Compound for preventing or treating lipid metabolism-related diseases

Abstract

The present invention relates to the field of biopharmaceuticals, and specifically to an "LC3 binding moiety-lipid droplet binding moiety conjugate" formed by covalently bonding a structure capable of binding to LC3 with a structure capable of binding to lipid droplets, its pharmaceutically acceptable salts, stereoisomers, solvates, polymorphs, tautomers, isotope compounds, metabolites or prodrugs, and its use in the manufacture of drugs for the prevention or treatment of lipid metabolism-related diseases.

Description

[Technical Field]

[0001] The present invention relates to the field of biopharmaceuticals, in particular to the compound of formula (I), its pharmaceutically acceptable salts, stereoisomers, solvates, polymorphs, tautomers, isotopic compounds, metabolites or prodrugs, and its use in the manufacture of medicaments for the prevention or treatment of lipid metabolism-related diseases. [Background technology]

[0002] Lipid droplets (LDs) (also called liposomes) are present in all cells and are intracellular storage organelles that store neutral lipids. In different tissues, neutral lipids may vary in composition, but are primarily triglycerides and sterol esters. Lipid droplets are highly dynamic organelles that not only store neutral lipids but also participate in various physiological and pathological processes, such as metabolic disorders, immune responses, and pathogen infections. Their number and levels are associated with various diseases, and many common metabolic disorders, such as metabolic syndrome and obesity, consistently result in the abnormal accumulation of lipid droplets in non-adipose tissues. For example, abnormal accumulation of lipid droplets in the liver is also known as hepatic steatosis. Emerging evidence suggests that the accumulation of lipid droplets in cells is involved in lipotoxicity and precedes neurodegeneration.

[0003] Many diseases are caused by the excessive level of lipid droplets in certain cells or tissues, and for such diseases, the general treatment method is to reduce the level of lipid or lipid droplets.At present, some methods for controlling the level of lipid or lipid droplets are in the basic research stage, and often have low specificity, so a viable treatment method is to control the level of lipid or lipid droplets by using compounds (abbreviated as compounds) that reduce the number and size of lipid droplets.

[0004] Therefore, there is a need in the art for effective compounds that can treat or prevent lipid droplet-associated diseases. Summary of the Invention

[0005] In one aspect, the present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite, or prodrug thereof: LCM-L-TM (I) (In the formula, LCM is the LC3 binding moiety; L is a linker moiety, TM is the lipid droplet-binding moiety.

[0006] The LCM portion is a portion that has affinity for the LC3 protein, and the TM portion is a portion that can interact non-covalently with lipid droplets.

[0007] In another aspect, the present invention provides use of a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotopic compound, metabolite or prodrug thereof, or a pharmaceutical composition of the present invention, in the manufacture of a medicament for the treatment of a lipid metabolism-related disease, in one embodiment, the lipid metabolism-related disease is selected from MADD, obesity, NAFLD, type II diabetes, hepatocellular carcinoma, Alzheimer's disease and atherosclerosis.

[0008] In another aspect, the present invention provides a method for producing a compound of the present invention, the method comprising covalently linking a structure capable of binding to LC3 with a structure capable of binding to lipid droplets to form an "LC3 binding moiety-lipid droplet binding moiety conjugate" ("conjugate compound").

[0009] In a further aspect, the present invention provides a method for reducing intracellular lipid droplets, comprising contacting a cell or tissue containing lipid droplets with a conjugated compound comprising an LC3-binding moiety and a lipid droplet-binding moiety, wherein the lipid droplets are contained in the cell under physiological or pathological conditions and / or are induced to be produced by the cell. In one embodiment, the conjugated compound is a compound of Formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite, or prodrug thereof. [Brief explanation of the drawings]

[0010] In the figures, C1 represents Compound 1A, C2 represents Compound 2A, C3 represents Compound 3A, C4 represents Compound 4A, C5 represents Compound 5A, C6 represents Compound 6, C7 represents Compound 7, C8 represents Compound 8, C9 represents Compound 9, C10 represents Compound 10A, C11 represents Compound 11A, OA represents sodium oleate, SIV or ORBB represents Sudan IV (Oil Red BB), SIII represents Sudan III, GW5074 represents Compound A1, DP or AN2 represents Compound A5, and Linker represents 10-bromo-1-decanol.

