MASP-2 inhibitors and methods of use

Abstract

To provide: small molecule synthetic inhibitors of mannan-binding lectin-associated serine protease-2 (MASP-2), including small molecule inhibitors that are selective for MASP-2 over thrombin; compositions thereof; and methods for the manufacture and use thereof.SOLUTION: The present disclosure provides a pharmaceutical composition comprising: a compound having a specific structure or a pharmaceutically acceptable salt thereof; and at least one pharmaceutically acceptable carrier or excipient. The pharmaceutical composition is a compound that is useful in treatment of MASP-2-associated diseases and disorders, and in manufacture of medicaments for treating MASP-2-associated diseases and disorders.SELECTED DRAWING: None

Description

[Technical Field]

[0001] Cross-reference of related applications This application claims the benefits of U.S. Provisional Application No. 62677472, No. 62677538, No. 62677495, and No. 62677514, all filed on 29 May 2018. Each of the aforementioned related applications is incorporated herein by reference in its entirety.

[0002] Description regarding sequence listings The sequence listing relating to this application is provided in text format instead of on copy paper and is incorporated herein by reference. The name of the text file containing the sequence listing is MP_1_0281_PCT_SequenceListing_20190528. The text file is 7KB in size, was created on May 28, 2019, and is currently being submitted via EFS-Web in connection with the filing of this specification.

[0003] field This disclosure generally relates to compositions and methods useful in the field of medicine. More specifically, this disclosure provides MASP-2 small molecule synthesis inhibitors, compositions thereof, and methods for producing and using the same, including small molecule inhibitors that are more selective for mannan-binding lectin-related serine protease 2 (MASP-2) than for thrombin. [Background technology]

[0004] background The complement system plays a role in inflammatory responses and is activated by tissue injury or microbial infection. Strict control of complement activation is necessary to ensure selective targeting of invading microorganisms and avoid self-inflicted injury (Ricklin et al., Nat. Immunol. 11:785-797, 2010 (Non-Patent Literature 1)). It is now widely recognized that the complement system can be activated through three distinct pathways: the classical pathway, the lectin pathway, and the alternative pathway. The classical pathway is typically triggered by a complex composed of host antibodies bound to an exogenous particle (i.e., an antigen), and generally requires prior exposure to the antigen for the generation of a specific antibody response. Because the activation of the classical pathway depends on a prior adaptive immune response by the host, it is part of the adaptive immune system. In contrast, both the lectin pathway and the alternative pathway are unrelated to adaptive immunity and are part of the innate immune system.

[0005] Mannan-binding lectin-associated serine protease 2 (MASP-2) has been shown to be necessary for the function of the lectin pathway, one of the major complement activation pathways (Vorup-Jensen et al., J. Immunol 165:2093-2100, 2000 (Non-Patent Literature 2); Ambrus et al., J Immunol. 170: 1374-1382, 2003 (Non-Patent Literature 3); Schwaeble et al., PNAS 108:7523-7528, 2011 (Non-Patent Literature 4)). Importantly, inhibition of MASP-2 does not appear to interfere with the antibody-dependent classical complement activation pathway, which is a critically important component of the acquired immune response to infectious diseases. As described in U.S. Patent No. 9,011,860 (Patent Document 1) (assigned to Omeros Corporation), incorporated herein by reference, a fully human monoclonal antibody targeting human MASP-2 was generated that binds to human MASP-2 with high affinity, blocks lectin pathway complement activity, and is therefore useful for treating various lectin complement pathway-related diseases and disorders.

[0006] MASP-2-dependent complement activation has been suggested to be involved in the development of numerous acute and chronic disease states. Therefore, there is a need for small molecule compounds suitable for administration to treat patients suffering from MASP-2 complement pathway-related diseases and disorders.

[0007] A protein crucial to mammalian immunity is mannan-binding lectin-associated serine protease 2 (MASP-2), which has been shown to be required for the function of the lectin pathway, one of the major complement activation pathways (Vorup-Jensen et al., J. Immunol 165:2093-2100, 2000 (Non-Patent Literature 2); Ambrus et al., J Immunol. 170: 1374-1382, 2003 (Non-Patent Literature 3); Schwaeble et al., PNAS 108:7523-7528, 2011 (Non-Patent Literature 4)). Inhibition of MASP-2 does not appear to interfere with the antibody-dependent classical complement activation pathway, which is a critically important component of the acquired immune response to infection. Inhibiting human MASP-2 to block lectin pathway complement activity is useful for treating various lectin-complement pathway-related diseases and disorders.

[0008] Because therapeutic compounds and small molecule MASP-2 inhibitors are important for treating various lectin complement pathway-related diseases and disorders, including those that cannot be adequately or efficiently treated with large biological molecule inhibitors, there is a need for methods to identify them. [Prior art documents] [Patent Documents]

[0009] [Patent Document 1] U.S. Patent No. 9,011,860 [Non-patent literature]

[0010] [Non-Patent Document 1] Ricklin et al., Nat. Immunol. 11:785-797, 2010 [Non-Patent Document 2] Vorup-Jensen et al., J. Immunol 165:2093-2100, 2000 [Non-Patent Document 3] Ambrus et al., J Immunol. 170: 1374-1382, 2003 [Non-Patent Document 4] Schwaeble et al., PNAS 108:7523-7528, 2011 [Overview of the project]

[0011] overview This disclosure provides, in particular, compounds of formulas (I-1) and (I-2) or salts thereof: In formula TIFF0007829249000001.tif75128, the variable elements are defined as follows:

[0012] The disclosure also provides a pharmaceutical composition comprising a compound of formula (I-1) or (I-2) or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

[0013] Compounds of formula (I-1) or (I-2) are useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2 related diseases and disorders. The disclosure also provides a method for treating MASP-2 related diseases and disorders, comprising the step of administering a therapeutically effective amount of a compound of formula (I-1) or (I-2) or a salt thereof to a patient.

[0014] This disclosure provides, in particular, compounds of formulas (IIA) and (IIB) or salts thereof: In formula TIFF0007829249000002.tif63128, the variable elements are defined as follows. Various embodiments of the compound of formula (IIA) or (IIB) are also described.

[0015] The disclosure also provides a pharmaceutical composition comprising a compound of formula (IIA) or (IIB) or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

[0016] Compounds of formula (IIA) or (IIB) are useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of pharmaceuticals for the treatment of MASP-2 related diseases and disorders. The disclosure also provides a method for treating MASP-2 related diseases and disorders, comprising the step of administering a therapeutically effective amount of a compound of formula (IIA) or (IIB) or a salt thereof to a patient.

[0017] This disclosure provides, in particular, compounds of formula (III) or salts thereof: In formula TIFF0007829249000003.tif22128, the variable elements are defined as follows. Various embodiments of the compound of formula (III) are also described.

[0018] The disclosure also provides a pharmaceutical composition comprising a compound of formula (III) or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient.

[0019] Compounds of formula (III) are useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2 related diseases and disorders. The disclosure also provides a method for treating MASP-2 related diseases and disorders, comprising the step of administering a therapeutically effective amount of compound (III) or a salt thereof to a patient.

[0020] This disclosure provides, in particular, compounds of formula (IV) or salts thereof: In formula TIFF0007829249000004.tif24128, the variable elements are defined as follows. Various embodiments of the compound of formula (IV) are also described.

[0021] The disclosure also provides a pharmaceutical composition comprising a compound of formula (IV) or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient.

[0022] Compounds of formula (IV) are useful as MASP-2 inhibitors. Compounds of formula (IV) are useful in therapy. Compounds of formula (IV) are useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2 related diseases and disorders. The disclosure also provides a method for treating MASP-2 related diseases and disorders, comprising the step of administering a therapeutically effective amount of compound (IV) or a salt thereof to a patient.

[0023] This disclosure provides, in particular, compounds of formula (VA) or (VB) or salts thereof: In formula TIFF0007829249000005.tif43128, the variable elements are defined below. Various embodiments of the compound of formula (VA) or (VB) are also described.

[0024] The disclosure also provides a pharmaceutical composition comprising a compound of formula (VA) or (VB) or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

[0025] Compounds of formulas (VA) and (VB) are useful as MASP-2 inhibitors. Compounds of formulas (VA) and (VB) are useful in therapy. Compounds of formulas (VA) and (VB) are useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2 related diseases and disorders. The disclosure also provides a method for treating MASP-2 related diseases and disorders, comprising the step of administering a therapeutically effective amount of a compound of formula (VA) or (VB) or a salt thereof to a patient.

[0026] This disclosure provides, in particular, compounds of formula (VIA) or (VIB) or salts thereof: TIFF0007829249000006.tif41128 wherein the variable elements are as defined below. Various aspects of the compounds of formula (VIA) or (VIB) are also described.

[0027] The present disclosure also provides a pharmaceutical composition comprising a compound of formula (VIA) or (VIB) or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient.

[0028] The compounds of formula (VIA) and (VIB) are useful as MASP-2 inhibitors. The compounds of formula (VIA) and (VIB) are useful in therapy. The compounds of formula (VIA) and (VIB) are useful in the treatment of MASP-2 related diseases and disorders and in the manufacture of medicaments for treating MASP-2 related diseases and disorders. The present disclosure also provides a method of treating MASP-2 related diseases and disorders, the method comprising administering to a patient a therapeutically effective amount of a compound of formula (VIA) or (VIB) or a salt thereof.

[0029] The present disclosure particularly provides a compound of formula (VIIA) or (VIIB) or a salt thereof: TIFF0007829249000007.tif69128 wherein the variable elements are as defined below. Various aspects of the compounds of formula (VIIA) or (VIIB) are also described.

[0030] The present disclosure also provides a pharmaceutical composition comprising a compound of formula (VIIA) or (VIIB) or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient.

[0031] The compounds of formula (VIIA) and (VIIB) are useful as MASP-2 inhibitors. The compounds of formula (VIIA) and (VIIB) are useful in therapy. The compounds of formula (VIIA) and (VIIB) are useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of medicaments for treating MASP-2 related diseases and disorders. The present disclosure also provides a method of treating MASP-2 related diseases and disorders, the method comprising administering to a patient a therapeutically effective amount of a compound of formula (VIIA) or (VIIB) or a salt thereof.

[0032] The present disclosure provides, in particular, small molecule compounds exhibiting MASP-2 inhibitory activity, especially for therapeutic use. Small molecule compounds exhibiting MASP-2 inhibitory activity interact with the MASP-2 serine protease domain in an enzyme-inhibitor complex by a plurality of intermolecular interactions. In certain aspects, the small molecule is described with complete specificity and description by the number and type of intermolecular interactions within the MASP-2 binding site, using an experimentally derived set of rules. The inhibitor follows one or more interaction rules.

[0033] In certain aspects, the present disclosure provides a small molecule compound exhibiting MASP-2 inhibitory activity for therapeutic use, the compound exhibiting one or more of the following interactions (a)-(e), for example one, two, three, four, or five: (a) binds to one or more of PRO 606, ASP 627, SER 628, ARG 630, SER 633, SER 654, GLY 656, SER 657, CYS 660, and GLN 665 in MASP-2 by hydrogen bonding; (b) binds to one or more of ASP 627 and ARG 630 in MASP-2 by ionic interaction or electrostatic interaction or hydrogen bonding; (c) Water molecules in MASP-2 interact with one or more of the following in MASP-2: TYR 602, TYR 607, ASP 627, SER 628, SER 657, ASN 659, GLU 662, TRP 655, GLY 656, CYS 660, GLN 665, TYR 666, VAL 668, and ARG 630; (d) Interacting with one or more of PHE 529, TYR 607, and TRP 655 in MASP-2 via π-π interactions; and (e) Interact with one or more of the following in MASP-2 via van der Waals contact: ALA 468, ALA 469, HIS 483, ASP 526, ALA 527, GLY 528, PHE 529, LEU 575, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, GLY 631, ASP 632, SER 633, GLY 634, GLY 635, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLN 665, GLY 667, and TYR 669.

[0034] In some embodiments, this compound is not an endogenous MASP-2 ligand.

[0035] In some embodiments, this compound is a synthetic small molecule MASP-2 inhibitor.

[0036] In some embodiments, this compound inhibits MASP-2 more selectively than thrombin.

[0037] Various embodiments of the compound as defined by interaction rules are described. This disclosure provides compositions comprising the compound or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient. The compound is useful as a MASP-2 inhibitor. The compound is useful in therapeutic applications. The compound is useful in the treatment of MASP-2-related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2-related diseases and disorders. This disclosure also provides a method for treating MASP-2-related diseases and disorders, comprising the step of administering to a patient a therapeutically effective amount of the compound as defined by the interaction rules described herein.

[0038] This disclosure provides, in particular, compounds of formula (VIII) or salts thereof: In formula TIFF0007829249000008.tif30128, the elements of the formula may represent the values ​​described below. Various embodiments of the compound of formula (VIII) are also described. The disclosure also provides a pharmaceutical composition comprising the compound of formula (VIII) or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient. The compound of formula (VIII) is useful as a MASP-2 inhibitor. The compound of formula (VIII) is useful in therapy. The compound of formula (VIII) is useful in the treatment of MASP-2 related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2 related diseases and disorders. The disclosure also provides a method for treating MASP-2 related diseases and disorders, comprising the step of administering a therapeutically effective amount of the compound of formula (VIII) or a salt thereof to a patient.

[0039] This disclosure provides a pharmacophore model for describing small molecule compounds, including synthetic compounds that inhibit MASP-2, and compounds that are specifically defined with reference to the pharmacophore model.

[0040] In some embodiments, compounds active as MASP-2 inhibitors may include one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve, thirteen, fourteen, fifteen, sixteen, seventeen, eighteen, nineteen, twenty, twenty, twenty-one, or twenty-two of the pharmacophore elements listed in Table 1, preferably a combination of three, four, five, six, seven, eight, nine, ten, eleven, twelve, thirteen, or fourteen of the pharmacophore elements. In some embodiments, the compound may have pharmacophore elements corresponding to the pharmacophore elements listed in Table 1, where the (x, y, z) coordinates of the pharmacophore elements are within four standard deviations, preferably within three standard deviations, more preferably within two standard deviations, and most preferably within one standard deviation, as listed in Table 1.

[0041] In some cases, (a) S1 pharmacophore group comprising CA1 and N1 pharmacophore elements or CA1 and C5 pharmacophore elements; and / or (b) S2 pharmacophore group containing H4 and O2 pharmacophore elements; and / or (c) S3 pharmacophore group containing a C2 pharmacophore element and an N2 or H3 pharmacophore element Includes combinations of pharmacophore elements, C2 and C5 are hydrophobic groups; CA1 is an aromatic ring; H3 and H4 are hydrogen bond donors; N1 and N2 are cationic groups; O2 is a hydrogen bond acceptor; Compounds are provided in which C2, C5, CA1, H3, H4, N1, N2, and O2 have coordinates within the ranges shown in Table 3, Table 4, or Table 5 below.

[0042] In some cases, (a) S1 pharmacophore group containing CA1 and N1 pharmacophore elements or CA1 and C5 pharmacophore elements; (b) S2 pharmacophore group containing H4 and O2 pharmacophore elements; and (c) S3 pharmacophore group containing a C2 pharmacophore element and an N2 or H3 pharmacophore element A compound is provided that contains a combination of pharmacophore elements including the following.

[0043] Various embodiments of small molecule compounds defined by a pharmacophore model are described. This disclosure provides compositions comprising the compound or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier or excipient. The compound is useful as a MASP-2 inhibitor. The compound is useful in therapeutic applications. The compound is useful in the treatment of MASP-2-related diseases and disorders, and in the manufacture of pharmaceuticals for treating MASP-2-related diseases and disorders. This disclosure also provides a method for treating MASP-2-related diseases and disorders, comprising the step of administering a therapeutically effective amount of the compound defined by a pharmacophore model to a patient.

[0044] This disclosure also provides small molecule compounds exhibiting MASP-2 inhibitory activity, which interact with the MASP-2 binding site and are defined by reference to “binding rules” or “rule sets” derived using a virtual docking model between the crystallographically derived MASP-2 enzyme cocrystal structure and the binding site within the MASP-2 enzyme. In certain contexts, the amino acids of the MASP-2 binding site and each of their atoms for which the small molecule MASP-2 inhibitor is available are described. By using various compounds and their intermolecular interactions, it becomes possible to design a set of “binding rules” or “rule sets” through which the MASP-2 inhibitor is specifically described.

[0045] In certain aspects, small molecule MASP-2 inhibitors are described by a set of rules. Compounds exhibiting MASP-2 inhibitory activity interact with the binding site of MASP-2 as an enzyme-inhibitor complex through multiple intermolecular interactions. In certain aspects, the molecules are described with complete specificity and full description by the number and type of in silico intermolecular interactions between the atoms of the MASP-2 amino acid residues at the binding site and the atoms of the inhibitor molecule. These rules are derived experimentally using a virtual docking model of the crystallographically derived MASP-2 enzyme co-crystal structure and the binding site within the MASP-2 enzyme. In certain cases, a set of rules can be generated using multiple MASP-2 enzyme-inhibitor models-for example, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30, or more protein models.

[0046] In some embodiments, the disclosure provides a compound having MASP-2 inhibitory activity, wherein the compound interacts with a binding site, and the interaction is one or more of (a)-(e): (a) interacting with one or more amino acid residues in the binding site of MASP-2 (SEQ ID NO: 1) by hydrogen bonding; (b) interacting in the binding site of SEQ ID NO: 1 by ionic or electrostatic interactions or hydrogen bonding; (c) interacting in the binding site of SEQ ID NO: 1 by water molecules; (d) interacting with one or more amino acid residues in the binding site of SEQ ID NO: 1 by π-π interactions; and / or (e) interacting with one or more amino acid residues in the binding site of SEQ ID NO: 1 by van der Waals contacts; wherein the compound is not an endogenous ligand or substrate.

[0047] In certain situations, this compound exhibits one, two, three, four, or five of the interactions (a) to (e).

[0048] In another aspect, the present disclosure relates to a method for identifying small molecules capable of inhibiting MASP-2, (a) A step of screening a small molecule library using in silico docking for candidate small molecules selectively identified for their ability to target and bind to MASP-2 at the binding site of the MASP-2 model; and (b) Testing / evaluating the candidate agents identified in step (a) through one or more in vitro assays for their ability to target and bind to the MASP-2 binding site, thereby identifying small molecules capable of inhibiting MASP-2. Methods including To provide.

[0049] In certain contexts, candidate small molecules contain a unique chemical scaffold identified in step (b) and are optimized with respect to their ability to inhibit MASP-2.

