10 These are N, CH, CF, C-Cl, or C-Br; X 11 is C-CN and X 12 is either CH, CF, C-Cl, or C-Br, or X 12 is C-CN and X 11 These are CH, CF, C-Cl, or C-Br; X 13 These are N, CH, CF, C-Cl, or C-Br; X 10 and X 13 One or fewer of these is N; R 18 and R 19 is independently selected from hydrogen or fluoro, methyl or fluoromethyl groups, or R 18and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and R 20 and R 21 Both are hydrogen.

[0211] In one embodiment of the seventh exemplary embodiment, R 18 and R 19 Both are hydrogen.

[0212] In the corresponding eighth exemplary embodiment, a compound of formula (II) as defined above is provided, where, R 1 is hydrogen; R 4 Fluoro, chloro, bromo, -R 44 OR 44 Selected from the basis; R 44 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 5 is hydrogen; R 6 This is a methyl or fluoromethyl group; R 7 is hydrogen or fluoro, -L 71 -COOH, -L 71 -COOR 75 , -L 71 -OH, -L 71 -OR 75 or -R 75 Selected from the basis; -L 71 - is selected from -CH2-, -CHMe-, or -CMe2- groups, where any -CH2-, -CHMe-, or -CMe2- group may be optionally fluorosubstituted; R 75 The group is selected from C1-C3 alkyl, cyclopropyl, C1-C3 fluoroalkyl, or fluorocyclopropyl groups; R 8 This is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; X 10 These are N, CH, CF, C-Cl, or C-Br; X 11 is C-CN and X 12 is either CH, CF, C-Cl, or C-Br, or X 12 is C-CN and X 11 These are CH, CF, C-Cl, or C-Br; X 13 These are N, CH, CF, C-Cl, or C-Br; X 10 and X 13 One or fewer of these is N; R 14 and R 15 Both are hydrogen; R 16 and R 17 Both are hydrogen; R 18 and R 19 is independently selected from hydrogen or fluoro, methyl or fluoromethyl groups, or R 18 and R 19 They, together with the carbon atoms to which they are bonded, form a C=O group; and R 20 and R 21 Both are hydrogen.

[0213] In one embodiment of the eighth exemplary embodiment, R 18 and R 19 Both are hydrogen.

[0214] In any one embodiment of the above embodiments, the compound of formula (I) or formula (II) has a molecular weight of 248 to 750 Da. Typically, the compound of formula (I) or formula (II) has a molecular weight of 260 to 600 Da, or 260 to 500 Da. More typically, the compound of formula (I) or formula (II) has a molecular weight of 280 to 400 Da.

[0215] A third aspect of the present invention provides a compound selected from the group consisting of: [ka]

[0216] A fourth aspect of the present invention provides pharmaceutically acceptable salts and / or solvates and / or prodrugs of any compound of the first, second, or third aspect of the present invention.

[0217] In one embodiment, a fourth aspect of the present invention provides a pharmaceutically acceptable salt and / or solvate of any of the compounds of the first, second, or third aspect of the present invention. For example, a fourth aspect of the present invention provides (i) a pharmaceutically acceptable salt of any of the compounds of the first, second, or third aspect of the present invention, or (ii) a pharmaceutically acceptable solvate of any of the compounds of the first, second, or third aspect of the present invention, or (iii) a pharmaceutically acceptable solvate of a pharmaceutically acceptable salt of any of the compounds of the first, second, or third aspect of the present invention.

[0218] The compounds of the present invention can be used in both their free base form and their acid addition salt form. For the purposes of the present invention, the “salt” of the compounds of the present invention includes an acid addition salt. The acid addition salt is preferably a pharmaceutically acceptable nontoxic addition salt with a suitable acid, such as an inorganic acid such as a hydrohalic acid (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 an organic carboxylic acid (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, malic succinic acid, malic acid, hydroxysuccinic acid, tartaric acid, fumaric acid, malic acid, malic acid, acetic acid, benzoic acid, benzoic acid, hydroxysuccinic acid, tartaric acid, fumaric acid, malic acid, malic acid, acetic acid, benzoic acid, benzoic acid, hydroxysuccinic acid, hydroxysuccinic acid, tartaric acid, fumaric acid, malic acid, hydroxysuccinic acid, hydroxysuccinic acid, hydroxysuccinic acid, tartaric acid, fumaric acid, malic acid, hydroxysuccinic acid, hydroxysuccinic acid, hydroxys Examples of organic acids include, but are not limited to, ionic acids (such as ic acid, hydroxymaleic acid, mucoic acid or galactaric acid, gluconic acid, pantothenic acid or pamoic acid), organic sulfonic acids (e.g., methanesulfonic acid, trifluoromethanesulfonic acid, ethanesulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, toluene-p-sulfonic acid, naphthalene-2-sulfonic acid or camphorsulfonic acid), or amino acids (e.g., ornithine, glutamic acid or aspartic acid). The acid addition salt may be a monoacid, diacid, triacid, or polyacid. Preferred salts are hydrohalic acid, sulfuric acid, phosphoric acid, or organic acid addition salts. Preferred salts are hydrochloric acid addition salts.

[0219] When the compound of the present invention contains a quaternary ammonium group, the compound is typically used in salt form. The counterion for the quaternary ammonium group may be any pharmaceutically acceptable, non-toxic counterion. Examples of suitable counterions include the conjugate bases of protic acids mentioned above with respect to acid addition salts.

[0220] The compounds of the present invention can also be used in both their free acid form and their salt form. For the purposes of the present invention, the “salts” of the compounds of the present invention include those formed between the protic acidic functional group (such as a carboxylic acid group) of the compound of the present invention and a suitable cation. Examples of suitable cations include, but are not limited to, lithium, sodium, potassium, magnesium, calcium, and ammonium. The salts may be monosalts, disalts, trisalts, or polysalts. Preferably, the salts are monolithium or dilithium, sodium, potassium, magnesium, calcium, or ammonium salts. More preferably, the salts are monosodium or monopotassium salts.

[0221] Preferably, any salt is a pharmaceutically acceptable, non-toxic salt. However, in addition to pharmaceutically acceptable salts, other salts are also included in the present invention for reasons such as having the potential to function as intermediates in the purification or preparation of pharmaceutically acceptable salts, or being useful in the identification, characterization, or purification of free acids or bases.

[0222] The compounds and / or salts of the present invention may be in the form of anhydrous or hydrates (e.g., hemihydrate, monohydrate, dihydrate, or trihydrate) or other solvates. Such other solvates may be formed using alcohol solvents, including but not limited to common organic solvents such as methanol, ethanol, or isopropanol.

[0223] In one embodiment, a fourth aspect of the present invention provides a prodrug of any compound of the first, second, or third aspect of the present invention. Similarly, a fourth aspect of the present invention may provide a pharmaceutically acceptable salt and / or solvate of such a prodrug. For example, a fourth aspect of the present invention may provide (i) a pharmaceutically acceptable salt of a prodrug, or (ii) a pharmaceutically acceptable solvate of a prodrug, or (iii) a pharmaceutically acceptable solvate of a pharmaceutically acceptable salt of a prodrug.

[0224] In some embodiments of the present invention, therapeutically inactive prodrugs are provided. A prodrug is a compound that, when administered to a subject such as a human, is converted in whole or in part to a compound of the present invention. In most embodiments, the prodrug is a pharmacologically inactive chemical derivative that is converted in vivo to an active drug molecule to exert a therapeutic effect. Any of the compounds described herein may be administered as a prodrug to improve the activity, bioavailability, or stability of the compound, or to alter the properties of the compound. Typical examples of prodrugs include compounds having a biologically unstable protecting group in the functional portion of the active compound. Prodrugs include, but are not limited to, compounds that can be oxidized, reduced, aminated, deaminated, hydroxylated, dehydroxylated, hydrolyzed, dehydrolyzed, alkylated, dealkylated, acylated, deacylated, phosphorylated, and / or dephosphorylated to produce an active compound. The present invention also includes salts and solvates of such prodrugs as described above.

[0225] The compounds, salts, solvates, and prodrugs of the present invention can be obtained in all grades of purity, for example, by conventional techniques such as recrystallization and / or column chromatography.

[0226] 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 when measured by HPLC.

[0227] 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 when measured by LCMS.

[0228] Alternatively, the compounds, salts, solvates, and prodrugs of the present invention are: 1When measured by 1H NMR, it 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.

[0229] 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 encompasses racemic mixtures of the compounds, salts, solvates, and prodrugs of the present invention, as well as enantiomerically concentrated and substantially enantiomerically pure isomers. For the purposes of the present invention, a "substantially enantiomerically pure" isomer of a compound contains less than 5% by weight, more typically less than 2% by weight, and most typically less than 0.5% by weight, of the other isomer of the same compound.

[0230] The compounds, salts, solvates, and prodrugs of the present invention are 12 C, 13 C, 1 H, 2 H(D), 14 N, 15 N, 16 O, 17 O, 18 O, 19 F and 127 I is one example, but is not limited to any other stable isotope, and 11 C, 14 C, 3 H(T), 13 N, 15 O, 18 F, 123 I, 124 I, 125 I and 131 I is one example, but it may contain any radioactive isotope, not limited to these.