[0011] [Figure 1] This is a diagram of the 1H NMR and 1H-1H NOESY spectra of compound 1A. In the diagram of the 1H-1H NOESY spectrum, the two auxiliary lines intersecting at right angles and the auxiliary circle at the intersection indicate the Ha and Hb-related signals in the diagram. [Figure 2] 1H NMR and 1H-1H NOESY spectra of compound 2A. In the 1H-1H NOESY spectrum, the two auxiliary lines intersecting at right angles and the auxiliary circle at the intersection indicate the Ha and Hb-related signals in the figure. [Figure 3] FIG. 1 is a nuclear magnetic resonance spectrum of compound 3A. [Figure 4] FIG. 1 is a nuclear magnetic resonance spectrum of compound 4A. [Figure 5]FIG. 1 is a nuclear magnetic resonance spectrum of compound 5A. [Figure 6] FIG. 1 is a nuclear magnetic resonance spectrum of Compound 6. [Figure 7] FIG. 1 is a nuclear magnetic resonance spectrum of Compound 7. [Figure 8] FIG. 1 is a nuclear magnetic resonance spectrum of Compound 8. [Figure 9] FIG. 1 is a nuclear magnetic resonance spectrum of Compound 9. [Figure 10] FIG. 1 is a nuclear magnetic resonance spectrum of Compound 10A. [Figure 11] FIG. 1 is a nuclear magnetic resonance spectrum of compound 10B. [Figure 12] FIG. 1 is a nuclear magnetic resonance spectrum of compound 11A. [Figure 13] This is a representative diagram showing the induction of lipid droplets in wild-type MEF cells, Atg5 knockout MEF cells, and SH-SY5Y cells (green indicates lipid droplets, and blue indicates cell nuclei). The compound concentrations are shown in the diagram, the treatment time is 24 hours, and the lipid droplets were stained with BODIPY (registered trademark) 493 / 503. The scale bar is 50 μm. [Figure 14] This is a diagram showing the induction of lipid droplets by treatment with extracellular oleic acid (OA). The BODIPY493 / 503 staining images show the staining results of cells induced by adding OA for 6 hours and control cells to which no OA was added. [Figure 15] Unconjugated LC3-binding compounds or lipid droplet-binding compounds do not affect BODIPY signaling. (B) Lipid droplets in SH-SY5Y cells induced by OA were stained with BODIPY in the presence of 50 μM Sudan IV, and no reduction in lipid droplet signaling was observed. (C-D) BODIPY493 / 503 staining results when lipid droplets in OA-induced cells were treated with unconjugated LC3-binding compounds or lipid droplet-binding compounds. [Figure 16A]The left figure is a representative diagram showing the reduction of induced lipid droplets in wild-type MEF cells by Compound 1A (green indicates lipid droplets, blue indicates cell nuclei). The compound concentrations are shown in the figure, and the treatment time is 24 h. Lipid droplets were stained with BODIPY® 493 / 503. The scale bar is 50 μm. The right figure shows the statistics of the changes in the number and size of lipid droplets (n=8 for each concentration). Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 16B] The left figure is a representative diagram showing the reduction of induced lipid droplets in wild-type MEF cells with compound 2A (green indicates lipid droplets, blue indicates cell nuclei). The compound concentrations are shown in the figure, and the treatment time is 24 h. Lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. The right figure shows the statistics of the change in the number and size of lipid droplets (n = 9 for each concentration). Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 17] The left panel shows a representative example of the case where Compound 1A and Compound 2A did not reduce lipid droplets in autophagy-deficient MEF cells (green indicates lipid droplets, blue indicates cell nuclei). After adding Compound 1A or Compound 2A (at the concentrations indicated), treatment with Compound 1A or Compound 2A did not alter the level of lipid droplets in autophagy-deficient MEF (Atg5- / -) cells. The compound treatment time was 24 h. Lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. The right panel shows the statistical changes in the number and size of lipid droplets (n = 6 for each concentration). Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 18]Representative images (left) and quantification (right) of the reduction of lipid droplets in SH-SY5Y cells by Compound 1A (Figure 18A) and Compound 2A (Figure 18B) (green indicates lipid droplets, blue indicates cell nuclei) are shown. Induction of autophagy by 4-h starvation (EBSS) after replacing the culture medium with EBSS or inhibition of autophagy by treatment with 5 mM NH4Cl significantly reduced or slightly increased lipid droplets, respectively. After addition of Compound 1A or Compound 2A (at the indicated concentrations), treatment with Compound 1A or Compound 2A significantly reduced lipid droplet levels in SH-SY5Y cells. The compound treatment time was 24 h. Lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. The right panel shows the statistical changes in lipid droplet number and size (n = 9 for each concentration). Statistical analysis will be performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 19] The left panel shows a representative example of the case where Compound 1A and Compound 2A did not reduce lipid droplets in SH-SY5Y cells in the presence of the autophagy inhibitor NH4Cl (5 mM) (lipid droplets are indicated in green, and cell nuclei are indicated in blue). After adding Compound 1A or Compound 2A (at the concentrations indicated) and NH4Cl (5 mM), treatment with Compound 1A or Compound 2A did not alter the lipid droplet levels in SH-SY5Y cells. The compound treatment time was 24 h. Lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. The right panel shows the statistical changes in the number and size of lipid droplets (n = 6 for each concentration). Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 20]Representative images (left) and quantification (right) of the effects of compounds on lipid droplets induced by OA in SH-SY5Y cells (Figure 20A) and wild-type MEF cells (Figure 20B) (lipid droplets are indicated in green and cell nuclei in blue). Compound concentrations are indicated in the figures, and the treatment time is 24 h. Lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. The right panel shows the statistics of changes in lipid droplet number and size (n = 9 for each concentration in panel A, n = 6 for each concentration in panel B). Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis against the DMSO group. Unconjugated LC3-binding compounds or lipid droplet probes did not reduce the number or size of lipid droplets in SH-SY5Y or MEF cells. [Figure 21] The upper image shows a representative image of adipocytes differentiated from 3T3-L1 preadipocytes without induction (green indicates lipid droplets, blue indicates cell nuclei). The compound significantly reduced lipid droplets in WAC, whereas treatment with 5 mM NH4Cl to inhibit autophagy slightly increased lipid droplets. Other control compounds had no effect on lipid droplets. The compound treatment time was 24 h. Lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. The right image shows the statistical changes in the number and size of lipid droplets (n = 15). Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 22] The affinity of the conjugate compounds Sudan III and Sudan IV to LC3B was measured using MST. When the Kd of the conjugate compounds was in the submicromolar to micromolar range, no affinity between the lipid droplet probe and LC3B was observed. [Figure 23] The left panel shows a schematic of how ternary complex formation is measured using a modified ELISA, and the right panel shows sample ELISA signals (n=3) after blank correction. [Figure 24]In the left panel, the autophagosome marker protein LC3B puncta (red) indicated by mCherry indicate autophagosomes, BODIPY® 493 / 503 staining indicates lipid droplets (green), and DAPI indicates cell nuclei (blue). The average size of lipid droplets is larger than autophagosomes. The percentage of red overlapping or closely surrounding the green indicates colocalization of autophagosomes with lipid droplets. The right panel shows the percentage of sample lipid droplets that colocalized with autophagosomes. Experimental results are from two independent transfection batches. Analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis against the DMSO group. [Figure 25] The compounds are shown to process lipid droplets in wild-type and LC3B knockout HEK293T cells. Stained with BODIPY 493 / 503. Scale bar: 20 μm. [Figure 26] Compounds do not affect the level of autophagy. (A) The number of LC3B signal points remains unchanged in mCherry-LC3B-transfected MEF cells treated with compounds. (B) Lysotracker staining shows no change in the number of lysosomes. (C) MEF cells transfected with mRFP-GFP-LC3B treated with compounds or starved (4 hours after replacing the medium with EBSS). Regarding color, only red dots represent autolysosomes, and yellow dots represent autophagosomes. No change in the ratio of autolysosomes (ALYS, red+, green-) to autophagosomes (APHG, red+, green+) was observed, indicating that compounds do not affect autophagic flux. (D) Western blots show no change in LC3B and SQSTM1 / p62 in compound-treated MEF cells. LC3-II indicates autophagosomes, and tubulin is used as an internal control. The statistical results are shown in the following figures: Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 27] (A-B) Representative staining images (from >3 replicate experiments) show that the compounds do not damage the nuclear membrane (A, Lamin B1 immunostaining) or the cell membrane (B, CellMask™ staining). (C) Red indicates healthy mitochondria (MitoTracker™ Red), and green indicates total mitochondria (MitoTracker™ Green). For each well, the ratio of red + green + total area / green + area represents the percentage of healthy mitochondria and indicates mitochondrial membrane integrity. [Figure 28] This is a representative image (n=6) of endogenous lipid droplets (green indicates lipid droplets, blue indicates cell nuclei) in the human normal hepatocyte cell line QSG 7701 without induction. Compound 1A and Compound 2A significantly reduced lipid droplets in WAC, while treatment with 5 mM NH4Cl to inhibit autophagy slightly increased lipid droplets, while other control compounds had no effect on lipid droplets. The compound treatment time was 24 h, and lipid droplets were stained