[0050] [Invention 1001] Small molecule compounds exhibiting MASP-2 inhibitory activity for therapeutic use in the treatment of MASP-2-related diseases or disorders, wherein the following interactions (a) to (e): (a) Binding to one or more of the following in MASP-2 via H bonds: PRO 606, ASP 627, SER 628, ARG 630, SER 633, SER 654, GLY 656, SER 657, CYS 660, and GLN 665; (b) Bonding to one or more of ASP 627 and ARG 630 in MASP-2 by ionic interaction, electrostatic interaction, or hydrogen bonding; (c) Water molecules in MASP-2 interact with one or more of the following in MASP-2: TYR 602, TYR 607, ASP 627, SER 628, SER 657, ASN 659, GLU 662, TRP 655, GLY 656, CYS 660, GLN 665, TYR 666, VAL 668, and ARG 630; (d) Interacting with one or more of PHE 529, TYR 607, and TRP 655 in MASP-2 via π-π interactions; and (e) Interacting with one or more of the following in MASP-2 via van der Waals contact: ALA 468, ALA 469, HIS 483, ASP 526, ALA 527, GLY 528, PHE 529, LEU 575, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, GLY 631, ASP 632, SER 633, GLY 634, GLY 635, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLN 665, GLY 667, and TYR 669 Show one or more of the following: It is not an endogenous MASP-2 ligand. compound. [Invention 1002] Small molecule compounds exhibiting MASP-2 inhibitory activity for therapeutic use in the treatment of MASP-2-related diseases or disorders, wherein the following interactions (a) to (e): (a) Binding to one or more of ASP 627, SER 628, SER 654, GLY 656, GLN 665, and SER 657 in MASP-2 via H bonds; (b) Bonded to ASP 627 in MASP-2 by ionic interaction, electrostatic interaction, or hydrogen bonding; (c) Water molecules in MASP-2 interact with one or more of the following in MASP-2: ASP 627, GLN 665, SER 657, ASN 659, SER 628, GLU 662, VAL 668, TYR 607, TYR 602, and ARG 630; (d) Interacting with one or more of PHE 529, TYR 607, and TRP 655 in MASP-2 via π-π interactions; and (e) Interacting with one or more of the following in MASP-2 via van der Waals contact: HIS 483, PHE 529, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, SER 633, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLN 665, GLY 667, and TYR 669 Show one or more of the following: It is not an endogenous MASP-2 ligand. compound. [Invention 1003] A compound of the present invention 1001 or 1002 that exhibits one, two, three, four, or five of the interactions (a) to (e). [Invention 1004] A compound according to any of the invention 1001 to 1003, which is bonded by an H bond to one or more of PRO 606, ASP 627, SER 628, SER 633, SER 654, GLY 656, SER 657, CYS 660, and GLN 665 in MASP-2. [Invention 1005] A compound according to any of the present invention 1001 to 1004, which is bonded by an H bond to one or more of ASP 627, SER 628, SER 654, GLY 656, GLN 665, and SER 657 in MASP-2. [Invention 1006] A compound according to any of the invention 1001 to 1005, which is bonded by 1 to 10 H bonds. [Invention 1007] A compound according to any of the present invention 1001 to 1006, wherein the compound is bonded to SER 654 and GLY 656 by three H bonds, and two H bonds to GLY 656 are present in MASP-2. [Invention 1008] A compound according to any of the present invention 1001 to 1007, which is bonded to one or both of ASP 627 and ARG 630 in MASP-2 by ionic interaction, electrostatic interaction, or hydrogen bonding. [Invention 1009] A compound according to any of the invention 1001 to 1008, which is bonded to ASP 627 in MASP-2 by ionic interaction, electrostatic interaction, or hydrogen bonding. [Invention 1010] A compound according to any of the present invention 1001 to 1007 that does not bind to ASP 627 and ARG 630 in MASP-2 by ionic interaction. [Invention 1011] A compound according to any of the present invention 1001 to 1007 that does not bind to ASP 627 in MASP-2 by ionic interaction. [Invention 1012] A compound according to any of the invention 1001 to 1011, which is bonded by a water molecule in MASP-2 to one or more of TYR 602, TYR 607, ASP 627, SER 628, SER 657, ASN 659, GLU 662, TRP 655, GLY 656, CYS 660, GLN 665, TYR 666, VAL 668, and ARG 630 in MASP-2. [Invention 1013] A compound according to any of the invention 1001 to 1012, which is bonded to one or more of ASP 627, GLN 665, SER 657, ASN 659, SER 628, GLU 662, VAL 668, TYR 607, TYR 602, and ARG 630 by a water molecule in MASP-2. [Invention 1014] A compound according to any of the invention 1001 to 1013, which is bonded by 1 to 20 water molecules in MASP-2. [Invention 1015] A compound according to any of the invention 1001 to 1014, which is bonded by 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, or 17 water molecules in MASP-2. [Invention 1016] A compound according to any of the present invention 1001 to 1015, which interacts with one or more of PHE 529, TYR 607, and TRP 655 in MASP-2 by π-π interaction. [Invention 1017] Van der Waals contact affected MASP-2, specifically ALA 468, ALA 469, HIS 483, ASP 526, ALA 527, GLY 528, PHE 529, LEU 575, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, GLY 631, ASP 632, SER 633, GLY 634, GLY 635, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLN 665, GLY 667, and TYR A compound according to any of the present invention 1001 to 1016 that interacts with one or more of 669. [Invention 1018] A compound according to any of the present invention 1001 to 1017, which interacts with one or more of HIS 483, PHE 529, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, SER 633, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLN 665, GLY 667, and TYR 669 in MASP-2 by van der Waals contact. [Invention 1019] Formula (VIII): A compound of any of the present invention 1001 to 1018 having TIFF0007829249000009.tif30128. [The present invention 1020] The compound of the present invention 1019, wherein M1 is a member selected from the group consisting of: TIFF0007829249000010.tif28146 wherein each R 5 is independently a member selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, amino, C1-C6 alkylamino, and halo; each n is an independently selected integer from 0 to 4; R 7 is a member selected from the group consisting of hydrogen, hydroxyl, and C1-C6 alkyl; R 8 is a member selected from the group consisting of hydrogen and C1-C6 alkyl. [The present invention 1021] The compound of the present invention 1019 or 1020, wherein M5 has the following formula: TIFF0007829249000011.tif15128 wherein R 5 is a member selected from the group consisting of C3-C7 cycloalkyl, C4-C8 cycloalkylalkyl, heteroaryl, and C7-C 12 arylalkyl or heteroarylalkyl (having 0 to 3 R 13 substituents); or alternatively, R[[ID=3P]] 5 and R 6 together form a heterocyclic ring having 0 to 3 R 13 substituents; R 6 is a member selected from the group consisting of hydrogen, C\(_1\)-C6 alkyl, C3-C7 cycloalkyl, carboxy(C1-C6 alkyl), C7-C 12 arylalkyl or heteroarylalkyl (having 0 to 3 R 13 substituents), amino(C1-C8 alkyl), and amido(C1-C8 alkyl); or alternatively, R 6 and R 5 together form a heterocyclic ring having 0 to 3 R 13 substituents. [Invention 1022] Formula (VIIIA): A compound according to any of the present invention 1001 to 1021, having TIFF0007829249000012.tif32128. [Invention 1023] A compound according to any of the present invention 1001 to 1022, having a molecular weight of approximately 300 g / mol to approximately 600 g / mol. [Invention 1024] A compound according to any of the invention 1001 to 1023, wherein the Ki for MASP-2 is lower than that for thrombin. [Invention 1025] A pharmaceutical composition comprising any compound of the present invention 1001 to 1024 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1026] Small molecule compounds for use in the treatment of MASP-2 related diseases or disorders, (a) S1 pharmacophore group containing CA1 and N1 pharmacophore elements or CA1 and C5 pharmacophore elements; (b) S2 pharmacophore group containing H4 and O2 pharmacophore elements; and (c) S3 pharmacophore group containing a C2 pharmacophore element and an N2 or H3 pharmacophore element Includes combinations of pharmacophore elements, C2 and C5 are hydrophobic groups; CA1 is an aromatic ring; H3 and H4 are hydrogen bond donors; N1 and N2 are cationic groups; O2 is a hydrogen bond acceptor; Compounds in which C2, C5, CA1, H3, H4, N1, N2, and O2 are located within the coordinate ranges shown in Table 3. [Invention 1027] The compound of Invention 1026, wherein C2, C5, CA1, H3, H4, N1, N2, and O2 are coordinates within the ranges shown in Table 4. [Invention 1028] Compounds of the present invention 1026 or 1027, wherein C2, C5, CA1, H3, H4, N1, N2, and O2 have coordinates within the ranges shown in Table 5. [Invention 1029] A compound according to any of invention 1026 to 1028, wherein the S1 pharmacophore group contains CA1 and N1 pharmacophore elements. [Invention 1030] The compound of the present invention 1029, wherein the S1 pharmacophore group further contains a C3 pharmacophore element, and the C3 is a hydrophobic group, with coordinates within the range shown in Table 6. [Invention 1031] The compound of the present invention 1030, wherein C3 represents a coordinate within the range shown in Table 7. [Invention 1032] The compound of the present invention 1031, wherein C3 is located within the coordinate range shown in Table 8. [Invention 1033] A compound according to any of invention 1026 to 1032, wherein the S1 pharmacophore group contains CA1 and C5 pharmacophore elements. [Invention 1034] The S1 pharmacophore group further comprises one, two, or three pharmacophore elements selected from the group consisting of C7, H2, and O4. C7 is a hydrophobic group; H2 is a hydrogen bond donor; O4 is a hydrogen bond receptor; Compound 1033 of the present invention, wherein C7, H2, and O4 are coordinates within the ranges shown in Table 9. [Invention 1035] Compound 1034 of the present invention, wherein C7, H2, and O4 are coordinates within the ranges shown in Table 10. [Invention 1036] Compound 1035 of the present invention, wherein C7, H2, and O4 are coordinates within the ranges shown in Table 11. [Invention 1037] A compound according to any of invention 1033 to 1036, wherein the S1 pharmacophore group contains a C7 pharmacophore element. [Invention 1038] A compound according to any of invention 1033 to 1037, wherein the S1 pharmacophore group contains an H2 pharmacophore element. [Invention 1039] A compound according to any of invention 1033 to 1038, wherein the S1 pharmacophore group contains an O4 pharmacophore element. [Invention 1040] The S2 pharmacophore group further comprises one or two pharmacophore elements selected from the group consisting of CA6 and O1. CA6 is an aromatic ring; O1 is a hydrogen bond acceptor; A compound according to any of the present invention 1026 to 1039, wherein CA6 and O1 have coordinates within the range shown in Table 12. [Invention 1041] Compound 1040 of the present invention, wherein CA6 and O1 are coordinates within the ranges shown in Table 13. [Invention 1042] Compound 1041 of the present invention, wherein CA6 and O1 are coordinates within the range shown in Table 14. [Invention 1043] A compound according to any of invention 1040 to 1042, wherein the S1 pharmacophore group contains a CA6 pharmacophore element. [Invention 1044] A compound according to any of invention 1040 to 1043, wherein the S1 pharmacophore group contains an O1 pharmacophore element. [Invention 1045] A compound according to any of invention 1026 to 1044, wherein the S3 pharmacophore group contains C2 and N2 pharmacophore elements. [Invention 1046] The compound of the present invention 1045, wherein the S3 pharmacophore group further contains an H3 pharmacophore element. [Invention 1047] Further containing an S4 pharmacophore group; The S4 pharmacophore group contains a C4, CA2, CA4, or CA5 pharmacophore element; C4 is a hydrophobic group; CA2, CA4, and CA5 are aromatic rings; A compound of any of the present invention 1026 to 1046, wherein C4, CA2, CA4, and CA5 have coordinates within the range shown in Table 15. [Invention 1048] Compound 1047 of the present invention, wherein C4, CA2, CA4, and CA5 have coordinates within the ranges shown in Table 16. [Invention 1049] Compound 1048 of the present invention, wherein C4, CA2, CA4, and CA5 have coordinates within the ranges shown in Table 17. [Invention 1050] A compound from any of the inventions 1047 to 1049, wherein the S4 pharmacophore group contains C4. [Invention 1051] A compound from any of the present inventions 1047 to 1050, wherein the S4 pharmacophore group contains CA2. [Invention 1052] The S4 pharmacophore group further comprises one, two, three, or four additional pharmacophore elements selected from the group consisting of C6, C7, CA4, and CA5. C6 and C7 are hydrophobic groups; CA4 and CA5 are aromatic rings; Compound 1051 of the present invention, wherein C6, C7, CA4, and CA5 are coordinates within the ranges shown in Table 18. [Invention 1053] Compound 1052 of the present invention, wherein C6, C7, CA4, and CA5 are coordinates within the ranges shown in Table 19. [Invention 1054] Compound 1053 of the present invention, wherein C6, C7, CA4, and CA5 have coordinates within the ranges shown in Table 20. [Invention 1055] A compound according to any of invention 1047 to 1054, wherein the S4 pharmacophore group contains a C6 pharmacophore element. [Invention 1056] A compound according to any of invention 1047 to 1055, wherein the S4 pharmacophore group contains a C7 pharmacophore element. [Invention 1057] A compound according to any of invention 1047 to 1056, wherein the S4 pharmacophore group contains a CA4 pharmacophore element. [Invention 1058] A compound according to any of invention 1047 to 1057, wherein the S4 pharmacophore group contains a CA5 pharmacophore element. [Invention 1059] A compound of any of the present invention 1026 to 1058, further comprising an RM pharmacophore group; wherein the RM pharmacophore group comprises a CA3 pharmacophore element, and CA3 is an aromatic ring exhibiting coordinates within the range shown in Table 21. [Invention 1060] Compound 1059 of the present invention, wherein CA3 has coordinates within the range shown in Table 22. [Invention 1061] Compound 1060 of the present invention, wherein CA3 has coordinates within the range shown in Table 23. [Invention 1062] The RM pharmacophore group further comprises one or two additional pharmacophore elements selected from the group consisting of H1 and O3. H1 is a hydrogen bond donor; O3 is a hydrogen bond acceptor; A compound according to any of the inventions 1059 to 1061, wherein H1 and O3 have coordinates within the ranges shown in Table 24. [Invention 1063] Compound 1062 of the present invention, wherein H1 and O3 are coordinates within the ranges shown in Table 25. [Invention 1064] Compound 1063 of the present invention, wherein H1 and O3 are coordinates within the ranges shown in Table 26. [Invention 1065] A compound according to any of invention 1062 to 1064, wherein the RM pharmacophore group contains H1. [Invention 1066] A compound according to any of invention 1062 to 1065, wherein the RM pharmacophore group contains O3. [Invention 1067] A pharmaceutical composition comprising any compound from invention 1026 to 1066 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1068] Compounds of formula (I-1) or their salts: TIFF0007829249000013.tif31128In formula, Cy 1A is either non-substituted or substituted C 6~10 It is an aryl or unsubstituted or substituted 5-10 member heteroaryl; Cy 1A The ring atoms of the 5-10 membered heteroaryl that form the Cy 1A Substitution C that forms 6~10 Aryl or substituted 5-10 member heteroaryls are R Cy1A , halogen, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 Rd11 、 S(O)R b11 、 S(O)NR c11 R d11 、 S(O)₂R b11 、 NR c11 S(O)₂R b11 、 S(O)₂NR c11 R d11 、 and substituted with 1, 2, 3, 4, or 5 substituents each independently selected from oxo; Each R Cy1A is independently selected from C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 6~10 aryl, 5- to 10-member heteroaryl, C 3~10 cycloalkyl, and 4- to 10-member heterocycloalkyl, and the ring atoms of the 5- to 10-member heteroaryl or 4- to 10-member heterocycloalkyl forming R Cy1A consist of carbon atoms and 1, 2, 3, or 4 heteroatoms selected from O, N, and S, and each C Cy1A alkyl, C 1~6 alkenyl, or C 2~6 alkynyl forming R 2~6 is independently unsubstituted or substituted with halogen, CN, OR a11 、 SR a11 、 C(O)R b11 、 C(O)NR c11 R d11 、 C(O)OR a11 、 OC(O)R b11 、 OC(O)NR c11 R d11 、 NR c11 R d11 、 NR c11 C(O)R b11 、 NR c11 C(O)NR c11 R d11 、 NR c11 C(O)OR a11 、 C(=NR e11 )NR c11 R d11 、 NR c11 C(=NR e11 )NR c11 ​d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo, R Cy1A Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11, and are substituted with one, two, or three substituents independently selected from the oxo; R 11 is H, or C 1~6 Alkyl, C 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 It is alkyl, R 11 C that forms 1~6 Alkyls are either unsubstituted or contain halogens, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo, R 11 C that forms 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 Alkyl is either unsubstituted or C 1~6 Alkyl, C 2~6 Alkenil, C 2~6Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R 12 is H or C 1~6 It is alkyl; or, R 11 and R 12 These, together with the groups to which they are bonded, form a 4-6 membered heterocycloalkyl ring; A 11 CR 13 R 15 or N; Each R 13 Cy 1B , (CR 13A R 13B ) n3 Cy 1B , (C 1~6 Alkilen)Cy 1B , (C2~6 Alkenylene) Cy 1B , (C 2~6 Alkinylene)Cy 1B , or OCy 1B And R 13 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 The alkylylene component is either unsubstituted or contains halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 Substituting with one, two, three, four, or five substituents independently selected from the group consisting of , and oxo; Each R 14 H and C are independent of each other. 1~6 Selected from alkyl groups; R 15 H, R 13 , C 1~6 Selected from alkyl and OH; R bonded to an adjacent carbon atom 14R is bonded to pairs of groups or to adjacent carbon atoms. 14 Base and R 15 The pair with the base is the other R 14 Independent of the existence of, together with, R 14 pairs of groups or R 14 Base and R 15 The bond may be replaced by a bond connecting the adjacent carbon atom to which the group is bonded, thereby connecting the adjacent carbon atoms by a double bond; or, R bonded to the same carbon atom 14 R groups bonded to each other, or to the same carbon atom 13 Base and R 15 The pair with the base is the other R 14 Independent of the existence of R 14 pairs of groups or R 13 Base and R 15 The pair with the group forms a spirocondensation with the carbon atom it is bonded to. 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring may be formed, and the ring atoms of the formed 4-10 membered heterocycloalkyl ring consist of a carbon atom and one, two, or three heteroatoms selected from O, N, and S, and the spirocondensation C formed 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring is a halogen, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NRc11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and may be further substituted with one, two, or three substituents independently selected from the oxo; or, R bonded to an adjacent carbon atom 14 R is bonded to pairs of groups or to adjacent carbon atoms. 14 Base and R 15 The pair with the base is the other R 14 Independent of the existence of R 14 pairs of groups or R 14 Base and R 15 It condenses together with the adjacent carbon atom to which it is bonded with the group. 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring may be formed, and the ring atoms of the formed 4-10 membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the formed condensation C 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring is a halogen, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 Rd11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and may be further substituted with one, two, or three substituents independently selected from the oxo; or, Four R atoms bonded to two adjacent carbon atoms 14 A group of R groups, or two R groups bonded to two adjacent carbon atoms 14 Base and 1 R 13 Base and 1 R 15 The group of elements is other R 14 Independent of the existence of the four R 14 A group of elements or two R 14 Base and 1 R 13 Base and 1 R 15 The group of atoms combines with the two adjacent carbon atoms to which it is bonded, forming a condensed C 6~10 Aryl ring or 5-10 membered heteroaryl ring, C 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring may be formed, and the ring atoms of the formed 5-10 membered heteroaryl ring or 4-10 membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the formed condensation C 6~10 Aryl ring or 5-10 membered heteroaryl ring, C 3~10 A cycloalkyl ring, or a 4- to 10-membered heterocycloalkyl ring, is a halogen, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)Rb11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and may be further substituted with one, two, or three substituents independently selected from the oxo; n1 is either 1 or 2; n2 is 0, 1, or 2; However, the sum of n1 and n2 is 1, 2, or 3; However, if n1 is 1 or n2 is 0, A 11 CR 13 R 15 and; n3 is 0, 1, or 2; Each R 13A H or C 1~6 It is alkyl; Each R 13B H or C 1~6 It is alkyl; or, R bonded to the same carbon atom 13A and R 13B is any other R 13A base and R 13BOriginally independent, yet united - (CH2) 2~5 - may be formed, thereby forming a 3- to 6-membered cycloalkyl ring; Cy 1B is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 1B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 1B Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy1B , halogen, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NRe11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy1B C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy1B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy1B Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NRe11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy1B Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11, and are substituted with one, two, or three substituents independently selected from the oxo; R 16 H, Cy 1C , C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkinyl, R 16 C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkinyl is either not substituted or Cy 1C , halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 It is substituted with one, two, three, four, or five substituents selected from the group consisting of , and oxo, however, R 16 One or fewer of the substituents are Cy 1C and; Cy 1C is either non-substituted or substituted C 6~10Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 1C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 1C Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy1C , halogen, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11, NR c11 S(O)2R b11 , S(O)2NR c11 R d11 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy1C C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy1C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy1C Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NRc11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy1C Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R a11 , R b11 , R c11 , and R d11 H and C are independent of each other.1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a11 , R b11 , R c11 , and R d11 The C that forms 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Each alkyl group is C 1~6 Alkyl, Halo, CN, OR a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 Rd12 , NR c12 C(=NR e12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 S(O)2R b12 , NR c12 S(O)2R b12 , S(O)2NR c12 R d12 , and may be substituted with one, two, three, four, or five substituents independently selected from the oxo; or, R bonded to the same N atom c11 and R d11 These together with the N atom to which they are both bonded form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each with C 1~6 Alkyl, Halo, CN, OR a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 R d12 , NR c12 C(=NR e12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 S(O)2R b12 , NR c12 S(O)2R b12 , S(O)2NR c12 R d12and may be substituted with one, two, or three substituents independently selected from oxo; R a12 R b12 R c12 and R d12 are each independently H, C 1~6 alkyl, C 1~6 haloalkyl, C 2~6 alkenyl, C 2~6 alkynyl, phenyl, C 3~7 cycloalkyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, phenyl-C 1~3 alkyl, 5- to 6-membered heteroaryl-C 1~3 alkyl, C 3~7 cycloalkyl-C 1~3 alkyl, and 4- to 7-membered heterocycloalkyl-C 1~3 alkyl, R a12 R b12 R c12 and R d12 forming the C 1~6 alkyl, C 1~6 haloalkyl, C 2~6 alkenyl, C 2~6 alkynyl, phenyl, C 3~7 cycloalkyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, phenyl-C 1~3 alkyl, 5- to 6-membered heteroaryl-C 1~3 alkyl, C 3~7 cycloalkyl-C 1~3 alkyl, and 4- to 7-membered heterocycloalkyl-C 1~3 alkyl may each be substituted with one, two, or three substituents independently selected from OH, CN, amino, NH(C 1~6 alkyl), N(C 1~6 alkyl)2, halo, C 1~6 alkyl, C 1~6 alkoxy, C 1~6 haloalkyl, C 1~6 haloalkoxy, and may be substituted with one, two, or three substituents independently selected from oxo; or R c12 and R d12together with the N atom to which they are both attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is unsubstituted or substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, NH(C 1~6 alkyl), N(C 1~6 alkyl)2, halo, C 1~6 alkyl, C 1~6 alkoxy, C 1~6 haloalkyl, C 1~6 haloalkoxy, and oxo; R e11 and R e12 are each independently H, CN, or NO2. [Inventive Concept 1069] Formula (I-2): The compound of Inventive Concept 1068 or a salt thereof, which is a compound of TIFF0007829249000014.tif40128. [Inventive Concept 1070] Cy 1A is unsubstituted or substituted aryl, the compound of Inventive Concept 1068 or 1069 or a salt thereof. [Inventive Concept 1071] Cy 1A is unsubstituted or substituted phenyl, the compound of Inventive Concept 1070 or a salt thereof. [Inventive Concept 1072] Cy 1A is substituted phenyl, the compound of Inventive Concept 1071 or a salt thereof. [Inventive Concept 1073] Cy 1A has at least one OR a11 or at least one C(=NR e11 )NR c11 R<​​​​​​​​​​​​​​​​​​A compound or salt thereof according to any of the inventions 1068 to 1072, which is substituted with [the specified compound]. [Invention 1074] Cy 1A at least one OR a11 It is replaced with and C 1~6 Alkyl, C 1~6 A compound or salt thereof according to any of the invention 1068 to 1073, which is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens. [Invention 1075] Cy 1A It is substituted with at least one OH group, and C 1~6 Alkyl, C 1~6 A compound or salt thereof according to any of the invention 1068 to 1074, which is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens. [Invention 1076] Cy 1A Preferably at position 4, at least one C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 A compound or salt thereof according to any of the inventions 1068 to 1075, which is substituted with [the specified compound]. [Invention 1077] Cy 1A Preferably at position 4, at least one C(=NR e11 )NR c11 R d11 A compound of the present invention 1076 or a salt thereof, which is substituted with [the specified compound]. [Invention 1078] Cy 1A A compound of the present invention 1077 or a salt thereof, wherein preferably at the 4-position, is substituted with at least one C(=NH)NH2. [Invention 1079] Cy 1A The formula is as follows: A compound of the present invention 1072 or a salt thereof, which is one of TIFF0007829249000015.tif211130. [Invention 1080] Cy 1A In the formula defining R, Cy1A C 1~6 A compound of the present invention 1079 or a salt thereof, wherein the compound is alkyl, for example methyl, or halogen, for example Cl or Br, or amino. [Invention 1081] Cy 1A The formula is as follows: A compound of the present invention 1072 or a salt thereof, which is one of TIFF0007829249000016.tif45131. [Invention 1082] Cy 1A In the formula defining R a11 C 1~6 Alkyl, for example, methyl, R b11 C 1~6 Alkyl, for example, methyl, R b11 C 1~6 Haloalkyls, for example, trifluoromethyl, R c11 Compounds of the present invention 1081 or salts thereof, wherein the alkyl group is, for example, methyl. [Invention 1083] Cy 1A A compound or salt thereof according to the present invention 1068 or 1069, wherein is unsubstituted or substituted heteroaryl. [Invention 1084] Cy 1A A compound of the present invention 1083 or a salt thereof, wherein is unsubstituted or substituted pyridine-3-yl, 1H-pyrrolo[2,3-b]pyridine-5-yl, or 1H-benzo[d]imidazole-6-yl. [Invention 1085] Cy 1A The formula is as follows: One of TIFF0007829249000017.tif45128, TIFF0007829249000018.tif220130, TIFF0007829249000019.tif222136, TIFF0007829249000020.tif217136, TIFF0007829249000021.tif217135, TIFF0007829249000022.tif60128, a compound of the present invention 1083 or a salt thereof. [The present invention 1086] Cy 1A Each R in the formula defining Cy1A is independently C 1~6 alkyl, such as methyl or ethyl, preferably methyl, or halogen, such as F, Cl, or Br, preferably Cl, or amino, a compound of the present invention 1085 or a salt thereof. [The present invention 1087] Cy 1A Each R bonded to the nitrogen in the formula defining Cy1A is C 1~6 alkyl, such as methyl or ethyl, a compound of the present invention 1085 or 1086 or a salt thereof. [The present invention 1088] R 11 is C 1~6 alkyl, a compound of any one of the present inventions 1068 to 1087 or a salt thereof. [The present invention 1089] R 11 is methyl, a compound of the present invention 1088 or a salt thereof. [The present invention 1090] R 11 is H, a compound of any one of the present inventions 1068 to 1087 or a salt thereof. [The present invention 1091] R[[ID=Z5]] 12 is H, a compound of any one of the present inventions 1068 to 1090 or a salt thereof. [The present invention ten ninety-two] R 12 is C 1~6 alkyl, such as methyl or ethyl, preferably methyl, a compound of any one of the present inventions 1068 to 1090 or a salt thereof. [Invention 1093] R 11 and R 12 A compound or salt thereof according to any of the present invention 1068 to 1087, wherein these compounds, together with the groups to which they are bonded, form a 4-6 membered heterocycloalkyl ring. [Invention 1094] A compound or salt thereof from any of the invention 1068 to 1093, wherein n1 is 1. [Invention 1095] A compound or salt thereof from any of the inventions 1068 to 1093, wherein n1 is 2. [Invention 1096] A compound or salt thereof from any of the invention 1068 to 1095, wherein n2 is 0. [Invention 1097] A compound or salt thereof from any of the inventions 1068 to 1095, wherein n2 is 1. [Invention 1098] A compound or salt thereof from any of the inventions 1068 to 1095, wherein n2 is 2. [Invention 1099] The following equations (I-1a) to (I-1f) and (I-2a) to (I-2r): A compound or salt thereof from any of the 1068-1098 of this invention, which matches any of the following: TIFF0007829249000023.tif170143, TIFF0007829249000024.tif202143, or TIFF0007829249000025.tif120143. [Invention 1100] The following equations (I-1g)~(I-1o) and (I-2aa)~(I-2az): A compound or salt thereof from any of the 1068-1099 of this invention that matches any of the following: TIFF0007829249000026.tif59134, TIFF0007829249000027.tif196137, TIFF0007829249000028.tif209137, or TIFF0007829249000029.tif138137. [Invention 1101] The following equations (I-3) to (I-9): A compound or salt thereof from any of the inventions 1068 to 1100 that matches any of TIFF0007829249000030.tif144142. [Invention 1102] The following equations (I-3a) to (I-3k): A compound or salt thereof from any of the invention 1068 to 1101 that matches any of TIFF0007829249000031.tif197142. [Invention 1103] The following equations (I-4a) to (I-4bf): A compound or salt thereof according to any of the inventions 1068 to 1101, which matches any of the following: TIFF0007829249000032.tif138142TIFF0007829249000033.tif208142TIFF0007829249000034.tif208142TIFF0007829249000035.tif200142TIFF0007829249000036.tif195142. [Invention 1104] The following equations (I-5a)~(I-5u): A compound or salt thereof according to any of the invention 1068 to 1101, which matches either TIFF0007829249000037.tif228142 or TIFF0007829249000038.tif125141. [Invention 1105] The following equations (I-6a) to (I-6cw): TIFF0007829249000039.tif68142TIFF0007829249000040.tif209142TIFF0007829249000041.tif2 08142TIFF0007829249000042.tif215142TIFF0007829249000043.tif222142TIFF0007829249000044 A compound or salt thereof according to any of the invention 1068 to 1101, which matches any one of the following: .tif211141TIFF0007829249000045.tif208141TIFF0007829249000046.tif213142TIFF0007829249000047.tif217141TIFF0007829249000048.tif34141. [Invention 1106] The following equations (I-7a) to (I-7co): A compound or salt thereof according to any of the invention 1068 to 1101, which matches any one of the following: TIFF0007829249000049.tif173142TIFF0007829249000050.tif208142TIFF0007829249000051.tif209142TIFF0007829249000052.tif198142TIFF0007829249000053.tif228142TIFF0007829249000054.tif217142TIFF0007829249000055.tif213142TIFF0007829249000056.tif217141. [Invention 1107] The following equations (I-8a)~(I-8z): A compound or salt thereof according to any of the invention items 1068 to 1101, which matches any of TIFF0007829249000057.tif208134, TIFF0007829249000058.tif209134, or TIFF0007829249000059.tif32134. [Invention 1108] The following equations (I-9a)~(I-9z): A compound or salt thereof from any of the inventions 1068 to 1101 that matches any of the following: TIFF0007829249000060.tif173132, TIFF0007829249000061.tif209132, or TIFF0007829249000062.tif68132. [Invention 1109] R 13 Cy 1B A compound or salt thereof according to any of the invention items 1068 to 1108. [Invention 1110] R 13 (C 1~6 Alkilen)Cy 1B , (C 2~6 Alkenylene) Cy 1B , or (C 2~6 Alkinylene)Cy 1B A compound or salt thereof according to any of the invention items 1068 to 1108. [Invention 1111] R 13 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 A compound of the present invention 1110 or a salt thereof, wherein the alkynylene component is not substituted. [Invention 1112] R 13 (CR 13A R 13B ) n3 Cy 1B A compound or salt thereof according to any of the invention items 1068 to 1108. [Invention 1113] Each R 13A A compound of the present invention 1112 or a salt thereof, wherein H is present. [Invention 1114] Each R 13B A compound of the present invention 1112 or a salt thereof, wherein H is present. [Invention 1115] A compound or salt thereof from any of the inventions 1068 to 1114, wherein n3 is 0. [Invention 1116] A compound or salt thereof from any of the inventions 1068 to 1114, wherein n3 is 1. [Invention 1117] A compound or salt thereof from any of the inventions 1068 to 1114, wherein n3 is 2. [Invention 1118] R 13 (CH2) 0~2 Cy 1B A compound or salt thereof according to any of the inventions 1068 to 1114. [Invention 1119] R 13 CH2Cy 1B A compound or salt thereof according to any of the inventions 1068 to 1114. [Invention 1120] R 13 CH2CH2Cy 1B A compound or salt thereof according to any of the inventions 1068 to 1114. [Invention 1121] R 13 OCy 1B A compound or salt thereof according to any of the invention items 1068 to 1108. [Invention 1122] Cy 1B is non-substituted C 6~10 A compound or salt thereof according to any of the invention items 1068 to 1121, which is an aryl compound. [Invention 1123] Cy 1B A compound of the present invention 1122 or a salt thereof, wherein is an unsubstituted phenyl. [Invention 1124] Cy 1B Compounds of the present invention 1122 or salts thereof, wherein is an unsubstituted naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1125] Cy 1B A compound or salt thereof according to any of the present invention 1068 to 1124, wherein is an unsubstituted 5- to 10-membered heteroaryl compound. [Invention 1126] Cy 1BA compound of the present invention 1125 or a salt thereof, wherein is an unsubstituted pyridyl, for example, an unsubstituted 2-, 3-, or 4-pyridyl, or an unsubstituted quinolyl, for example, an unsubstituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl. [Invention 1127] Cy 1B Substitution C 6~10 A compound or salt thereof according to any of the invention items 1068 to 1121, which is an aryl compound. [Invention 1128] Cy 1B A compound of the present invention 1127 or a salt thereof, wherein is a substituted phenyl compound. [Invention 1129] Cy 1B A compound of the present invention 1128 or a salt thereof, wherein is biphenylyl (i.e., phenyl-substituted phenyl), for example, 2-, 3-, or 4-biphenylyl. [Invention 1130] Cy 1B A compound of the present invention 1129 or a salt thereof, wherein is a substituted naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1131] Cy 1B A compound or salt thereof according to any of the invention 1068 to 1121, wherein is a substituted 5- to 10-membered heteroaryl compound. [Invention 1132] Cy 1B Compounds of the present invention 1131 or salts thereof, wherein is a substituted pyridyl, for example, a substituted 2-, 3-, or 4-pyridyl, or a substituted quinolyl, for example, a substituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl. [Invention 1133] Cy 1B However, R Cy1B , halogen, and C 1~6 Each R is substituted with one, two, three, four, or five substituents independently selected from the haloalkyl groups; Cy1B C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 6~10Selected from aryl or 5-10 member heteroaryl, R Cy1B Each C that forms 6~10 Aryl or 5-10 member heteroaryl compounds, either unsubstituted or halogenated, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 A compound or salt thereof according to any of the inventions 1127 to 1132, substituted with one, two, or three substituents independently selected from alkynyl and haloalkyl groups. [Invention 1134] R 13 The formula is as follows: A compound or salt thereof of any of the compounds 1068 to 1133 of the present invention, selected from the groups TIFF0007829249000063.tif156132, TIFF0007829249000064.tif219136, TIFF0007829249000065.tif228127, TIFF0007829249000066.tif207131, and TIFF0007829249000067.tif173133. [Invention 1135] R 13 R in the expression representing Cy1B C 1~6 A compound or salt thereof according to the present invention 1134, wherein the compound is an alkyl group, for example methyl or ethyl, preferably methyl, or a halogen, for example fluorine or chlorine, preferably fluorine. [Invention 1136] R 13 R in the expression representing Cy1B C 1~6 A compound of the present invention 1134 or a salt thereof, wherein the compound is alkyl, for example, methyl or ethyl, preferably methyl. [Invention 1137] R 13 R in the expression representing Cy1B A compound or salt thereof according to the present invention 1134, wherein the halogen is, for example, fluorine or chlorine, preferably fluorine. [Invention 1138] One or fewer R 14 A compound or salt thereof according to any of the inventions 1068 to 1137, wherein the compound is other than hydrogen. [Invention 1139] One or fewer R 14 is anything other than hydrogen, and one R 14 C 1~6 A compound of the present invention 1138 or a salt thereof, wherein the compound is alkyl, for example, methyl. [Invention 1140] Each R 14 A compound or salt thereof according to the present invention 1139, wherein the compound is hydrogen. [Invention 1141] A 11 A compound or salt thereof according to any of the inventions 1068 to 1140, wherein the element is N. [Invention 1142] R 15 A compound or salt thereof according to any of the inventions 1068 to 1141, wherein the compound is hydrogen. [Invention 1143] R 15 C 1~6 A compound or salt thereof from any of the invention items 1068 to 1141, which is alkyl, for example, methyl. [Invention 1144] R 15 A compound or salt thereof from any of the invention items 1068 to 1141, wherein the compound is a hydroxyl group. [Invention 1145] R 16 A compound or salt thereof according to any of the inventions 1068 to 1144, wherein the compound is hydrogen. [Invention 1146] R 16 C is either non-substitutive or substituted. 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 A compound or salt thereof that is an alkynyl, as specified in any of the invention items 1068 to 1144. [Invention 1147] R 16 is non-substituted C 1~6 A compound of the present invention 1146 or a salt thereof, wherein the compound is alkyl, for example, methyl. [Invention 1148] R 16 Substitution C 1~6 A compound of the present invention 1146 or a salt thereof, which is alkyl. [Invention 1149] R 16 Substitution C that forms 1~6 Alkyl, halogen, CN, C(O)NR c11 R d11 , and C(O)OR a11 A compound of the present invention 1148 or a salt thereof, which is substituted with one, two, three, four, or five substituents selected from the group consisting of the following, for example, one, two, or three substituents, preferably one substituent. [Invention 1150] R 16 (CH2) 1~6 C(O)OR a11 The compound or salt thereof according to the present invention 1149. [Invention 1151] R 16 R defines a11 is H or C 1~6 A compound of the present invention 1150 or a salt thereof, wherein the compound is alkyl, for example, methyl. [Invention 1152] R 16 R defines a11 A compound of the present invention 1150 or a salt thereof, wherein H is present. [Invention 1153] R a11 , R b11 , R c11 , and R d11 , R a12 , R b12 , R c12 , and R d12 H and C are independent of each other. 1~6 A compound selected from alkyl groups, any of the compounds 1068 to 1152 of this invention, or a salt thereof. [Invention 1154] Each R e11 and each R e12 A compound or salt thereof according to any of the inventions 1068 to 1153, wherein the compound is H. [Invention 1155] A pharmaceutical composition comprising any compound according to invention 1068 to 1154 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1156] Compounds of formula (IIA) or (IIB), or their salts: TIFF0007829249000068.tif63128In formula, Cy 2A is either non-substituted or substituted C 6~10 It is an aryl or unsubstituted or substituted 5-10 member heteroaryl; Cy 2A The ring atoms of the 5-10 membered heteroaryl that form the Cy 2A Substitution C that forms 6~10 Aryl or substituted 5-10 member heteroaryls are R Cy2A , halogen, C 1~6 Haloalkyl, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , C(=NOR a21 )NR c21 R d21 , C(=NOC(O)R b21 )NR c21 R d21 , C(=NR e21 )NR c21 C(O)OR a21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NRc21 S(O)2R b21 , S(O)2NR c21 R d21 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy2A C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy2A The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R group consist of one, two, three, or four heteroatoms selected from carbon atoms and O, N, and S. Cy2A Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NRc21 S(O)2R b21 , S(O)2NR c21 R d21 , and are substituted with one, two, or three substituents independently selected from the oxo, R Cy2A Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2R b21 , S(O)2NR c21 R d21 , and are substituted with one, two, or three substituents independently selected from the oxo; R 21 is H, or C 1~6 Alkyl, C 6~10 Aryl-C 1~6Alkyl or 5-10 member heteroaryl-C 1~6 It is alkyl, R 21 C that forms 1~6 Alkyls are either unsubstituted or contain halogens, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2R b21 , S(O)2NR c21 R d21 , and are substituted with one, two, or three substituents independently selected from the oxo, R 21 C that forms 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 Alkyl is either unsubstituted or C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2R b21 , S(O)2NR c21 R d21 , and are substituted with one, two, or three substituents independently selected from the oxo; R 22 is H or C 1~6 It is alkyl; or, R 21 and R 22 These, together with the groups to which they are bonded, form a 4-6 membered heterocycloalkyl ring; A 23 is N or NR 23 and; A 24 CR 24 , N, or NR 24 and; A 26 CR 26 Or it is S; however, A in equation (IIA) 23 , A 24 , and A 26 is, A 23 , A 24 , and A 26 The ring containing the symbol is selected such that it is a heteroaryl ring. TIFF0007829249000069.tif2128 represents an aromatic ring (normalized) bond; R 23 is H or C 1~6 It is alkyl; R 24 H, C 1~6 Alkyl or phenyl; R 25 is Cy 2B , (CR 25A R 25B ) n25 Cy 2B , (C 1~6 Alkilen)Cy 2B , (C 2~6 Alkenylene) Cy 2B , or (C 2~6 Alkinylene)Cy 2B And R 25 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 The alkylylene component is either unsubstituted or contains halogen, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2Rb21 , S(O)2NR c21 R d21 Substituting with one, two, three, four, or five substituents independently selected from the group consisting of , and oxo; R 26 is H or C 1~6 It is alkyl; Each R 25A is H or C 1~6 It is alkyl; Each R 25B is H or C 1~6 It is alkyl; n25 is 0, 1, or 2; Cy 2B is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 2B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 2B Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy2B , halogen, C 1~6 Haloalkyl, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)ORa21 , C(=NR e21 )NR c21 R d21 , C(=NOR a21 )NR c21 R d21 , C(=NOC(O)R b21 )NR c21 R d21 , C(=NR e21 )NR c21 C(O)OR a21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2R b21 , S(O)2NR c21 R d21 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy2B C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy2B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy2B Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21 R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2R b21 , S(O)2NR c21 R d21 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy2B Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a21 , SR a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , NR c21 R d21 , NR c21 C(O)R b21 , NR c21 C(O)NR c21 R d21 , NR c21 C(O)OR a21 , C(=NR e21 )NR c21R d21 , NR c21 C(=NR e21 )NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 S(O)2R b21 , NR c21 S(O)2R b21 , S(O)2NR c21 R d21 , and are substituted with one, two, or three substituents independently selected from the oxo; H and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a21 , R b21 , R c21 , and R d21 The C that forms 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Each alkyl group is C 1~6 Alkyl, Halo, CN, OR a22 , SR a22 , C(O)R b22, C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22 , OC(O)NR c22 R d22 , NR c22 R d22 , NR c22 C(O)R b22 , NR c22 C(O)NR c22 R d22 , NR c22 C(O)OR a22 , C(=NR e22 )NR c22 R d22 , NR c22 C(=NR e22 )NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 S(O)2R b22 , NR c22 S(O)2R b22 , S(O)2NR c22 R d22 , and may be substituted with one, two, three, four, or five substituents independently selected from the oxo; or, R bonded to the same N atom c21 and R d21 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each being C 1~6 Alkyl, Halo, CN, OR a22 , SR a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22 , OC(O)NR c22 R d22 , NR c22 R d22 , NR c22 C(O)R b22 , NR c22 C(O)NR c22 R d22, NR c22 C(O)OR a22 , C(=NR e22 )NR c22 R d22 , NR c22 C(=NR e22 )NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 S(O)2R b22 , NR c22 S(O)2R b22 , S(O)2NR c22 R d22 , and may be substituted with one, two, or three substituents independently selected from the oxo; R a22 , R b22 , R c22 , and R d22 H and C are independent of each other. 