[0231] The compounds, salts, solvates, and prodrugs of the present invention may be polymorphic or amorphous.

[0232] 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.

[0233] Conventional procedures for selecting and preparing appropriate pharmaceutical compositions can be found, for example, in “Aulton's Pharmaceutics - The Design and Manufacture of Medicines”, MEAulton and KMG Taylor, Churchill Livingstone Elsevier, 4 th It is described in Ed., 2013.

[0234] pharmaceutically acceptable excipients, including adjuvants, diluents, or carriers, that may be used in the pharmaceutical compositions of the present invention are those conventionally used in the field of pharmaceutical compositions and include, but are not limited to, sugars, sugar alcohols, starch, ion exchange substances, alumina, aluminum stearate, lecithin, serum proteins such as human serum albumin, buffering substances such as phosphates, glycerin, sorbic acid, potassium sorbate, partial glyceride mixtures of saturated vegetable fatty acids, water, salts or electrolytes such as protamine sulfate, disodium hydrogen phosphate, potassium hydrogen phosphate, sodium chloride, zinc salts, colloidal silica, magnesium trisilicate, polyvinylpyrrolidone, cellulosic substances, polyethylene glycol, sodium carboxymethylcellulose, polyacrylate, wax, polyethylene-polyoxypropylene-block polymer, polyethylene glycol, and lanolin.

[0235] A sixth aspect of the present invention provides a compound according to the first, second, or third aspect of the present invention, or a pharmaceutically acceptable salt, solvate, or prodrug according to the fourth aspect of the present invention, or a pharmaceutical composition according to the fifth aspect of the present invention, for use in pharmaceuticals and / or for use in the treatment or prevention of disease, disorder, or pathological condition. Typically, use involves administration to a subject of the compound, salt, solvate, prodrug, or pharmaceutical composition.

[0236] As used herein, the term “treatment” means curative treatment and equivalents to remission or symptomatic treatment. This term includes obtaining beneficial or desired physiological outcomes, which may or may not be clinically established. Beneficial or desired clinical outcomes include, but are not limited to, symptom relief, prevention of symptoms, reduction of disease severity, stabilization of the condition (i.e., no worsening), delay or slowing of disease / symptom progression / worsening, reduction or temporary relief of disease / symptoms, and remission (whether partial or complete), whether detectable or undetectable. The term “temporary relief,” and its variations thereof, as used herein, means that the severity of a physiological condition or symptom and / or undesirable signs are reduced and / or the time course of progression is slowed or prolonged compared to no administration of the compounds, salts, solvates, prodrugs or pharmaceutical compositions of the present invention. The term “prevention,” as used herein with respect to disease, disorder or condition, refers to preventive or protective therapies, as well as therapies that reduce the risk of developing a disease, disorder or condition. The term “prevention” encompasses both avoiding the onset of a disease, disorder, or condition, and delaying its onset. Any statistically significant (p ≤ 0.05) avoidance of onset, delay of onset, or reduction of risk, as measured by controlled clinical trials, may be considered prevention of a disease, disorder, or condition. Target populations for prevention include those at high risk of a disease, disorder, or condition, as identified by genetic or biochemical markers. Typically, genetic or biochemical markers are appropriate for the disease, disorder, or condition under consideration and may include, for example, inflammatory biomarkers such as C-reactive protein (CRP) and monocyte chemotactic protein-1 (MCP-1) in the case of inflammation, as well as 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).

[0237] A seventh aspect of the present invention provides the use of a compound according to the first, second, or third aspect, or a pharmaceutically effective salt, solvate, or prodrug according to the fourth aspect, in the manufacture of a pharmaceutical for the treatment or prevention of a disease, disorder, or pathological condition. Typically, the treatment or prevention involves administering the compound, salt, solvate, prodrug, or pharmaceutical to a subject.

[0238] An eighth aspect of the present invention provides a method for treating or preventing a disease, disorder, or condition, the method comprising the step 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, thereby treating or preventing a disease, disorder, or condition. Typically, the administration is performed on a subject in need thereof.

[0239] Dysregulation of alternative complement pathways, whether hereditary or due to the presence of autoantibodies, can lead to a wide variety of diseases. Common polymorphisms or rare mutations in complement proteins can cause complement system dysfunction or dysregulation due to hyperactivation or maladjustment. Autoantibodies can bind to self-cells and drive the complement system, resulting in the overwhelmed protective capacity of natural regulators. In some cases, natural cellular defense mechanisms, such as shedding of the active complex, can lead to symptoms resulting from the loss of important molecules, such as acetylcholine receptors, from the cell surface. However, in many diseases, the complement system is not the primary trigger for the disease, but rather acts secondarily on other disease-causing factors, creating a vicious cycle of inflammation propagated by the complement system. In these diseases, inhibiting the complement system may produce therapeutic effects.

[0240] In some cases, gain-of-function mutations in complement C3 and / or factor B, and / or loss-of-function mutations in regulatory proteins, can lead to uncontrolled C3 activation (Garred, P., Tenner, AJ, and Mollnes, TEPharmacol. Rev. 2021, 73, 792-827). In some cases, common polymorphisms or rare mutations may result in specific phenotypes due to specific effects on function, such as membrane-binding ability. Certain gene changes can lead to proteins with altered ability to bind to specific structures (such as glycosaminoglycans or disease-associated epitopes), resulting in tissue-specific diseases. Domains in which mutations or polymorphisms exist may influence the disease phenotype.

[0241] Accordingly, a ninth aspect of the present invention provides a compound of the first, second, or third aspect of the present invention, or a pharmaceutically acceptable salt, solvate, or prodrug of the fourth aspect of the present invention, or a pharmaceutical composition of the fifth aspect of the present invention, for use in the treatment or prevention of a disease, disorder, or pathological condition in an individual, wherein the individual has a germline mutation or somatic mutation in complement C3 or factor B, or in a regulator of another pathway, or in an enzyme that directly or indirectly causes the production or activation of factor B. The mutation may be, for example, a gain-of-function mutation in factor B that results in increased factor B or C3 / C5 convertase activity, or other mutations. Alternatively, the mutation may be a gain-of-function mutation in complement C3 that increases factor B or C3 / C5 convertase activity, or other mutations. Similarly, mutations can be loss-of-function mutations in negative regulators that increase alternative pathway activity (such as factor H), gain-of-function mutations in positive regulators that increase alternative pathway activity (such as propagin), or gain-of-function mutations in enzymes that cause the production or activation of factor B. Such mutations are discussed in Rodriguez de Cordoba, Immunological Reviews, 2023, 313, 71-90, and Kouser et al., Front. Immunol., 2013, 4(93), 1-12. Typically, use involves administering compounds, salts, solvates, prodrugs, or pharmaceutical compositions to an individual. Use may also involve diagnosing an individual with germline or somatic mutations in (i) complement C3, (ii) factor B, (iii) regulators of alternative pathways, or (iv) enzymes that directly or indirectly cause the production or activation of factor B, where the compound, salt, solvate, prodrug, or pharmaceutical composition is administered to the individual based on a positive diagnosis of the mutation. Typically, the identification of mutations in an individual's complement C3, B factor, regulatory factors, or enzymes may be performed by any appropriate genetic or biochemical means.

[0242] A tenth aspect of the present invention provides the use of a compound of the first, second, or third aspect of the present invention, or a pharmaceutically acceptable salt, solvate, or prodrug of the fourth aspect of the present invention, in the manufacture of a pharmaceutical product for the treatment or prevention of a disease, disorder, or pathological condition in an individual, wherein the individual has a germline mutation or somatic mutation in complement C3 or factor B, or in a regulator of another pathway, or in an enzyme that directly or indirectly causes the production or activation of factor B. The mutation may be, for example, a gain-of-function mutation in factor B that results in increased factor B or C3 / C5 convertase activity, or other mutations. Alternatively, the mutation may be a gain-of-function mutation in complement C3 that increases factor B or C3 / C5 convertase activity, or other mutations. Similarly, the mutation may be a loss-of-function mutation in a negative regulator (such as factor H) that increases the activity of another pathway, a gain-of-function mutation in a positive regulator (such as propagin) that increases the activity of another pathway, or a gain-of-function mutation in an enzyme that causes the production or activation of factor B. Typically, treatment or prevention involves administering a compound, salt, solvate, prodrug, or pharmaceutical to an individual. Treatment or prevention may also involve diagnosing an individual with germline or somatic mutations in (i) complement C3, (ii) factor B, (iii) regulators of other pathways, or (iv) enzymes that directly or indirectly cause the production or activation of factor B, where the compound, salt, solvate, prodrug, or pharmaceutical is administered to the individual based on a positive diagnosis of the mutation. Typically, identification of mutations in complement C3, factor B, regulators, or enzymes in an individual may be performed by any appropriate genetic or biochemical means.