with BODIPY® 493 / 503. Scale bar = 50 μm. There are no statistical results because the endogenous lipid droplets in this hepatocyte cell line were too few and too small to accurately count. [Figure 29] In the upper panel, the compound reduces lipid droplets induced in wild-type MEF cells. The compound concentration is 5 μM, the treatment time is 24 h, and the lipid droplets were stained with BODIPY® 493 / 503. The scale bar is 50 μm. The middle left panel, middle right panel, and bottom panel show the statistics of the changes in the number and size of lipid droplets, as well as the measurement results of the cellular TAG level. Statistical analysis was performed using one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 30](A) The left panel shows body weight (measured daily and normalized to the average body weight on day 0), and the middle panel shows the fat / lean body mass ratio (12 days after injection) and liver weight (endpoint measurement 14 days after injection). (B) shows the endpoint measurement of liver triglyceride (TAG) and total cholesterol (TC) levels (14 days after injection). (C) shows serum triglyceride (TAG) and total cholesterol (TC) levels in db / db mice at different time points after injection. (D) shows endogenous lipid droplets in mouse liver section samples stained with BODIPY493 / 503 14 days after injection. For statistics, images of at least three sections were averaged for each mouse. (E) shows absolute quantification of liver lipidomics in db / db mice (four mice per group). The left panel shows the lipid concentration in the samples, expressed as log10. Deep red or light green indicates low concentrations. The blue dashed boxes indicate some key regions. For ease of comparison, DMSO data are placed in the middle. The right panel shows the log2FC of different lipids (X-axis) versus DMSO. A few lipids with very low abundance (total concentration <1 μg / g) are ignored. The area of ​​each symbol represents the lipid abundance in the DMSO group. Red indicates significant changes (log2FC absolute value >0.6, p<0.05 via two-tailed unpaired t-test). For measurements at multiple time points, statistical analysis was performed using two-way ANOVA and Dunnett's post-hoc analysis for the DMSO group; for endpoint measurements at multiple groups, one-way ANOVA and Dunnett's post-hoc analysis for the DMSO group. [Figure 31](A) shows the measurement of compound 3A concentrations in liver and plasma samples collected at the indicated time points after intraperitoneal injection of compound 3A (30 mg / kg). (B) shows the body weight, serum TC, and TAG levels in db / db mice injected with DMSO vehicle and db / db mice not injected with DMSO vehicle. It shows that DMSO does not decrease these indicators, nor does it significantly increase serum TAG. The DMSO group is the same as the group used in Figure 25. (C) shows an experiment similar to (B) conducted in NASH mice. The DMSO group is the same as the group used in Figure 33. (D) shows body weight-normalized food and water intake, using the same groups as Figures 25 and 30. The WT_DMSO group is the same as the Chow_DMSO group. In db mice, compound 4A and compound 3A caused a slight but significant increase in body weight-normalized food and water intake, respectively. (E-F) Serum (E) and endpoint liver (F) free fatty acid (FFA) levels for the indicated groups. The same groups are used as in Figures 25 and 30. Statistical analysis for multiple time-point measurements was performed using two-way ANOVA with Dunnett's post-hoc analysis for the DMSO group, and for multiple endpoint measurements was performed using one-way ANOVA with Dunnett's post-hoc analysis for the DMSO group. [Figure 32] Representative lipid analysis of liver based on lipidomics data. (A) shows the levels of ChE, TAG, PE, or PI with different fatty acid chain carbon numbers (chain carbon number #). The numbers in parentheses indicate the overall change in liver samples from mice treated with the compound compared to the DMSO control. [Figure 33](A) The left panel shows body weight (measured daily and normalized to the average body weight on day 0), and the middle panel shows the fat / lean body mass ratio (12 days after injection) and liver weight (endpoint measurement 14 days after injection). (B) Endpoint measurement of liver triglyceride (TAG) and total cholesterol (TC) levels (14 days after injection). (C) Serum triglyceride (TAG) and total cholesterol (TC) levels in NASH mice at different time points after injection. (D) Endogenous lipid droplets in mouse liver section samples stained with BODIPY493 / 503 after 14 days after injection (Scale bar = 50 μm). (E) Interstitial fibrosis assessment of mouse liver samples by picro-sirius staining after 14 days after injection. The red+ area was normalized to the green+ area and used to assess the degree of liver fibrosis. For measurements at multiple time points, statistical analysis was performed using two-way ANOVA analysis with Dunnett's post-hoc analysis for the DMSO group, and for endpoint measurements at multiple groups, one-way ANOVA analysis with Dunnett's post-hoc analysis for the DMSO group. DETAILED DESCRIPTION OF THE INVENTION