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a22 , R b22 , R c22 , and R d22 The C that forms 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3Alkyl and 4-7 member heterocycloalkyl-C 1~3 Alkyl compounds are OH, CN, amino, and NH(C) respectively. 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 It may be substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; or, R bonded to the same N atom c22 and R d22 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is either unsubstituted or OH, CN, amino, NH(C) 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 Substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; R e21 and R e22 Each of these is independently H, CN, or NO2. [Invention 1157] Cy 2A A compound or salt thereof according to Invention 1156, wherein is unsubstituted or substituted aryl. [Invention 1158] Cy 2A A compound of the present invention 1157 or a salt thereof, wherein is an unsubstituted or substituted phenyl. [Invention 1159] Cy 2A A compound of the present invention 1158 or a salt thereof, wherein is a substituted phenyl compound. [Invention 1160] Cy 2A at least one OR a21 or at least one C(=NR) e21 )NRc21 R d21 , C(=NOR a21 )NR c21 R d21 , C(=NOC(O)R b21 )NR c21 R d21 , or C(=NR e21 )NR c21 C(O)OR a21 A compound or salt thereof according to any of the inventions 1156 to 1159, which is substituted with [the specified compound]. [Invention 1161] Cy 2A at least one OR a21 It is replaced with and C 1~6 Alkyl, C 1~6 A compound or salt thereof according to any of the present inventions 1156 to 1160, which is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens. [Invention 1162] Cy 2A It is substituted with at least one OH group, and C 1~6 Alkyl, C 1~6 A compound or salt thereof according to any of the invention 1156 to 1161, which is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens. [Invention 1163] Cy 2A Preferably at position 4, at least one C(=NR e21 )NR c21 R d21 , C(=NOR a21 )NR c21 R d21 , C(=NOC(O)R b21 )NR c21 R d21 , C(=NR e21 )NR c21 C(O)OR a21 A compound or salt thereof according to any of the inventions 1156 to 1162, which is substituted with [the specified compound]. [Invention 1164] Cy 2A Preferably at position 4, at least one C(=NRe21 )NR c21 R d21 A compound of the present invention 1163 or a salt thereof, which is substituted with [the specified compound]. [Invention 1165] Cy 2A A compound of the present invention 1164 or a salt thereof, wherein preferably at the 4-position, is substituted with at least one C(=NH)NH2. [Invention 1166] Cy 2A The formula is as follows: A compound of the present invention 1159 or a salt thereof, which is one of TIFF0007829249000070.tif218135. [Invention 1167] Cy 2A In the formula defining R, Cy2A C 1~6 A compound of the present invention 1166 or a salt thereof, wherein the compound is alkyl, for example methyl, or halogen, for example Cl or Br, or amino. [Invention 1168] Cy 2A The formula is as follows: A compound of the present invention 1159 or a salt thereof, which is one of TIFF0007829249000071.tif46131. [Invention 1169] R a21 C 1~6 It is alkyl, R b21 C 1~6 A compound or salt thereof according to Invention 1168, which is alkyl. [Invention 1170] Cy 2A A compound of the present invention 1156 or a salt thereof, wherein is an unsubstituted or substituted heteroaryl, for example, pyridine-3-yl, 1H-pyrrolo[2,3-b]pyridine-5-yl, or 1H-benzo[d]imidazole-6-yl. [Invention 1171] Cy 2A The formula is as follows: A compound of the present invention 1170 or a salt thereof, which is one of the following: TIFF0007829249000072.tif113132TIFF0007829249000073.tif219136TIFF0007829249000074.tif221136TIFF0007829249000075.tif218137TIFF0007829249000076.tif201137TIFF0007829249000077.tif27135. [Invention 1172] Cy 2A Each R in the formula defining Cy2A C 1~6 A compound or salt thereof according to the present invention 1171, wherein the compound is an alkyl group, for example methyl or ethyl, preferably methyl, or a halogen, for example F, Cl, or Br, preferably Cl. [Invention 1173] Cy 2A Each R bonded to nitrogen in the formula defining the Cy2A C 1~6 Compounds of the present invention 1171 or 1172 or salts thereof, wherein the compound is alkyl, for example, methyl or ethyl. [Invention 1174] R 21 C 1~6 A compound or salt thereof that is alkyl, according to any of the compounds 1156 to 1173 of the present invention. [Invention 1175] R 21 A compound of the present invention 1174 or a salt thereof, wherein the compound is methyl. [Invention 1176] R 21 A compound or salt thereof according to any of the inventions 1156 to 1173, wherein the compound is H. [Invention 1177] R 22 A compound or salt thereof from any of the inventions 1156 to 1176, wherein the compound is H. [Invention 1178] R 22 C 1~6 A compound or salt thereof from any of the compounds 1156 to 1176 of the present invention, which is alkyl. [Invention 1179] R 22 A compound of the present invention 1178 or a salt thereof, wherein the compound is methyl. [Invention 1180] R 21 and R 22 A compound or salt thereof according to any of the present invention 1156 to 1179, wherein these compounds together with the groups to which they are bonded form a 4-6 membered heterocycloalkyl ring. [Invention 1181] A compound or salt thereof according to any of the inventions 1156 to 1180, which is formula (IIA). [Invention 1182] The following formula (IIA-1a) or (IIA-1b): A compound of the present invention 1181 or a salt thereof that matches any of TIFF0007829249000078.tif34144. [Invention 1183] The following equations (IIA-2) to (IIA-5): A compound or salt thereof from either of the inventions 1181 or 1182, which matches any of TIFF0007829249000079.tif72147. [Invention 1184] The following equations (IIA-2a) to (IIA-5b): A compound of the present invention 1183 or a salt thereof that matches any of TIFF0007829249000080.tif153148. [Invention 1185] A compound or salt thereof according to any of the inventions 1156 to 1180, which is formula (IIB). [Invention 1186] The following formula (IIB-1a) or (IIB-1b): A compound of the present invention 1185 or a salt thereof that matches any of TIFF0007829249000081.tif37141. [Invention 1187] R 23 A compound or salt thereof according to any of the inventions 1156 to 1184, wherein the compound is H. [Invention 1188] R 23 C 1~6A compound or salt thereof that is alkyl, according to any of the compounds 1156 to 1184 of the present invention. [Invention 1189] R 24 A compound or salt thereof according to any of the inventions 1156 to 1188, wherein the compound is H. [Invention 1190] R 24 C 1~6 A compound or salt thereof from any of the compounds described in items 1156 to 1188 of the present invention, which is alkyl. [Invention 1191] R 24 A compound or salt thereof from any of the inventions 1156 to 1188, wherein the compound is phenyl. [Invention 1192] R 25 Cy 2B A compound or salt thereof according to any of the invention items 1156 to 1191. [Invention 1193] R 25 (C 1~6 Alkilen)Cy 2B , (C 2~6 Alkenylene) Cy 2B , or (C 2~6 Alkinylene)Cy 2B And R 25 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 A compound or salt thereof from any of the inventions 1156 to 1191, wherein the alkynylene component is either unsubstituted or substituted. [Invention 1194] R 25 (C 1~6 Alkilen)Cy 2B , (C 2~6 Alkenylene) Cy 2B , or (C 2~6 Alkinylene)Cy 2B And R 25 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 A compound or salt thereof from any of the compounds 1156 to 1193 of the present invention, in which the alkynylene component is not substituted. [Invention 1195] R 25 (CR 25A R 25B ) n25 Cy 2B A compound or salt thereof according to any of the inventions 1156 to 1194. [Invention 1196] Each R 25A A compound or salt thereof according to Invention 1195, wherein H is present. [Invention 1197] Each R 25B A compound or salt thereof according to Invention 1194 or 1195, wherein H is present. [Invention 1198] A compound or salt thereof from any of the compounds 1194 to 1196 of the present invention, wherein n25 is 0. [Invention 1199] A compound or salt thereof from any of the compounds 1194 to 1196 of the present invention, wherein n25 is 1. [Invention 1200] A compound or salt thereof from any of the compounds 1194 to 1196 of the present invention, wherein n25 is 2. [Invention 1201] R 25 CH2Cy 2B A compound or salt thereof according to any of the inventions 1194 to 1196. [Invention 1202] R 25 CH2CH2Cy 2B A compound or salt thereof according to any of the inventions 1194 to 1196. [Invention 1203] Cy 2B is non-substituted C 6~10 A compound or salt thereof according to any of the invention items 1156 to 1202, which is an aryl compound. [Invention 1204] Cy 2B A compound of the present invention 1203 or a salt thereof, wherein is an unsubstituted phenyl. [Invention 1205] Cy 2B A compound or salt thereof of the present invention 1203, wherein is an unsubstituted naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1206] Cy 2B A compound or salt thereof according to any of the invention items 1156 to 1202, wherein is an unsubstituted 5- to 10-membered heteroaryl compound. [Invention 1207] Cy 2B A compound of the present invention 1206 or a salt thereof, wherein is an unsubstituted pyridyl, for example, an unsubstituted 2-, 3-, or 4-pyridyl, or an unsubstituted quinolyl, for example, an unsubstituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl. [Invention 1208] Cy 2B Substitution C 6~10 A compound or salt thereof according to any of the invention items 1156 to 1202, which is an aryl compound. [Invention 1209] Cy 2B A compound of the present invention 1208 or a salt thereof, wherein is a substituted phenyl compound. [Invention 1210] Cy 2B A compound of the present invention 1209 or a salt thereof, wherein is biphenylyl (i.e., phenyl-substituted phenyl), for example, 2-, 3-, or 4-biphenylyl. [Invention 1211] Cy 2B A compound of the present invention 1208 or a salt thereof, wherein is a substituted naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1212] Cy 2B A compound or salt thereof according to any of the inventions 1156 to 1202, wherein is a substituted 5- to 10-membered heteroaryl compound. [Invention 1213] Cy 2B Compounds of the present invention 1212 or salts thereof, wherein is a substituted pyridyl, for example, a substituted 2-, 3-, or 4-pyridyl, or a substituted quinolyl, for example, a substituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl. [Invention 1214] Cy 2B However, R Cy2B , halogen, and C 1~6Each R is substituted with one, two, three, four, or five substituents independently selected from the haloalkyl groups; Cy2B C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 6~10 Selected from aryl or 5-10 member heteroaryl, R Cy2B Each C that forms 6~10 Aryl or 5-10 member heteroaryl compounds, either unsubstituted or halogenated, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 A compound or salt thereof according to any of the inventions 1208 to 1213, substituted with one, two, or three substituents independently selected from alkynyl and haloalkyl groups. [Invention 1215] R 25 The formula is as follows: A compound or salt thereof of any of the compounds 1156 to 1214 of the present invention, selected from the groups TIFF0007829249000082.tif227136TIFF0007829249000083.tif227132TIFF0007829249000084.tif224131TIFF0007829249000085.tif213131TIFF0007829249000086.tif87133. [Invention 1216] R 25 R in the expression representing Cy2B C 1~6 A compound or salt thereof according to the present invention 1215, wherein the compound is an alkyl group, for example methyl or ethyl, preferably methyl, or a halogen, for example fluorine or chlorine, preferably fluorine. [Invention 1217] R 25 R in the expression representing Cy2B C 1~6 A compound of the present invention 1215 or a salt thereof, wherein the compound is alkyl, for example, methyl or ethyl, preferably methyl. [Invention 1218] R 25 R in the expression representing Cy2BA compound or salt thereof according to the present invention 1215, wherein the halogen is, for example, fluorine or chlorine, preferably fluorine. [Invention 1219] R a21 , R b21 , R c21 , R d21 , R a22 , R b22 , R c22 , R d22 H and C are independent of each other. 1~6 A compound selected from alkyl groups, any of the compounds described in items 1156 to 1218 of this invention, or a salt thereof. [Invention 1220] Each R e21 and each R e22 A compound or salt thereof according to any of the inventions 1156 to 1219, wherein the compound is H. [Invention 1221] A pharmaceutical composition comprising any compound according to invention 1156 to 1220 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1222] Compounds of formula (III) or salts thereof for use in the treatment of MASP-2 related diseases or disorders: TIFF0007829249000087.tif22128In formula, Cy 3A is either non-substituted or substituted C 6~10 It is an aryl or unsubstituted or substituted 5-10 member heteroaryl; Cy 3A The ring atoms of the 5-10 membered heteroaryl that form the Cy 3A Substitution C that forms 6~10 Aryl or substituted 5-10 member heteroaryls are R Cy3A , halogen, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NRc31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , C(=NOR a31 )NR c31 R d31 , C(=NOC(O)R b31 )NR c31 R d31 , C(=NR e31 )NR c31 C(O)OR a31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy3A C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy3A The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R group consist of one, two, three, or four heteroatoms selected from carbon atoms and O, N, and S. Cy3A Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6Alkynnyls are independently unsubstituted or halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo, R Cy3A Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NRc31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo; R 31 is H, or C 1~6 Alkyl, C 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 It is alkyl, R 31 C that forms 1~6 Alkyls are either unsubstituted or contain halogens, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo, R 31 C that forms 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 Alkyl is either unsubstituted or C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31, and are substituted with one, two, or three substituents independently selected from the oxo; R 32 is H or C 1~6 It is alkyl; or, R 31 and R 32 These, together with the groups to which they are bonded, form a 4-6 membered heterocycloalkyl ring; R 33 is Cy 3B , (CR 33A R 33B ) n33 Cy 3B , (C 1~6 Alkilen)Cy 3B , (C 2~6 Alkenylene) Cy 3B , or (C 2~6 Alkinylene)Cy 3B And R 35 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 The alkylylene component is either unsubstituted or contains halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2Rb31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 Substituting with one, two, three, four, or five substituents independently selected from the group consisting of , and oxo; Each R 33A H or C 1~6 It is alkyl; Each R 33B H or C 1~6 It is alkyl; or, R bonded to the same carbon atom 33A and R 33B is any other R 33A base and R 33B Originally independent, yet united - (CH2) 2~5 - may be formed, thereby forming a 3- to 6-membered cycloalkyl ring; n33 is 0, 1, 2, or 3; Cy 3B is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 3B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 3B Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy3B , halogen, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 Rd31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , C(=NOR a31 )NR c31 R d31 , C(=NOC(O)R b31 )NR c31 R d31 , C(=NR e31 )NR c31 C(O)OR a31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy3B C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy3B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy3B Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6Alkynnyls are independently unsubstituted or halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy3B Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NRc31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo; R 34 H and C 1~6 Selected from alkyl groups; R 35 is H, unsubstituted or substituted C 1~6 Alkyl, and Cy 3C More selected, R 35 Substitution C that forms 1~6 Alkyl is Cy 3C , halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31, NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 It is substituted with one, two, three, four, or five substituents selected from the group consisting of , and oxo; however, R 35 One or fewer of the substituents are Cy 3C and; Cy 3C is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 3C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 3C Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy3C , halogen, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)ORa31 , C(=NR e31 )NR c31 R d31 , C(=NOR a31 )NR c31 R d31 , C(=NOC(O)R b31 )NR c31 R d31 , C(=NR e31 )NR c31 C(O)OR a31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy3C C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy3C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy3C Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy3C Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 , and are substituted with one, two, or three substituents independently selected from the oxo; R 36 H and C 1~6 Selected from alkyl groups; R a31 , R b31 , R c31 , and R d31 H and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a31 , R b31 , R c31 , and R d31 The C that forms 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3Alkyl and 4-10 member heterocycloalkyl-C 1~3 Each alkyl group is C 1~6 Alkyl, Halo, CN, OR a32 , SR a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 ,OC(O)R b32 , OC(O)NR c32 R d32 , NR c32 R d32 , NR c32 C(O)R b32 , NR c32 C(O)NR c32 R d32 , NR c32 C(O)OR a32 , C(=NR e32 )NR c32 R d32 , NR c32 C(=NR e32 )NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 S(O)2R b32 , NR c32 S(O)2R b32 , S(O)2NR c32 R d32 , and may be substituted with one, two, three, four, or five substituents independently selected from the oxo; or, R bonded to the same N atom c31 and R d31 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each being C 1~6 Alkyl, Halo, CN, OR a32 , SR a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 ,OC(O)R b32 , OC(O)NR c32 Rd32 , NR c32 R d32 , NR c32 C(O)R b32 , NR c32 C(O)NR c32 R d32 , NR c32 C(O)OR a32 , C(=NR e32 )NR c32 R d32 , NR c32 C(=NR e32 )NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 S(O)2R b32 , NR c32 S(O)2R b32 , S(O)2NR c32 R d32 , and may be substituted with one, two, or three substituents independently selected from the oxo; R a32 , R b32 , R c32 , and R d32 H and C are independent of each other. 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a32 , R b32 , R c32 , and R d32 The C that forms 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Alkyl compounds are OH, CN, amino, and NH(C) respectively. 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 It may be substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; or, R bonded to the same N atom c32 and R d32 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is either unsubstituted or OH, CN, amino, NH(C) 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 Substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; R e31 and R e32 Each of these is independently H, CN, or NO2. [Invention 1223] Cy 3A A compound or salt thereof according to Invention 1222, wherein is unsubstituted or substituted aryl. [Invention 1224] Cy 3A A compound of the present invention 1223 or a salt thereof, wherein is an unsubstituted or substituted phenyl. [Invention 1225] Cy 3AThe compound of the present invention 1224 or a salt thereof, wherein it is a substituted phenyl. [The present invention 1226] Cy 3A is at least one OR a31 or at least one C(=NR e31 )NR c31 R d31 , C(=NOR a31 )NR c31 R d31 , C(=NOC(O)R b31 )NR c31 R d31 , or C(=NR e31 )NR c31 C(O)OR a31 The compound of any one of the present inventions 1222 - 1225 or a salt thereof, which is substituted with the above. [The present invention 1227] Cy 3A is substituted with at least one OR a31 and is substituted with at least one additional substituent selected from the group consisting of C 1~6 alkyl, C 1~6 haloalkyl, and halogen. The compound of any one of the present inventions 1222 - 1226 or a salt thereof. [The present invention 1228] Cy 3A is substituted with at least one OH and is substituted with at least one additional substituent selected from the group consisting of C 1~6 alkyl, C 1~6 haloalkyl, and halogen. The compound of any one of the present inventions 1222 - 1227 or a salt thereof. [The present invention 1229] Cy 3A is preferably at the 4 - position and has at least one C(=NR e31 )NR c31 R d31 , C(=NOR a31 )NR c31 R d31 , C(=NOC(O)R b31 )NR c31 R d31 , C(=NR e31 )NR c31C(O)OR a31 A compound or salt thereof according to any of the inventions 1222 to 1228, which is substituted with [the specified compound]. [Invention 1230] Cy 3A Preferably at position 4, at least one C(=NR e31 )NR c31 R d31 A compound of the present invention 1229 or a salt thereof, which is substituted with [the specified compound]. [Invention 1231] Cy 3A A compound of the present invention 1230 or a salt thereof, wherein preferably at the 4-position, is substituted with at least one C(=NH)NH2. [Invention 1232] Cy 3A The formula is as follows: A compound of the present invention 1225 or a salt thereof, which is one of TIFF0007829249000088.tif187134. [Invention 1233] Cy 3A The formula is as follows: A compound of the present invention 1225 or a salt thereof, which is one of TIFF0007829249000089.tif46131. [Invention 1234] Cy 3A In the formula defining R a31 C 1~6 Alkyl, for example, methyl; R b31 C 1~6 Alkyl, for example, methyl, or R b31 C 1~6 Haloalkyls, for example, trifluoromethyl; R c31 A compound or salt thereof according to the present invention 1233, wherein the alkyl group is, for example, methyl. [Invention 1235] Cy 3A A compound or salt thereof according to Invention 1222, wherein is unsubstituted or substituted heteroaryl. [Invention 1236] Cy 3AA compound of the present invention 1235 or a salt thereof, wherein is unsubstituted or substituted pyridine-3-yl, 1H-pyrrolo[2,3-b]pyridine-5-yl, or 1H-benzo[d]imidazole-6-yl. [Invention 1237] Cy 3A The formula is as follows: A compound or salt thereof of the present invention 1234 or 1235, which is one of the following: TIFF0007829249000090.tif67128TIFF0007829249000091.tif220129TIFF0007829249000092.tif206136TIFF0007829249000093.tif225137TIFF0007829249000094.tif204137TIFF0007829249000095.tif28128. [Invention 1238] Cy 3A Each R in the formula defining Cy3A C 1~6 A compound or salt thereof according to Invention 1237, wherein the compound is an alkyl group, for example methyl or ethyl, preferably methyl, or a halogen, for example F, Cl, or Br, preferably Cl, or amino. [Invention 1239] Cy 3A Each R bonded to nitrogen in the formula defining the Cy3A C 1~6 Compounds of the present invention 1237 or 1238 or salts thereof, wherein the compound is alkyl, for example, methyl or ethyl. [Invention 1240] R 31 C 1~6 A compound or salt thereof that is alkyl, according to any of the compounds 1222 to 1239 of the present invention. [Invention 1241] R 31 A compound of the present invention 1240 or a salt thereof, wherein the compound is methyl. [Invention 1242] R 31 A compound or salt thereof according to any of the inventions 1222 to 1241, wherein the compound is H. [Invention 1243] R 32A compound or salt thereof from any of the inventions 1222 to 1242, wherein the element is H. [Invention 1244] R 32 C 1~6 A compound or salt thereof from any of the compounds 1222 to 1242 of this invention, which is alkyl. [Invention 1245] R 32 A compound of the present invention 1244 or a salt thereof, wherein the compound is methyl. [Invention 1246] R 31 and R 32 However, any compound or salt thereof according to invention 1222 to 1239, wherein these compounds together with the groups to which they are bonded form a 4-6 membered heterocycloalkyl ring. [Invention 1247] The following equations (III-1a) to (III-1h): A compound or salt thereof from any of the inventions 1222 to 1246 that matches any of TIFF0007829249000096.tif121129. [Invention 1248] R 33 Cy 3B A compound or salt thereof according to any of the inventions 1222 to 1247. [Invention 1249] R 33 (C 1~6 Alkilen)Cy 3B , (C 2~6 Alkenylene) Cy 3B , or (C 2~6 Alkinylene)Cy 3B And R 35 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 A compound or salt thereof from any of the compounds 1222 to 1247 of the present invention, in which the alkynylene component is not substituted. [Invention 1250] R 33 (C 1~6 Alkilen)Cy 3B , (C 2~6 Alkenylene) Cy 3B , or (C2~6 Alkinylene)Cy 3B And R 35 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 Alkinylene component is halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)R b31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 A compound or salt thereof according to any of the inventions 1222 to 1249, which is substituted with one, two, three, four, or five substituents independently selected from the group consisting of , and oxo. [Invention 1251] R 33 (CR 33A R 33B ) n33 Cy 3B A compound or salt thereof according to any of the inventions 1222 to 1247. [Invention 1252] Each R 33A A compound or salt thereof according to the present invention 1251, wherein H is present. [Invention 1253] Each R 33B A compound or salt thereof according to the present invention 1251 or 1252, wherein H is present. [Invention 1254] A compound or salt thereof from any of the inventions 1251 to 1253, wherein n33 is 0. [Invention 1255] A compound or salt thereof from any of the compounds 1251 to 1253 of the present invention, wherein n33 is 1. [Invention 1256] A compound or salt thereof from any of the compounds 1251 to 1253 of the present invention, wherein n33 is 2. [Invention 1257] A compound or salt thereof from any of the inventions 1251 to 1253, wherein n33 is 3. [Invention 1258] R 33 CH2Cy 3B A compound or salt thereof according to any of the inventions 1222 to 1247. [Invention 1259] R 33 CH2CH2Cy 3B A compound or salt thereof according to any of the inventions 1222 to 1247. [Invention 1260] The following equations (III-2) to (III-4): A compound of Invention 1259 or a salt thereof that matches any of TIFF0007829249000097.tif78129. [Invention 1261] The following equations (III-2a) to (III-2h): A compound of the present invention 1260 or a salt thereof that matches any of TIFF0007829249000098.tif162129. [Invention 1262] The following equations (III-3a) to (III-3h): A compound of the present invention 1260 or a salt thereof that matches any of TIFF0007829249000099.tif165128. [Invention 1263] The following equations (III-4a) to (III-4h): A compound of the present invention 1260 or a salt thereof that matches any of TIFF0007829249000100.tif165132. [Invention 1264] R 33 CH2CH2CH2Cy 3B A compound or salt thereof according to any of the inventions 1222 to 1247. [Invention 1265] Cy 3B is non-substituted C 6~10 A compound or salt thereof according to any of the inventions 1222 to 1264, which is aryl. [Invention 1266] Cy 3B A compound of the present invention 1265 or a salt thereof, wherein is an unsubstituted phenyl. [Invention 1267] R 33 A compound of the present invention 1266 or a salt thereof, wherein the compound is CH2CH2Ph. [Invention 1268] Cy 3B A compound or salt thereof of the present invention 1266, wherein is an unsubstituted naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1269] R 33 A compound of the present invention 1268 or a salt thereof, wherein is CH2CH2-1-naphthyl or CH2CH2-2-naphthyl. [Invention 1270] Cy 3B A compound or salt thereof according to any of the present invention 1222 to 1264, wherein is an unsubstituted 5- to 10-membered heteroaryl compound. [Invention 1271] Cy 3BCompounds of the present invention 1270 or salts thereof, wherein is an unsubstituted pyridyl, e.g., unsubstituted 2-, 3-, or 4-pyridyl; an unsubstituted quinolyl, e.g., unsubstituted 2-, 3-, 4-, 5-, 6-, or 8-quinolyl; an unsubstituted benzo[b]thiophenyl, e.g., unsubstituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or an unsubstituted indolyl, e.g., unsubstituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl. [Invention 1272] Cy 3B is non-substituted C 3~10 A cycloalkyl compound or a salt thereof from any of the compounds 1222 to 1264 of the present invention. [Invention 1273] Cy 3B A compound of the present invention 1272 or a salt thereof, wherein is unsubstituted cyclopentyl, cyclohexyl, or cycloheptyl. [Invention 1274] Cy 3B A compound or salt thereof according to any of the present invention 1222 to 1264, wherein is an unsubstituted 4- to 10-membered heterocycloalkyl group. [Invention 1275] Cy 3B Substitution C 6~10 A compound or salt thereof according to any of the inventions 1222 to 1264, which is aryl. [Invention 1276] Cy 3B A compound of the present invention 1275 or a salt thereof, wherein is a substituted phenyl compound. [Invention 1277] Cy 3B A compound of the present invention 1275 or a salt thereof, wherein is a substituted naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1278] Cy 3B A compound or salt thereof according to any of the present invention 1222 to 1264, wherein is a substituted 5- to 10-membered heteroaryl compound. [Invention 1279] Cy 3BCompounds of the present invention 1278 or salts thereof, wherein is a substituted pyridyl, e.g., a substituted 2-, 3-, or 4-pyridyl; a substituted quinolyl, e.g., a substituted 2-, 3-, 4-, 5-, 6-, or 8-quinolyl; a substituted benzo[b]thiophenyl, e.g., a substituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or a substituted indolyl, e.g., a substituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl. [Invention 1280] Cy 3B Substitution C 3~10 A cycloalkyl compound or a salt thereof from any of the compounds 1222 to 1264 of the present invention. [Invention 1281] Cy 3B Compounds of the present invention 1280 or salts thereof, wherein is substituted with cyclopentyl, cyclohexyl, or cycloheptyl. [Invention 1282] Cy 3B A compound or salt thereof according to any of the present invention 1222 to 1264, wherein is a substituted 4- to 10-membered heterocycloalkyl group. [Invention 1283] Cy 3B However, R Cy3B , halogen, and C 1~6 Each R is substituted with one, two, three, four, or five substituents independently selected from the haloalkyl groups; Cy3B C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 6~10 Selected from aryl or 5-10 member heteroaryl, R Cy3B Each C that forms 6~10 Aryl or 5-10 member heteroaryl compounds, either unsubstituted or halogenated, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 A compound or salt thereof according to any of the inventions 1275 to 1282, substituted with one, two, or three substituents independently selected from alkynyl and haloalkyl groups. [Invention 1284] R 33 However, the following is based on: Phenyl; Benzyl; 2-phenylethyl; 2,3-dihydro-1H-inden-2-yl; 2-(2-methylphenyl)ethyl; 2-(3-methylphenyl)ethyl; 2-(4-methylphenyl)ethyl; 2-(2,4-dimethylphenyl)ethyl; 2-(2,5-dimethylphenyl)ethyl; 2-(3,5-dimethylphenyl)ethyl; 2-(2-ethylphenyl)ethyl; 2-(3-ethylphenyl)ethyl; 2-(4-ethylphenyl)ethyl; 2-(2,4-diethylphenyl)ethyl; 2-(2,5-dimethylphenyl)ethyl; 2-(3,5-dimethylphenyl)ethyl; 2-(2-trifluoromethylphenyl)ethyl; 2-(3-trifluoromethylphenyl)ethyl; 2-(4-trifluoromethylphenyl)ethyl; 2-(2-fluorophenyl)ethyl; 2-(3-fluorophenyl)ethyl; 2-(4-fluorophenyl)ethyl; 2-(2,4-difluorophenyl)ethyl; 2-(2,5-difluorophenyl)ethyl; 2-(3,5-difluorophenyl)ethyl; 2-(2-chlorophenyl)ethyl; 2-(3-chlorophenyl)ethyl; 2-(4-chlorophenyl)ethyl; 2-(2,4-dichlorophenyl)ethyl; 2-(2,5-dichlorophenyl)ethyl; 2-(3,5-dichlorophenyl)ethyl; 2-(2-methoxyphenyl)ethyl; 2-(3-methoxyphenyl)ethyl; 2-(4-methoxyphenyl)ethyl; 2-(2,4-dimethoxyphenyl)ethyl; 2-(2,5-dimethoxyphenyl)ethyl; 2-(3,5-dimethoxyphenyl)ethyl; 2-(cyclopentyl)ethyl; 2-(cyclohexyl)ethyl; 2-(cycloheptyl)ethyl; 2-(2-(aminomethyl)phenyl)ethyl; 2-(3-(aminomethyl)phenyl)ethyl; 2-(4-(aminomethyl)phenyl)ethyl; 2-(2-cyanophenyl)ethyl; 2-(3-cyanophenyl)ethyl; and 2-(4-cyanophenyl)ethyl; and The basis of the following formula: A compound or salt thereof from any of the 1222-1283 of the present invention, selected from TIFF0007829249000101.tif54131. [Invention 1285] R 34 A compound or salt thereof according to any of the inventions 1222 to 1284, wherein the compound is hydrogen. [Invention 1286] R 34 C 1~6 A compound or salt thereof from any of the compounds described in invention 1222 to 1284, which is alkyl, for example, methyl. [Invention 1287] R 35 A compound or salt thereof according to any of the inventions 1222 to 1286, wherein the compound is H. [Invention 1288] R 35 Cy 3C A compound or salt thereof according to any of the compounds 1222 to 1286 of the present invention. [Invention 1289] R 35 is non-substituted C 1~6 A compound or salt thereof from any of the compounds 1222 to 1286 of the present invention, which is alkyl. [Invention 1290] R 35 Substitution C 1~6 A compound or salt thereof from any of the compounds 1222 to 1286 of the present invention, which is alkyl. [Invention 1291] R 35 Substitution C that forms 1~6 The alkyl group is substituted with at least one substituent, R 35 The substituents of Cy 3C , halogen, CN, OR a31 , SR a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , NR c31 R d31 , NR c31 C(O)Rb31 , NR c31 C(O)NR c31 R d31 , NR c31 C(O)OR a31 , C(=NR e31 )NR c31 R d31 , NR c31 C(=NR e31 )NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 S(O)2R b31 , NR c31 S(O)2R b31 , S(O)2NR c31 R d31 A compound of the present invention 1290 or a salt thereof, wherein one, two, or three substituents are selected from the group consisting of , and oxo. [Invention 1292] R 35 Substitution C that forms 1~6 The alkyl group is substituted with at least one substituent, and the substituent is Cy 3C Compounds of the present invention 1290 or 1291 or salts thereof, including the compound or salt of the present invention. [Invention 1293] R 35 Substitution C that forms 1~6 The alkyl group is substituted with one substituent, and the substituent is Cy 3C The compound or salt thereof according to the present invention 1292. [Invention 1294] R 35 (CH2) 1~5 Cy 3C A compound or salt thereof according to any of the inventions 1290 to 1293. [Invention 1295] R 35 CH2Cy 3C The compound or salt thereof according to the present invention 1294. [Invention 1296] Cy 3C is non-substituted C 6~10 A compound or salt thereof according to any of the inventions 1222 to 1295, which is aryl. [Invention 1297] Cy 3C A compound of the present invention 1296 or a salt thereof, wherein is an unsubstituted phenyl or naphthyl, for example, 1-naphthyl or 2-naphthyl. [Invention 1298] Cy 3C A compound or salt thereof according to any of the invention items 1222 to 1295, wherein is an unsubstituted 5- to 10-membered heteroaryl compound. [Invention 1299] Cy 3C Compounds of the present invention 1298 or salts thereof, wherein is an unsubstituted pyridyl, e.g., unsubstituted 2-, 3-, or 4-pyridyl; an unsubstituted quinolyl, e.g., unsubstituted 2-, 3-, 4-, 5-, 6-, or 8-quinolyl; an unsubstituted benzo[b]thiophenyl, e.g., unsubstituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or an unsubstituted indolyl, e.g., unsubstituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl. [Invention 1300] Cy 3C is non-substituted C 3~10 A compound or salt thereof from any of the compounds of the present invention 1222 to 1295, such as cycloalkyl, for example cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. [Invention 1301] Cy 3C A compound or salt thereof according to any of the invention items 1222 to 1295, wherein is an unsubstituted 4- to 10-membered heterocycloalkyl group. [Invention 1302] Cy 3C Substitution C 6~10 A compound or salt thereof according to any of the inventions 1222 to 1295, which is aryl. [Invention 1303] Cy 3C A compound of the present invention 1302 or a salt thereof, wherein is a substituted phenyl or substituted naphthyl, for example, substituted 1-naphthyl or 2-naphthyl. [Invention 1304] Cy 3CA compound or salt thereof according to any of the inventions 1222 to 1295, wherein is a substituted 5- to 10-membered heteroaryl compound. [Invention 1305] Cy 3C Compounds of the present invention 1304 or salts thereof, wherein is a substituted pyridyl, e.g., a substituted 2-, 3-, or 4-pyridyl; a substituted quinolyl, e.g., a substituted 2-, 3-, 4-, 5-, 6-, or 8-quinolyl; a substituted benzo[b]thiophenyl, e.g., a substituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or a substituted indolyl, e.g., a substituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl. [Invention 1306] Cy 3C Substitution C 3~10 A compound or salt thereof from any of the inventions 1222 to 1295, which is a cycloalkyl compound, for example, substituted cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. [Invention 1307] Cy 3C A compound or salt thereof according to any of the invention items 1222 to 1295, wherein is a substituted 4- to 10-membered heterocycloalkyl group. [Invention 1308] R 36 A compound or salt thereof according to any of the inventions 1222 to 1307, wherein the compound is H. [Invention 1309] R 36 C 1~6 A compound or salt thereof from any of the compounds in Invention 1222 to 1307, which is alkyl, for example, methyl. [Invention 1310] R a31 , R b31 , R c31 , R d31 , R a32 , R b32 , R c32 , and R d32 H and C are independent of each other. 1~6 A compound selected from alkyl groups, any of the compounds described in Invention 1222 to 1309, or a salt thereof. [Invention 1311] Each R e31 and each R e32 A compound or salt thereof from any of the inventions 1222 to 1310, wherein the element is H. [Invention 1312] A pharmaceutical composition comprising any compound according to invention 1222 to 1311 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1313] Compounds of formula (IV) or salts thereof for use in the treatment of MASP-2 related diseases or disorders: TIFF0007829249000102.tif24128In formula, Cy 4A is either non-substituted or substituted C 6~10 It is an aryl or unsubstituted or substituted 5-10 member heteroaryl; Cy 4A The ring atoms of the 5-10 membered heteroaryl that form the Cy 4A Substitution C that forms 6~10 Aryl or substituted 5-10 member heteroaryls are R Cy4A , halogen, C 1~6 Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)Rb41 )NR c41 R d41 , C(=NR e41 )NR c41 C(O)OR a41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy4A C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy4A The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R group consist of one, two, three, or four heteroatoms selected from carbon atoms and O, N, and S. Cy4A Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 Rd41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo, R Cy4A Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo; R 41 is H, or C 1~6 Alkyl, C 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 It is alkyl, R 41 C that forms 1~6 Alkyls are either unsubstituted or contain halogens, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo, R 41 C that forms 6~10 Aryl-C 1~6Alkyl or 5-10 member heteroaryl-C 1~6 Alkyl is either unsubstituted or C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo; R 42 H, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, or Cy 4B And; R 42 C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Each alkynyl is either unsubstituted or Cy 4B , halogen, CN, OR a41 , SRa41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 It is substituted with one, two, three, four, or five substituents selected from the group consisting of , and oxo; however, one or fewer substituents are Cy 4B and; Cy 4B is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 4B The ring atoms of the 5-10 membered heteroaryl or unsubstituted or substituted 4-10 membered heterocycloalkyl rings consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 4B Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or 4-10 member heterocycloalkyls, are R Cy4B , halogen, C1~6 Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)R b41 )NR c41 R d41 , C(=NR e41 )NR c41 C(O)OR a41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy4B C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy4BThe ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S, R Cy4B Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo; each R Cy4B Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo; or, R 41 and R 42 These are the atoms to which they are bonded, as well as R 41 and R 42 Together with the nitrogen atom linking the bonded atom, it forms a 4-7 membered heterocycloalkyl ring, which is R Cy4B , halogen, C 1~6 Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NRc41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)R b41 )NR c41 R d41 , C(=NR e41 )NR c41 C(O)OR a41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 They may be further substituted with one, two, three, four, or five substituents independently selected from the oxo; R 43 H, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, or Cy 4C And; R 43 C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Each alkynyl is either unsubstituted or Cy 4C , halogen, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 Rd41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 Substituting with 1, 2, 3, 4, or 5 substituents independently selected from 0, 1, 2, 3, 4, or 5 substituents selected from the group consisting of , and oxo, however, R 43 C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 The substituents of the alkynyl molecule are Cy 4C and; Cy 4C is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 4B The ring atoms of the 5-10 membered heteroaryl or unsubstituted or substituted 4-10 membered heterocycloalkyl rings consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 4C Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or 4-10 member heterocycloalkyls, are R Cy4C , halogen, C 1~6 Haloalkyl, CN, OR a41, SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)R b41 )NR c41 R d41 , C(=NR e41 )NR c41 C(O)OR a41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy4C C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy4CThe ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S, R Cy4C Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo; each R Cy4A Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 , and are substituted with one, two, or three substituents independently selected from the oxo; R a41 , R b41 , R c41 , and R d41 H and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a41, R b41 , R c41 , and R d41 The C that forms 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Each alkyl group is C 1~6 Alkyl, Halo, CN, OR a42 , SR a42 , C(O)R b42 , C(O)NR c42 R d42 , C(O)OR a42 ,OC(O)R b42 , OC(O)NR c42 R d42 , NR c42 R d42 , NR c42 C(O)R b42 , NR c42 C(O)NR c42 R d42 , NR c42 C(O)OR a42 , C(=NR e42 )NR c42 R d42 , NR c42 C(=NR e42 )NR c42 R d42 , S(O)R b42 , S(O)NR c42 R d42 S(O)2R b42 , NR c42 S(O)2R b42 , S(O)2NR c42 R d42 , and may be substituted with one, two, three, four, or five substituents independently selected from the oxo; or, R bonded to the same N atom c41 and R d41 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each being C 1~6 Alkyl, Halo, CN, OR a42 , SR a42 , C(O)R b42 , C(O)NR c42 R d42 , C(O)OR a42 ,OC(O)R b42 , OC(O)NR c42 R d42 , NR c42 R d42 , NR c42 C(O)R b42 , NR c42 C(O)NR c42 R d42 , NR c42 C(O)OR a42 , C(=NR e42 )NR c42 R d42 , NR c42 C(=NR e42 )NR c42 R d42 , S(O)R b42 , S(O)NR c42 R d42 S(O)2R b42 , NR c42 S(O)2R b42 , S(O)2NR c42 R d42 , and may be substituted with one, two, or three substituents independently selected from the oxo; R a42 , R b42 , R c42 , and R d42 H and C are independent of each other. 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a42 , R b42 , R c42 , and R d42 The C that forms 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Alkyl compounds are OH, CN, amino, and NH(C) respectively. 