[0243] An eleventh aspect of the present invention provides a method for treating or preventing a disease, disorder, or pathological condition, the method comprising the steps of: diagnosing an individual having a germline or somatic mutation in (i) complement C3, (ii) factor B, (iii) a regulator of another pathway, or (iv) an enzyme that directly or indirectly causes the production or activation of factor B; and administering an effective amount of a compound of the first, second, or third aspect of the present invention, or a pharmaceutically acceptable salt, solvate, or prodrug of the fourth aspect of the present invention, or a pharmaceutical composition of the fifth aspect of the present invention, to the previously diagnosed individual, thereby treating or preventing a disease, disorder, or pathological condition. Typically, the administration is performed on a subject in need thereof.

[0244] In any general embodiment of the sixth to eleventh aspects of the present invention, the disease, disorder, or condition may be a disorder, disorder, or condition of the immune system, cardiovascular system, renal system, respiratory system, central nervous system, reproductive system, visual system, metabolic system, or hematological system, and may be cancer or other malignant tumors, and / or may be caused by or related to a pathogen.

[0245] It will be understood that these general embodiments, defined according to a broad category of diseases, disorders, and pathologies, are not mutually exclusive. In this regard, any particular disease, disorder, or pathology may be classified according to several of the above general embodiments. A non-limiting example is type 1 diabetes, which is an autoimmune disease and a disorder of the endocrine system.

[0246] In one embodiment of the sixth, seventh, eighth, ninth, tenth, or eleventh aspect of the present invention, a disease, disorder, or condition responds to factor B inhibition. As used herein, the term “factor B inhibition” means a complete or partial reduction in the level of activity of factor B that is not bound to or complexed with C3b / C3(H2O), and includes, for example, (i) inhibition of active factor B or Bb, (ii) inhibition of latent factor B (zymogen), and / or (iii) inhibition of the conversion of latent factor B to active factor B.

[0247] In particular, age-related macular degeneration (Schramm, E. et al, Mol.Immunol. 2014, 61, 118-125), retinal detachment (Sweigard, J. Het al, Sci.Transl. Med. 2015, 7, 297ra116-297ra116), Doyne's honeycomb retinal dystrophy (also known as malattia leventinese) (DHRD / ML) (Crowley, MA et al, Hum.Mol.Genet. 2023, ddac187), diabetic macular edema and diabetic retinopathy (Murray, H. et al, Investig. Ophthalmol. Vis. Sci. 2018, 59, 5476-5476; Xu et al, Eur. J.Pharmacol. 2016, 787, 94-104; Gerl et al, Invest. Opthalmol. Vis. Sci, 2002, 43(4), 1104-1108; Zhang et al, Diabetes 2002, 51(12), 3499-3504; and Murray' Defining the Role of Complement Factor B of the Alternative Complement Pathway in Diabetic Retinopathy', PhD thesis, University of Sheffield, 2019; retinal ischemia-reperfusion (Inafuku, S., Klokman, G., and Connor, KM Front. Mol. Neurosci. 2018, 11, 278); non-infectious uveitis (Yang, M. et al, Immunol. Res. 2016, 64, 610-618; Eskandarpour et al, Am. J. Pathol. 2021, 191(2), 320-334; and Tanaka et al. Several ocular conditions, including polypoid choroidal neovascularization and ocular neovascularization (Murray, H. et al, Int. J. Mol. Sci. 2021, 22, 9580), have been shown to be associated with factor B.

[0248] Factor B is associated with SARS-CoV-2 (Yan, B. et al, Sci. Immunol. 2021, 6, eabg0833), Covid-19 (Fujimura, Y., and Holland, LZ Int. J. Hematol. 2022, 115, 457-469), smoking-induced mucosal injury (Davis, K. Set al, Otolaryngol. Head Neck Surg. 2010, 143, 152-158), airway hyperresponsive allergic asthma (Herbert, C. et al, Clin. Sci. (Lond) 2017, 131, 499-509), idiopathic pulmonary fibrosis (Meliconi, R. et al, Clin. Immunol. Immunopathol. 1990, 57, 64-73), and airway hyperresponsiveness with inflammation (Taube, C. et al. It is associated with several respiratory conditions and pulmonary diseases, including those caused by (al, Proc. Natl. Acad. Sci. USA 2006, 103, 8084-8089).

[0249] Factor B is also associated with ischemic stroke (Turek-Jakubowska, A. et al, J. Clin. Med. 2022, 11, 339; and Elvington, A. et al, J. Immunol. 2012, 189(9), 4640-4647), traumatic brain injury (Lindblad, C. et al, Crit. Care 2021, 25, 103; Mallah, K. et al, Acta Neuropathol. Commun. 2021, 9(1), 72; and Alawieh, A. et al, J. Neurosci. 2018, 38(10), 2519-2532), and spinal cord injury (Baldan-Martin, M. et al, Adv. Wound Care (New Rochelle) 2020, 9, 277-294; and Qiao, F. et al. al, Am. J. Pathol. 2010, 177(6), 3061-3070), Toxoplasma infection-induced neuropathy (Shinjyo, N. et al, Front. Immunol. 2020, 11, 603924), prion diseases (Chen, C. et al, Med. Microbiol. Immunol. 2020, 209, 81-94; and Klein, MA et al, Mat. Med. 2001, 7(4), 488-492), multiple sclerosis (Solmaz, I. et al, J. Neuroimmunol. 2020, 348, 577359; and Linzey, M. et al, Front. Immunol. 2022, 13, 924734), amyotrophic lateral sclerosis (Lee, J. Det al, J. Neuroinflammation (2018, 15, 171), depression (Wang, Q. et al, Psychiatry Research 2019, 272, 404-410; and Reddy, PV et al, Clin. Psychopharmacol. Neurosci. 2023, 21(2), 313-319), pain (Wahlen, K. et al, Front. Psychol. 2018, 9, 2400), schizophrenia (Mayilyan, KR, Weinberger, DR and Sim, RBDrug News Perspect. 2008, 21, 200; and Boyajyan, A.It has also been associated with several central nervous system conditions, including autosomal dominant cerebral arterial disease with subcortical infarction and leukoencephalopathy (Unlu, M. et al, Neurosci. Lett. 2000, 282, 149-152), lupus encephalitis (Alexander, J. et al, Eur. J. Immunol. 2007, 37, 1691-1701), and Alzheimer's disease (Morgan, A. et al, Alzheimers Dement. 2019, 15, 776-787; and Strohmeyer, R. et al, Brain Res. Mol. Brain Res. 2000, 81(1-2), 7-18).

[0250] Several cardiovascular diseases, including heart failure (Holt, MF et al, Front. Immunol. 2021, 12, 800978), cardiac remodeling (Yang, Y. et al, Eur. J.Immunol. 2020, 50, 220-233), aortic stenosis (Shahini, N. et al, J.Immunol. 2019, 203, 1973-1980), cardiac metabolic diseases (Coan, PM et al, Hypertension 2017, 70, 624-633), and myocardial ischemia and reperfusion (Chun, N. et al, PLOS ONE 2017, 12, e0179450), have been shown to be associated with factor B.

[0251] Factor B is associated with idiopathic thrombocytopenic purpura (ITP) (Weitz, ICet al, Br. J.Haematol.2023,203(1),96-100; and Shindo, R. et al, Immunol. Med.2023,1-9), paroxysmal nocturnal hemoglobinuria (PNH) (Brodsky, RABlood). 2014, 124, 2804-2811; and Schubart, A. et al, Proc. Natl. Acad. Sci. USA 2019, 116(6), 7926-7931), atypical hemolytic uremic syndrome (Rodriguez de Cordoba, S. et al, Semin. Thromb. Hemost.2014,40,422-430; and Goicoechea de Jorge,E.et It has been suggested that it plays a role in several hematological and blood disorders, including al, Proc. Natl. Acad. Sci. USA 2007, 104(1), 240-245, transplant-associated thrombotic microangiopathy (Sartain, S. et al, Pediatr. Blood Cancer 2020, 67, e28070), occlusive attacks in sickle cell disease, and delayed hemolytic transfusion reaction (DHTR) in individuals with sickle cell disease (Merle, N. Set al, Transfus. Clin. Biol. 2019, 26(2), 116-124; and Chudwin, D. Set al, Clin. Immunol. Immunopathol. 1994, 71(2), 199-202).

[0252] Factor B is associated with pancreatic cancer (Shimazaki, R. et al, Cell Oncol. 2021, 44, 937-950), photocarcinogenesis (Byrne, SNet al, Photochem. Photobiol. Sci. 2015, 14, 801-806), and breast cancer (Suman, S. et al, J. Proteomics). 2016, 148, 183-193), gastroesophageal cancer (Wu, C. et al, Br. J. Cancer 2015, 113, 220-225), head and neck squamous cell carcinoma (Ohshiro, K. et al. al,Int.J.Oncol.2007,30,743-749), and adenoma to carcinoma, and cutaneous squamous cell carcinoma (Riihila, P. et al. It is associated with the pathogenesis of various cancers, including those described in (al, Am.J. Pathol. 2017, 187, 1186-1197).