[0012] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by those skilled in the art to which this invention belongs. In the event of any discrepancy, the definitions in this application shall prevail. When a trade name is mentioned in this specification, it is intended to refer to the product corresponding to this trade name or its active ingredient. All patents, patent applications and publications cited in this specification are incorporated herein by reference.

[0013] General Terms and Definitions Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by those skilled in the art to which this invention belongs. In the event of any discrepancy, the definitions in this application shall prevail. When a trade name is mentioned in this specification, it is intended to refer to the product corresponding to this trade name or its active ingredient. All patents, patent applications and publications cited in this specification are incorporated herein by reference.

[0014] The terms "comprise," "include," "have," "contain," or "refer to," and other variations herein, are inclusive or open-ended and do not exclude other unrecited elements or method steps. As should be understood by those skilled in the art, the above terms, such as "comprise," cover the meaning of "consisting of."

[0015] The term "one or more" or similar expression "at least one" can refer to, for example, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more.

[0016] Where the lower and upper limits of a numerical range are disclosed, any value within that range and any included range is also specifically disclosed. In particular, each value range disclosed herein should be understood to represent each value and range within the broader range covered.

[0017] As used herein, the expression m to n refers to a range of m to n, a subrange consisting of each value in the range, and each value. For example, "C1 to C8" or "C 1-8 " should be understood to cover the range of 1 to 8 carbon atoms, and further cover any subranges of that range, such as C2 to C5, C3 to C4, C1 to C2, C1 to C3, C1 to C4, C1 to C5, C1 to C6, C1 to C7, and each value, such as C1, C2, C3, C4, C5, C6, C7, C8, etc. For example, "C3 to C 10 " or "C 3-10" should be understood in the same way, and includes, for example, C3 to C9, C6 to C9, C6 to C8, C6 to C7, C7 to C 10 , C7~C9, C7~C8, C8~C9, and any subranges such as C3, C4, C5, C6, C7, C8, C9, C 10 For example, the expression "3-membered to 10-membered" should be understood to cover any subrange of that range, such as 3-membered to 5-membered, 3-membered to 6-membered, 3-membered to 7-membered, 3-membered to 8-membered, 4-membered to 5-membered, 4-membered to 6-membered, 4-membered to 7-membered, 4-membered to 8-membered, 5-membered to 7-membered, 5-membered to 8-membered, 6-membered to 7-membered, 6-membered to 8-membered, 9-membered to 10-membered, etc., and each value of 3-membered, 4-membered, 5-membered, 6-membered, 7-membered, 8-membered, 9-membered, 10-membered, etc. Other similar expressions herein should be understood in the same manner.

[0018] The term "optionally" or "optionally" means that the subsequently described event or circumstance may or may not occur, and the description includes instances where the event or circumstance occurs and instances where the event or circumstance does not occur.

[0019] The terms "substituted" and "substituted" refer to the selective replacement of one or more (e.g., one, two, three, or four) hydrogens of a specified atom with a specified group, provided that the normal valence of the specified atom in its current context is not exceeded and that such substitution results in the formation of a stable compound. Combinations of substituents and / or variables are not permissible unless they result in the formation of a stable compound. When a substituent is described as absent, it is understood that the substituent may be one or more hydrogen atoms, provided that the compound remains stable according to the structure shown.

[0020] When it is stated that each carbon atom of a group may be optionally replaced with a heteroatom, it is provided that the normal valences of all atoms of the group in their current state are not exceeded and a stable compound is formed.

[0021] If a substituent is described as "...optionally substituted," the substituent may be unsubstituted or substituted. If an atom or group is described as being optionally substituted with one or more of a list of substituents, one or more hydrogens on the atom or group may be replaced with any independently selected substituent. If the substituent is oxo (i.e., =O), this means that two hydrogen atoms are replaced.

[0022] Unless otherwise specified, as used herein, the point of attachment of a substituent may be at any suitable position on the substituent. When a bond to a substituent is shown to cross a bond connecting two atoms in a ring, such substituent may be attached to any of the ring-forming atoms in that ring that are substitutable.

[0023] Any variable (e.g., R) and labeled variables (e.g., R X1 , R X2 , R X3 , R 2 , R 7 , R 8 , R a1 , R b1 , R c1 , R a2 , R b2 , R c2 , R 19 , R E , R F , R G , R a , R b , R c , R d When any of the following occurs more than one time in a composition or structure of a compound, each definition is independent at each occurrence. For example, if a group is substituted with 0, 1, 2, 3, or 4 R substituents, then said group is optionally substituted with at most 4 R substituents, and the options for each R substituent at each occurrence are all independent of each other.

[0024] The terms "halo" or "halogen" or "halogenated" shall be understood to refer to a fluorine (F), chlorine (Cl), bromine (Br) or iodine (I) atom, preferably a fluorine, chlorine or bromine atom.