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 It may be substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; or, R bonded to the same N atom c42 and R d42 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is either unsubstituted or OH, CN, amino, NH(C) 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 Substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; Re41 and R e42 Each of these is independently H, CN, or NO2. [Invention 1314] Cy 4A A compound or salt thereof according to Invention 1313, wherein is unsubstituted or substituted aryl. [Invention 1315] Cy 4A A compound of the present invention 1314 or a salt thereof, wherein is an unsubstituted or substituted phenyl. [Invention 1316] Cy 4A A compound of the present invention 1315 or a salt thereof, wherein is a substituted phenyl compound. [Invention 1317] Cy 4A at least one OR a41 or at least one C(=NR) e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)R b41 )NR c41 R d41 , or C(=NR e41 )NR c41 C(O)OR a41 A compound or salt thereof according to any of the inventions 1313 to 1316, which is substituted with [the specified compound]. [Invention 1318] Cy 4A at least one OR a41 It is replaced with and C 1~6 Alkyl, C 1~6 A compound or salt thereof according to any of the present invention 1313 to 1317, which is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens. [Invention 1319] Cy 4A It is substituted with at least one OH group, and C 1~6 Alkyl, C 1~6A compound or salt thereof according to any of the inventions 1313 to 1318, which is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens. [Invention 1320] Cy 4A Preferably at position 4, at least one C(=NR e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)R b41 )NR c41 R d41 , C(=NR e41 )NR c41 C(O)OR a41 A compound or salt thereof according to any of the inventions 1313 to 1319, which is substituted with [the specified compound]. [Invention 1321] Cy 4A Preferably at position 4, at least one C(=NR e41 )NR c41 R d41 , for example, a compound of the present invention 1320 or a salt thereof, which is substituted with C(=NH)NH2. [Invention 1322] Cy 4A The formula is as follows: A compound of the present invention 1316 or a salt thereof, which is one of TIFF0007829249000103.tif76131 or TIFF0007829249000104.tif177136. [Invention 1323] Cy 4A In the formula defining R a41 C 1~6 Alkyl, for example, methyl, R b41 C 1~6 Alkyl, for example, methyl, R b41 C 1~6 Haloalkyls, for example, trifluoromethyl, R c41 A compound of the present invention 1322 or a salt thereof, wherein the alkyl group is, for example, methyl. [Invention 1324] Cy4A A compound or salt thereof according to Invention 1313, wherein is unsubstituted or substituted heteroaryl. [Invention 1325] Cy 4A A compound of the present invention 1324 or a salt thereof, wherein is unsubstituted or substituted pyridine-3-yl, 1H-pyrrolo[2,3-b]pyridine-5-yl, or 1H-benzo[d]imidazole-6-yl. [Invention 1326] Cy 4A The formula is as follows: A compound or salt thereof of the present invention 1324 or 1325, which is one of the following: TIFF0007829249000105.tif178128TIFF0007829249000106.tif219137TIFF0007829249000107.tif224134TIFF0007829249000108.tif228137TIFF0007829249000109.tif126134. [Invention 1327] Cy 4A Each R in the formula defining Cy4AA C 1~6 A compound of the present invention 1326 or a salt thereof, wherein the compound is an alkyl group, for example methyl or ethyl, preferably methyl, or a halogen, for example F, Cl, or Br, preferably Cl. [Invention 1328] Cy 4A Each R bonded to nitrogen in the formula defining the Cy4A C 1~6 Compounds of the present invention 1326 or 1327 or salts thereof, wherein the compound is alkyl, for example, methyl or ethyl. [Invention 1329] R 41 A compound or salt thereof from any of the inventions 1313 to 1328, wherein the compound is H. [Invention 1330] R 41 C 1~6 A compound or salt thereof from any of the compounds 1313 to 1328 of the present invention, which is alkyl. [Invention 1331] R 41A compound of the present invention 1330 or a salt thereof, wherein the compound is methyl. [Invention 1332] R 42 A compound or salt thereof according to any of the inventions 1313 to 1331, wherein the element is H. [Invention 1333] R 42 is non-substituted C 1~6 A compound or salt thereof from any of the compounds 1313 to 1331 of the present invention, which is alkyl, for example, methyl. [Invention 1334] R 42 Cy 4B A compound or salt thereof according to any of the inventions 1313 to 1331. [Invention 1335] R 42 Substitution C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 A compound or salt thereof that is an alkynyl, as described in any of the invention items 1313 to 1331. [Invention 1336] R 42 Substitution C 1~6 A compound of the present invention 1335 or a salt thereof, which is alkyl. [Invention 1337] R 42 Substitution C 1~6 It is alkyl, R 42 C that forms 1~6 Alkyl, Cy 4B , halogen, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41, C(=NR e41 )NR c41 R d41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 Substituting with one, two, or three substituents selected from the group consisting of , and oxo; provided that one or fewer substituents are Cy 4B The compound of the present invention 1335 or a salt thereof. [Invention 1338] R 42 Substitution C that forms 1~6 The alkyl group is substituted with at least one substituent, and the substituent is Cy 4B Compounds of the present invention 1336 or 1337 or salts thereof, including the compound or salt of the present invention. [Invention 1339] R 35 Substitution C that forms 1~6 The alkyl group is substituted with one substituent, and the substituent is Cy 4B The compound or salt thereof according to the present invention 1338. [Invention 1340] R 42 (CH2) 1~5 Cy 4B The compound or salt thereof according to the present invention 1339. [Invention 1341] R 42 CH2Cy 4B The compound of the present invention 1340 or a salt thereof. [Invention 1342] Cy 4B is non-substituted C 6~10 Aryl, for example, unsubstituted phenyl or naphthyl, for example, 1-naphthyl or 2-naphthyl, Cy 4Bis an unsubstituted 5-10 member heteroaryl, for example, unsubstituted pyridyl, for example, unsubstituted 2-, 3-, or 4-pyridyl; unsubstituted quinolyl, for example, unsubstituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl; unsubstituted benzo[b]thiophenyl, for example, unsubstituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or unsubstituted indolyl, for example, unsubstituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl, and Cy 4B is non-substituted C 3~10 Cycloalkyl, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, or Cy 4B A compound or salt thereof according to any of the invention items 1313 to 1341, wherein is an unsubstituted 4- to 10-membered heterocycloalkyl group. [Invention 1343] Cy 4B Substitution C 6~10 Aryl, for example substituted phenyl or naphthyl, for example 1-naphthyl or 2-naphthyl, Cy 4B is a substituted 5- to 10-membered heteroaryl, for example, a substituted pyridyl, for example, a substituted 2-, 3-, or 4-pyridyl; a substituted quinolyl, for example, a substituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl; a substituted benzo[b]thiophenyl, for example, a substituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or a substituted indolyl, for example, a substituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl, and Cy 4B Substitution C 3~10 Cycloalkyl, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, or Cy 4B A compound or salt thereof from any of the invention items 1313 to 1341, wherein is a substituted 4- to 10-membered heterocycloalkyl group. [Invention 1344] R 41 and R 42 However, the atoms to which they are bonded, as well as R 41 and R 42Together with the nitrogen atom linking the bonded atom, it forms a 4-7 membered heterocycloalkyl ring, which is R Cy4B , halogen, C 1~6 Haloalkyl, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41 , C(=NOR a41 )NR c41 R d41 , C(=NOC(O)R b41 )NR c41 R d41 , C(=NR e41 )NR c41 C(O)OR a41 , NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 A compound or salt thereof from any of the inventions 1313 to 1328, which may be further substituted with one, two, three, four, or five substituents independently selected from the oxo and the oxo. [Invention 1345] R 41 and R 42 However, the atoms to which they are bonded, as well as R 41and R 42 A compound or salt thereof according to the present invention 1344, wherein the bonded atom, together with a nitrogen atom linking the bonded atom, forms a five-membered or six-membered heterocycloalkyl ring. [Invention 1346] The following equations (IV-1), (IV-2), (IV-1a), (IV-1b), (IV-2a), or (IV-2b): A compound of Invention 1345 or a salt thereof that matches any of TIFF0007829249000110.tif101128. [Invention 1347] R 43 Cy 4C A compound or salt thereof according to any of the inventions 1313 to 1346. [Invention 1348] R 43 is non-substituted C 1~6 A compound or salt thereof from any of the compounds 1313 to 1346 of the present invention, which is alkyl. [Invention 1349] R 43 Substitution C 1~6 A compound or salt thereof from any of the compounds 1313 to 1346 of the present invention, which is alkyl. [Invention 1350] R 43 Substitution C that forms 1~6 Alkyl, Cy 4C , halogen, CN, OR a41 , SR a41 , C(O)R b41 , C(O)NR c41 R d41 , C(O)OR a41 ,OC(O)R b41 , OC(O)NR c41 R d41 , NR c41 R d41 , NR c41 C(O)R b41 , NR c41 C(O)NR c41 R d41 , NR c41 C(O)OR a41 , C(=NR e41 )NR c41 R d41, NR c41 C(=NR e41 )NR c41 R d41 , S(O)R b41 , S(O)NR c41 R d41 S(O)2R b41 , NR c41 S(O)2R b41 , S(O)2NR c41 R d41 A compound of the present invention 1349 or a salt thereof, substituted with at least one substituent independently selected from one, two, or three substituents selected from the group consisting of , and oxo. [Invention 1351] R 43 Substitution C that forms 1~6 The alkyl group is substituted with at least one substituent, and the substituent is Cy 4C Compounds of the present invention 1349 or 1350 or salts thereof, including the compound or salt of the present invention. [Invention 1352] R 43 Substitution C that forms 1~6 The alkyl group is substituted with one substituent, and the substituent is Cy 4C The compound of the present invention 1351 or a salt thereof. [Invention 1353] R 43 (CH2) 1~5 Cy 4C A compound or salt thereof according to any of the inventions 1349 to 1352. [Invention 1354] R 43 CH2Cy 4C The compound of the present invention 1353 or a salt thereof. [Invention 1355] R 43 CH2CH2Cy 4C The compound of the present invention 1353 or a salt thereof. [Invention 1356] R 43 CF2Cy 4C Or CF2CH2Cy 4C The compound of the present invention 1351 or a salt thereof. [Invention 1357] Cy 4C is non-substituted C 6~10 A compound or salt thereof from any of the compounds in Invention 1313 to 1356, for example, aryl, such as phenyl, 1-naphthyl, or 2-naphthyl. [Invention 1358] Cy 4C A compound or salt thereof according to any of the Invention 1313 to 1356, wherein is an unsubstituted 5- to 10-membered heteroaryl, for example, unsubstituted pyridyl, for example, unsubstituted 2-, 3-, or 4-pyridyl; an unsubstituted quinolyl, for example, unsubstituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl; an unsubstituted benzo[b]thiophenyl, for example, unsubstituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or an unsubstituted indolyl, for example, unsubstituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl. [Invention 1359] Cy 4C is non-substituted C 3~10 A compound or salt thereof from any of the compounds in Invention 1313 to 1356, for example, cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. [Invention 1360] Cy 4C A compound or salt thereof according to any of the present invention 1313 to 1356, wherein is an unsubstituted 4- to 10-membered heterocycloalkyl group. [Invention 1361] Cy 4C Substitution C 6~10 A compound or salt thereof according to any of the inventions 1313 to 1356, which is an aryl compound, for example, a substituted phenyl, a substituted 1-naphthyl, or a substituted 2-naphthyl. [Invention 1362] Cy 4CA compound or salt thereof according to any of the Invention 1313 to 1356, wherein is a substituted 5- to 10-membered heteroaryl, for example, a substituted pyridyl, for example, a substituted 2-, 3-, or 4-pyridyl; a substituted quinolyl, for example, a substituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyl; a substituted benzo[b]thiophenyl, for example, a substituted 2-, 3-, 4-, 5-, 6-, or 7-benzo[b]thiophenyl; or a substituted indolyl, for example, a substituted indole-2-yl, -3-yl, -4-yl, -5-yl, -6-yl, or -7-yl. [Invention 1363] Cy 4C Substitution C 3~10 A compound or salt thereof from any of the compounds in Invention 1313 to 1356, for example, a cycloalkyl compound, such as substituted cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. [Invention 1364] Cy 4C A compound or salt thereof from any of the invention items 1313 to 1356, wherein is a substituted 4- to 10-membered heterocycloalkyl group. [Invention 1365] The following equations (IV-3) to (IV-7), (IV-3a), (IV-3b), (IV-5a), (IV-5b), (IV-7a), or (IV-7b): A compound or salt thereof from any of the inventions 1313 to 1364 that matches any of TIFF0007829249000111.tif198138. [Invention 1366] R a41 , R b41 , R c41 , R d41 , R a42 , R b42 , R c42 , and R d42 H and C are independent of each other. 1~6 A compound selected from alkyl groups, any of the compounds 1313 to 1365 of this invention, or a salt thereof. [Invention 1367] Each R e41 and each R e42 A compound or salt thereof according to any of the inventions 1313 to 1366, wherein the compound is H. [Invention 1368] A pharmaceutical composition comprising any compound according to invention 1313 to 1367 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1369] MASP-2 inhibitory compounds of formula (VA) or (VB) or a salt thereof, for therapeutic use in the treatment of MASP-2-related diseases or disorders: TIFF0007829249000112.tif46128In formula, A 1 -(C=NH)-, -(C=NOR a )-,-[C=NO(C=O)R a ]-,-[C=N[O(C=O)ZR b The member is selected from the group consisting of ]}-, condensed 5-membered or 6-membered heterocyclyls, and condensed 5-membered or 6-membered heteroaryls; A 1 If Y is -(C=NH)-, 1 -NH2, -NH(C=O)R a , and -NH(C=O)ZR b Selected from the group consisting of; A 1 -(C=NOR a )-,-[C=NO(C=O)R a ]-, or -{C=N[O(C=O)ZR b ]}- If Y 1 is -NH2; A 1 If Y is a condensed heterocyclyl or heteroaryl, 1 is -NH2 or halo, A 1 m further R 1 It is substituted with the base; Each R a and R b These are independently C1-C6 alkyl and C3-C 10 Cycloalkyl, C6~C 10 Aryl, and C7~C 12 Selected from the group consisting of arylalkyl groups; R aIt has m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 alkylamino, and halo; or alternatively, R a and R b Together, they form a heterocyclyl ring having m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, and halo; Each Z is independently selected from the group consisting of O and S; A 2 This is a member selected from the group consisting of C3-C6 heteroaryls, C6 aryls, and C2-C6 alkyls; A 2 If Y is a C3-C6 heteroaryl, 2 -NH2, -CH2NH2, chloro, -(C=NH)NH2, -(C=NH)NH(C=O)R a -(C=NH)NH(C=O)ZR b ,-(C=NOR a )NH2, -[C=NO(C=O)R a ]NH2, and -{C=N[O(C=O)ZR b Selected from the group consisting of ]}NH2; A 2 m further R 1 It is substituted with the base; A 2 If it is a C6 aryl, then Y 2 A is selected from the group consisting of aminomethyl, hydroxy, and halo. 2 m further R 1 It is substituted with the base; A 2 If it is a C2-C6 alkyl group, Y 2 is -NH(C=NH)NH2, -NH(C=NH)NH(C=O)R a , and -NH(C=NH)NH(C=O)ZR b Selected from the group consisting of; Each R 1is a member independently selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, amino, C1-C6 alkylamino, and halo; Each m and n is an independently selected integer between 0 and 3; L is -(O) p -(C(R 2a )(R 2b )) q -and, Each R 2a or R 2b is a member independently selected from the group consisting of hydrogen and fluoro; p is an integer between 0 and 1; q is an integer between 1 and 2; R 3 is a member selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 fluoroalkyl, and carboxy(C1-C6 alkyl); or alternatively, R 3 and R 4 They combine to form an azetidine ring, a pyrrolidine ring, or a piperidine ring; R 4 is a member selected from the group consisting of hydrogen and C1-C6 alkyl groups; or alternatively, R 4 and R 3 They combine to form an azetidine ring, a pyrrolidine ring, or a piperidine ring; R 5 These include C3-C7 cycloalkyl, C4-C8 cycloalkylalkyl, heteroaryl, and C7-C 12 Arylalkyl or heteroarylalkyl (0-3 R 13 A member selected from the group consisting of (having substituents); or alternatively, R 5 and R 6 Together, they form 0 to 3 R 13 Forming a heterocycle with substituents; R 6 These are hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, carboxy(C1-C6 alkyl), C7-C 12 Arylalkyl or heteroarylalkyl (0-3 R13 A member selected from the group consisting of (having substituents), amino(C1-C8 alkyl), and amide(C1-C8 alkyl); or alternatively, R 6 and R 5 Together, they form 0 to 3 R 13 Forming a heterocycle with substituents; Each R 13 C1-C6 alkyl, C6-C 10 Ariel, (C6~C 10 Aryl)C1-C6 alkyl, carboxy(C1-C6 alkyloxy), heteroaryl, (C6-C 10 A member independently selected from the group consisting of heteroaryl)C1-C6 alkyl, heterocyclyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 amide, C1-C6 alkylamino, and halo; or alternatively, two R 13 The groups combine and condense C6~C 10 Aryl ring, C6~C 10 It forms a heteroaryl ring or a C5-C7 cycloalkyl ring. [Invention 1370] MASP-2 inhibitory compounds of formula (VA) or (VB) or a salt thereof, for therapeutic use in the treatment of MASP-2-related diseases or disorders: TIFF0007829249000113.tif47128In formula, A 1 -(C=NH)-, -(C=NOR a )-,-[C=NO(C=O)R a ]-,-[C=N[O(C=O)ZR b The member is selected from the group consisting of ]}-, condensed 5-membered or 6-membered heterocyclyls, and condensed 5-membered or 6-membered heteroaryls; A 1 If Y is -(C=NH)-, 1 -NH2, -NH(C=O)R a , and -NH(C=O)ZR b Selected from the group consisting of; A1 -(C=NOR a )-,-[C=NO(C=O)R a ]-, or -{C=N[O(C=O)ZR b ]}- If Y 1 is -NH2; A 1 If Y is a condensed heterocyclyl or heteroaryl, 1 is -NH2 or halo, A 1 m further R 1 It is substituted with the base; Each R a and R b These are independently C1-C6 alkyl and C3-C 10 Cycloalkyl, C6~C 10 Aryl, and C7~C 12 Selected from the group consisting of arylalkyl groups; R a It has m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 alkylamino, and halo; or alternatively, R a and R b Together, they form a heterocyclyl ring having m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, and halo; Each Z is independently selected from the group consisting of O and S; A 2 This is a member selected from the group consisting of C3-C6 heteroaryls, C6 aryls, and C2-C6 alkyls; A 2 If Y is a C3-C6 heteroaryl, 2 -NH2, -CH2NH2, chloro, -(C=NH)NH2, -(C=NH)NH(C=O)R a -(C=NH)NH(C=O)ZR b ,-(C=NOR a )NH2, -[C=NO(C=O)R a ]NH2, and -{C=N[O(C=O)ZR bSelected from the group consisting of ]}NH2; A 2 m further R 1 It is substituted with the base; A 2 If it is a C6 aryl, then Y 2 A is selected from the group consisting of aminomethyl, hydroxy, and halo. 2 m further R 1 It is substituted with the base; A 2 If it is a C2-C6 alkyl group, Y 2 is -NH(C=NH)NH2, -NH(C=NH)NH(C=O)R a , and -NH(C=NH)NH(C=O)ZR b Selected from the group consisting of; Each R 1 is a member independently selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, amino, C1-C6 alkylamino, and halo; Each m and n is an independently selected integer between 0 and 3; L is -(O) p -(C(R 2a )(R 2b )) q -and, Each R 2a or R 2b is a member independently selected from the group consisting of hydrogen and fluoro; p is an integer between 0 and 1; q is an integer between 1 and 2; R 3 is a member selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 fluoroalkyl, and carboxy(C1-C6 alkyl); or alternatively, R 3 and R 4 They combine to form an azetidine ring, a pyrrolidine ring, or a piperidine ring; R 4 is a member selected from the group consisting of hydrogen and C1-C6 alkyl groups; or alternatively, R 4 and R 3They combine to form an azetidine ring, a pyrrolidine ring, or a piperidine ring; R 5 These include C3-C7 cycloalkyl, C4-C8 cycloalkylalkyl, heteroaryl, and C7-C 12 Arylalkyl or heteroarylalkyl (0-3 R 13 A member selected from the group consisting of (having substituents); or alternatively, R 5 and R 6 Together, they form 0 to 3 R 13 Forming a heterocycle with substituents; R 6 These are hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, carboxy(C1-C6 alkyl), C7-C 12 Arylalkyl or heteroarylalkyl (0-3 R 13 A member selected from the group consisting of (having substituents), amino(C1-C8 alkyl), and amide(C1-C8 alkyl); or alternatively, R 6 and R 5 Together, they form 0 to 3 R 13 Forming a heterocycle with substituents; Each R 13 C1-C6 alkyl, C6-C 10 A member independently selected from the group consisting of aryl, carboxy(C1-C6 alkyloxy), heteroaryl, heterocyclyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 amide, C1-C6 alkylamino, and halo; or alternatively, two R 13 The groups combine and condense C6~C 10 Aryl ring, C6~C 10 It forms a heteroaryl ring or a C5-C7 cycloalkyl ring; However, the compound is not melagatran. [Invention 1371] A compound of formula VA, which is a compound of invention 1369 or 1370 or a salt thereof. [Invention 1372] A compound or salt thereof selected from the group consisting of compounds of formula (VC) to (VF) and their salts, as described in any of the inventions 1369 to 1371: TIFF0007829249000114.tif63144In formula, R 7 This is a member selected from the group consisting of hydrogen, hydroxyl, and C1-C6 alkyl groups; R 8 is a member selected from the group consisting of hydrogen and C1-C6 alkyl groups; Each m and n is an independently selected integer between 0 and 2. [Invention 1373] R 7 A compound or salt thereof according to any of the inventions 1369 to 1372, wherein the compound is hydrogen. [Invention 1374] R 8 A compound or salt thereof according to any of the inventions 1369 to 1373, wherein the compound is hydrogen. [Invention 1375] A 1 A compound of the present invention 1371 or a salt thereof, wherein the compound is -(C=NH)-. [Invention 1376] A 1 A compound or salt thereof according to the present invention 1371, wherein is a condensed heteroaryl compound. [Invention 1377] Y 1 A compound or salt thereof of the present invention 1375 or 1376, wherein -NH2. [Invention 1378] A compound of formula VB, which is a compound of invention 1369 or 1370 or a salt thereof. [Invention 1379] A 2 A compound or salt thereof according to Invention 1378, wherein the compound is a C6 aryl compound. [Invention 1380] Y 2 A compound or salt thereof of the present invention 1378 or 1379, wherein the compound is 3-chloro. [Invention 1381] A 2A compound of the present invention 1378 or a salt thereof, wherein the compound is a C2-C6 alkyl group. [Invention 1382] Y 2 A compound or salt thereof according to any of the inventions 1378 to 1381, wherein -NH(C=NH)NH2. [Invention 1383] The following R 3 Stereochemical configuration A compound or salt thereof according to any of the invention items 1369 to 1382, showing TIFF0007829249000115.tif15128. [Invention 1384] R 3 A compound or salt thereof from any of the inventions 1369 to 1383, wherein the compound is a member selected from the group consisting of hydrogen or methyl. [Invention 1385] R 3 A compound of the present invention 1384 or a salt thereof, wherein the compound is methyl. [Invention 1386] R 4 A compound or salt thereof from any of the invention items 1369 to 1385, wherein the compound is a member selected from the group consisting of hydrogen or methyl. [Invention 1387] R 4 A compound or salt thereof according to Invention 1386, wherein the compound is hydrogen. [Invention 1388] R 3 and R 4 A compound or salt thereof according to any of the inventions 1369 to 1383, wherein the compounds together form an azetidine ring, a pyrrolidine ring, or a piperidine ring. [Invention 1389] R 3 and R 4 A compound or salt thereof according to the present invention 1388, wherein these elements combine to form a pyrrolidine ring. [Invention 1390] R 3 and R 4 A compound or salt thereof according to the present invention 1388, wherein these compounds combine to form a piperidine ring. [Invention 1391] R5 However, 2,3-dihydro-1H-inden-2-yl, cyclohexyl, cyclohexylmethyl, phenyl, benzyl, phenethyl, and phenpropyl (0-5 R 13 A compound or salt thereof from any of the inventions 1369 to 1390, which is a member selected from the group consisting of (having substituents). [Invention 1392] R 5 A compound of the present invention 1391 or a salt thereof, wherein the compound is a member selected from the group consisting of phenethyl, 4-methylphenethyl, 4-chlorophenethyl, 4-fluorophenethyl, 3-methylphenethyl, 3-chlorophenethyl, 3-fluorophenethyl, 2-methylphenpropyl, 2-chlorophenpropyl, 2-fluorophenpropyl, 3-methylphenpropyl, 3-chlorophenpropyl, 3-fluorophenpropyl, 2-methylphenpropyl, 2-chlorophenpropyl, and 2-fluorophenpropyl. [Invention 1393] R 6 However, amino(C1~C8 alkyl) and C7~C 12 Arylalkyl (0-3 R 13 A compound or salt thereof from any of the inventions 1369 to 1392, which is a member selected from the group consisting of (having substituents). [Invention 1394] R 6 A compound or salt thereof from any of the inventions 1369 to 1393, wherein the compound is a member selected from the group consisting of hydrogen and carboxymethyl. [Invention 1395] R 6 and R 5 A compound or salt thereof according to any of the inventions 1369 to 1391, wherein the elements together form a pyrrolidine ring, an octahydro-1H-indole ring, a 3-phenylpyrrolidine ring, a piperidine ring, a 1,2,3,4-tetrahydroisoquinoline ring, a 2,5-dihydro-1H-pyrrole ring, or a 1,2,3,6-tetrahydropyridine ring. [Invention 1396] R 1 A compound or salt thereof from any of the inventions 1369 to 1395, wherein the compound is a hydroxyl or C1-C6 alkoxy. [Invention 1397] A compound or salt thereof according to any of the inventions 1369 to 1396, wherein n is 0. [Invention 1398] A compound or salt thereof according to any of the inventions 1369 to 1397, wherein p is 0. [Invention 1399] A compound or salt thereof from any of the inventions 1369 to 1398, wherein q is 1. [Invention 1400] Each R 2a or R 2b A compound or salt thereof according to any of the inventions 1369 to 1399, wherein the compound is hydrogen. [Invention 1401] A compound of the present invention 1400 or a salt thereof, wherein L is methylene. [Invention 1402] A pharmaceutical composition comprising any compound according to invention 1369 to 1401 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1403] MASP-2 inhibitory compounds of formula (VIA) or (VIB) or a salt thereof, for therapeutic use in the treatment of MASP-2-related diseases or disorders: TIFF0007829249000116.tif40128In formula, A 1 -(C=NH)-, -(C=NOR a )-,-[C=NO(C=O)R a ]-,-[C=N[O(C=O)ZR b The member is selected from the group consisting of ]}-, condensed 5-membered or 6-membered heterocyclyls, and condensed 5-membered or 6-membered heteroaryls; A 1 If Y is -(C=NH)-, 1 -NH2, -NH(C=O)R a , and -NH(C=O)ZR b Selected from the group consisting of; A 1 -(C=NOR a )-,-[C=NO(C=O)R a ]-, or -{C=N[O(C=O)ZR b ]}- If Y 1 is -NH2; A 1 If Y is a condensed heterocyclyl or heteroaryl, 1 is -NH2 or halo, A 1 m further R 1 It is substituted with the base; Each R a and R b These are independently C1-C6 alkyl and C3-C 10 Cycloalkyl, C6~C 10 Aryl, and C7~C 12 Selected from the group consisting of arylalkyl groups; R a It has m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 alkylamino, and halo; or alternatively, R a and R b Together, they form a heterocyclyl ring having m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, and halo; Each Z is independently selected from the group consisting of O and S; A 2 This is a member selected from the group consisting of C3-C6 heteroaryl and C2-C6 alkyl groups; A 2 If Y is a C3-C6 heteroaryl, 2 -NH2, -CH2NH2, chloro, -(C=NH)NH2, -(C=NH)NH(C=O)R a -(C=NH)NH(C=O)ZR b ,-(C=NOR a )NH2, -[C=NO(C=O)R a ]NH2, and -{C=N[O(C=O)ZR bSelected from the group consisting of ]}NH2; A 2 m further R 1 It is substituted with the base; A 2 If it is a C2-C6 alkyl group, Y 2 is -NH(C=NH)NH2, -NH(C=NH)NH(C=O)R a , and -NH(C=NH)NH(C=O)ZR b Selected from the group consisting of; Each R 1 is a member independently selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, amino, C1-C6 alkylamino, and halo; Each m and n is an independently selected integer between 0 and 3; X and X 2 These are, respectively, NR 8 , CH, and CR 10 A member selected from the group consisting of; Each R 8 is a member independently selected from the group consisting of hydrogen and C1-C6 alkyl groups; Each R 10 These are C1-C6 alkyl, heteroaryl, or C6-C 10 Aryl(0-3 R) 13 A member independently selected from the group consisting of (with substituents), hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 alkylamino, and halo; or alternatively, two R 10 The groups combine to form a condensed C6 aryl ring, a heteroaryl ring, or a C5-C7 cycloalkyl ring (0-3 R groups). 13 Forms (having substituents); r is an integer between 0 and 4; Each R 13 C1-C6 alkyl, C6-C 10A member independently selected from the group consisting of aryl, carboxy(C1-C6 alkyloxy), heteroaryl, heterocyclyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 amide, C1-C6 alkylamino, and halo; or alternatively, two R 13 The groups combine and condense C6~C 10 Aryl ring, C6~C 10 It forms a heteroaryl ring or a C5-C7 cycloalkyl ring. [Invention 1404] A compound of the present invention 1403 or a salt thereof, selected from the group consisting of compounds of the following formula and their salts: TIFF0007829249000117.tif24129In formula, Each R 7 This is a member selected from the group consisting of hydrogen, hydroxyl, and C1-C6 alkyl groups; m is an integer between 0 and 2. [Invention 1405] R 7 A compound or salt thereof according to the present invention 1403 or 1404, wherein the compound is hydrogen. [Invention 1406] (i) The compound is VIA or a salt thereof, and m is 0; or (ii) The compound is VIB or a salt thereof, and r is 0, and is a salt thereof, according to any of the compounds in Invention 1403 to 1405. [Invention 1407] X is NR 8 A compound or salt thereof according to any of the compounds 1403 to 1406 of the present invention. [Invention 1408] R 8 A compound or salt thereof according to Invention 1407, wherein the compound is hydrogen. [Invention 1409] X 2 is CH or CR 10 A compound or salt thereof according to any of the inventions 1403 to 1408. [Invention 1410] R 10However, C1-C6 alkyl, 0-3 R 13 A compound according to any of the invention 1403 to 1409 or a salt thereof, which is a member independently selected from the group consisting of substituted C6 aryl, C1-C6 alkoxy, and C2-C9 alkoxyalkyl compounds. [Invention 1411] 2 R 10 The bases come together, resulting in 0 to 3 R 13 A compound or salt thereof from any of the present inventions 1403 to 1410, which forms a fused C6 aryl ring having a substituent. [Invention 1412] R 1 A compound or salt thereof from any of the inventions 1403 to 1411, wherein the compound is a hydroxyl or C1-C6 alkoxy. [Invention 1413] A compound or salt thereof from any of the inventions 1403 to 1412, wherein p is 0. [Invention 1414] A compound or salt thereof from any of the inventions 1403 to 1413, wherein q is 1. [Invention 1415] Each R 2a or R 2b A compound or salt thereof according to any of the inventions 1403 to 1414, wherein the compound is hydrogen. [Invention 1416] A compound or salt thereof from any of the inventions 1403 to 1415, wherein L is methylene. [Invention 1417] A pharmaceutical composition comprising any compound from invention 1403 to 1416 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1418] MASP-2 inhibitory compounds for therapeutic use in the treatment of MASP-2-related diseases or disorders, comprising the following formula or a salt thereof: TIFF0007829249000118.tif69128In formula, A 1 -(C=NH)-, -(C=NOR a )-,-[C=NO(C=O)R a]-,-[C=N[O(C=O)ZR b The member is selected from the group consisting of ]}-, condensed 5-membered or 6-membered heterocyclyls, and condensed 5-membered or 6-membered heteroaryls; A 1 If Y is -(C=NH)-, 1 -NH2, -NH(C=O)R a , and -NH(C=O)ZR b Selected from the group consisting of; A 1 -(C=NOR a )-,-[C=NO(C=O)R a ]-, or -{C=N[O(C=O)ZR b ]}- If Y 1 is -NH2; A 1 If Y is a condensed heterocyclyl or heteroaryl, 1 is -NH2 or halo, A 1 m further R 1 It is substituted with the base; Each R a and R b These are independently C1-C6 alkyl and C3-C 10 Cycloalkyl, C6~C 10 Aryl, and C7~C 12 Selected from the group consisting of arylalkyl groups; R a It has m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 alkylamino, and halo; or alternatively, R a and R b Together, they form a heterocyclyl ring having m substituents selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, and halo; Each Z is independently selected from the group consisting of O and S; A 2 This is a member selected from the group consisting of C3-C6 heteroaryl and C2-C6 alkyl groups; A2 If Y is a C3-C6 heteroaryl, 2 -NH2, -CH2NH2, chloro, -(C=NH)NH2, -(C=NH)NH(C=O)R a -(C=NH)NH(C=O)ZR b ,-(C=NOR a )NH2, -[C=NO(C=O)R a ]NH2, and -{C=N[O(C=O)ZR b Selected from the group consisting of ]}NH2; A 2 m further R 1 It is substituted with the base; A 2 If it is a C2-C6 alkyl group, Y 2 is -NH(C=NH)NH2, -NH(C=NH)NH(C=O)R a , and -NH(C=NH)NH(C=O)ZR b Selected from the group consisting of; Each R 1 is a member independently selected from the group consisting of C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, amino, C1-C6 alkylamino, and halo; Each m and n is an independently selected integer between 0 and 3; L is -(O) p -(C(R 2a )(R 2b )) q -and, Each R 2a or R 2b is a member independently selected from the group consisting of hydrogen and fluoro; p is an integer between 0 and 1; q is an integer between 1 and 2; R 3 This is a member selected from the group consisting of hydrogen, C1-C6 alkyl, and carboxy(C1-C6 alkyl); Each R 11 C1-C6 alkyl, hydroxyl, C1-C6 alkoxy, amino, C1-C6 alkylamino, halo, and (R 14 )(R 14A member independently selected from the group consisting of )N(CO)-; or alternatively, two R 11 The groups combine to form a condensed C6 aryl ring, a heteroaryl ring, or a C5-C7 cycloalkyl ring (0-3 R groups). 13 Forms (having substituents); r is an integer between 0 and 4; Each Z is O and NR 8 A member independently selected from the group consisting of; Each R 8 is a member independently selected from the group consisting of hydrogen and C1-C6 alkyl groups; Each R 12 These are hydrogen, C1-C6 alkyl, and C7-C 14 Arylalkyl (0-3 R 13 A member independently selected from the group consisting of (having substituents); Each R 13 is a member independently selected from the group consisting of C1-C6 alkyl, hydroxyl, hydroxyl(C1-C6 alkyl), C1-C6 alkoxy, C2-C9 alkoxyalkyl, amino, C1-C6 alkylamino, and halo; or alternatively, two R 13 The groups combine to form condensed C6 aryl rings, heteroaryl rings, or C5-C7 cycloalkyl rings; Each R 14 These are hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C4-C8 cycloalkylalkyl, and C7-C 14 A member independently selected from the group consisting of arylalkyls and heteroaryls (C1-C6 alkyls); or alternatively, two R 13 The groups combine to form a condensed heterocyclyl ring. [Invention 1419] Compounds of the present invention 1418, which are of formula (VIIC) or a salt thereof, or a salt thereof: TIFF0007829249000119.tif38128In formula, each R 7 This member is selected from the group consisting of hydrogen, hydroxyl, and C1-C6 alkyl groups. [Invention 1420] R 7 A compound or salt thereof according to Invention 1418 or 1419, wherein the compound is hydrogen. [Invention 1421] R 3 A compound or salt thereof from any of the inventions 1418 to 1420, wherein the compound is a member selected from the group consisting of hydrogen or methyl. [Invention 1422] R 3 A compound of the present invention 1421 or a salt thereof, wherein the compound is methyl. [Invention 1423] A compound or salt thereof from any of the inventions 1418 to 1422, wherein Z is O. [Invention 1424] R 11 (R 14 )(R 14 A compound or salt thereof according to any of the inventions 1418 to 1423, wherein the compound is N(CO)-. [Invention 1425] R 11 (R 14 A compound of the present invention 1424 or a salt thereof, which is (H)N(CO)-. [Invention 1426] R 14 A compound of the present invention 1425 or a salt thereof, wherein the compound is a C1-C6 alkyl, a C3-C7 cycloalkyl, or a C4-C8 cycloalkylalkyl. [Invention 1427] R 12 is hydrogen or C7~C 14 A compound or salt thereof from any of the compounds described in invention 1418 to 1426, which is an arylalkyl compound. [Invention 1428] R 1 A compound or salt thereof from any of the inventions 1418 to 1427, wherein the compound is a hydroxyl or C1-C6 alkoxy. [Invention 1429] A compound or salt thereof from any of the inventions 1418 to 1428, wherein p is 0. [Invention 1430] A compound or salt thereof from any of the inventions 1418 to 1429, wherein q is 1. [Invention 1431] Each R 2a or R 2b A compound or salt thereof according to any of the present inventions 1418 to 1430, wherein the compound is hydrogen. [Invention 1432] A compound or salt thereof from any of the inventions 1418 to 1431, wherein L is methylene. [Invention 1433] A pharmaceutical composition comprising any compound according to invention 1418 to 1432 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. [Invention 1434] A small molecule compound exhibiting MASP-2 inhibitory activity for use in therapies for the treatment of MASP-2-related diseases or disorders, wherein the compound interacts with a certain binding site, and the interaction is one or more of (a) to (e): (a) Interacts with one or more amino acid residues in the binding site of MASP-2 (SEQ ID NO: 1) via H-bonds; (b) Interacting at the binding site of SEQ ID NO: 1 by ionic interaction, electrostatic interaction, or hydrogen bonding; (c) Water molecules interact with the binding site of SEQ ID NO: 1; (d) Interacts with one or more amino acid residues in the binding site of SEQ ID NO: 1 via π-π interactions; and / or (e) Interacts with one or more amino acid residues in the binding site of SEQ ID NO: 1 via van der Waals contact; where the compound is not an endogenous MASP-2 ligand. [Invention 1435] A compound of the present invention 1434 that exhibits one, two, three, four, or five of the interactions (a) to (e). [Invention 1436] Compounds of the present invention 1434 or 1435, which are bound to one or more amino acid residues in the binding site of SEQ ID NO: 1 by 1 to 10 H bonds. [Invention 1437] A compound according to any of the invention 1434-1436, which binds at the binding site of SEQ ID NO: 1 by a water molecule. [Invention 1438] A compound according to any of the present invention 1434 to 1437, which is bound at the binding site of SEQ ID NO: 1 by 1 to 20 water molecules. [Invention 1439] A compound according to any of the inventions 1434-1438, which is bound at the binding site of SEQ ID NO: 1 by 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, or 17 water molecules. [Invention 1440] A compound according to any of the invention 1434-1439, which interacts with one or more amino acid residues in the binding site of SEQ ID NO: 1 by van der Waals contact. [Invention 1441] A compound according to any of the present invention 1434 to 1440, having a molecular weight of approximately 300 g / mol to approximately 600 g / mol. [Invention 1442] A method for identifying small molecules capable of inhibiting MASP-2, (a) A step of screening a small molecule library using in silico docking for candidate small molecules selectively identified for their ability to target and bind to MASP-2 surface residues at the binding site of the MASP-2 model; and (b) Testing / evaluating the candidate agents identified in step (a) through one or more in vitro assays for their ability to target and bind to MASP-2 surface residues, thereby identifying small molecules capable of inhibiting MASP-2. Methods that include... [Invention 1443] The method of the present invention 1442, wherein the candidate small molecule comprises a unique chemical scaffold identified in step (b) and is optimized with respect to its ability to inhibit MASP-2. [Invention 1444] The method of the present invention 1442 or 1443, wherein the binding site is identified using the MASP-2 model. [Invention 1445] Any of the methods described in Invention 1442 to 1444, wherein the MASP-2 protein model is computationally derived from crystallographic data. [Invention 1446] The method of the present invention 1445, wherein the MASP-2 protein model is confirmed by RMSD (mean squared deviation) and superposition for each crystal structure. [Invention 1447] Any method 1442 to 1446 of the present invention, wherein in silico docking includes computational docking of a small molecule onto a surface-exposed residue of the binding site of the MASP-2 model. [Invention 1448] Any method 1442 to 1447 of the present invention, wherein the docked ligand orientation is sampled, scored, and binned to specify a distance cutoff value for matching ligand atoms to MASP-2 surface-exposed atoms. [Invention 1449] (a) A step of screening a small molecule library using in silico docking for candidate small molecules selectively identified for their ability to target and bind to MASP-2 surface residues at the binding site of the MASP-2 model; and (b) Testing / evaluating the candidate agents identified in step (a) through one or more in vitro assays for their ability to target and bind to MASP-2 surface residues, thereby identifying small molecules capable of inhibiting MASP-2. A compound that is a candidate small molecule agent identified by a method including the following. [Invention 1450] Compound 1449 of the present invention, having a molecular weight of approximately 300 g / mol to approximately 600 g / mol. [Invention 1451] Compounds of the present invention 1449 or 1450 having a lower Ki to MASP-2 than thrombin. [Invention 1452] A method for treating a MASP-2-related disease or disorder in a subject in need, comprising the step of administering to the subject an effective amount of a small molecule MASP-2 inhibitor that binds to the catalytic substrate-binding domain of MASP-2. [Invention 1453] A method for treating a MASP-2-related disease or disorder in a subject in need, comprising the step of administering to the subject an effective amount of a small molecule MASP-2 inhibitor that binds to a binding site comprising the S1, S2, and S3 regions of MASP-2, and optionally further comprising the S4 and RM regions. [Invention 1454] A method for treating MASP-2-related diseases or disorders in subjects requiring such treatment, comprising the amino acids ALA 468, ALA 469, HIS 483, ASP 526, ALA 527, GLY 528, PHE 529, LEU 575, TYR 602, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, GLY 631, ASP 632, SER 633, GLY 634, GLY 635, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLU 662, GLN 665, TYR 666, GLY 667, VAL 668, and TYR 669, amino acids ALA 468, ALA 469, HIS 483, ASP 526, ALA 527, GLY 528, PHE 529, LEU 575, TYR 602, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, GLY 631, ASP 632, SER 633, GLY 634, GLY 635, VAL 653, SER 654, TRP 655, GLY 656, SER 657, MET 658, ASN 659, CYS 660, GLU 662, GLN 665, TYR 666, GLY 667, VAL A method comprising the step of administering to a subject an effective amount of a small molecule MASP-2 inhibitor that binds to a binding site comprising any one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelfth, thirteen, fourteenth, fifteenth, sixteenth, seventeenth, eighteenth, nineteenth, twenty-one, twenty-one, twenty-two, twenty-two, twenty-threeteenth, twenty-fiveth, twenty-sixth, twenty-seventh, twenty-eighth, twenty-nineth, thirty-one, thirty-one, thirty-two, thirty-two, thirty-two, thirty-threeteenth, thirty-fiveth, thirty-fiveth, thirty-one or thirty-sixth subset of 668 and / or TYR 669. [Invention 1455] A method for treating a MASP-2 related disease or disorder in a subject in need, comprising the step of administering to the subject an effective amount of any small molecule MASP-2 inhibitor or pharmaceutically active composition thereof according to Invention 1001 to 1441. [Invention 1456] A method according to any one of the present invention 1452 to 1455, wherein the compound is administered in an amount sufficient to inhibit MASP-2-dependent complement activation in a target. [Invention 1457] A method according to any of items 1452 to 1456 of the present invention, wherein the subject has been diagnosed with a lectin complement-related disorder or condition requiring treatment. [Invention 1458] Any method of the present invention 1452 to 1457, wherein the disease or disorder is thrombotic microangiopathy (TMA), renal condition, inflammatory response resulting from tissue or organ transplantation, ischemia-reperfusion injury, complications associated with diabetes, cardiovascular disease or cardiovascular disorder, inflammatory gastrointestinal disorder, lung disorder, eye disease or eye disorder, disseminated intravascular coagulation, graft-versus-host disease, venous occlusion, or diffuse alveolar hemorrhage. [Invention 1459] The method according to any of the present invention 1452 to 1457, wherein the disease or disorder is thrombotic microangiopathy (TMA), thrombotic thrombocytopenic purpura (TTP), refractory TTP, Upshaw-Schulmann syndrome (USS), hemolytic uremic syndrome (HUS), atypical hemolytic uremic syndrome (aHUS), factor H-independent atypical hemolytic uremic syndrome, aHUS secondary to infection, plasma therapy-resistant aHUS, TMA secondary to cancer, TMA secondary to chemotherapy, TMA secondary to transplantation, or TMA associated with hematopoietic stem cell transplantation. [Invention 1460] A method according to any of the present invention 1452 to 1457, wherein the disease or disorder is graft-versus-host disease. [Invention 1461] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is diffuse alveolar hemorrhage (DAH). [Invention 1462] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is veno-occlusive disease (VOD). [Invention 1463] Any method of the present invention 1452 to 1457, wherein the disease or disorder is a renal condition. [Invention 1464] The method of the present invention 1463, wherein the renal condition is mesangial proliferative glomerulonephritis, membranous glomerulonephritis, membranoproliferative glomerulonephritis (mesangial capillary glomerulonephritis), acute post-infectious glomerulonephritis (post-streptococcal glomerulonephritis), C3 glomerulopathy, cryoglobulinemia glomerulonephritis, microimmune necrotizing crescentic glomerulonephritis, lupus nephritis, Henoch-Schönlein purpura nephritis, or IgA nephropathy. [Invention 1465] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is renal fibrosis and / or renal proteinuria. [Invention 1466] A method according to any of items 1452 to 1457 of the present invention, wherein the disease or disorder is an inflammatory response resulting from tissue transplantation or parenchymal organ transplantation. [Invention 1467] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is ischemia-reperfusion injury (I / R). [Invention 1468] Any method of the present invention 1452 to 1457, wherein the disease or disorder is a complication associated with non-obese diabetes and / or a complication associated with type 1 or type 2 (adult-onset) diabetes. [Invention 1469] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is a cardiovascular disease or cardiovascular disorder. [Invention 1470] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is an inflammatory gastrointestinal disorder. [Invention 1471] A method according to any of the present invention 1452 to 1457, wherein the disease or disorder is lung disorder. [Invention 1472] Any method of the present invention 1452 to 1457, wherein the disease or disorder is an extracorporeal exposure-induced inflammatory response, and the method includes a step of treating a subject undergoing an extracorporeal circulation procedure. [Invention 1473] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is inflammatory or non-inflammatory arthritis, or other musculoskeletal disorder. [Invention 1474] A method of any of the present invention 1452 to 1457, wherein the disease or disorder is a skin disorder. [Invention 1475] Any method of the present invention 1452 to 1457, wherein the disease or disorder is a disorder or injury of the peripheral nervous system (PNS) and / or the central nervous system (CNS). [Invention 1476] A method according to any of the present invention 1452 to 1457, wherein the disease or disorder is sepsis or a condition resulting from sepsis. [Invention 1477] A method according to any of the present invention 1452 to 1457, wherein the disease or disorder is a urogenital disorder. [Invention 1478] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is an inflammatory response in a subject being treated with a chemotherapeutic agent and / or radiotherapy. [Invention 1479] A method of any of the present invention 1452 to 1457, wherein the disease or disorder is angiogenesis-dependent cancer. [Invention 1480] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is an angiogenesis-dependent benign tumor. [Invention 1481] A method according to any of the present invention 1452 to 1457, wherein the disease or disorder is an endocrine disorder. [Invention 1482] A method of any of the present invention 1452 to 1457, wherein the disease or disorder is an eye disease or eye disorder. [Invention 1483] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is an intraocular neovascular disease or an intraocular neovascular state. [Invention 1484] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is disseminated intravascular coagulation (DIC) or another complement-mediated coagulation disorder. [Invention 1485] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is acute radiation syndrome, dense deposit disease, Degos disease, fulminant antiphospholipid syndrome (CAPS), Behçet's disease, cryoglobulinemia, paroxysmal nocturnal hemoglobinuria ("PNH"), or cold agglutinin disease. [Invention 1486] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is atypical hemolytic uremic syndrome (aHUS). [Invention 1487] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is hematopoietic stem cell transplant-related TMA. [Invention 1488] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is immunoglobulin A nephropathy (IgAN). [Invention 1489] A method according to any one of the present invention 1452 to 1457, wherein the disease or disorder is lupus nephritis (LN). These and other aspects, purposes, and embodiments will become even clearer when read in conjunction with the detailed description and drawings below. [Brief explanation of the drawing]