[0253] The above-mentioned atypical hemolytic uremic syndrome, IgA nephropathy (Zhou, XJ et al, Clin. J. Am. Soc. Nephrol. 2021, 16, 213-224; Rizk, DV et al, Kidney Int. Rep. 2023, 8(5), 968-979; Poppelaars, F. et al, J. Clin. Med. 2021, 10(20), 4715; and Daha, MR et al, J. Nephrol. 2016, 29(1), 1-4), primary membranous nephropathy and membranous nephropathy (Couser, WGClin. J. Am. Soc. Nephrol. 2017, 12, 983-997; and Novartis Investor) Presentation,'Iptacopan (LNP023)update'22 June 2021), C3 glomerulonephritis and C3 glomerulonephritis (C3G) (Barbour, TDet al,Nephrol.Dial.Transplant.2013,28,1685-1693;Zhang,Y.et al,Clin.J.Am.Soc.Nephrol.2012,7,265-274;Pickering,MCet al,Kidney Int.2013,84(6),1079-1089;Zanchi,C.et al,Mol.Immunol.2023,161,25-32;Bombback,ASet al,Kidney Int.Rep.2022,7(10),2150-2159; and Novartis Press Release'Novartis iptacopan meets primary endpoints in Phase II study in rare kidney disease C3 glomerulopathy (C3G)',4 November 2021), immune complex-mediated membranous proliferative glomerulonephritis (IC-MPGN) (Iatropoulos,P. et al,JASoc.Nephrol.2018,29(1),283-294), thrombotic microangiopathy (TMA)-mediated acute kidney injury (AKI) (Guzzo,G. et al,BMC Nephrol.2021,22,252), and nephrosclerosis (Zhang,Y. et al,Nephrol. Dial.Transplant.).2021,36,1222-1233), glomerulosclerosis (Zhang,Y.et al,J.Proteomics 2015,123,89-100), allograft kidney (Jager,NMet al,Front. Immunol.2019,10,2528), autosomal dominant polycystic kidney disease (Su,Z.et al. Several kidney diseases, including Physiol. 2007, 293(2), F555-F564; Peng, Y. et al, Front. Pediatr. 2023, 11, 1137375; and Turnberg, D. et al, J. Immunol. 2006, 177(6), 4094-4102), and post-infectious glomerulonephritis (Sethi, S. et al, Kidney Int., 2013, 83(2), 293-299), as well as Wang, F. et al, Front. Genet. 2021, 12, 690952, have been shown to be associated with factor B.

[0254] Factor B has been suggested to play a role in several metabolic conditions, particularly diabetes-related conditions including gestational diabetes (Shen, Y. et al, Gynecol. Endocrinol. 2022, 38, 158-163), cardiac metabolic diseases (Coan, PM et al, Hypertension, 2017, 70, 624-633), diabetic macular edema and diabetic retinopathy as mentioned above, diabetic nephropathy (Lu, Q. et al, JCI Insight 2021, 6, e147716), and metabolic disorders including diet-induced fatty liver and dyslipidemia (Sadana, P. et al, Int. J. Mol. Sci. 2020, 21, 7472).

[0255] In the reproductive system, factor B is associated with infertility (Sim, YJ, Ryu, AR, and Lee, MYBiotechnol. Appl. Biochem. 2022, 69, 289-295), inflammation during pregnancy (Livson, S. et al, Front. Immunol. 2022, 13, 925630), spontaneous premature birth (Lynch, A et al, Am. J. Obstet. Gynecol. 2008, 199, 354.e1-8), and miscarriage in antiphospholipid antibody syndrome (Breen, KA et al, Thromb. Haemost. 2012, 107(3), 423-429; Salmon, JE et al, Lupus. 2012, 12(7), 535-538; and Salmon, JE et al, Curr. Dir. It has been associated with Autoimmun. 2004, 7, 133-148, pyelonephritis during pregnancy (Soto, E. et al, J. Matern. Fetal Neonatal Med. 2010, 23, 1085-1090), amniotic fluid infection / inflammation (Vaisbuch, E. et al, J. Matern. Fetal Neonatal Med. 2009, 22, 905-916), and pre-eclampsia (Jia, K. et al, Med. Sci. Monit. 2019, 25, 7087-7093; Lynch, A et al, Am. J. Obstet. Gynecol. 2008, 198(4), 385; and Blakey, H. et al, Pregnancy Hypertens. 2023, 32, 43-49).

[0256] Factor B is also associated with dengue fever-related DHF (dengue hemorrhagic fever) and DSS (dengue shock syndrome) (Cabezas-Falcon, S. et al, J. Gen. Virol. 2021, 102, 001547; and Dalrymple, NA et al, J. Virol. 2012, 86(12), 6408-6415), excessive inflammatory complications of severe sepsis (Li, D. et al, Crit. Care Med. 2016, 44, e289-299; and Zou, L. et al, J. Immunol. 2013, 191(11), 5625-5635), fulminant meningococcal sepsis (Brandtzaeg, P. et al, J. Infect. Dis. 1996, 173, 647-655), and leprosy caused by Mycobacterium leprae (El It has been associated with several pathogenic diseases, including Idrissi, NB et al, Clin. Exp. Immunol. 2016, 184(3), 338-346; and El Idrissi, NB et al, Acta Neuropathol. 2015, 129(5), 653-667), and post-infectious glomerulonephritis (Chauvet, S. et al, J. Am. Soc. Nephrol. 2020, 31, 829-840).

[0257] Other diseases, disorders, or conditions in which factor B is known to be associated with or involved include: - Liver diseases, such as chronic hepatitis B (Chen, H. et al, Aliment. Pharmacol. Ther. 2020, 51, 469-478; Seo, T. et al, BMC Med. Genet. 2020, 21(1), 241; and Jiang, D. K. et al, Hepatology, 2015, 62(1), 118-128), acute alcohol-associated hepatitis (Fan, X. et al, Hepatology 2021, 73, 983-997), as well as major bile duct obstruction and viral hepatitis (Potter, B. J. et al, Digestion 1978, 18, 371-383); - Autoimmune pathology, for example, cold agglutinin syndrome (Berentsen, S. Semin. Hematol. 2018, 55, 141-149), ANCA vasculitis (Xiao, H. et al, Am. J. Pathol. 2007, 170, 52-64), IgA vasculitis (Demir, S. et al, Diagnostics (Basel) 2023, 13(10), 1729), lupus nephritis and systemic lupus erythematosus (Kono, DH, Theofilopoulos, AN(2011) Chapter 4-Genetics of Lupus in Mice, in Systemic Lupus Erythematosus (Fifth Edition) (Lahita, RGed.), Academic Press, San Diego; Chen, K. et al, Biomed. Pharmacother. 2022, 153, 113433; and Wilson, MR et al, Clin. Exp. Immunol. 1976, 26(1), 11-20), Shingles syndrome (Larssen, E. et al, SAGE Open Med. 2019, 7, 2050312119850390), myasthenia gravis (Subias, M. et al, J. Immunology 2014, 193, 5567-5575), acquired thrombotic thrombocytopenic purpura (TTP) (Cao, W. et al, Haematologica 2016, 101, 1319-1326), optic nerve myasthenia gravis (Palace, J. et al, Clinical Trial 2021, 47, 102641), ギラン·バレー syndrome (Campbell, CI et al, Brain Commun. 2022, 4 (6), fcac306l and Halstead, SK et al. Brain 2004,127(9),2109-2123); Chronic inflammatory adenocarcinoma polychondrosis (CIDP)(Querol,L.et al,J.Peripher. Nerv. Syst.,2023,28(2),276-285); - Muscle and bone disorders and muscle inflammation (Ghafouri, B. et al, BMC Musculoskelet. Disord. 2016, 17, 206; and Frenette, J. et al, Am. J. Pathol. 2000, 156, 2103-2110), joint inflammation (Krick, EHet al, Clin. Exp. Immunol. 1978, 34, 1-9; and Holers, VM et al, Front. Immunol., 2018, 9, 1057), and arthritis (Assirelli, E. et al, Front. Immunol. 2020, 11, 535010); - Inflammatory bowel disease (Shi, D. et al, J. Hum. Genet. 2020, 65, 241-249); - Primary varicose vein (Shadrina, A. et al, Gene 2018, 659, 93-99); - Anti-lin lipid antibody syndrome (Breen, K.A. et al., Thromb. Haemost. 2012, 107, 423-429; Kim, MY, et al., Ann. Rheum. Dis. 2018, 77(4), 549-555; and Piccoli, V.F. et al., Lupus. 2016, 25(4), 412-417); - Vesicular pemphigoid (Nelson, K.C. et al., J. Clin. Invest. 2006, 116, 2892-2900); - Hemodialysis (Ekdahl, KNet al, Immunol. Rev. 2023, 313(1), 91-103); - Serotonin disease (da Rosa Utiyama, SR et al, Int. J. Immunogenet. 2005, 32, 307-314); - Heat injury (Wan, KC et al., Burns 1998, 24, 241-244); - Suppurative hidradenitis and gangrenous pyoderma (Giamarellos-Bourboulis, EJet al, Br. J. Dermatol. 2020, 183(1), 176-178); - Rhabdomyolysis (Boudhabhay, I. et al, Kidney Int. 2021, 99(3), 581-597); - Non-alcoholic fatty liver disease (NAFLD), including non-alcoholic steatohepatitis (NASH) (Segers, FM et al, PLoS One 2014, 9(10), e110053; and Zhao et al, Front. Immunol. 2022, 13, 1054159); - Gaucher disease (Pandey, MK et al, Nature, 2017, 543(7643), 108-112; and Serfecz, JC et al, Int. J. Mol. Sci. 2021, 22(18), 9912); and - Examples include acquired partial lipodystrophy (Misra, A. et al, Medicine (Baltimore), 2004, 83(1), 18-31, and Sissons, J. Get al, New England Journal of Medicine, 1976, 294(9), 461-465).