[0025] The term "alkyl group" refers to a straight or branched chain saturated aliphatic hydrocarbon group composed of carbon and hydrogen atoms and attached to the rest of the molecule by a single bond. An "alkyl group" may have 1 to 8 carbon atoms, i.e., C 1-4 Alkyl group, C 1-3 Alkyl group, C 1-2 Alkyl group, C3 alkyl group, C4 alkyl group, C 1-6 Alkyl group, C 3-6 and "C1-C8 alkyl groups" such as alkyl groups. Non-limiting examples of alkyl groups include methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, isobutyl, s-butyl, t-butyl, isopentyl, 2-methylbutyl, 1-methylbutyl, 1-ethylpropyl, 1,2-dimethylpropyl, neopentyl, 1,1-dimethylpropyl, 4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl, 2-ethylbutyl, 1-ethylbutyl, 3,3-dimethylbutyl, 2,2-dimethylbutyl, 1,1-dimethylbutyl, 2,3-dimethylbutyl, 1,3-dimethylbutyl, or 1,2-dimethylbutyl groups, or isomers thereof. A "ylidene group" refers to a group obtained by removing one hydrogen atom from a carbon atom having a free valence electron and having two bonding sites for bonding to other parts of the molecule. For example, an "alkylene group" or an "alkylenylidene group" refers to a saturated, straight- or branched-chain divalent hydrocarbon group. When the described groups are bonded to each other, it is understood that this increases the bonding sites of each bonded group. For example, when an alkyl group is further bonded to another group so that it has two bonding sites, the alkyl group is considered to be an alkylene group.

[0026] The term "alkylene group," as used herein, alone or in combination with other groups, refers to a straight-chain or branched-chain saturated divalent hydrocarbon group. For example, the term "C 1-8The term "alkylene group" refers to an alkylene group having 1 to 8 carbon atoms, such as methylene, ethylene, propylene, butylene, pentylene, hexylene, 1-methylethylene, 2-methylethylene, methylpropylene, or ethylpropylene. The term "cycloalkylene group" refers to a cyclic saturated divalent hydrocarbon group. For example, the term "C 3-6 The term "cycloalkylene group" refers to a cycloalkylylidene group having 3 to 6 carbon atoms, such as a cyclopropylylidene group, a cyclobutylylidene group, a cyclopentylidene group, a cyclohexylidene group, etc. The term "alkoxyylidene group" refers to an "-O-alkylene group" or an "alkylene group -O-". 1-8 Examples of the "alkoxyylidene group" include, but are not limited to, -O-methylene, -O-ethylene, -O-propylene, -O-butylene, methylene group-O-, ethylene group-O-, propylene group-O-, butylene group-O-, and the like.

[0027] The term "alkenyl group" refers to a straight or branched chain unsaturated aliphatic hydrocarbon group composed of carbon and hydrogen atoms and having at least one double bond. An alkenyl group may have 2 to 8 carbon atoms, i.e., C 2-4 Alkenyl group, C 3-4 Alkenyl groups, etc. 2-8 An alkenyl group is an "alkenyl group." Non-limiting examples of alkenyl groups include, but are not limited to, vinyl, allyl, (E)-2-methylvinyl, (Z)-2-methylvinyl, (E)-butane-2-alkenyl, (Z)-butane-2-alkenyl, (E)-butane-1-alkenyl, (Z)-butane-1-alkenyl, and the like. When an alkenyl group is further bonded to another group such that it has two bonding sites, the alkenyl group is considered to be an alkenylidene group.

[0028] The term "alkynyl group" refers to a straight or branched chain unsaturated aliphatic hydrocarbon group composed of carbon and hydrogen atoms and having at least one triple bond. An alkynyl group may have 2 to 8 carbon atoms, i.e., C2-4 Alkynyl group, C 3-4 Alkynyl groups, etc. 2-8 An alkynyl group is an "alkynyl group." Non-limiting examples of alkynyl groups include, but are not limited to, ethynyl, propane-1-alkynyl, propane-2-alkynyl, butane-1-alkynyl, butane-2-alkynyl, butane-3-alkynyl, and the like. When an alkynyl group is further bonded to another group such that it has two bonding sites, the alkynyl group is considered to be an alkynylidene group.

[0029] The term "cyclic hydrocarbon group" refers to a saturated or unsaturated non-aromatic cyclic hydrocarbon group composed of carbon atoms and hydrogen atoms, preferably containing one or two rings. The cyclic hydrocarbon group may be a monocyclic, fused-ring polycyclic, bridged cyclic, or spirocyclic structure. The cyclic hydrocarbon group may have 3 to 10 carbon atoms, i.e., C 3-8 Cyclic hydrocarbon group, C 3-6 "C cyclic hydrocarbon group" such as C5 cyclic hydrocarbon group, C6 cyclic hydrocarbon group, C7 cyclic hydrocarbon group 3-10 The term "cyclic hydrocarbon group" refers to a "cyclic hydrocarbon group." Non-limiting examples of cyclic hydrocarbon groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclo[2.2.1]heptyl, and spiro[3.3]heptyl groups. The term also covers the case where a C atom may be substituted with oxo (=O). When a cyclic hydrocarbon group is further bonded to another group so that it has two bonding sites, the cyclic hydrocarbon group is considered to be a cycloalkylene group.