[0051] [Figure 1] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1129) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 2]This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1034) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 3] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1024) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 4] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1059) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 5] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1088) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å), using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 6]This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1036) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 7] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1081) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 8] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1063) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 9] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1065) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å), using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 10]This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1030) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 11] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1037) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 12] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1118) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å), using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 13] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1090) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 14]This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1007) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 15] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1021) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 16] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1097) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 17] This plot shows a schematic diagram of one aspect of the atoms of the inhibitor compound (1089) and the atoms of the MASP-2 amino acid, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 18]This plot shows a schematic diagram of one aspect of the atoms of the inhibitory compound melagatoran and the atoms of the MASP-2 amino acids, calculated using LigPlot+ software settings for hydrogen bond calculation parameters (maximum distance of 3.35 Å between hydrogen bond donors and hydrogen bond acceptors; and non-bonding contact parameters between any contacts such as hydrophobic contacts and van der Waals interactions, with a maximum contact distance of 3.90 Å) using a model derived from the corresponding crystallographic MASP-2-compound costructure. [Figure 19] This plot shows the binding of compound (14) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 20] This plot shows the binding of compound (54) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 21] This plot shows the binding of compound (1042) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 22] This plot shows the binding of compound (2018) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 23] This plot shows the binding of compound (1149) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 24] This plot shows the binding of compound (1031) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 25] This plot shows the binding of compound (1153) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 26] This plot shows the binding of compound (1025) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 27] This plot shows the bonding of compound (1012) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 28] This plot shows the binding of compound (1078) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 29] This plot shows the binding of compound (1145) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 30] This plot shows the binding of compound (1050) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 31] This plot shows the binding of compound (1253) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 32] This plot shows the bonding of compound (1257) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 33] This plot shows the binding of compound (1297) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 34] This plot shows the binding of compound (1304) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 35] This plot shows the bonding of compound (1306) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 36] This plot shows the binding of compound (1307) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 37] This plot shows the binding of compound (1328) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 38] This plot shows the binding of compound (1334) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 39]This plot shows the binding of compound (1335) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 40] This plot shows the binding of compound (1338) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 41] This plot shows the binding of compound (1345) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 42] This plot shows the binding of compound (1351) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 43] This plot shows the binding of compound (1353) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 44] This plot shows the bonding of compound (1360) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 45] This plot shows the binding of compound (1367) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 46] This plot shows the binding of compound (1368) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 47] This plot shows the binding of compound (1371) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 48] This plot shows the bonding of compound (1372) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 49] This plot shows the binding of compound (1373) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 50]This plot shows the bonding of compound (1492) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 51] This plot shows the binding of compound (1399) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 52] This plot shows the bonding of compound (1406) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 53] This plot shows the bonding of compound (1411) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 54] This plot shows the binding of compound (1433) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 55] This plot shows the binding of compound (1435) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 56] This plot shows the binding of compound (1441) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 57] This plot shows the binding of compound (1450) to MASP-2, which exhibits hydrogen bonding, as calculated by LigPlot+ software. [Figure 58] This plot shows melagatran bound to thrombin. [Figure 59] This plot shows thrombin-bound melagatoran superimposed with MASP-2-selective compound (1065) bound to MASP-2. [Figure 60] This plot shows compound (1065) bound to the SP domain of MASP-2. [Figure 61] This plot shows the compound (1334) bound to thrombin. [Figure 62] This plot shows the compound (1334) bound to the SP domain of MASP-2. [Figure 63] This plot shows the compound (1334) bound to MASP-2, superimposed on the compound (1334) bound to thrombin. [Figure 64] This plot shows the S3-S4 binding pockets of MASP-2. [Figure 65] This plot shows the S3-S4 binding pockets of thrombin. [Figure 66] This plot shows the MASP-2 binding subpocket. [Figure 67] This diagram shows the distances between pharmacophore elements describing the S1 and S2 regions. The S2 region includes H4, O1, O2, and CA6. The S1 region consists of H2, O4, CA1, C3, C5, C7, and N1. Distances mentioned in the text are illustrated. [Figure 68] This plot shows the angles between the pharmacophore elements describing the S1 and S2 regions. [Figure 69] This plot shows the definition of the twist angle used in the text. [Figure 70] This plot shows the definition of the twist angle used in the text. [Figure 71] This plot shows the definition of the twist angle used in the text. [Figure 72] This plot shows the distances between pharmacophore elements describing the S2, S4, and RM regions. [Figure 73] This plot shows the angle definitions used in the text. [Figure 74] This plot shows the definition of the twist angle used in the text. [Figure 75] This plot shows the definition of the twist angle used in the text. [Figure 76] This is a flowchart illustrating one aspect of the process of this disclosure. [Modes for carrying out the invention]