[0258] Therefore, any of the diseases, disorders, or conditions listed above may be treated or prevented according to the sixth, seventh, eighth, ninth, tenth, or eleventh aspect of the present invention. Specific examples of diseases, disorders, or conditions that may respond to factor B inhibition and may be treated or prevented according to the sixth, seventh, eighth, ninth, tenth, or eleventh aspect of the present invention include: (i) Eye diseases, disorders or conditions, such as age-related macular degeneration, retinal detachment, Doyne's honeycomb retinal dystrophy (also known as Malattia reventinase) (DHRD / ML), retinal ischemia-reperfusion, non-infectious uveitis, and diabetic retinopathy and diabetic macular edema; (ii) Hematological disorders, conditions, or conditions, such as cold agglutinin disease, paroxysmal nocturnal hemoglobinuria (PNH), atypical hemolytic uremic syndrome, transplant-associated thrombotic microangiopathy, occlusive attacks in sickle cell disease, and delayed hemolytic transfusion reactions (DHTR) in individuals with sickle cell disease; (iii) Renal diseases, disorders or conditions, such as IgA nephropathy, primary membranous nephropathy, dense deposit disease and C3 glomerulopathy (C3G), immune complex-mediated membranoproliferative glomerulonephritis (IC-MPGN), thrombotic microangiopathy (TMA)-mediated acute kidney injury (AKI), malignant nephrosclerosis, glomerulosclerosis, atypical hemolytic uremic syndrome, focal segmental glomerulosclerosis (FSGS), post-infectious glomerulonephritis, allogeneic transplant kidney, and acute kidney injury; (iv) Respiratory diseases, disorders, or conditions, such as inflammatory airway hyperresponsiveness, idiopathic pulmonary fibrosis, and those related to SARS-CoV-2; (v) Disorders, disorders, or conditions of the central nervous system, such as Alzheimer's disease, multiple sclerosis, ischemic stroke, traumatic brain injury, spinal cord injury, amyotrophic lateral sclerosis, schizophrenia, and lupus encephalitis; (vi) Cardiovascular diseases, disorders or conditions, such as heart failure, cardiac remodeling, aortic stenosis, cardiac metabolic diseases, and myocardial ischemia and reperfusion; (vii) Genital disorders, disorders, or conditions, such as pre-eclampsia; (viii) Metabolic disorders, conditions, or conditions, such as complications of type 2 diabetes, including diabetic retinopathy and diabetic nephropathy; (ix) Cancer, for example, pancreatic cancer, photocarcinogenesis, and cutaneous squamous cell carcinoma; (x) Autoimmune diseases, disorders or conditions, such as cold agglutinin disease, ANCA-associated vasculitis, systemic lupus erythematosus including lupus nephritis, myasthenia gravis, celiac disease, neuromyelitis optica, Guillain-Barré syndrome, and acquired thrombotic thrombocytopenic purpura (TTP); (xi) Musculoskeletal disorders, conditions, or pathologies, such as rheumatoid arthritis and osteoarthritis; (xii) Antiphospholipid syndrome; (xiii) Skin diseases, disorders or conditions, such as bullous pemphigoid. (xiv) hemodialysis; and (xv) Any disease in which an individual has been identified by a germline or somatic nonsilent mutation in factor B.

[0259] More typically, a disease, disorder, or condition is (i) Eye diseases, disorders, or conditions; (ii) Blood disorders, conditions, or pathologies; (iii) Renal disease, disorder, or condition; (iv) cancer; or (v) Select from autoimmune diseases, disorders, or conditions.

[0260] In on...

Claims

1. Compound of formula (I): 【Transformation 60】 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof; During the ceremony, R １ is hydrogen; R ２ is selected from hydrogen or a halo group; R ３ is hydrogen or halo, -SO ２ NH ２ , or C １ -C ８ Selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed; R ４ is selected from hydrogen or halo, —OH, —NH ２ , —SO ２ NH ２ , or C １ —C ８ a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group is linear or branched, or is one or more cyclic groups, or may contain them, the hydrocarbyl group may be optionally substituted with one or more halo groups, the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any —S— moiety is optionally substituted with one or two groups independently selected from oxo (═O) and ═NH to form —SO—, —SO ２ —, —S(═NH)—, or —SO(═NH)— moieties may be formed; R ５ is selected from hydrogen or a halo group; R ６ is hydrogen or halo, -R ６０ OR ６０ Selected from the base, where R ６０ C １ -C ４ Alkyl, C ３ -C ４ Cycloalkyl, C １ -C ４ Fluoroalkyl, or C ３ -C ４ Selected from fluorocycloalkyl groups; R ７ and R ８ is hydrogen or fluorocarbon, or C １ -C １２ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- moieties may be formed, provided that the remaining molecule is directly bonded to R ７ or R ８ Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R ７ and R ８ These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R ７ and R ８ Each ring atom of the cyclic group directly bonded to the carbon atom to which the group is bonded is a ring carbon atom, where the cyclic group is a halo, oxo (=O), -OH, -NH ２ , or C １ -C ４ The hydrocarbyl group may be optionally substituted with one or more substituents independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear, branched, cyclic, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R ３ and R ７ , or R ４ and R ７ They came together, C １ -C ６ A saturated or unsaturated hydrocarbilene group is formed, where the hydrocarbilene group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbilene group may be optionally substituted with one or more halo groups, and the hydrocarbilene group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed, however R ８ Provided that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is bonded is a carbon atom; X １０ is N or CR １０ And; X １１ is N or CR １１ And; X １２ is N or CR １２ And; X １３ is N or CR １３ And; X １０ , X １１ , X １２ , and X １３ If two or fewer of them are N; Each R １０ , R １１ , R １２ , and R １３ is hydrogen or halo, -OH, -SH, -NH ２ , -SO ２ NH ２ , or C １ -C １２ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed; R １８ and R １９ is hydrogen or fluorocarbon, or C １ -C １２ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- moieties may be formed, provided that the remaining molecule is directly bonded to R １８ or R １９ Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R １８ and R １９ These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R １８ and R １９ Each ring atom of the cyclic group directly bonded to the carbon atom to which the group is bonded is a ring carbon atom, where the cyclic group is a halo, oxo (=O), -OH, -NH ２ , or C １ -C ４ The hydrocarbyl group may be optionally substituted with one or more substituents independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear, branched, cyclic, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R １８ and R １９ They, together with the carbon atoms to which they are bonded, form a C=O group; and R ２０ and R ２１ are each independently selected from hydrogen or a fluoro group, or R ２０ and R ２１ together with the carbon atom to which they are attached form a C=O group, said compound, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof.

2. R ２ The compound according to claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, selected from a hydrogen, fluoro, chloro, or bromo group.

3. R ３ is hydrogen or fluoro, chloro, bromo, -R ３０ , -CN, -CHO, -COR ３０ , -CO ２ H or -CO ２ R ３０ group selected from, where R ３０ is C １ -C ６ alkyl, C １ -C ６ fluoroalkyl, C ２ -C ６ alkenyl, C ２ -C ６ fluoroalkenyl or -R ３１ group selected from, R ３１ is a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is one or more fluoro, chloro, and / or bromo groups and / or one or two groups R ３２ optionally substituted with, each R ３２ is independently selected from methyl or fluoromethyl groups, provided that the group R ３ containing any optional substituent contains 8 or fewer carbon atoms, the compound according to claim 1 or claim 2, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof.