[0030] The term "cycloalkyl group" refers to a saturated cyclic hydrocarbon group. A cycloalkyl group may have 3 to 10 carbon atoms, i.e., C 3-8 Cycloalkyl groups, C 3-6 "C cycloalkyl group" such as C5 cycloalkyl group, C6 cycloalkyl group and C7 cycloalkyl group 3-10When a cycloalkyl group is further attached to another group so that it has two attachment points, the alkyl group is considered to be a cycloalkylene group.

[0031] The term "heterocyclic group" or "heterocyclic hydrocarbon group" refers to a monocyclic or bicyclic ring system (3-10-membered, 3-8-membered, 3-7-membered, 4-6-membered) having, for example, 3 to 10 (suitably 3 to 8, more suitably 3 to 7, particularly suitably 4 to 6) ring atoms, in which at least one ring atom (e.g., 1, 2 or 3) is a heteroatom selected from N, O, S and P, and the remaining ring atoms are C. The ring system may be saturated (to be understood as the corresponding "heterocycloalkyl group") or unsaturated (i.e., having one or more double and / or triple bonds within the ring). A "heterocyclic group" or "heterocyclic hydrocarbon group" does not have aromatic character. The term further covers when a C atom is replaced by oxo (=O), and / or when a ring S atom is replaced by one or two oxo (=O), and / or when a ring P atom is replaced by one or two oxo (=O). When a heterocyclic group is further bonded to another group so that it has two bonding sites, the heterocyclic group is considered to be a heterocyclylidene group.

[0032] The heterocyclic group may be, for example, a four-membered ring such as an azetidinyl group or an oxetanyl group, or a five-membered ring such as a tetrahydrofuranyl group, a dioxolinyl group, a pyrrolidinyl group, an imidazolidinyl group, a pyrazolidinyl group, a pyrrolinyl group, an oxopyrrolidinyl group, or a 2-oxoimidazolidin-1-yl group, or a six-membered ring such as a tetrahydropyranyl group, a piperidinyl group, a morpholinyl group, a dithiane group, a thiomorpholinyl group, a piperazinyl group, a 1,1-dioxo-1,2-thiazan-2-yl group, or a trithiane group, or a seven-membered ring such as a diazepine ring. Optionally, the heterocyclic group may be benzo-fused.

[0033] Heterocyclic groups may be bicyclic, for example, but are not limited to, 5-membered / 5-membered rings such as hexahydrocyclopenta[c]pyrrol-2(1H)-yl rings, or 5-membered / 6-membered bicyclic rings such as hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl rings.

[0034] As described above, the heterocycle may be unsaturated, i.e., may contain one or more double bonds, but is not limited thereto. For example, an unsaturated heterocycle containing a nitrogen atom may be a 1,6-dihydropyrimidine, 1,2-dihydropyrimidine, 1,4-dihydropyrimidine, 1,6-dihydropyridine, 1,2-dihydropyridine, 1,4-dihydropyridine, 2,3-dihydro-1H-pyrrole, 3,4-dihydro-1H-pyrrole, 2,5-dihydro-1H-pyrrolyl, 4H-[1,3,4]thiadiazine, 4,5-dihydrooxazole, or 4H-[1,4]thiazine ring. An unsaturated heterocycle containing an oxygen atom may be a 2H-pyran, 4H-pyran, or 2,3-dihydrofuran ring. An unsaturated heterocycle containing a sulfur atom may be a 2H-thiopyran or 4H-thiopyran. The heterocycle may be, but is not limited to, a benzo-fused ring, for example, a dihydroisoquinoline ring.

[0035] The term "aryl group" refers to an all-carbon monocyclic or fused-ring polycyclic (e.g., bicyclic) aromatic ring group having a conjugated π-electron system. For example, an aryl group may have 6 to 14 carbon atoms, suitably 6 to 10, and more suitably 6 or 10. Examples of "aryl groups" include, but are not limited to, phenyl, naphthyl, anthryl, and the like. When an aryl group is further bonded to another group so as to provide two bonding sites, the aryl group is considered to be an arylylidene group.