[0052] explanation I. Definition Unless otherwise defined, all technical and scientific terms used herein have the same meaning as those commonly understood by those skilled in the art to which the present invention pertains. Similar or equivalent methods and materials may be used in carrying out or testing the present invention, but preferred methods and materials are described below. Furthermore, the materials, methods, and examples are illustrative and not intended to be limiting.

[0053] In the above summary, this description, and the claims below, specific features and aspects of the invention, including method steps, are referred to. The disclosure of the invention herein includes all possible combinations of these specific features within the scope of the disclosed aspects of the invention, insofar as these combinations are not contradictory. For example, where a description indicates aspects A, B, and C of one aspect, this will be understood to disclose specific aspects including both aspects A and B, both aspects B and C, and both aspects A and C, as well as a single aspect involving aspects A, B, and C.

[0054] a. General definition The terms "a," "an," or "the" include not only situations involving one member, but also situations involving two or more members. For example, the singular forms "a," "an," and "the" include multiple references unless otherwise clearly indicated by the context. Thus, for example, a reference to "cells" includes multiple such cells, and a reference to "agent" includes a reference to one or more agents known to those skilled in the art.

[0055] The terms “about” and “approximately” refer to the degree of error in a measurement of a quantity that is acceptable given the nature or precision of the measurement. Typically, an exemplary degree of error is within 20 percent (%) of a given value or range of values, preferably within 10 percent, and more preferably within 5 percent. Any reference to “about X” specifically indicates at least the values ​​X, 0.95X, 0.96X, 0.97X, 0.98X, 0.99X, 1.01X, 1.02X, 1.03X, 1.04X, and 1.05X. Thus, “about X” is intended to teach and present written support for a limitation in a claim, for example, “0.98X.” Alternatively, in biological systems, the terms “about” and “approximately” may refer to a value that is within 10 times, preferably within 5 times, and more preferably within 2 times, a given value. The quantities shown herein are approximate unless otherwise stated; that is, the terms “about” and “approximately” can be assumed unless explicitly stated. When “about” is applied to the beginning of a numerical range, it applies to both ends of the range. Thus, “about 5 to 20%” is equal to “about 5% to about 20%”. When “about” is applied to the first value in a set of values, it applies to all values ​​in that set. Thus, “about 7, 9, or 11 mg / kg” is equal to “about 7, about 9, or about 11 mg / kg”.

[0056] The term "MASP-2" refers to mannan-binding lectin-related serine protease 2. It is the human MASP-2 protein (SEQ ID NO:1) with UniProt accession code O00187. The serine protease domain ("B chain" = B chain of mannan-binding lectin serine protease 2, based on UniProtKB - O00187(MASP-2_HUMAN)) contains (or consists of) residues 445-686.

[0057] The term "MASP-2-dependent complement activation" refers to the activation of complements under physiological conditions (i.e., Ca ++This refers to MASP-2-dependent activation of the lectin pathway, which occurs in the presence of MASP-2, leading to the formation of lectin pathway C3 convertase C4b2a, followed by the accumulation of C3 cleavage product C3b, which produces C5 convertase C4b2a(C3b)n.

[0058] The term "MASP-2-dependent complement-related disorder or condition" refers to a disorder or condition associated with MASP-2-dependent complement activation.

[0059] The term "MASP-2-related disease or disorder" means a disease or disorder associated with MASP-2 activation or activity, including MASP-2-dependent complement-related disease or disorder, where inhibition of MASP-2 is therapeutically beneficial or expected to be therapeutically beneficial.

[0060] The term "lectin pathway" refers to complement activation resulting from the specific binding of serum and non-serum carbohydrate-binding proteins, including mannan-binding lectins (MBL), CL-11, and phycolin (H-phycolin, M-phycolin, or L-phycolin).

[0061] The term "classical pathway" refers to complement activation induced by an antibody bound to an external particle and requiring the binding of the recognition molecule Clq.

[0062] Amino acid residues are abbreviated as follows: alanine (Ala; A), asparagine (Asn; N), aspartic acid (Asp; D), arginine (Arg; R), cysteine ​​(Cys; C), glutamic acid (Glu; E), glutamine (Gln; Q), glycine (Gly; G), histidine (His; H), isoleucine (Ile), leucine (Leu), lysine (Lys; K), methionine (Met; M), phenylalanine (Phe; F), proline (Pro; P), serine (Ser; S), threonine (Thr; T), tryptophan (Trp; W), tyrosine (Tyr; Y), and valine (Val; V).

[0063] In its broadest sense, natural amino acids can be grouped based on the chemical properties of their side chains. "Hydrophobic" amino acids are His, Leu, Met, Phe, Trp, Tyr, Val, Ala, Cys, or Pro. "Hydrophilic" amino acids are Gly, Asn, Gln, Ser, Thr, Asp, Glu, Lys, Arg, or His. This group of amino acids can be further divided into subclasses as follows: "Uncharged hydrophilic" amino acids are Ser, Thr, Asn, or Gln. "Acidic" amino acids are Glu or Asp. "Basic" amino acids are Lys, Arg, or His.

[0064] The term "conservative amino acid substitution" is exemplified by substitutions between amino acids within the following groups: (1) glycine, alanine, valine, leucine, and isoleucine; (2) phenylalanine, tyrosine, and tryptophan; (3) serine and threonine; (4) aspartic acid and glutamic acid; (5) glutamine and asparagine; and (6) lysine, arginine, and histidine.

[0065] The term "subjects" includes all mammals, including, but not limited to, humans, non-human primates, dogs, cats, horses, sheep, goats, cows, rabbits, pigs, and rodents.

[0066] The terms "small molecule" and "small organic molecule" refer to carbon-containing small molecules having a molecular weight of approximately 2500 daltons or less. In some embodiments, small molecules have a molecular weight of approximately 2000 daltons or less. In some embodiments, small molecules have a molecular weight of approximately 1500 daltons or less. In some embodiments, small molecules have a molecular weight of approximately 1000 daltons or less. In some embodiments, small molecules have a molecular weight of approximately 750 daltons or less. In some embodiments, small molecules have a molecular weight of approximately 500 daltons or less. In some embodiments, small molecules have a molecular weight of approximately 50 daltons or more. In some embodiments, small molecules have a molecular weight of approximately 75 daltons or more. In some embodiments, small molecules have a molecular weight of approximately 100 daltons or more. In some embodiments, small molecules have a molecular weight of approximately 150 daltons or more. In some embodiments, small molecules have a molecular weight of approximately 250 daltons or more. In some embodiments, small molecules may have molecular weights in the range of approximately 50 to 500 daltons, approximately 50 to 750 daltons, approximately 50 to 1000 daltons, approximately 50 to 1500 daltons, approximately 50 to 2000 daltons, or approximately 50 to 2500 daltons. Where the term “compound” is used herein, it is explicitly intended to include small molecule compounds (including any embodiment thereof) as defined herein.

[0067] In this specification, the term “pharmaceutically acceptable” is used to mean a compound, raw material, composition, and / or dosage form that, within the bounds of sound medical judgment, is suitable for use in contact with human and animal tissues, without excessive toxicity, irritation, allergic response, or other problems or complications, and that corresponds to a reasonable benefit-risk ratio.

[0068] The terms “disorder,” “disease,” and “condition” are used interchangeably to describe a state in an object. Disorder is an impairment or disruption that affects the normal functioning of the object’s body. Disease is a pathological condition of an organ, body part, or system caused by various factors, such as infection, genetic abnormalities, or environmental stress, characterized by a set of identifiable symptoms.

[0069] The term "effective amount" or "effective dose" means a sufficient amount to achieve the desired result, and therefore depends on the ingredients and the desired result. Nevertheless, once the desired effect is identified, determining the effective amount is within the scope of the skill of those skilled in the art.

[0070] The term "subcutaneous administration" means the administration of the formulation beneath all layers of the target skin.

[0071] Unless otherwise specified, the term "histidine" specifically includes L-histidine.

[0072] The term "isotonic" refers to a preparation that exhibits essentially the same osmotic pressure as human blood. Generally, isotonic preparations have an osmotic pressure of approximately 250 to 350 mOsmol / L. Isotonicity can be measured, for example, using a vapor pressure osmometer or a freezing point depression osmometer.

[0073] The term "hypertonic" refers to a formulation whose osmotic pressure exceeds that of the human body (i.e., exceeds 350 mOsm / L).

[0074] The term "hydrogen bond" refers to the partial electrostatic attraction between a hydrogen atom (H) bonded to a relatively electronegative atom, such as nitrogen (N) or oxygen (O), and another adjacent atom with a lone pair of electrons. For example, when nitrogen is described as acting as a "hydrogen bond donor," it means that the hydrogen atom (H) bonded to nitrogen (N) is donated by nitrogen and then electrostatically attracted or accepted by an adjacent atom, such as oxygen, which has a lone pair of electrons. Similarly, when oxygen is described as acting as a "hydrogen bond acceptor," it means that the hydrogen atom (H) bonded to a relatively electronegative atom, such as nitrogen (N), is electrostatically attracted or "accepted" by an adjacent atom, such as oxygen, which has a lone pair of electrons. The atom to which hydrogen is bonded may be specified without explicitly stating the origin and presence of the intermediate hydrogen atom. The term "hydrogen bond" is used whenever LigPlot+ software predicts hydrogen bond interactions using its algorithm and the parameter 3.35 Å applied to the maximum distance between the hydrogen bond donor and hydrogen bond acceptor. Not all hydrogen bonds may actually exist in fixed positions at the same time. This is evident in atoms that have been shown to form four presumed hydrogen bonds, but where only three hydrogen bonds are chemically possible at any given time. In general, crystal structures such as cocrystal structure information herein do not directly indicate or detect hydrogen bonds, but the software used to describe cocrystals predicts the presence of these H bonds. Thus, throughout this disclosure, if an H bond is present and described, it can be said that it is “predicted” by the software to be present.

[0075] The term ionic bonding encompasses a type of chemical bond that includes the electrostatic attraction between ions with opposite charges and is a primary interaction that occurs in ionic compounds.

[0076] The term "van der Waals" interaction encompasses weak, short-lived electrostatic attraction between uncharged molecules resulting from the interaction of permanent or transient electric dipole moments. These interactions include all contacts calculated using the unbonded contact parameter between hydrophobic contact and arbitrary contact, with respect to interactions having a maximum contact distance of 3.90 Å, as determined by LigPlot+ software using a model derived from the corresponding crystallographic MASP-2-compound costructure.

[0077] The term “π-π interaction or π-π stacking” interaction includes attractive non-covalent interactions between aromatic rings that are oriented nearly parallel or nearly perpendicular to each other (for example, like “end-face” interactions) because they contain π bonds.

[0078] Typically, the active site of serine proteases such as MASP-2 is formed as a gap to which a polypeptide substrate or inhibitor binds. Schechter and Berger labeled the amino acid residues from the N-terminus to the C-terminus of polypeptide substrates as follows: Pi, ..., P3, P2, P1, P1', P2', P3', ..., Pj, and their respective binding subsites Si, ..., S3, S2, S1, S1', S2', S3', ..., Sj. Cleavage is catalyzed between P1 and P1' (Schechter, I. & Berger, A. On the size of the active site in proteases. I. Papain. Biochem. Biophys. Res. Commun. 27 (1967)).

[0079] The term "binding site" refers to a region on a protein with which a small molecule can interact, such as a region on the surface of MASP-2 that reduces or inactivates the MASP-2 molecule even though it does not overlap with or only partially overlaps with the active site.

[0080] The term "or" implies a choice and should generally be interpreted as non-exclusive. For example, the claim "a composition comprising A or B" usually presents one aspect of a composition containing both A and B. However, "or" should be interpreted to exclude presented aspects that cannot be combined in a consistent manner (e.g., composition pH of 9-10 or 7-8).

[0081] The group "A or B" is equivalent to the group "selected from the group consisting of A and B".

[0082] The conjunctions "comprising" or "comprise" are not closed. For example, "a composition containing A" must contain at least component A, but may also contain one or more other components (e.g., B; B and C; B, C, and D; etc.). Therefore, the term "contains" should generally be interpreted as not excluding further components. For example, the claim "a composition containing A" encompasses compositions containing A and B; A, B, and C; A, B, C, and D; A, B, C, D, and E; etc.

[0083] The term "hypertonic" refers to a formulation whose osmotic pressure exceeds that of the human body (i.e., exceeds 350 mOsm / KglHhO).

[0084] The term "agent" refers to a compound or mixture of compounds that, when added to a composition, tends to produce a specific effect on the properties of that composition. For example, a composition containing a thickening agent is more likely to have a higher viscosity than a comparable composition that is otherwise identical but lacks the thickening agent.

[0085] "Subjects" include all mammals, including, but not limited to, humans, non-human primates, dogs, cats, horses, sheep, goats, cows, rabbits, pigs, and rodents.

[0086] A "synthetic" compound means a compound that is not naturally occurring but has been synthesized by humans. Unless otherwise indicated in the context, references to compounds in this specification should be understood to include references to synthetic compounds.

[0087] The terms “to treat,” “to treat,” or “treatment” include administering or applying a composition (e.g., a composition described herein) in an amount, pattern (e.g., a schedule of administration), and manner (e.g., a route of administration) effective for improving a disorder or its symptoms, or for preventing, delaying, or slowing the progression of a disorder or its symptoms. These improvements may include, but are not limited to, reduction or remission of one or more symptoms or conditions, whether partial or complete, detectable or undetectable; a reduction in the severity of the disease; stabilization of the disease state (i.e., prevention of exacerbation); prevention of disease transmission or dissemination; delay or slowing the progression of the disease; remission or mitigation of the disease state; reduction of disease recurrence; and remission.

[0088] "To treat" and "treatment" include prophylactic treatment. In certain embodiments, the treatment method includes a step of administering a therapeutically effective amount of the active agent to the subject. The administration step may consist of a single dose or a series of doses. The length of the treatment period depends on various factors, such as the severity of the condition, the age of the subject, the concentration of the active agent, the activity of the composition used for treatment, or a combination thereof. It will also be recognized that the effective dose of the agent used for treatment or prevention may increase or decrease during a particular treatment or prophylactic regimen. Changes in dosage may occur and become apparent by standard diagnostic assays known in the art. In one aspect, chronic administration may be necessary. For example, the composition may be administered to the subject in an amount and for a period of time sufficient to treat the subject.

[0089] As used herein, the terms “ambient temperature” and “room temperature” are understood in the art to mean a temperature close to the temperature of the room in which the reaction takes place, for example, the reaction temperature, for example, a temperature of about 20°C to about 30°C.

[0090] b. Chemical definition In various places within this specification, certain characteristics of compounds are disclosed as groups or ranges. This disclosure is specifically intended to include any individual partial combination of members of these groups and ranges. For example, "C 1~6 The terms “alkyl” and “C1-C6 alkyl” are specifically intended to disclose methyl, ethyl, C3 alkyl, C4 alkyl, C5 alkyl, and C6 alkyl (non-restrictively) individually.

[0091] In various places in this specification, the variable elements that define divalent linking groups are described. Each linking substituent is specifically intended to include both the forward and reverse forms of the linking substituent. For example, -NR(CR'R'') n - is -NR(CR'R'') n -and-(CR'R'') n This includes both NR- forms, and each form is intended to be disclosed individually. Where a structure requires a linking group, the Markush group definitions listed with respect to that group will be understood to be linking groups. For example, if a structure requires a linking group and the Markush group definitions for that group list "alkyl" or "aryl," then "alkyl" or "aryl" will be understood to represent a linked alkylene group or a linked arylene group, respectively.

[0092] The term "substituted" means that an atom or group of atoms formally replaces a hydrogen atom as a "substituent" bonded to another group. Unless otherwise specified, the term "substituted" means any level of substitution, e.g., monosubstituted, disubstituted, trisubstituted, tetrasubstituted, or pentasubstituted, where substitution is permitted. Substituents are independently selected, and substitutions can occur at any chemically available position. Substitutions in a given atom should be understood as being limited by valence. The phrase "may be substituted" means either substituted or not substituted. The term "substituted" means that a hydrogen atom is formally removed and replaced by a substituent. One divalent substituent, e.g., oxo, can substitute two hydrogen atoms.

[0093] n and m are integers in "C n~m " and "C n ~C m The term "group" refers to a group containing n to m carbon atoms. An example is C 1~4 , C 1~6 These are some examples. This term refers to all members within the scope, i.e., C n , C n+1 , C n+2 ...C m-2 , C m-1 , C m It is intended to be clearly disclosed. For example, C 1~6 It is intended to disclose C1, C2, C3, C4, C5 and C6. n~m " is "C n ~C m It has the same meaning as "[...]."

[0094] When used alone or in combination with other terms, the term "alkyl" refers to a saturated hydrocarbon group that can be linear or branched. n~m "Alkyl" and "C n ~C m The term "alkyl" refers to an alkyl group having n to m carbon atoms. For example, C1 to C 12This indicates that the group may have between 1 and 12 carbon atoms within it. Unless otherwise specified, alkyl groups have approximately 1 to 20 carbon atoms. An alkyl group formally corresponds to an alkane in which one CH bond is replaced by the alkyl group's bond site to the rest of the compound. In some embodiments, alkyl groups contain 1 to 6 carbon atoms, 1 to 4 carbon atoms, 1 to 3 carbon atoms, or 1 to 2 carbon atoms. Examples of alkyl moieties include chemical groups such as methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, isobutyl, and sec-butyl; and higher homologs such as 2-methyl-1-butyl, 1,1-dimethylpropyl, n-pentyl, 3-pentyl, n-hexyl, 1,2,2-trimethylpropyl, hexyl, heptyl, octyl, nonyl, decyl, and dodecyl. The term "lower alkyl" refers to an alkyl group having 1 to 6 carbon atoms in the chain. A "substituted alkyl" group is an alkyl group substituted with one or more substituents.

[0095] When used alone or in combination with other terms, the term “alkenyl” refers to a linear or branched hydrocarbon group corresponding to an alkyl group having one or more carbon-carbon double bonds. An alkenyl group formally corresponds to an alkene in which one CH bond is replaced by the alkenyl group's bond site relative to the rest of the compound. n~m "Alkenil" and "C n ~C m The term "alkenyl" refers to an alkenyl group having n to m carbon atoms. In some embodiments, the alkenyl moiety contains 2 to 6, 2 to 4, or 2 to 3 carbon atoms. Exemplary alkenyl groups include, but are not limited to, ethenyl, n-propenyl, isopropenyl, n-butenyl, and sec-butenyl.

[0096] When used alone or in combination with other terms, the term "alkynyl" refers to a linear or branched hydrocarbon group corresponding to an alkyl group having one or more carbon-carbon triple bonds. An alkynyl group formally corresponds to an alkyne in which one CH bond is replaced by the alkyl group's bond site to the rest of the compound. n~m "Alkinyl" and "C n ~C m The term "alkynyl" refers to an alkynyl group having n to m carbon atoms. Examples of alkynyl groups include, but are not limited to, ethynyl, propyne-1-yl, and propyne-2-yl. In some embodiments, the alkynyl moiety contains 2 to 6, 2 to 4, or 2 to 3 carbon atoms.

[0097] When used alone or in combination with other terms, the term "alkylene" refers to a divalent alkyl linking group. The alkylene group formally corresponds to an alkane in which two CH bonds are replaced by the alkylene group's bonding site to the rest of the compound. n~m The term "alkylene" refers to an alkylene group having n to m carbon atoms. Examples of alkylene groups include, but are not limited to, methylene, ethane-1,2-diyl, propane-1,3-diyl, propane-1,2-diyl, butane-1,4-diyl, butane-1,3-diyl, butane-1,2-diyl, and 2-methyl-propane-1,3-diyl. In some embodiments, "C n~m "Alkylene" refers to a chain of n to m methylene (CH2) groups -(CH2) n~m - can mean, for example, -CH2-, -CH2CH2-, -CH2CH2CH2-, etc.

[0098] When used alone or in combination with other terms, the term "alkoxy" refers to a group of the formula -O-alkyl, where the alkyl group is as defined above. n~mThe term "alkoxy" refers to an alkoxy group in which the alkyl group has n to m carbon atoms. Exemplary alkoxy groups include methoxy, ethoxy, propoxy (e.g., n-propoxy and isopropoxy), and t-butoxy. In some embodiments, the alkyl group has 1 to 6, 1 to 4, or 1 to 3 carbon atoms.

[0099] The term "alkoxyalkyl" refers to an alkyl group in which one or more hydrogen atoms are replaced by an alkoxy group. n~m Alkoxy-C p~q The term "alkyl" is C n~m C substituted with an alkoxy group p~q This refers to an alkyl group. In some embodiments, a hydroxyalkyl group has one alkoxy group. In some embodiments, an alkoxyalkyl group has one or two alkoxy groups on different carbon atoms. Examples include, but are not limited to, methoxymethyl, ethoxymethyl, 3-ethoxyethyl, and 1-methoxyethyl.

[0100] The term "amino" refers to the group of the formula -NH2.

[0101] The term "carbamyl" refers to the group of the formula -C(O)NH2.

[0102] When used alone or in combination with other terms, the term "carbonyl" refers to a -C(=O)- group, which is sometimes written as C(O).

[0103] The terms "cyano" or "nitrile" refer to the group of the formula -C≡N, which is sometimes written as -CN.

[0104] The term "halo" or "halogen," used alone or in combination with other terms, refers to fluoro, chloro, bromo, and iodine atoms. In some embodiments, "halo" refers to a halogen atom selected from F, Cl, or Br. In some embodiments, halo is F.

[0105] The term "haloalkyl" refers to an alkyl group in which one or more hydrogen atoms are replaced by halogen atoms. n~m The term "haloalkyl" refers to a system having n to m carbon atoms and at least one to a maximum of {2(n to m) + 1} halogen atoms, which may be the same or different. n~m This refers to an alkyl group. In some embodiments, the halogen atom is a fluoro atom. In some embodiments, the haloalkyl group has 1 to 6 or 1 to 4 carbon atoms. Exemplary haloalkyl groups include CF3, C2F5, CHF2, CCl3, CHCl2, and C2Cl5. In some embodiments, the haloalkyl group is a fluoroalkyl group.

[0106] When used alone or in combination with other terms, the term "haloalkoxy" refers to a group of the formula -O-haloalkyl, where the haloalkyl group is as defined above. n~m The term "haloalkoxy" refers to a haloalkoxy group in which the haloalkyl group has n to m carbon atoms. Examples of haloalkoxy groups include trifluoromethoxy. In some embodiments, the haloalkoxy group has 1 to 6, 1 to 4, or 1 to 3 carbon atoms.

[0107] The term "hydroxyalkyl" refers to an alkyl group in which one or more hydrogen atoms are replaced by hydroxyls. n~m The term "hydroxyalkyl" refers to a C atom having n to m carbon atoms and at least one hydroxyl group. n~m This refers to an alkyl group. In some embodiments, a hydroxyalkyl group has one alcohol group. In certain aspects, a hydroxyalkyl group has one or two alcohol groups on different carbon atoms. In certain aspects, a hydroxyalkyl group has one, two, three, four, five, or six alcohol groups. Examples include, but are not limited to, hydroxymethyl, 2-hydroxyethyl, and 1-hydroxyethyl.

[0108] The term "oxo" refers to an oxygen atom as a divalent substituent that forms a carbonyl group when bonded to a carbon atom, and a sulfoxide, sulfone, or N-oxide group when bonded to a heteroatom.

[0109] The term "sulfide" refers to a sulfur atom as a divalent substituent that forms a thiocarbonyl group (C=S) when bonded to a carbon atom.

[0110] The term "n-membered," where n is an integer, typically describes the number of ring-forming atoms in a part where the number of ring-forming atoms is n. The term "n-m-membered," where n and m are integers, describes the range where the number of ring-forming atoms is n-m. For example, piperidinyl is an example of a 6-membered heterocycloalkyl ring, pyrazolyl is an example of a 5-membered heteroaryl ring, pyridyl is an example of a 6-membered heteroaryl ring, and 1,2,3,4-tetrahydronaphthalene is an example of a 10-membered cycloalkyl group.

[0111] The term "aromatic" refers to a carbocyclic or heterocyclic ring having one or more polyunsaturated rings that are aromatic (i.e., having (4n + 2) delocalized π (pi) electrons where n is an integer).

[0112] When used alone or in combination with other terms, the term “aryl” refers to an aromatic hydrocarbon group that can be monocyclic or polycyclic (e.g., having two, three, or four fused rings). n~m The term "aryl" refers to an aryl group having n to m ring carbon atoms. Examples of aryl groups include phenyl, naphthyl, anthracenyl, phenantrenyl, indanyl, indenyl, and tetraceryl. In some embodiments, the aryl group has 6 to about 20 carbon atoms, 6 to about 18 carbon atoms, 6 to about 15 carbon atoms, or 6 to about 10 carbon atoms. In some embodiments, the aryl group is phenyl.

[0113] The terms “arylalkyl” or “aralkyl” or “alkylaryl,” used alone or in combination with other terms, mean a group of the formula -alkylene-aryl, and mean an alkyl group as defined herein, in which at least one hydrogen is replaced by an aryl group as defined herein. In some embodiments, the arylalkyl is C 6~10 Aryl-C 1~3 It is alkyl. In some embodiments, arylalkyl is C 6~10 Aryl-C 1~4 It is alkyl. In some embodiments, arylalkyl is C 6~10 Aryl-C 1~3 It is alkyl. In some embodiments, the arylalkyl is phenyl-C 1~3 It is an alkyl group. Examples include, but are not limited to, benzyl, 1-phenylethyl, 4-methylbenzyl, and 1,1,-dimethyl-1-phenylmethyl. In some embodiments, the arylalkyl group is benzyl.

[0114] The terms “heteroaryl” or “heteroaromatic,” used alone or in combination with other terms, mean a monocyclic or polycyclic aromatic heterocycle having at least one heteroatom ring member selected from sulfur, oxygen, and nitrogen. “n-membered heteroaryl” or “n-membered heteroaromatic,” where n is an integer, means a heteroaryl having n ring-forming atoms. “n-m-membered heteroaryl” or “n-m-membered heteroaromatic,” where n and m are integers, means a heteroaryl having n-m ring-forming atoms. The number of carbon atoms in the ring is less than the number of heteroatoms. Therefore, in some embodiments, an n-membered heteroaryl may have n-1, n-2, n-3, or n-4 ring carbon atoms, and an n-m-membered heteroaryl may have n-1, n-2, n-3, or n-4 ring carbon atoms and m-1, m-2, m-3, or m-4 ring carbon atoms. In some embodiments, an n-m-membered heteroaryl may have 1-m-1 ring carbon atoms. In some embodiments, the heteroaryl ring has one, two, three, or four heteroatom ring members independently selected from nitrogen, sulfur, and oxygen. In some embodiments, any ring-forming nitrogen in the heteroaryl portion may be an N-oxide. In some embodiments, the heteroaryl has 5 to 10 ring atoms, including a carbon atom and one, two, three, or four heteroatom ring members independently selected from nitrogen, sulfur, and oxygen. In some embodiments, the heteroaryl has 5 to 6 ring atoms and one or two heteroatom ring members independently selected from nitrogen, sulfur, and oxygen. In some embodiments, the heteroaryl is a 5- or 6-membered heteroaryl ring. In other embodiments, the heteroaryl is an 8-, 9-, or 10-membered fused bicyclic heteroaryl ring.Examples of heteroaryl groups include, but are not limited to, pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, pyrazole, azolyl, oxazole, isoxazole, thiazole, isothiazole, imidazole, furan, thiophene, quinoline, isoquinoline, naphthyridine (including 1,2-, 1,3-, 1,4-, 1,5-, 1,6-, 1,7-, 1,8-, 2,3-, and 2,6-naphthyridine), indole, azaindole, benzothiophene, benzofuran, benzoisoxazole, benzimidazole, imidazo[1,2-b]thiazole, purine, furazan, triazole, tetrazole, 1,2,4-thiadiazole, quinazoline, phthalazine, imidazo[1,2-a]pyridine, and imidazo[2,1-b]thiazolyl.

[0115] A five-membered heteroaryl ring is a heteroaryl group having one or more (e.g., one, two, or three) ring atoms, each independently selected from N, O, and S. Examples of five-membered heteroaryl rings include thienyl, furyl, pyrrolyl, imidazolyl, thiazolyl, oxazolyl, pyrazolyl, isothiazolyl, isoxazolyl, 1,2,3-triazolyl, tetrazolyl, 1,2,3-thiadiazolyl, 1,2,3-oxadiazolyl, 1,2,4-triazolyl, 1,2,4-thiadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-triazolyl, 1,3,4-thiadiazolyl, and 1,3,4-oxadiazolyl.