4. Compound of formula (II): 【Chemistry 61】 or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof; During the ceremony, R １ is hydrogen; R ４ is hydrogen or halo, -OH, -NH ２ , -SO ２ NH ２ , or C １ -C ８ Selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed; R ５ is selected from hydrogen or a halo group; R ６ is hydrogen or halo, -R ６０ OR ６０ Selected from the base, where R ６０ C １ -C ４ Alkyl, C ３ -C ４ Cycloalkyl, C １ -C ４ Fluoroalkyl, or C ３ -C ４ Selected from fluorocycloalkyl groups; R ７ and R ８ is hydrogen or fluorocarbon, or C １ -C １２ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- moieties may be formed, provided that the remaining molecule is directly bonded to R ７ or R ８ Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R ７ and R ８ These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R ７ and R ８ Each ring atom of the cyclic group directly bonded to the carbon atom to which the group is bonded is a ring carbon atom, where the cyclic group is a halo, oxo (=O), -OH, -NH ２ , or C １ -C ４ The hydrocarbyl group may be optionally substituted with one or more substituents independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear, branched, cyclic, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; X １０ is N or CR １０ And; X １１ is N or CR １１ And; X １２ is N or CR １２ And; X １３ is N or CR １３ And; X １０ , X １１ , X １２ , and X １３ If two or fewer of them are N; Each R １０ , R １１ , R １２ , and R １３ is hydrogen or halo, -OH, -SH, -NH ２ , -SO ２ NH ２ , or C １ -C １２ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed; Each R １４ and R １５ is hydrogen or C １ -C ４ Alkyl, C ３ -C ４ Cycloalkyl, C １ -C ４ Fluoroalkyl, or C ３ -C ４ Independently selected from fluorocycloalkyl groups, or R １４ and R １５ These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted; R １６ is hydrogen or fluoro, -SO ２ NH ２ , or C １ -C ８ Selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed; R １７ is hydrogen or fluoro, C １ -C ４ Alkyl, C ３ -C ４ Cycloalkyl, C １ -C ４ Fluoroalkyl, or C ３ -C ４ Selected from fluorocycloalkyl groups; Alternatively, R １６ and R １７ These, together with the carbon atoms to which they are bonded, form a 3- to 6-membered cyclic group, where the cyclic group may be optionally substituted with one or more substituents independently selected from fluoro, -OH, oxo (=O), methyl, or ethyl groups, where any methyl or ethyl group may be optionally fluorosubstituted; Alternatively, R １７ and R ７ , or R ４ and R ７ They came together, C １ -C ６ A saturated or unsaturated hydrocarbilene group is formed, where the hydrocarbilene group may be linear or branched, or consist of one or more cyclic groups, and the hydrocarbilene group may be optionally substituted with one or more halo groups, and the hydrocarbilene group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed, however R ８ Provided that the atom of the hydrocarbylene group directly bonded to the carbon atom to which the group is bonded is a carbon atom; R １８ and R １９ is hydrogen or fluorocarbon, or C １ -C １２ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or one or more cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or more heteroatoms independently selected from N, O, and S in its carbon skeleton, and any -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, resulting in -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- moieties may be formed, provided that the remaining molecule is directly bonded to R １８ or R １９ Provided that any atom in the hydrocarbyl group is a carbon atom; Alternatively, R １８ and R １９ These, together with the carbon atoms to which they are bonded, form a 3- to 10-membered cyclic group, in which case R １８ and R １９ Each ring atom of the cyclic group directly bonded to the carbon atom to which the group is bonded is a ring carbon atom, where the cyclic group is a halo, oxo (=O), -OH, -NH ２ , or C １ -C ４ The hydrocarbyl group may be optionally substituted with one or more substituents independently selected from saturated or unsaturated hydrocarbyl groups, wherein the hydrocarbyl group may be linear, branched, cyclic, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more halo groups, and the hydrocarbyl group may optionally contain one or two heteroatoms independently selected from N and O in its carbon skeleton; Alternatively, R １８ and R １９ They, together with the carbon atoms to which they are bonded, form a C=O group; and R ２０ and R ２１ is independently selected from hydrogen or a fluoro group, or R ２０ and R ２１ The compound, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, which, together with the carbon atoms to which they are bonded, form a C=O group.

5. Each R １４ and R １５ is hydrogen or C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ A group independently selected from a fluoroalkyl or fluorocyclopropyl group, or R １４ and R １５ The compound according to claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein the carbon atoms to which they are bonded together form a cyclopropyl or cyclobutyl group, wherein the cyclopropyl or cyclobutyl group may be optionally substituted with one or more fluoro groups.

6. R １６ is hydrogen or fluoro, -R １６０ , -CN, -CHO, -COR １６０ , -CO ２ H or -CO ２ R １６０ R is selected from the group, but contains any of the substituents. １６ Provided that it contains eight or fewer carbon atoms; R １６０ C １ -C ６ Alkyl, C １ -C ６ Fluoroalkyl, C ２ -C ６ Alkenil, C ２ -C ６ Fluoroalkenyl or -R １６１ Selected from the basis; R １６１ R is a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is one or more fluoro, chloro, and / or bromo groups, and / or one or two groups R １６２ It can be optionally replaced; Each R １６２ is independently selected from methyl or fluoromethyl groups; and R １７ is hydrogen or fluoro, C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ Selected from a fluoroalkyl or fluorocyclopropyl group; Alternatively, R １６ and R １７ The compounds according to claim 4 or 5, or pharmaceutically acceptable salts and / or solvates and / or prodrugs thereof, wherein the carbon atoms to which they are bonded together form a 3- to 5-membered saturated monocyclic group, where the saturated monocyclic group may be optionally substituted with one or more fluoro groups and / or one or two substituents independently selected from oxo(=O) or methyl or fluoromethyl groups.

7. R ４ は、フルオロ、クロロ、ブロモ、-OH、-OR ４１ 、-N(R ４２ ) ２ 、-SO ２ -R ４１ 、-SO ２ -N(R ４２ ) ２ 、-L ４ -OH、-L ４ -OR ４１ 、-L ４ -N(R ４２ ) ２ 、-L ４ -SO ２ -R ４１ 、-L ４ -SO ２ -N(R ４２ ) ２ 、-O-L ４ -OH、-O-L ４ -OR ４１ 、-O-L ４ -N(R ４２ ) ２ 、-O-L ４ -SO ２ -R ４１ 、-O-L ４ -SO ２ -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 -SO ２ -R ４１ 、-NR ４３ -L ４ -SO ２ -N(R ４２ ) ２ 、-SO ２ -L ４ -OH、-SO ２ -L ４ -OR ４１ 、-SO ２ -L ４ -N(R ４２ ) ２ , -R ４４ , -R ４５ or -L ４ -R ４５ R is selected from the group, but contains any of the substituents. ４ Provided that it contains eight or fewer carbon atoms; R ４１ is, -R ４４ or -R ４５ Selected from the basis; Each R ４２ is hydrogen or -R ４４ or -R ４５ Either selected independently of the base, or any two R ４２ However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L ４ L is a linear alkylene group, where the linear alkylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, where L ４ It has a chain length of 1 to 4 atoms, and L ４ is composed of one or two oxo (=O) groups and / or one or more groups R Ｌ４ It can be optionally replaced; Each R Ｌ４ This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any R Ｌ４ and R ４１ , or any R Ｌ４ and any R ４２ These may, together with the atoms to which they are bonded, form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; R ４３ is hydrogen or -R ４４ Selected from the basis; Each R ４４ C １ -C ４ Alkyl or C ３ -C ６ Selected independently from cycloalkyl groups, where C １ -C ４ Alkyl or C ３ -C ６ The cycloalkyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and Each R ４５ is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group is one or more groups independently selected from fluoro, chloro, and bromo, and / or methyl (Me), -CN, -OH, -OMe, -NH ２ , -NHMe, and -NMe ２ R can be optionally substituted with one or two groups independently selected from each of the above, where R ４５ Any methyl group of the compound according to any one of claims 1 to 6, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein any methyl group may be optionally fluorosubstituted.

8. R ５ The compound according to any one of claims 1 to 7, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, selected from a hydrogen, fluoro, chloro, or bromo group.

9. R ６ is chloro, bromo, -R ６０ OR ６０ Selected from the basis; and R ６０ C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ A compound according to any one of claims 1 to 8, selected from a fluoroalkyl or fluorocyclopropyl group, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof.

10. R ７ is hydrogen or fluoro, -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 R is selected from the group, but contains any of the substituents. ７ R contains 12 or fewer carbon atoms and is directly bonded to the remaining molecule. ７ Provided that the atom is a carbon, hydrogen, or fluorine atom; R ７１ is, -R ７３ or -R ７４ Selected from the basis; Each R ７２ is hydrogen or -R ７３ or -R ７４ Either selected independently of the base, or any two R ７２ However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L ７ L is a linear alkylene or alkenylene group, where the linear alkylene or alkenylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton. ７ It has a chain length of 1 to 4 atoms, and L ７ is composed of one or two oxo (=O) groups and / or one or more groups R Ｌ７ It can be optionally replaced; Each R Ｌ７ This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R Ｌ７ These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R Ｌ７ and R ７１ , or any R Ｌ７ and any R ７２ -L is where they are joined together. ７ - COOR ７１ , -L ７ -CO-N(R) ７２ ) ２ , -L ７ -OR ７１ or L ７ -N(R) ７２ ) ２ Together with the atoms of the group, they may form a 3- to 6-membered monocyclic heterocyclic group, where the 3- to 6-membered monocyclic heterocyclic group is saturated or monounsaturated, and the 3- to 6-membered saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Each R ７３ C １ -C ４ Alkyl or C ２ -C ４ Alkenil, C ３ -C ６ Cycloalkyl, or C ５ -C ６ Independently selected from the cycloalkenyl group, where the C １ -C ４ Alkyl, C ２ -C ４ Alkenil, C ３ -C ６ Cycloalkyl, or C ５ -C ６ The cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; Each R ７４ is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group is one or more groups independently selected from fluoro, chloro, and bromo, and / or methyl (Me), -CN, -OH, -OMe, -NH ２ , -NHMe, and -NMe ２ R can be optionally substituted with one or two groups independently selected from each of the above, where R ７４ Any methyl group may be optionally fluorosubstituted; and R ８ is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R ７ and R ８ They come together as base-L ７８ - forms, where -L ７８ - is -CH ２ -CH ２ -ien-CH ２ -CH ２ -CH ２ -ien-CH ２ -NH-CH ２ -ien-CH ２ -O-CH ２ -ien-CH ２ -CH ２ -CH ２ -CH ２ -ien-CH ２ -CH ２ -NH-CH ２ -ien-CH ２ -CH ２ -O-CH ２ -ien-CH ２ -NH-CH ２ -CH ２ - or -CH ２ -O-CH ２ -CH ２ - Selected from the base, where -L ７８ - represents one or more fluoro groups, and / or oxo (=O), -CN, methyl (Me), -OH, -OMe, -NH ２ -NHMe or -NMe ２ The group may be optionally substituted with one or two substituents independently selected from each group, and -L ７８ - Any methyl group of the substituent may be optionally fluorosubstituted, the compound according to any one of claims 1 to 9, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof.

11. X １０ is N or CR １０ And; X １１ CR １１ and X １２ CR １２ is or X １１ CR １１ and X １２ is N, or X １１ is N and X １２ CR １２ And; X １３ is N or CR １３ and X １０ , X １１ , X １２ and X １３ A compound according to any one of claims 1 to 10, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein one or less of the compounds is N.

12. R １１ and R １２ One of the following is present, and fluoro, chloro, bromo, fluoromethyl, methoxy, fluoromethoxy, -CH ２ OH, -CN, -COOH, -CONH ２ or -C(=NH)NH ２ Selected from the basis; and One remaining R １０ , R １１ , R １２ or R １３ is hydrogen or fluoro, chloro, bromo, -OH, -SH, -NH ２ , -SO ２ NH ２ , or C １ -C １０ A hydrocarbyl group is independently selected from saturated or unsaturated hydrocarbyl groups, where the hydrocarbyl group may be linear or branched, or consist of one or two cyclic groups, or contain thereof, and the hydrocarbyl group may be optionally substituted with one or more fluoro, chloro, and / or bromo groups, and the hydrocarbyl 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 -S- moiety may be optionally substituted with one or two groups independently selected from oxo (=O) and =NH, such as -SO-, -SO ２ -, -S (=NH)-, or -SO (=NH)- parts may be formed; and If present, further remaining R １０ , R １１ , R １２ or R １３ Each of the compounds according to any one of claims 1 to 11, or pharmaceutically acceptable salts and / or solvates and / or prodrugs thereof, each independently selected from a hydrogen, fluoro, chloro, or bromo group.

13. R １８ is hydrogen or fluoro, -CN, -COOH, -COOR １８１ , -CO-N(R １８２ ) ２ , -L １８ -COOH, -L １８ - COOR １８１ , -L １８ -CO-N(R) １８２ ) ２ , -L １８ -OH, -L １８ -OR １８１ , -L １８ -N(R) １８２ ) ２ , -R １８３ , -R １８４ or -L １８ -R １８４ R is selected from the group, but contains any of the substituents. １８ R contains 12 or fewer carbon atoms and is directly bonded to the remaining molecule. １８ The condition is that the atom is a carbon, hydrogen, or fluorine atom; and R １９ is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; Alternatively, R １８ and R １９ These, together with the carbon atoms to which they are bonded, form a C=O group; R １８１ is, -R １８３ or -R １８４ Selected from the basis; Each R １８２ is hydrogen or -R １８３ or -R １８４ Either selected independently of the base, or any two R １８２ However, together with the nitrogen atom to which they are bonded, they may form a 3-6 member saturated monocyclic heterocyclic group, where the 3-6 member saturated monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; L １８ is a linear alkylene, alkenylene, or alkynylene group, where the linear alkylene, alkenylene, or alkynylene group optionally contains one or two heteroatoms independently selected from O and N in its carbon skeleton, the linear alkylene, alkenylene, or alkynylene group has a chain length of 1 to 4 atoms, and the linear alkylene, alkenylene, or alkynylene group comprises one or two oxo (=O) groups and / or one or more groups R Ｌ１８ It can be optionally replaced; Each R Ｌ１８ This is independently selected from fluoro, methyl, or fluoromethyl groups; Alternatively, any two R Ｌ１８ These may, together with the atom(s) to which they are bonded, form a 3- to 6-membered monocyclic group, where the 3- to 6-membered monocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Alternatively, any R Ｌ１８ and R １８１ , or any R Ｌ１８ and any R １８２ -L is where they are joined together. １８ - COOR １８１ , -L １８ -CO-N(R) １８２ ) ２ , -L １８ -OR １８１ or -L １８ -N(R) １８２ ) ２ Together with the atoms of the group, they may form a 3- to 6-membered monocyclic heterocyclic group, where the 3- to 6-membered monocyclic heterocyclic group is saturated or monounsaturated, and the 3- to 6-membered monocyclic heterocyclic group may be optionally substituted with one or two oxo (=O) groups and / or one or more fluoro, methyl, and / or fluoromethyl groups; Or, L １８ is a divalent phenyl or a divalent five- or six-membered heteroaryl group, where the divalent phenyl or the divalent five- or six-membered heteroaryl group may be optionally substituted with one or more groups independently selected from fluoro, chloro, bromo, methyl, and fluoromethyl; Each R １８３ C １ -C ４ Alkyl or C ２ -C ４ Alkenil, C ３ -C ６ Cycloalkyl, or C ５ -C ６ Independently selected from the cycloalkenyl group, where the C １ -C ４ Alkyl, C ２ -C ４ Alkenil, C ３ -C ６ Cycloalkyl, or C ５ -C ６ The cycloalkenyl group may be optionally substituted with one or more fluoro groups and / or one or two oxo (=O) groups; and Each R １８４ is independently selected from phenyl or a 5 or 6-membered heteroaryl group, where the phenyl or the 5 or 6-membered heteroaryl group is one or more groups independently selected from fluoro, chloro, and bromo, and / or methyl (Me), -CN, -OH, -OMe, -NH ２ , -NHMe, and -NMe ２ R can be optionally substituted with one or two groups independently selected from each of the above, where R １８４ The methyl group of the compound according to any one of claims 1 to 12, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein the methyl group may be optionally fluorosubstituted.

14. R ２０ and R ２１ The compound according to any one of claims 1 to 13, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, independently selected from a hydrogen or a fluoro group.

15. R １ is hydrogen; R ２ is hydrogen; R ３ The group is selected from hydrogen, fluoro, chloro, or bromo groups; R ４ is fluoro, chloro, bromo, -R ４４ OR ４４ Selected from the basis; R ４４ C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ Selected from a fluoroalkyl or fluorocyclopropyl group; R ５ is hydrogen; R ６ is a methyl or fluoromethyl group; R ７ is hydrogen or fluoro, -L ７１ -COOH, -L ７１ - COOR ７５ , -L ７１ -OH, -L ７１ -OR ７５ or -R ７５ Selected from the basis; -L ７１ - is -CH ２ -, -CHMe- or -CMe ２ - Selected from the group, where any - CH ２ -, -CHMe- or -CMe ２ - The group may be optionally substituted with a fluoropolymer; R ７５ C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ Selected from a fluoroalkyl or fluorocyclopropyl group; R ８ is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; X １０ These are N, C-H, C-F, C-Cl, or C-Br; X １１ is C-CN and X １２ is either C-H, C-F, C-Cl, or C-Br, or X １２ is C-CN and X １１ These are C-H, C-F, C-Cl, or C-Br; X １３ These are N, C-H, C-F, C-Cl, or C-Br; X １０ and X １３ One or fewer of these is N; R １８ and R １９ is independently selected from hydrogen or fluoro, methyl or fluoromethyl groups, or R １８ and R １９ They, together with the carbon atoms to which they are bonded, form a C=O group; and R ２０ and R ２１ The compound according to claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein both are hydrogen.

16. R １ is hydrogen; R ４ is fluoro, chloro, bromo, -R ４４ OR ４４ Selected from the basis; R ４４ C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ Selected from a fluoroalkyl or fluorocyclopropyl group; R ５ is hydrogen; R ６ is a methyl or fluoromethyl group; R ７ is hydrogen or fluoro, -L ７１ -COOH, -L ７１ - COOR ７５ , -L ７１ -OH, -L ７１ -OR ７５ or -R ７５ Selected from the basis; -L ７１ - is -CH ２ -, -CHMe- or -CMe ２ - Selected from the group, where any - CH ２ -, -CHMe- or -CMe ２ - The group may be optionally substituted with a fluoropolymer; R ７５ C １ -C ３ Alkyl, cyclopropyl, C １ -C ３ Selected from a fluoroalkyl or fluorocyclopropyl group; R ８ is selected from hydrogen, fluoro, methyl, or fluoromethyl groups; X １０ These are N, C-H, C-F, C-Cl, or C-Br; X １１ is C-CN and X １２ is either C-H, C-F, C-Cl, or C-Br, or X １２ is C-CN and X １１ These are C-H, C-F, C-Cl, or C-Br; X １３ These are N, C-H, C-F, C-Cl, or C-Br; X １０ and X １３ One or fewer of these is N; R １４ and R １５ Both are hydrogen; R １６ and R １７ Both are hydrogen; R １８ and R １９ is independently selected from hydrogen or fluoro, methyl or fluoromethyl groups, or R １８ and R １９ They, together with the carbon atoms to which they are bonded, form a C=O group; and R ２０ and R ２１ The compound according to claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, wherein both are hydrogen.