[0116] A six-membered heteroaryl ring is a heteroaryl group having one or more (e.g., one, two, or three) ring atoms independently selected from N, O, and S. Examples of six-membered heteroaryl rings include pyridyl, pyrazinyl, pyrimidinyl, triazinyl, and pyridazinyl.

[0117] The term "heteroarylalkyl," used alone or in combination with other terms, refers to a group of the formula -alkylene-heteroaryl. The term "n-membered heteroarylalkyl," where n is an integer, refers to a heteroarylalkyl group in which heteroaryl is an n-member group. The term "n-m-membered C" refers to an n-m-membered C group where n, m, p, and q are integers. p~q The term "-alkyl" refers to a heteroarylalkyl group in which the heteroaryl has n to m members and the alkyl has p to q carbon atoms. In some embodiments, the heteroarylalkyl group is a 5 to 10-membered heteroaryl-C 1~3 Alkyl or C 1~9 Heteroaryl-C 1~3 The alkyl group is an alkyl group in which the heteroaryl group is monocyclic or bicyclic and has one, two, three, four, or five heteroatom ring members independently selected from nitrogen, sulfur, and oxygen. In some embodiments, the heteroarylalkyl group is C 1~9 Heteroaryl-C 1~4 The alkyl group is such that the heteroaryl moiety is monocyclic or bicyclic and has one, two, three, or four heteroatom ring members independently selected from nitrogen, sulfur, and oxygen. Examples include pyridylmethyl, e.g., 2-pyridylmethyl, 3-pyridylmethyl, or 4-pyridylmethyl.

[0118] When used alone or in combination with other terms, the term "cycloalkyl" refers to a non-aromatic saturated monocyclic, bicyclic, or polycyclic hydrocarbon ring system. This term includes cyclized alkyl groups and cyclized alkenyl groups. n~m The term "cycloalkyl" refers to a cycloalkyl group having n to m ring-member carbon atoms. Cycloalkyl groups can be monocyclic or polycyclic (e.g., having two, three, or four fused rings), and may include spiro rings. Cycloalkyl groups can have three, four, five, six, or seven ring-forming carbon atoms (C 3~7In some embodiments, the cycloalkyl group has 3 to 6 ring members, 3 to 5 ring members, or 3 to 4 ring members. In some embodiments, the cycloalkyl group is monocyclic. In some embodiments, the cycloalkyl group is monocyclic or bicyclic. In some embodiments, the cycloalkyl group is C 3~6 These are monocyclic cycloalkyl groups. The ring-forming carbon atoms of the cycloalkyl group may be oxidized to form an oxo group or a sulfide group. Cycloalkyl groups also include cycloalkylides. In some embodiments, cycloalkyls are cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl. Moles having one or more aromatic rings condensed to a cycloalkyl ring (i.e., having a common bond with the cycloalkyl ring), such as benzo or thienyl derivatives of cyclopentane, cyclohexane, etc., are also included in the definition of cycloalkyl. Cycloalkyl groups containing condensed aromatic rings may be bonded through any ring-forming atoms, including the ring-forming atoms of the condensed aromatic ring. Examples of cycloalkyl groups include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 4,4-dimethylcyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptatrienyl, norbornyl, norpinyl, norcarnyl, bicyclo[1.1.1]pentanyl, and bicyclo[2.1.1]hexanyl. In some embodiments, the cycloalkyl group is cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.

[0119] When used alone or in combination with other terms, the term "cycloalkylalkyl" refers to the group of the formula -alkylene-cycloalkyl, where n, m, p, and q are integers. n~m Cycloalkyl-C p~q The term alkyl refers to a cycloalkyl group having n to m carbon atoms bonded to an alkyl group having p to q carbon atoms. In some embodiments, cycloalkylalkyl groups are C 3~7 Cycloalkyl-C 1~3These are alkyl groups, where the cycloalkyl portion is monocyclic or bicyclic. Examples include cyclopropylmethyl, cyclobutylmethyl, cyclopentanemethyl, and cyclohexylmethyl.

[0120] When used alone or in combination with other terms, the term “heterocycloalkyl” means a non-aromatic ring or non-aromatic ring system having at least one heteroatom ring member, independently selected from nitrogen, sulfur, and oxygen, and which may include one or more alkenylene groups as part of its ring structure. “n-membered heterocycloalkyl” means a heteroaryl having n ring-forming atoms. “n-m-membered heterocycloalkyl” means a heterocycloalkyl having n-m ring-forming atoms. The number of carbon atoms in the ring is less than the number of heteroatoms than the number of ring-forming atoms. Therefore, in some embodiments, an n-membered heterocycloalkyl may have n-1, n-2, n-3, or n-4 ring carbon atoms, and an n-m-membered heterocycloalkyl may have n-1, n-2, n-3, or n-4 ring carbon atoms and m-1, m-2, m-3, or m-4 ring carbon atoms. In some embodiments, an n-m-membered heterocycloalkyl may have 1-m-1 ring carbon atoms. In some embodiments, heterocycloalkyl groups have 4 to 12 ring members, 4 to 10 ring members, 4 to 7 ring members, or 4 to 6 ring members. Monocyclic 4-membered, 5-membered, 6-membered, and 7-membered heterocycloalkyl groups are included in heterocycloalkyl groups. Heterocycloalkyl groups may include monocyclic or bicyclic (e.g., having two fused or bridging rings) ring systems. In some embodiments, heterocycloalkyl groups are monocyclic groups having one, two, or three heteroatoms independently selected from nitrogen, sulfur, and oxygen. The ring-forming carbon atoms and heteroatoms of heterocycloalkyl groups may be oxidized to form oxo groups or sulfide groups or other oxidative bonds (e.g., C(O), S(O), C(S), or S(O)2, N-oxide, etc.), and the nitrogen atom may be quaternized. Heterocycloalkyl groups may be bonded through ring-forming carbon atoms or ring-forming heteroatoms. In some embodiments, heterocycloalkyl groups contain 0 to 3 double bonds. In some embodiments, the heterocycloalkyl group contains 0 to 2 double bonds.Moles having one or more aromatic rings condensed to a heterocycloalkyl ring (i.e., sharing a common bond with the cycloalkyl ring), such as benzo or thienyl derivatives including piperidine, morpholine, and azepine, are also included in the definition of heterocycloalkyl. Heterocycloalkyl groups containing condensed aromatic rings can be bonded through any ring-forming atoms, including the ring-forming atoms of the condensed aromatic ring. Examples of heterocycloalkyl groups include azetidine, azepane, dihydrobenzofuran, dihydrofuran, dihydropyran, morpholine, 3-oxa-9-azaspiro[5.5]undecane, 1-oxa-8-azaspiro[4.5]decane, piperidine, piperazine, pyran, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, 1,2,3,4-tetrahydroquinoline, tropane, and thiomorpholine.

[0121] As used herein, the term "heterocycloalkylalkyl" alone or in combination with other terms means a group of the formula -alkylene-heterocycloalkyl. The term "n-membered heterocycloalkylalkyl" where n is an integer means a heteroarylalkylalkyl group in which the heterocycloalkyl is an n-member group. The term "n-m-membered C" where n, m, p, and q are integers. p~q The term "-alkyl" refers to a heterocycloalkyl group in which the heterocycloalkyl group has n to m members and the alkyl group has p to q carbon atoms. In some embodiments, the heterocycloalkyl group is a 4 to 10-membered heterocycloalkyl-C 1~3 Alkyl or C 1~9 Heterocycloalkyl-C 1~3 The alkyl group, where the heterocycloalkyl moiety is monocyclic or bicyclic and has one, two, three, four, or five heteroatom ring members independently selected from nitrogen, sulfur, and oxygen. In some embodiments, the heterocycloalkyl group is C 2~9 Heterocycloalkyl-C 1~4 Alkyl or C 2~9 Heterocycloalkyl-C 1~3The alkyl group is such that the heterocycloalkyl moiety is monocyclic or bicyclic and has one, two, three, or four heteroatom ring members independently selected from nitrogen, sulfur, and oxygen.

[0122] In certain contexts, the definition or aspect may refer to a specific ring (e.g., an azetidine ring, a pyridine ring, etc.). Unless otherwise indicated, these rings can bond to any ring member, provided that the bond does not exceed the valence of the atom. For example, an azetidine ring can bond at any position on the ring, while an azetidine-3-yl ring bonds at position 3.

[0123] If any two groups or two identical substituents are "independently selected" from the list of options, these groups may be the same or different. For example, R a and R b If is independently selected from the group consisting of alkyl, fluoro, amino, and hydroxyalkyl, then two R a Base and 2 R b A molecule having a group may have all groups as alkyl groups (for example, four different alkyl groups). Alternatively, the first R a The second R may be an alkyl group. a It may also be fluoro, and the first R b The second R may also be a hydroxyalkyl group. b R may be an amino (or any other substituent obtained from the group). Alternatively, both R a and the first R b It can also be fluoro, and the second R b The group may be alkyl (i.e., some pairs of substituents may be the same, while others may be different). Unless otherwise specified, if there are two or more groups with the same definition, and this definition specifies choices, it should be understood that each occurrence of the same group is independently selected from the possible choices. For example, two or more R groups. a The group is present in the compound, R a The definition is R a If it is specified that can be A, B, or C, then each R present in the compounda The group is independently selected from A, B, and C, and therefore R is present in the compound. a It should be understood that the base elements can be the same or different.

[0124] The compounds described herein may be asymmetric (e.g., having one or more stereocenters). Unless otherwise indicated, all stereoisomers, including enantiomers and diastereomers, are intended. Compounds described herein containing asymmetrically substituted carbon atoms can be isolated as optically active or racemic mixtures. Methods for preparing optically active compounds from optically inactive starting materials, such as racemic mixture resolution or stereoselective synthesis, are known in the art. Many geometric isomers, such as olefins and C=N double bonds, may be present in the compounds described herein, and all of these stable isomers are assumed in the present invention. The cis and trans geometric isomers of the compounds of the present invention are described as isomeric mixtures or as separate isomers and are isolated.

[0125] The separation of racemic mixtures of compounds can be carried out by any of the many methods known in the art. One method is fractional recrystallization using chiral dividing acids, which are optically active salt-forming organic acids. Suitable dividing agents for fractional recrystallization include, for example, tartaric acid, diacetyltartaric acid, dibenzoyltartaric acid, mandelic acid, malic acid, lactic acid, or various optically active camphorsulfonic acids such as β-camphorsulfonic acid, including D and L isomers. Other suitable dividing agents for fractional recrystallization include α-methylbenzylamine, 2-phenylglycinol, norephedrine, ephedrine, N-methylephedrine, cyclohexylethylamine, and stereoisomerically pure forms of 1,2-diaminocyclohexane (e.g., S and R isomers, or diastereoisomerically pure forms).

[0126] The racemic mixture may be separated by elution on a column packed with an optically active resolving agent (e.g., dinitrobenzoylphenylglycine). A suitable eluent composition can be determined by those skilled in the art.

[0127] In some embodiments, the compounds of the present invention exhibit an (R)-configuration. In other embodiments, the compounds exhibit an (S)-configuration. Unless otherwise specified, in compounds having two or more chiral centers, each chiral center in the compound may independently be (R) or (S).

[0128] The compounds described herein may include tautomers. Tautomers arise from the exchange of a single bond with an adjacent double bond, involving the simultaneous transfer of protons. Tautomers include prototropic tautomers, which are isomeric protonated states having the same empirical formula and total charge. Exemplary prototropic tautomers include ketone-enol pairs, amide-imoid acid pairs, lactam-lactim pairs, enamine-imine pairs, and cyclic compounds in which protons can occupy two or more positions in the heterocyclic system, such as 1H- and 3H-imidazoles, 1H-, 2H-, and 4H-1,2,4-triazoles, 1H- and 2H-isoindoles, and 1H- and 2H-pyrazoles. Tautomers may exist in equilibrium or be sterically fixed to one form by appropriate substitution. This disclosure is intended to encompass all of these tautomers of the compounds described.

[0129] Furthermore, the compounds described herein may include all isotopes of elements that result in the intermediate or final compound. Isotopes include atoms that have the same atomic number but different mass numbers. For example, tritium and deuterium are isotopes of hydrogen.

[0130] As used herein, the term “compound” is intended to include all stereoisomers, geometric isomers, tautomers, and isotopes of the illustrated structure.

[0131] The compounds described herein may contain acidic and / or basic groups and may be capable of forming salts. This disclosure should be understood as intended to include all salts of compounds capable of forming salts, including both acidic and basic salts of the compounds, whether or not the possibility of salts is explicitly stated. Furthermore, where a compound that is a salt is described, the disclosure of such compound should be understood as intended to include all forms of such compound, including free bases or free acids and their alternative salt forms. The term “salt” means a derivative of the disclosed compound in which the parent compound has been modified by converting an existing acidic or basic moiety to its salt form. Examples of salts include, but are not limited to, mineral or organic salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and so on. The terms “a salt thereof,” “salt thereof,” or “salts thereof” are applicable to any preceding member of the relevant Markush group. For example, the group consisting of A, B, C, and their salts would include, within its scope, embodiments that are salts of A, embodiments that are salts of B, and embodiments that are salts of C.

[0132] The salts of the compounds disclosed herein include pharmaceutically acceptable salts. The term “pharmaceutically acceptable salt” means a non-toxic salt of a parent compound formed, for example, from a non-toxic inorganic or organic acid. The pharmaceutically acceptable salts of the present invention can be synthesized by conventional chemical methods from parent compounds containing a basic or acidic moiety. Generally, these salts can be prepared by reacting the free acid or free base form of these compounds with a stoichiometric amount of a suitable base or acid in water, an organic solvent, or a mixture thereof, generally in non-aqueous media such as ether, ethyl acetate, alcohol (e.g., methanol, ethanol, isopropanol, or butanol), or acetonitrile (ACN). A list of suitable salts is found in Remington's Pharmaceutical Sciences, 17 thEd., (Mack Publishing Company, Easton, 1985), p. 1418; Berge et al., J. Pharm. Sci., 1977, 66(1), 1-19; and Stahl et al., Handbook of Pharmaceutical Salts: Properties, Selection, and Use, (Wiley, 2002). In some embodiments, the compounds described herein include the N-oxide form. Further information regarding preferred pharmaceutically acceptable salts can be found in Remington's, Pharmaceutical Sciences (current edition), Mack Publishing Co., Easton, PA, incorporated herein by reference.

[0133] Compounds, and their salts, including pharmaceutically acceptable salts, can be observed with other substances such as water and solvents (e.g., hydrates and solvates), or they can be isolated. The compounds and their salts described herein may occur in various forms when in the solid state, for example, in the form of solvates including hydrates. Compounds may be polymorphs or any solid form such as solvates, and therefore, unless otherwise clearly indicated, references to compounds and their salts should be understood to encompass any solid form of the compound.

[0134] In some embodiments, the compounds or salts thereof described herein are substantially isolated. "Substantially isolated" means that the compound is at least partially or substantially separated from the environment in which it was formed or detected. Partial isolation may include, for example, compositions in which the compounds of the present invention are concentrated. Substantial isolation may include compositions containing at least about 50% by weight, at least about 60% by weight, at least about 70% by weight, at least about 80% by weight, at least about 90% by weight, at least about 95% by weight, at least about 97%, or at least about 99% by weight of the compounds or salts thereof of the present invention.

[0135] c. Abbreviations The following abbreviations are permitted for use herein and, unless otherwise specified, have the meanings set forth below: μ (micrometer); °C (degrees Celsius); Ac (acetyl); ACN (acetonitrile); anhyd (anhydrous); aq (aqueous solution); atm (atmosphere); Bn (benzyl); Boc (tert-butoxycarbonyl); Bu (butyl); calcd (calculated value); Cbz (benzyloxycarbonyl); chrom.(Chromatography); CPME (Cyclopentyl methyl ether); CH2Cl2 (Dichloromethane); concd (Concentration); conc (Concentration); DCC (N,N'-Dicyclohexylcarbodiimide); DIAD (Diisopropyl azodicarboxylate); DIEA (N,N-Diisopropylethylamine); DMAP (4-(N,N-Dimethylamino)pyridine); DMF (Dimethylformamide); DMSO (Dimethyl sulfoxide); EDC (N-(3-Dimethylaminopropyl)-N'-Ethylcarbodiimide hydrochloride); equiv (Equivalent); ES (Electrospray); Et (Ethyl); Et2O (Diethyl ether); g (Gram); h (Hour); HATU (N-[(Dimethylamino)-1H-1,2,3-Triazolo-[4,5-b]pyridine-1-ylmethylene]-N-methylmethaneaminium hexafluorophosphate N-oxide); HBTU(O-(benzotriazole-1-yl)-N,N,N',N'-tetramethyl-O-(1H-benzotriazole-1-yl)uronium hexafluorophosphate); HPLC (High-Performance Liquid Chromatography); HOBt (1-hydroxybenzotriazole hydrate); L (liter); m (milli); m- (meth); M (moles); MeCN (acetonitrile); min (minute); mL (milliliters); mol (moles; molecules (like mol wt)); Ms (methanesulfonyl); MS (mass spectrometry); MW (molecular weight); NBS (N-bromosuccinimide); NCS (N-chlorosuccinimide); NIS (N-iodosuccinimide); NHS (N-hydroxysuccinimide); NMM (4-methylmorpholine); NMR (nuclear magnetic resonance); o- (ortho); obsd (observed value); p- (para); Ph (phenyl); Phth (phthalimide); ppt (precipitate); Pr (propyl); psi (pounds per square inch); temp (temperature); TFA (trifluoroacetic acid); THF (tetrahydrofuran); TPP (triphenylphosphine); and Tr (trityl). Other abbreviations are also usable and have meanings that will be understood by those skilled in the art.

[0136] II. Compounds A. Compound of formula I-1 In certain contexts, this disclosure provides compounds of formula (I-1) or salts thereof: TIFF0007829249000120.tif31128In formula, Cy 1A is either non-substituted or substituted C 6~10 It is an aryl or unsubstituted or substituted 5-10 member heteroaryl; Cy 1A The ring atoms of the 5-10 membered heteroaryl that form the Cy 1A Substitution C that forms 6~10 Aryl or substituted 5-10 member heteroaryls are R Cy1A , halogen, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11, S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy1A C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy1A The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R group consist of one, two, three, or four heteroatoms selected from carbon atoms and O, N, and S. Cy1A Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11, S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo, R Cy1A Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R 11is H, or C 1~6 Alkyl, C 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 It is alkyl, R 11 C that forms 1~6 Alkyls are either unsubstituted or contain halogens, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo, R 11 C that forms 6~10 Aryl-C 1~6 Alkyl or 5-10 member heteroaryl-C 1~6 Alkyl is either unsubstituted or C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)Rb11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R 12 is H or C 1~6 It is alkyl; or, R 11 and R 12 These, together with the groups to which they are bonded, form a 4-6 membered heterocycloalkyl ring; A 11 CR 13 R 15 or N; Each R 13 Cy 1B , (CR 13A R 13B ) n3 Cy 1B , (C 1~6 Alkilen)Cy 1B , (C 2~6 Alkenylene) Cy 1B , (C 2~6 Alkinylene)Cy 1B, or OCy 1B And R 13 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6 The alkylylene component is either unsubstituted or contains halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 Substituting with one, two, three, four, or five substituents independently selected from the group consisting of , and oxo; Each R 14 H and C are independent of each other. 1~6 Selected from alkyl groups; R 15 H, R 13 , C 1~6 Selected from alkyl and OH; R bonded to an adjacent carbon atom 14 R is bonded to pairs of groups or to adjacent carbon atoms. 14 Base and R 15 The pair with the base is the other R14 Independent of the existence of, together with, R 14 pairs of groups or R 14 Base and R 15 The bond may be replaced by a bond connecting the adjacent carbon atom to which the group is bonded, thereby connecting the adjacent carbon atoms by a double bond; or, R bonded to the same carbon atom 14 R groups bonded to each other, or to the same carbon atom 13 Base and R 15 The pair with the base is the other R 14 Independent of the existence of R 14 pairs of groups or R 13 Base and R 15 The pair with the group forms a spirocondensation with the carbon atom it is bonded to. 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring may be formed, and the ring atoms of the formed 4-10 membered heterocycloalkyl ring consist of a carbon atom and one, two, or three heteroatoms selected from O, N, and S, and the spirocondensation C formed 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring is a halogen, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NRc11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and may be further substituted with one, two, or three substituents independently selected from the oxo; or, R bonded to an adjacent carbon atom 14 R is bonded to pairs of groups or to adjacent carbon atoms. 14 Base and R 15 The pair with the base is the other R 14 Independent of the existence of R 14 pairs of groups or R 14 Base and R 15 It condenses together with the adjacent carbon atom to which it is bonded with the group. 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring may be formed, and the ring atoms of the formed 4-10 membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the formed condensation C 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring is a halogen, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11)NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and may be further substituted with one, two, or three substituents independently selected from the oxo; or, Four R atoms bonded to two adjacent carbon atoms 14 A group of R groups, or two R groups bonded to two adjacent carbon atoms 14 Base and 1 R 13 Base and 1 R 15 The group of elements is other R 14 Independent of the existence of the four R 14 A group of elements or two R 14 Base and 1 R 13 Base and 1 R 15 The group of atoms combines with the two adjacent carbon atoms to which it is bonded, forming a condensed C 6~10 Aryl ring or 5-10 membered heteroaryl ring, C 3~10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring may be formed, and the ring atoms of the formed 5-10 membered heteroaryl ring or 4-10 membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the formed condensation C 6~10 Aryl ring or 5-10 membered heteroaryl ring, C 3~10 A cycloalkyl ring, or a 4- to 10-membered heterocycloalkyl ring, is a halogen, C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and may be further substituted with one, two, or three substituents independently selected from the oxo; n1 is either 1 or 2; n2 is 0, 1, or 2; However, the sum of n1 and n2 is 1, 2, or 3; However, if n1 is 1 or n2 is 0, A 11 CR 13 R 15 and; n3 is 0, 1, or 2; Each R 13A H or C 1~6 It is alkyl; Each R 13B H or C 1~6 It is alkyl; or, R bonded to the same carbon atom 13A and R 13B is any other R 13A base and R 13B Originally independent, yet united - (CH2) 2~5 - may be formed, thereby forming a 3- to 6-membered cycloalkyl ring; Cy 1B is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10 Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 1B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 1B Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy1B , halogen, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11, S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy1B C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy1B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy1B Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NRc11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy1B Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R 16 H, Cy1C , C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkinyl, R 16 C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkinyl is either not substituted or Cy 1C , halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 It is substituted with one, two, three, four, or five substituents selected from the group consisting of , and oxo, however, R 16 One or fewer of the substituents are Cy 1C and; Cy 1C is either non-substituted or substituted C 6~10 Aryl, unsubstituted or substituted 5-10 member heteroaryl, unsubstituted or substituted C 3~10Cycloalkyl, or unsubstituted or substituted 4-10 member heterocycloalkyl; Cy 1C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 1C Substitution C that forms 6~10 Aryl, substituted 5-10 member heteroaryl, substituted C 3~10 Cycloalkyls, or substituted 4-10 member heterocycloalkyls, R Cy1C , halogen, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NRc11 R d11 Substituted with one, two, three, four, or five substituents independently selected from the , and oxo; Each R Cy1C C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Selected from cycloalkyl and 4-10 member heterocycloalkyl groups, R Cy1C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the R consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy1C Each C that forms 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NRc11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R Cy1C Each C that forms 6~10 Aryl, 5-10 member heteroaryl, C 3~10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 1~6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 S(O)2R b11 , NR c11 S(O)2R b11 , S(O)2NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R a11 , R b11 , R c11 , and R d11 H and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a11 , R b11 , R c11 , and R d11 The C that forms 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 6~10 Ariel, C 3~7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6~10 Aryl-C 1~3 Alkyl, 5-10 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-10 member heterocycloalkyl-C 1~3 Each alkyl group is C 1~6 Alkyl, Halo, CN, OR a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 R d12 , NR c12 C(=NRe12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 S(O)2R b12 , NR c12 S(O)2R b12 , S(O)2NR c12 R d12 , and may be substituted with one, two, three, four, or five substituents independently selected from the oxo; or, R bonded to the same N atom c11 and R d11 These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each being C 1~6 Alkyl, Halo, CN, OR a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 R d12 , NR c12 C(=NR e12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 S(O)2R b12 , NR c12 S(O)2R b12 , S(O)2NR c12 R d12, and may be substituted with one, two, or three substituents independently selected from the oxo; R a12 , R b12 , R c12 , and R d12 H and C are independent of each other. 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Selected from alkyl groups, R a12 , R b12 , R c12 , and R d12 The C that forms 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenil, C 2~6 Alkinyl, phenyl, C 3~7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1~3 Alkyl, 5-6 member heteroaryl-C 1~3 Alkyl, C 3~7 Cycloalkyl-C 1~3 Alkyl and 4-7 member heterocycloalkyl-C 1~3 Alkyl compounds are OH, CN, amino, and NH(C) respectively. 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 It may be substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; or, R bonded to the same N atom c12 and R d12These, together with the N atom to which they are both bonded, form a 4-membered, 5-membered, 6-membered, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is either unsubstituted or OH, CN, amino, NH(C) 1~6 Alkyl), N(C 1~6 Alkyl)2, Halo, C 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Haloalkyl, C 1~6 Substituted with one, two, or three substituents independently selected from haloalkoxys and oxos; R e11 and R e12 Each of these is independently H, CN, or NO2.

[0137] In some embodiments, the compound is of formula (I-2): This is the compound TIFF0007829249000121.tif40128.

[0138] In some aspects, Cy 1A It is either a non-substitutive or substitutive aryl.

[0139] In some aspects, Cy 1A It is an unsubstituted or substituted phenyl.

[0140] In some aspects, Cy 1A It is a substituted phenyl compound.

[0141] In some aspects, Cy 1A is at least one OR a11 or at least one C(=NR) e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , or C(=NR e11 )NR c11 C(O)OR a11It has been replaced with.

[0142] In some aspects, Cy 1A is at least one OR a11 It is replaced with and C 1~6 Alkyl, C 1~6 It is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens.

[0143] In some aspects, Cy 1A It is substituted with at least one OH group, and C 1~6 Alkyl, C 1~6 It is substituted with at least one further substituent selected from the group consisting of haloalkyls and halogens.

[0144] In some aspects, Cy 1A Preferably at position 4, at least one C(=NR) e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 It has been replaced with.

[0145] In some aspects, Cy 1A Preferably at position 4, at least one C(=NR) e11 )NR c11 R d11 It has been replaced with.

[0146] In some aspects, Cy 1A Preferably, at the 4th position, it is substituted with at least one C(=NH)NH2 molecule.

[0147] In some aspects, Cy 1A The formula is as follows: It is one of the following: TIFF0007829249000122.tif189147.

[0148] In some aspects, Cy 1A In the formula defining R, Cy1A C is independent 1~6 These are alkyl groups, such as methyl, or halogen groups, such as Cl or Br, or amino groups.

[0149] In some aspects, Cy 1A The formula is as follows: It is one of the following: TIFF0007829249000123.tif45131.

[0150] In some aspects, Cy 1A In the formula defining R a11 is C 1~6 Alkyl, for example, methyl, R b11 is C 1~6 Alkyl, for example, methyl, R b11 is C 1~6 Haloalkyls, for example, trifluoromethyl, R c11 This is an alkyl group, for example, methyl.

[0151] In some aspects, Cy 1A It is either unsubstituted or substituted heteroaryl.

[0152] In some aspects, Cy 1A These are unsubstituted or substituted pyridine-3-yl, 1H-pyrrolo[2,3-b]pyridine-5-yl, or 1H-benzo[d]imidazole-6-yl.

[0153] In some aspects, Cy 1A The formula is as follows: It is one of the following: TIFF0007829249000124.tif218149, TIFF0007829249000125, TIFF204136, TIFF0007829249000126, TIFF209141, TIFF0007829249000127, TIFF230144, or TIFF0007829249000128.tif60145.

[0154] In some aspects, Cy 1A Each R in the formula defining Cy1A C is independent 1~6 The alkyl group is, for example, methyl or ethyl, preferably methyl, or the halogen is, for example, F, Cl, or Br, preferably Cl, or amino.

[0155] In some aspects, Cy 1A Each R bonded to nitrogen in the formula defining the Cy1A is C 1~6 Alkyl, for example, methyl or ethyl.

[0156] In some embodiments, R 11 is C 1~6 It is alkyl.

[0157] In some embodiments, R 11 It is methyl.

[0158] In some embodiments, R 11 H is H.

[0159] In some embodiments, R 12 H is H.

[0160] In some embodiments, R 12 is C 1~6 Alkyl, for example, methyl or ethyl, preferably methyl.

[0161] In some embodiments, R 11 and R 12 These groups, together with the groups to which they are bonded, form a 4- to 6-membered heterocycloalkyl ring.

[0162] In some embodiments, n1 is 1.

[0163] In some embodiments, n1 is 2.

[0164] In some embodiments, n2 is 0.

[0165] In some embodiments, n2 is 1.

[0166] In some embodiments, n2 is 2.

[0167] In some embodiments, the compound is represented by the following formulas (I-1a) to (I-1f) and (I-2a) to (I-2r): It matches any of the following: TIFF0007829249000129.tif30143, TIFF0007829249000130.tif217143, TIFF0007829249000131.tif198143, or TIFF0007829249000132.tif37143.

[0168] In some embodiments, the compounds are of the following formulas (I-1g)~(I-1o) and (I-2aa)~(I-2az): It matches any of the following: TIFF0007829249000133.tif148134, TIFF0007829249000134, TIFF209137, TIFF0007829249000135, TIFF173137, TIFF0007829249000136, TIFF68137.

[0169] In some embodiments, the compound is based on the following formulas (I-3) to (I-9): Matches any of the following: TIFF0007829249000137.tif138142.

[0170] In some embodiments, the compound is given by the following formulas (I-3a) to (I-3k): Matches any of the following: TIFF0007829249000138.tif191142.

[0171] In some embodiments, the compound is given by the following formulas (I-4a) to (I-4bf): It matches any of the following: TIFF0007829249000139.tif208142TIFF0007829249000140.tif208142TIFF0007829249000141.tif208142TIFF0007829249000142.tif228142TIFF0007829249000143.tif96141.

[0172] In some embodiments, the compound is given by the following formulas (I-5a) to (I-5u): Matches any of the following: TIFF0007829249000144.tif96141, TIFF0007829249000145.tif226141, or TIFF0007829249000146.tif28128.

[0173] In some embodiments, the compound is given by the following formulas (I-6a) to (I-6cw): TIFF0007829249000147.tif173141TIFF0007829249000148.tif208141TIFF000782 9249000149.tif209141TIFF0007829249000150.tif226141TIFF0007829249000151. It matches any of the following: tif220141TIFF0007829249000152, tif209141TIFF0007829249000153, tif211141TIFF0007829249000154, tif214141TIFF0007829249000155, or tif149141.