17. Compounds selected from the group consisting of the following: 【Transformation 62】 Alternatively, a pharmaceutically acceptable salt and / or solvate and / or prodrug of the selected compound.

18. A pharmaceutical composition comprising a compound according to 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. A compound according to any one of claims 1 to 17, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, or a pharmaceutical composition according to claim 18, for use in pharmaceuticals.

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

21. The aforementioned disease, disorder, or condition is (i) Eye diseases, disorders, or conditions; (ii) Blood disorders, conditions, or pathologies; (iii) Renal disease, disorder, or condition; (iv) Respiratory disease, disorder, or condition; (v) Disorders, disorders, or conditions of the central nervous system; (vi) Cardiovascular disease, disorder, or condition; (vii) Genital disorders, disorders, or conditions; (viiii) Metabolic disorders, conditions, or pathologies; (ix) cancer; (x) Autoimmune disease, disorder, or condition; (xi) Musculoskeletal disorders, disorders, or conditions; (xi) Antiphospholipid antibody syndrome; (xiiii) Skin disease, disorder, or condition (xiv) hemodialysis; or A compound according to claim 19 or 20, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, or a pharmaceutical composition, for use in the treatment or prevention of any disease, disorder, or condition, selected from any disease in which an individual is identified as having a germline or somatic nonsilent mutation in factor (xv)B.

22. The aforementioned disease, disorder, or condition is (i) Acute kidney injury; (ii) Age-related macular degeneration; (iii) Airway hyperresponsiveness accompanied by inflammation; (iv) Alzheimer's disease; (v) Amyotrophic lateral sclerosis; (vi) ANCA vasculitis; (vii) Antiphospholipid antibody syndrome; (viiii) Aortic valve stenosis; (ix) Atypical hemolytic uremic syndrome; (x) Acquired partial lipodystrophy; (xi) Acquired thrombocytopenic purpura; (xi) Bullous pemphigoid; (xiiii) C3 glomerulosis; (xiv) Immune complex-mediated membranoproliferative glomerulonephritis (IC-MPGN); (xv) Cardiac ischemia and reperfusion; (xvi) Cardiac remodeling; (xvii) Cardiac metabolic diseases; (xviiii) Celiac disease; (xix) cold agglutinin disease; (xx) SARs: Respiratory conditions caused by Cov-2; (xxi) diabetic kidney disease; (xxii) diabetic retinopathy; (xxiii) Doyne honeycomb retinal dystrophy (DHRD / ML), also known as Malattia reventinese; (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; (xli) Pancreatic cancer; (xliiii) Paroxysmal nocturnal hemoglobinuria (PNH); (xliv) Photocarcinogenesis; (xlv) Post-infectious glomerulonephritis; (xlvi) preeclampsia; (xlvii) Membranous nephropathy; (xlviii) kidney allograft; (xlix) Retinal detachment; (l) Retinal ischemia-reperfusion; (i) Rheumatoid arthritis; (lii) Schizophrenia; (liiii) Delayed hemolytic transfusion reaction (DHTR) in individuals with sickle cell disease; (liv) Vascular occlusive attacks in sickle cell disease; (lv) Spinal cord injury; (lvi) squamous cell carcinoma; (lvi) Thrombotic microangiopathy (TMA)-mediated acute kidney injury (AKI); (lviii) transplant-associated thrombotic microangiopathy; or A compound according to claim 19 or 20, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, or a pharmaceutical composition, selected from (lix) traumatic brain injury, for use in the treatment or prevention of a disease, disorder or condition.

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

24. A method for synthesizing the compound described in claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) Reacting the compound of formula (SM-1) with the compound of formula (SM-2) to produce the intermediate of formula (It-1): 【Transformation 63】 (ii) The process includes the step of deprotecting the intermediate of formula (It-1) to produce a compound of formula (I) or a pharmaceutically acceptable salt and / or solvate thereof, 【Chemistry 64】 During the ceremony, R Ｐ It is a nitrogen protecting group; R Ｌ is a leaving group; and R １ ~R ８ , R １８ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 1.

25. A method for synthesizing the compound described in claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) Reacting the compound of formula (SM-3) with the compound of formula (SM-2) to produce the intermediate of formula (It-2): 【Transformation 65】 (ii) The process includes the step of deprotecting the intermediate of formula (It-2) to produce a compound of formula (II) or a pharmaceutically acceptable salt and / or solvate thereof, 【Chemical Formula 66】 During the ceremony, R Ｐ It is a nitrogen protecting group; R Ｌ is a leaving group; and R １ , R ４ ~R ８ , R １４ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 4.

26. A method for synthesizing the compound described in claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The process includes the step of subjecting a compound of formula (SM-4) together with a compound of formula (SM-2) to reductive amination to produce a compound of formula (P-4) or a pharmaceutically acceptable salt and / or solvate thereof, 【Transformation 67】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ is a nitrogen protecting group; and R ２ ~R ７ , R １８ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 1.

27. A method for synthesizing the compound described in claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The process includes the step of performing reductive amination of a compound of formula (SM-5) and a compound of formula (SM-2) to produce a compound of formula (P-5) or a pharmaceutically acceptable salt and / or solvate thereof, 【Transformation 68】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ is a nitrogen protecting group; and R ４ ~R ７ , R １４ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 4.

28. A method for synthesizing the compound described in claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The step of reacting a compound of formula (SM-6) with a compound of formula (SM-2) to produce a compound of formula (P-6) or a pharmaceutically acceptable salt and / or solvate thereof, 【Transformation 69】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ It is a nitrogen protecting group; R ７６ is hydrogen or fluoro or C １ -C ４ Selected from saturated hydrocarbyl groups, the saturated hydrocarbyl group may be linear, branched, or cyclic, and may contain one or more fluoro groups, and the saturated hydrocarbyl group may optionally be substituted with one or more fluoro groups, and the saturated hydrocarbyl group may optionally contain a single heteroatom selected from N and O in its carbon skeleton; R ７７ is hydrogen, -OH, -NH ２ , or C １ -C ４ Selected from saturated hydrocarbyl groups, wherein the saturated hydrocarbyl group may be linear, branched, or cyclic, and may contain one or more fluoro groups, and the saturated hydrocarbyl group may optionally be substituted with one or more fluoro groups, and the saturated hydrocarbyl group may optionally contain a single heteroatom selected from N and O in its carbon skeleton; and R ２ ~R ６ , R ８ , R １８ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 1.

29. A method for synthesizing the compound described in claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The step of reacting a compound of formula (SM-7) with a compound of formula (SM-2) to produce a compound of formula (P-7) or a pharmaceutically acceptable salt and / or solvate thereof, 【Transformation 70】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ It is a nitrogen protecting group; R ７６ is hydrogen or C １ -C ４ Selected from saturated hydrocarbyl groups, the saturated hydrocarbyl group may be linear, branched, or cyclic, and may contain one or more fluoro groups, and the saturated hydrocarbyl group may optionally be substituted with one or more fluoro groups, and the saturated hydrocarbyl group may optionally contain a single heteroatom selected from N and O in its carbon skeleton; R ７７ is hydrogen, -OH, -NH ２ , or C １ -C ４ Selected from saturated hydrocarbyl groups, wherein the saturated hydrocarbyl group may be linear, branched, or cyclic, and may contain one or more fluoro groups, and the saturated hydrocarbyl group may optionally be substituted with one or more fluoro groups, and the saturated hydrocarbyl group may optionally contain a single heteroatom selected from N and O in its carbon skeleton; and R ４ ~R ６ , R ８ , R １４ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 4.

30. A method for synthesizing the compound described in claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The step of reducing a compound of formula (SM-8) to a compound of formula (P-8) or a pharmaceutically acceptable salt and / or solvate thereof, 【Chemistry 71】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ It is a nitrogen protecting group; R ２ ~R ８ , R １８ ~R ２１ , and X １０ ~X １３ is as defined in accordance with claim 1; and R １４ ~R １７ The method, as defined in accordance with claim 4.

31. A method for synthesizing the compound described in claim 1, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The step of reacting a compound of formula (SM-9) with a compound of formula (SM-10) to produce a compound of formula (P-9) or a pharmaceutically acceptable salt and / or solvate thereof, 【Chemistry 72】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ It is a nitrogen protecting group; R Ｌ１ is a leaving group; R Ｌ２ is a leaving group; and R ２ ~R ８ , R ２０ ~R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 1.

32. A method for synthesizing the compound described in claim 4, or a pharmaceutically acceptable salt and / or solvate and / or prodrug thereof, (i) The step of reacting a compound of formula (SM-11) with a compound of formula (SM-10) to produce a compound of formula (P-10) or a pharmaceutically acceptable salt and / or solvate thereof, 【Transformation 73】 During the ceremony, R Ｘ is hydrogen or R Ｐ Selected from; R Ｐ It is a nitrogen protecting group; R Ｌ１ is a leaving group; R Ｌ２ is a leaving group; and R ４ ~R ８ , R １４ ~R １７ , R ２０ , R ２１ , and X １０ ~X １３ The method, as defined in accordance with claim 4.

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