[0174] In some embodiments, the compound is given by the following formulas (I-7a) to (I-7co): TIFF0007829249000156.tif32141TIFF0007829249000157.tif208142TIFF0007829 249000158.tif209142TIFF0007829249000159.tif206142TIFF0007829249000160.t It matches any of the following: if228142TIFF0007829249000161, tif200142TIFF0007829249000162, tif217142TIFF0007829249000163, tif217142TIFF0007829249000164, or tif142141.

[0175] In some embodiments, the compound is given by the following formulas (I-8a)~(I-8z): It matches one of the following: TIFF0007829249000165.tif67134, TIFF0007829249000166.tif209134, or TIFF0007829249000167.tif173134.

[0176] In some embodiments, the compound is given by the following formulas (I-9a) to (I-9z): It matches one of the following: TIFF0007829249000168.tif32132, TIFF0007829249000169.tif209132, or TIFF0007829249000170.tif209132.

[0177] In some embodiments, R 13 is Cy 1B That is the case.

[0178] In some embodiments, R 13 is (C 1~6 Alkilen)Cy 1B , (C 2~6 Alkenylene) Cy 1B , or (C 2~6 Alkinylene)Cy 1B In some embodiments, R 13 C 1~6 Alkilen, C 2~6 Alkenylene, or C 2~6The alkynylene component is not substituted.

[0179] In some embodiments, R 13 (CR 13A R 13B ) n3 Cy 1B That is the case.

[0180] In some embodiments, each R 13A H is H.

[0181] In some embodiments, each R 13B H is H.

[0182] In some embodiments, n3 is 0.

[0183] In some embodiments, n3 is 1.

[0184] In some embodiments, n3 is 2.

[0185] In some embodiments, R 13 (CH2) 0~2 Cy 1B That is the case.

[0186] In some embodiments, R 13 is CH2Cy 1B That is the case.

[0187] In some embodiments, R 13 is CH2CH2Cy 1B That is the case.

[0188] In some embodiments, R 13 OCy 1B That is the case.

[0189] In some aspects, Cy 1B is non-substituted C 6~10 It is Ariel.

[0190] In some aspects, Cy 1B It is an unsubstituted phenyl compound.

[0191] In some aspects, Cy 1B This is an unsubstituted naphthyl, such as 1-naphthyl or 2-naphthyl.

[0192] In some aspects, Cy 1B These are unsubstituted 5-10 member heteroaryls.

[0193] In some aspects, Cy 1B These are unsubstituted pyridyls, such as unsubstituted 2-, 3-, or 4-pyridyls, or unsubstituted quinolyls, such as unsubstituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyls.

[0194] In some aspects, Cy 1B is substitution C 6~10 It is Ariel.

[0195] In some aspects, Cy 1B It is a substituted phenyl compound.

[0196] In some aspects, Cy 1B This is biphenylyl (i.e., phenyl-substituted phenyl), for example, 2-, 3-, or 4-biphenylyl.

[0197] In some aspects, Cy 1B is a substituted naphthyl, for example, 1-naphthyl or 2-naphthyl.

[0198] In some aspects, Cy 1B These are substituted 5- to 10-membered heteroaryls.

[0199] In some aspects, Cy 1B These are substituted pyridyls, such as substituted 2-, 3-, or 4-pyridyls, or substituted quinolyls, such as substituted 2-, 3-, 4-, 5-, 6-, 7-, or 8-quinolyls.

[0200] In some aspects, Cy 1B R Cy1B , halogen, and C1~6 Each R is substituted with one, two, three, four, or five substituents independently selected from the haloalkyl groups; Cy1B C is independent 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 6~10 Selected from aryl or 5-10 member heteroaryl, R Cy1B Each C that forms 6~10 Aryl or 5-10 member heteroaryls are either unsubstituted or halogenated. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 It is substituted with one, two, or three substituents independently selected from alkynyl and haloalkyl groups.

[0201] In some embodiments, R 13 The formula is as follows: Selected from the following: TIFF0007829249000171.tif196140TIFF0007829249000172.tif205137TIFF0007829249000173.tif208132TIFF0007829249000174.tif207136TIFF0007829249000175.tif173139.

[0202] In some embodiments, R 13 R in the expression representing Cy1B is C 1~6 The alkyl group is, for example...

Claims

1. Compounds of formula (I-1), or their stereoisomers, tautomers, or pharmaceutically acceptable salts: During the ceremony, Cy d11 , c11 , b11 , e11 , d11 , b11 , b11 , c11 , c11 , b11 , 2 , 1～6 , c11 , c11 , e11 , c11 , c11 , d11 , e11 , c11 , c11 , d11 , c11 , a11 , d11 , d11 , c11 , 2 , d11 , c11 , b11 , d11 , b11 , c11 , a11 , a11 , b11 , <00000​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​ d11 Substituting with one, two, three, four, or five substituents, each selected independently; Each R Cy1A is independently H, C 1～6 alkyl, halogen, amino, C 2～6 alkenyl, C 2～6 alkynyl, C 6～10 aryl, 5- to 10-membered heteroaryl, C 3～10 cycloalkyl, and 4- to 10-membered heterocycloalkyl, and the R Cy1A forming 5- to 10-membered heteroaryl or 4- to 10-membered heterocycloalkyl ring atoms consist of carbon atoms and one, two, three, or four heteroatoms selected from O, N, and S, and each C Cy1A forming R 1～6 alkyl, C 2～6 alkenyl, or C 2～6 alkynyl is independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 , OC(O)R b11 ]>, OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR<* c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R[[ID=8l]] b11 , NR c11 , S(O) 2 R b11 , and S(O) 2 , NR c11 R d11 It is substituted with one, two, or three substituents that are selected more independently, R Cy1A Each C that forms 6～10 Aryl, 5-10 membered heteroaryl, C 3～10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 1～6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 Substituting with one, two, or three substituents selected more independently; R 11 is H, or C 1～6 It is alkyl, R 11 C that forms 1～6 Alkyls are either unsubstituted or contain halogens, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , S(O) 2 NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo; R 12 is H or C 1～6 It is alkyl; A 11 CR 13 R 15 or NH, N-naphthyl, N-benzyl, or N-2-methylbenzyl; and; R 13, R 14, and R 15 are defined as follows: (i) to (v): (i) Each R 13 Cy 1B , (CR 13A R 13B ) n3 Cy 1B , (C 1～6 Alkilen)Cy 1B , (C 2～6 Alkenylene) Cy 1B , (C 2～6 Alkinylene)Cy 1B , or OCy 1B And R 13 C 1～6 Alkylene, C 2～6 Alkenylene, or C 2～6 The alkylylene component is either unsubstituted or contains halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 It is substituted with one, two, three, four, or five substituents independently selected from the group consisting of; Each R 14 H and C are independent of each other. 1～6 Selected from alkyl; and R 15 H, R 13 , C 1～6 Selected from alkyl and OH groups; (ii) Each R 13 is independently Cy 1B, (CR 13A R 13B) n3 Cy 1B, (C 1-6 alkylene) Cy 1B, (C 2-6 alkenylene) Cy 1B, (C 2-6 alkynylene) Cy 1B, or OCy 1B, and the C 1-6 alkylene, C 2-6 alkenylene, or C 2-6 alkynylene component of R 13 is either unsubstituted or halogen, CN, OR a11, SR a11, C(O)R b11, C(O)NR c11 R d11, C(O)OR a11, OC(O)R b11, OC(O)NR c11 R d11, NR c11 R d11, NR c11 C(O)R b11, NR It is substituted with one, two, three, four, or five substituents independently selected from the group consisting of c11 C(O)NR c11 R d11, NR c11 C(O)OR a11, C(=NR e11)NR c11 R d11, NR c11 C(=NR e11)NR c11 R d11, S(O)R b11, S(O)NR c11 R d11, S(O) 2 R b11, NR c11 S(O) 2 R b11, and S(O) 2 NR c11 R d11; R bonded to an adjacent carbon atom 14 R bonded to at least one of the paired groups and / or to an adjacent carbon atom 14 Base and R 15 The pair with the base is the other R 14 Independent of the existence of, together with, R 14 pairs of groups or R 14 Base and R 15 The R group is replaced by a bond connecting the adjacent carbon atom to which it is bonded, thereby connecting the adjacent carbon atoms by a double bond, and each R that is not replaced by this bond 14 H and C are independent of each other. 1～6 R selected from alkyl groups and not replaced by the bond 15 H, R 13 , C 1～6 Selected from alkyl and OH groups; (iii) Each R 13 is independently Cy 1B, (CR 13A R 13B) n3 Cy 1B, (C 1-6 alkylene) Cy 1B, (C 2-6 alkenylene) Cy 1B, (C 2-6 alkynylene) Cy 1B, or OCy 1B, and the C 1-6 alkylene, C 2-6 alkenylene, or C 2-6 alkynylene component of R 13 is either unsubstituted or halogen, CN, OR a11, SR a11, C(O)R b11, C(O)NR c11 R d11, C(O)OR a11, OC(O)R b11, OC(O)NR c11 R d11, NR c11 R d11, NR c11 C(O)R b11, NR It is substituted with one, two, three, four, or five substituents independently selected from the group consisting of c11 C(O)NR c11 R d11, NR c11 C(O)OR a11, C(=NR e11)NR c11 R d11, NR c11 C(=NR e11)NR c11 R d11, S(O)R b11, S(O)NR c11 R d11, S(O) 2 R b11, NR c11 S(O) 2 R b11, and S(O) 2 NR c11 R d11; R bonded to the same carbon atom 14 R bonded to at least one of the pair of groups, or to the same carbon atom 13 Base and R 15 The pair with the base is the other R 14 Independent of the existence of R 14 pairs of groups or R 13 Base and R 15 The pair with the group forms a spirocondensation with the carbon atom it is bonded to. 3～10 A cycloalkyl ring or a 4- to 10-membered heterocycloalkyl ring is formed, and the ring atoms of the formed 4- to 10-membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the spirocondensation C is formed. 3～10 The cycloalkyl ring or 4- to 10-membered heterocycloalkyl ring is either unsubstituted or contains halogens. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , S(O) 2 NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo, where each R not forming the ring 14 H and C are independent of each other. 1～6 R selected from alkyl groups that do not form the ring 15 H, R 13 , C 1～6 Selected from alkyl and OH groups; (iv) Each R 13 is independently Cy 1B, (CR 13A R 13B) n3 Cy 1B, (C 1-6 alkylene) Cy 1B, (C 2-6 alkenylene) Cy 1B, (C 2-6 alkynylene) Cy 1B, or OCy 1B, and the C 1-6 alkylene, C 2-6 alkenylene, or C 2-6 alkynylene component of R 13 is either unsubstituted or halogen, CN, OR a11, SR a11, C(O)R b11, C(O)NR c11 R d11, C(O)OR a11, OC(O)R b11, OC(O)NR c11 R d11, NR c11 R d11, NR c11 C(O)R b11, NR It is substituted with one, two, three, four, or five substituents independently selected from the group consisting of c11 C(O)NR c11 R d11, NR c11 C(O)OR a11, C(=NR e11)NR c11 R d11, NR c11 C(=NR e11)NR c11 R d11, S(O)R b11, S(O)NR c11 R d11, S(O) 2 R b11, NR c11 S(O) 2 R b11, and S(O) 2 NR c11 R d11; R bonded to an adjacent carbon atom 14 R bonded to at least one of the paired groups, or to an adjacent carbon atom. 14 Base and R 15 The pair with the base is the other R 14 Independent of the existence of R 14 pairs of groups or R 14 Base and R 15 It condenses together with the adjacent carbon atom to which it is bonded with the group. 3～10 A cycloalkyl ring or a 4- to 10-membered heterocycloalkyl ring is formed, and the ring atoms of the formed 4- to 10-membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the condensed C is formed. 3～10 The cycloalkyl ring or 4- to 10-membered heterocycloalkyl ring is either unsubstituted or contains halogens. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , S(O) 2 NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from the oxo, where each R not forming the ring 14 H and C are independent of each other. 1～6 R selected from alkyl groups that do not form the ring 15 H, R 13 , C 1～6 Selected from alkyl and OH groups; (v) Four R atoms bonded to two adjacent carbon atoms 14 A group of R groups, or two R groups bonded to two adjacent carbon atoms 14 Base and 1 R 13 Base and 1 R 15 The group of elements is the other R 14 Independent of the existence of the four R 14 A group of elements or two R 14 Base and 1 R 13 Base and 1 R 15 The group of atoms combines with the two adjacent carbon atoms to which it is bonded, forming a condensed C 6～10 Aryl ring or 5-10 membered heteroaryl ring, C 3～10 A cycloalkyl ring or a 4-10 membered heterocycloalkyl ring is formed, and the ring atoms of the formed 5-10 membered heteroaryl ring or 4-10 membered heterocycloalkyl ring consist of carbon atoms and one, two, or three heteroatoms selected from O, N, and S, and the condensed C 6～10 Aryl ring or 5-10 membered heteroaryl ring, C 3～10 The cycloalkyl ring, or 4- to 10-membered heterocycloalkyl ring, is either unsubstituted or contains halogens. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 It is substituted with one, two, or three substituents that are more independently selected, where each R does not form the ring. 14 H and C are independent of each other. 1～6 R selected from alkyl groups that do not form the ring 15 H, R 13 , C 1～6 Selected from alkyl and OH, each R 13 that does not form the ring is independently Cy 1B, (CR 13A R 13B) n3 Cy 1B, (C 1-6 alkylene) Cy 1B, (C 2-6 alkenylene) Cy 1B, (C 2-6 alkylylene) Cy 1B, or OCy 1B, where the C 1-6 alkylene, C 2-6 alkenylene, or C 2-6 alkylylene component of R 13 is unsubstituted or halogen, CN, OR a11, SR a11, C(O)R b11, C(O)NR c11 R d11, C(O)OR a11, OC(O)R b11, OC(O)NR c11 R d11, NR c11 R d11, NR c11 Substituting with one, two, three, four, or five substituents independently selected from the group consisting of C(O)R b11, NR c11 C(O)NR c11 R d11, NR c11 C(O)OR a11, C(=NR e11)NR c11 R d11, NR c11 C(=NR e11)NR c11 R d11, S(O)R b11, S(O)NR c11 R d11, S(O) 2 R b11, NR c11 S(O) 2 R b11, and S(O) 2 NR c11 R d11; n1 is either 1 or 2; n2 is 0, 1, or 2; However, the sum of n1 and n2 is 1, 2, or 3; However, if n1 is 1 or n2 is 0, A 11 CR 13 R 15 and; n3 is 0, 1, or 2; R 13A and R 13B are defined as follows: (vi) to (vii); (vi) Each R 13A H or C 1～6 It is alkyl; and Each R 13B H or C 1～6 It is alkyl; (vii) R bonded to the same carbon atom 13A and R 13B At least one of the pairs is any other R 13A base and R 13B Originally independent, then together - (CH 2 ) 2～5 - forms, thereby forming a 3- to 6-membered cycloalkyl ring, where R does not form the ring 13A base and R 13B Each group is independently either H or C 1～6 It is alkyl; Cy 1B is either non-substituted or substituted C 6～10 Aryl, unsubstituted or substituted 5- to 10-membered heteroaryl, unsubstituted or substituted C 3～10 Cycloalkyl, or unsubstituted or substituted 4- to 10-membered heterocycloalkyl; Cy 1B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 1B Substitution C that forms 6～10 Aryl, substituted 5-10 member heteroaryl, substituted C 3～10 Cycloalkyls, or substituted 4- to 10-membered heterocycloalkyls, R Cy1B , C 1～6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 Substituting with one, two, three, four, or five substituents, each selected independently; Each R Cy1B C is independent 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 6～10 Aryl, 5-10 membered heteroaryl, C 3～10 Selected from cycloalkyls, 4-10 member heterocycloalkyls, and halogens, R Cy1B The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; R Cy1B Each C that forms 1～6 Alkyl, C 2～6 Alkenyl, or C 2～6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , S(O) 2 NR c11 R d11 , and are substituted with one, two, or three substituents independently selected from phenyl; R Cy1B Each C that forms 6～10 Aryl, 5-10 membered heteroaryl, C 3～10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 1～6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 Substituting with one, two, or three substituents selected more independently; R 16 H, Cy 1C , C 1～6 Alkyl, C 2～6 Alkenyl, or C 2～6 It is alkinyl, R 16 C that forms 1～6 Alkyl, C 2～6 Alkenyl, or C 2～6 Alkinyl is either not substituted or Cy 1C , halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 It is substituted with one, two, three, four, or five substituents selected from the group consisting of the following, however, R 16 One or fewer of the substituents are Cy 1C and; Cy 1C is either non-substituted or substituted C 6～10 Aryl, unsubstituted or substituted 5- to 10-membered heteroaryl, unsubstituted or substituted C 3～10 Cycloalkyl, or unsubstituted or substituted 4- to 10-membered heterocycloalkyl; Cy 1C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; Cy 1C Substitution C that forms 6～10 Aryl, substituted 5-10 member heteroaryl, substituted C 3～10 Cycloalkyls, or substituted 4- to 10-membered heterocycloalkyls, R Cy1C , halogen, C 1～6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , C(=NR e11 )NR c11 C(O)OR a11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 Substituting with one, two, three, four, or five substituents, each selected independently; Each R Cy1C C is independent 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 6～10 Aryl, 5-10 membered heteroaryl, C 3～10 Selected from cycloalkyl and 4- to 10-membered heterocycloalkyl groups, R Cy1C The ring atoms of the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl groups that form the ring consist of one, two, or three heteroatoms selected from carbon atoms and O, N, and S; R Cy1C Each C that forms 1～6 Alkyl, C 2～6 Alkenyl, or C 2～6 Alkynnyls are independently unsubstituted or halogen, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 Substituted with one, two, or three substituents selected more independently; R Cy1C Each C that forms 6～10 Aryl, 5-10 membered heteroaryl, C 3～10 Cycloalkyls and 4- to 10-membered heterocycloalkyls are independently unsubstituted or halogenated. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 1～6 Haloalkyl, CN, OR a11 , SR a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , NR c11 R d11 , NR c11 C(O)R b11 , NR c11 C(O)NR c11 R d11 , NR c11 C(O)OR a11 , C(=NR e11 )NR c11 R d11 , NR c11 C(=NR e11 )NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , NR c11 S(O) 2 R b11 , and S(O) 2 NR c11 R d11 Substituting with one, two, or three substituents selected more independently; R a11 , and R b11 H and C are independent of each other. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 6～10 Ariel, C 3～7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6～10 Aryl-C 1～3 Alkyl, 5-10 member heteroaryl-C 1～3 Alkyl, C 3～7 Cycloalkyl-C 1～3 Alkyl and 4- to 10-membered heterocycloalkyl-C 1～3 Selected from alkyl groups, R a11 , and R b11 The C that forms 1～6 Alkyl, C 2～6 Alkenyl and C 2～6 Each alkynyl is either unsubstituted, or halo, CN, or OR. a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 R d12 , NR c12 C(=NR e12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 , S(O) 2 R b12 , NR c12 S(O) 2 R b12 , and S(O) 2 NR c12 R d12 Substituted with one, two, three, four, or five substituents that are more independently selected, forming R a11 and R b11, the C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C6-10 aryl-C1-3 alkyl, 5-10 membered heteroaryl-C1-3 alkyl, C3-7 cycloalkyl-C1-3 alkyl, and 4-10 membered heterocycloalkyl-C1-3 alkyl are each unsubstituted or C1-6 alkyl, halo, CN, OR a12, SR a12, C(O)R b12, C(O)NR c12 R d12, C(O)OR a12, OC(O)R b12, OC(O)NR c12 R d12, NR c12 R d12, NR Substituted with one, two, three, four, or five substituents independently selected from c12 C(O)R b12, NR c12 C(O)NR c12 R d12, NR c12 C(O)OR a12, C(=NR e12)NR c12 R d12, NR c12 C(=NR e12)NR c12 R d12, S(O)R b12, S(O)NR c12 R d12, S(O) 2 R b12, NR c12 S(O) 2 R b12, and S(O) 2 NR c12 R d12; R c11 , and R d11 H and C are independent of each other. 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl, C 6～10 Ariel, C 3～7 Cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6～10 Aryl-C 1～3 Alkyl, 5-10 member heteroaryl-C 1～3 Alkyl, C 3～7 Cycloalkyl-C 1～3 Alkyl and 4- to 10-membered heterocycloalkyl-C 1～3 Selected from alkyl groups, R c11 , and R d11 The C that forms 1～6 Alkyl, C 2～6 Alkenyl and C 2～6 Each alkynyl is either unsubstituted, or halo, CN, or OR. a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 R d12 , NR c12 C(=NR e12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 , S(O) 2 R b12 , NR c12 S(O) 2 R b12 , and S(O) 2 NR c12 R d12 Substituted with one, two, three, four, or five substituents that are more independently selected, forming R c11 and R d11, the C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C6-10 aryl-C1-3 alkyl, 5-10 membered heteroaryl-C1-3 alkyl, C3-7 cycloalkyl-C1-3 alkyl, and 4-10 membered heterocycloalkyl-C1-3 alkyl are each unsubstituted or C1-6 alkyl, halo, CN, OR a12, SR a12, C(O)R b12, C(O)NR c12 R d12, C(O)OR a12, OC(O)R b12, OC(O)NR c12 R d12, NR c12 R d12 , substituted with one, two, three, four, or five substituents independently selected from NR c12 C(O)R b12, NR c12 C(O)NR c12 R d12, NR c12 C(O)OR a12, C(=NR e12)NR c12 R d12, NR c12 C(=NR e12)NR c12 R d12, S(O)R b12, S(O)NR c12 R d12, S(O) 2 R b12, NR c12 S(O) 2 R b12, and S(O) 2 NR c12 R d12; or, R groups attached to the same N atom c11 and R d11 together with the N atom to which they are both attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is unsubstituted or substituted with 1, 2, or 3 substituents independently selected from C 1～6 alkyl, halo, CN, OR a12 , SR a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 , OC(O)R b12 , OC(O)NR c12 R d12 , NR c12 R d12 , NR c12 C(O)R b12 , NR c12 C(O)NR c12 R d12 , NR c12 C(O)OR a12 , C(=NR e12 )NR c12 R d12 , NR c12 C(=NR e12 )NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 , S(O) 2 R b12 , NR c12 S(O) 2 R b12 , and S(O) 2 NR c12 R d12 and are substituted with 1, 2, or 3 substituents independently selected therefrom; R a12 , and R b12 H and C are independent of each other. 1～6 Alkyl, C 1～6 Haloalkyl, C 2～6 Alkenil, C 2～6 Alkinyl, phenyl, C 3～7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1～3 Alkyl, 5-6 member heteroaryl-C 1～3 Alkyl, C 3～7 Cycloalkyl-C 1～3 Alkyl and 4- to 7-membered heterocycloalkyl-C 1～3 Selected from alkyl groups, R a12 , and R b12 The C that forms 1～6 Alkyl, C 1～6 Haloalkyl, C 2～6 Alkenyl and C 2～6 Each alkynyl is either unsubstituted or has the following properties: OH, CN, amino, NH(C) 1～6 Alkyl), N(C 1～6 Alkyl) 2 Each of the phenyl, C3-7 cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C1-3 alkyl, 5-6 member heteroaryl-C1-3 alkyl, C3-7 cycloalkyl-C1-3 alkyl, and 4-7 member heterocycloalkyl-C1-3 alkyl groups, forming R a12 and R b12, is either unsubstituted or substituted with one, two, or three substituents independently selected from OH, CN, amino, NH(C1-6 alkyl), N(C1-6 alkyl)2, halo, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and C1-6 haloalkoxy; R c12 , and R d12 H and C are independent of each other. 1～6 Alkyl, C 1～6 Haloalkyl, C 2～6 Alkenil, C 2～6 Alkinyl, phenyl, C 3～7 Cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C 1～3 Alkyl, 5-6 member heteroaryl-C 1～3 Alkyl, C 3～7 Cycloalkyl-C 1～3 Alkyl and 4- to 7-membered heterocycloalkyl-C 1～3 Selected from alkyl groups, R c12 , and R d12 The C that forms 1～6 Alkyl, C 1～6 Haloalkyl, C 2～6 Alkenyl and C 2～6 Each alkynyl is either unsubstituted or has the following properties: OH, CN, amino, NH(C) 1～6 Alkyl), N(C 1～6 Alkyl) 2 , and halo are substituted with one, two, or three substituents independently selected from phenyl, C3-7 cycloalkyl, 5-6 member heteroaryl, 4-7 member heterocycloalkyl, phenyl-C1-3 alkyl, 5-6 member heteroaryl-C1-3 alkyl, C3-7 cycloalkyl-C1-3 alkyl, and 4-7 member heterocycloalkyl-C1-3 alkyl, each of which is unsubstituted or substituted with one, two, or three substituents independently selected from OH, CN, amino, NH(C1-6 alkyl), N(C1-6 alkyl)2, halo, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and C1-6 haloalkoxy; or, R groups attached to the same N atom c12 and R d12 together with the N atom to which they are both attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group or a 5-membered heteroaryl group, each of which is unsubstituted or substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, NH(C 1～6 alkyl), N(C 1～6 alkyl) 2 , halo, C 1～6 alkyl, C 1～6 alkoxy, C 1～6 haloalkyl, and C 1～6 haloalkoxy; R e11 and R e12 These are H, CN, or NO, respectively, independently. 2 That is the case.

2. Equation (I-2): The compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

3. Cy 1A at least one OR a11 , C(=NR e11 )NR c11 R d11 , C(=NOR a11 )NR c11 R d11 , C(=NOC(O)R b11 )NR c11 R d11 , or C(=NR e11 )NR c11 C(O)OR a11 The compound according to claim 1, or its stereoisomer, tautomer, or pharmaceutically acceptable salt, which is substituted with .

4. Cy 1A The formula is as follows: It is one of the following: In the formula, each R Cy1A , R a11 , and R b11 H or C 1～6 The compound according to claim 1, which is alkyl, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

5. Cy 1A The formula is as follows: It is one of the following: In the formula, each R bonded to the carbon atom Cy1A C 1～6 Each R is an alkyl, halogen, or amino compound bonded to the nitrogen atom. Cy1A is H or C 1～6 The compound according to claim 1, which is alkyl, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

6. R 11 The compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein is methyl.

7. R 12 The compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein is H.

8. The following equations (I-3) to (I-9): A compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, that matches any one of the following.

9. The following equations (I-9a) to (I-9z): A compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, which matches any one of the above.

10. R 13 Cy 1B CH 2 Cy 1B CH 2 CH 2 Cy 1B , or OCy 1B And Cy 1B However, substitution or non-substitution C 6～10 The compound according to claim 9, which is an aryl, or a substituted or unsubstituted 5- to 10-membered heteroaryl, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

11. Cy 1B However, R Cy1B , halogen, and C 1～6 Substituting with one, two, three, four, or five substituents independently selected from the haloalkyl group; Each R Cy1B C 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Alkinyl and C 6～10 Selected from aryl or 5- to 10-membered heteroaryl, R Cy1B Each C that forms 6～10 Aryl or 5- to 10-membered heteroaryl compounds, either unsubstituted or with halogens, C 1～6 Alkyl, C 2～6 Alkenil, C 2～6 Substituted with one, two, or three substituents independently selected from alkynyl and haloalkyl groups. The compound according to claim 10, or its stereoisomer, tautomer, or pharmaceutically acceptable salt.

12. The following equations (I-8a) to (I-8z): A compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, which matches any of the above.

13. R 13 Cy 1B CH 2 Cy 1B CH 2 CH 2 Cy 1B , or OCy 1B And Cy 1B However, substitution or non-substitution C 6～10 The compound according to claim 12, which is an aryl, or a substituted or unsubstituted 5- to 10-membered heteroaryl, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

14. Cy 1B However, R Cy1B , halogen, C 1～6 Haloalkyl, CN, OR a11 , and NR c11 C(O)R b11 They are substituted with one or two substituents that are selected more independently of each other; Each R Cy1B C 1～6 Alkyl, C 3～10 Cycloalkyl, OR a11 Haloalkoxy, cyano, arylalkyl, C 3～6 Cycloalkyl, aminoalkyl, C 6～10 Selected from aryls and 5- to 10-membered heteroaryls, R Cy1B Each C that forms 6～10 Aryl or 5- to 10-membered heteroaryls, either unsubstituted or with halogens, CN, and C(O)NR c11 R d11 Substituted with one or two substituents that are selected more independently, The compound according to claim 13, or its stereoisomer, tautomer, or pharmaceutically acceptable salt.

15. R 13 The formula is as follows: A base selected from the bases, In the formula, R Cy1B H, C 1～6 The compound according to claim 1, which is alkyl or halogen, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

16. Each R 14 The compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein the compound is hydrogen.

17. R 15 The compound according to claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein the compound is hydrogen.

18. R 16 is hydrogen, unsubstituted or substituted C 1～6 Alkyl, unsubstituted, or substituted C 2～6 Alkenyl, or unsubstituted or substituted C 2～6 The compound according to claim 1, which is an alkynyl, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

19. below: A compound or salt thereof according to claim 1, having a structure selected from the group consisting of the following.

20. A pharmaceutical composition comprising the compound described in claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.

21. A pharmaceutical composition for inhibiting MASP-2 in a subject, comprising the compound described in claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

22. A pharmaceutical composition for treating a disease or condition treatable by inhibiting MASP-2, comprising the compound described in claim 1, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof.

23. Thrombotic microangiopathy (TMA), thrombotic thrombocytopenic purpura (TTP), refractory TTP, Upshaw-Schulmann syndrome (USS), hemolytic uremic syndrome (HUS), atypical hemolytic uremic syndrome (aHUS), factor H-independent atypical hemolytic uremic syndrome, aHUS secondary to infection, plasma therapy-resistant aHUS, TMA secondary to cancer, TMA secondary to chemotherapy, TMA secondary to transplantation, TMA associated with hematopoietic stem cell transplantation, mesangial proliferative glomerulonephritis, membranoglionic glomerulonephritis, membranoglionic glomerulonephritis (mesangial capillary glomerulonephritis), acute post-infectious glomerulonephritis (post-streptococcal glomerulonephritis), C3 glomerulopathy, cryoglobulin A pharmaceutical composition for the treatment of MASP-2-related diseases or disorders selected from the group consisting of septic glomerulonephritis, microimmune necrotizing crescentic glomerulonephritis, lupus nephritis, Henoch-Schönlein purpura nephritis, IgA nephropathy, renal fibrosis, proteinuria, inflammatory reactions resulting from tissue or organ transplantation, ischemia-reperfusion injury, complications associated with diabetes, cardiovascular disease or cardiovascular disorder, inflammatory gastrointestinal disorder, lung disorder, eye disease or eye disorder, disseminated intravascular coagulation, graft-versus-host disease, venous occlusion, and diffuse alveolar hemorrhage, comprising the compound described in claim 1, or its stereoisomer, tautomer, or pharmaceutically acceptable salt.

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