[0036] The term "heteroaryl group" preferably denotes a monovalent, monocyclic, bicyclic, or tricyclic aromatic ring system having 5, 6, 7, 8, 9, or 10 ring atoms ("5- to 10-membered heteroaryl group"), in particular 5, 6, 9, or 10 ring atoms, including at least one (suitably 1 to 4, more suitably 1, 2, or 3) heteroatom, which may be the same or different, such as oxygen, nitrogen, or sulfur. In each case, the heteroaryl group may also be benzo-fused. In particular, heteroaryl groups include thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, and the like, and benzo derivatives thereof, such as benzofuryl, benzothienyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzotriazolyl, indazolyl, indolyl, isoisopropyl, and the like. and indolyl groups, etc., or pyridyl groups, pyridazyl groups, pyrimidyl groups, pyrazinyl groups, triazinyl groups, etc., and benzo derivatives thereof, such as quinolyl groups, quinazolinyl groups, isoquinolyl groups, etc., or azocinyl groups, indolizinyl groups, purine groups, etc., and benzo derivatives thereof, or cinnolinyl groups, phthalazinyl groups, quinazolinyl groups, quinoxalyl groups, naphthyridinyl groups, carbazolyl groups, acridinyl groups, etc. When a heteroaryl group is further bonded to another group so as to have two bonding sites, the heteroaryl group is considered to be an arylylidene group.

[0037] The term "hydrocarbon chain" refers to a linear group composed of carbon and hydrogen atoms, and may be linear or branched. The hydrocarbon chain may be saturated (i.e., an alkylene group) or unsaturated, i.e., it may contain one or more (preferably one) carbon-carbon double or triple bonds. Non-limiting examples of alkylene groups include, but are not limited to, methylene (-CH-), 1,1-ethylene (-CH(CH)-), 1,2-ethylene (-CHCH-), 1,1-propylene (-CH(CHCH)-), 1,2-propylene (-CHCH(CH)-), 1,3-propylene (-CHCHCH-), 1,4-butylene (-CHCHCHCHCH-), 1,7-heptylene (-CHCHCHCHCHCHCHCH-), and the like.

[0038] When a chemical bond is described herein as being attached to a molecule or a portion of a molecule, omitting the specific atoms bonded by the chemical bond refers to any atom in the molecule or portion that can be bonded by the chemical bond, provided that a stable structure can be formed. For example, when a portion of a molecule is described and placed in parentheses, e.g., parenthesis or square brackets, and another portion of the molecule is described as being bonded to the portion within the parentheses by a chemical bond, omitting the specific atoms within the parentheses that are bonded by the chemical bond refers to any atom in the portion within the parentheses that can be bonded by the chemical bond, provided that a stable structure can be formed.

[0039] The term "pharmaceutically acceptable" means capable, within the scope of sound medical judgment, of being in contact with the tissues of patients without causing excessive toxicity, irritation, allergic response or the like, and of being effectively used for its intended purpose with a reasonable benefit / risk ratio.

[0040] Pharmaceutically acceptable salts of the compounds of the present invention include their acid addition salts and base addition salts. Suitable acid addition salts are formed with acids that form pharmaceutically acceptable salts. Examples include hydrochloride, acetate, aspartate, benzoate, bicarbonate / carbonate, gluceptate, gluconate, nitrate, orotate, palmitate, and other similar salts. Suitable base addition salts are formed with bases that form pharmaceutically acceptable salts. Examples include aluminum salts, arginine salts, choline salts, magnesium salts, and other similar salts. Methods for preparing pharmaceutically acceptable salts of the compounds of the present invention are known to those skilled in the art.

[0041] The compounds of the present invention may exist in specific geometric or stereoisomeric forms. The present invention contemplates all compounds, including cis and trans isomers, (-)- and (+)-enantiomers, (R)- and (S)-enantiomers, diastereomers, (D)-isomers, (L)-isomers, and racemic and other mixtures thereof, e.g., enantiomerically or diastereomerically enriched mixtures, and all such mixtures are within the scope of the present invention. Substituents such as alkyl groups may have additional asymmetric carbon atoms. All of these isomers and mixtures thereof are within the scope of the present invention. In some embodiments, compounds are preferably isomeric compounds that exhibit superior biological activity. Purified or partially purified isomers and stereoisomers of the compounds of the present invention, or racemic or diastereomeric mixtures, are all within the scope of the present invention. Purification and separation of such materials can be achieved by standard techniques known in the art.

[0042] Optically pure enantiomers can be obtained by separation of racemic mixtures according to conventional methods, such as the formation of diastereomeric salts with optically active acids or bases, or by the formation of covalent diastereomers. Diastereomeric mixtures can be separated into their individual diastereomers based on their physical and / or chemical differences by methods known in the art (e.g., chromatography or fractional crystallization). The optically active enantiomeric base or acid is then released from the separated diastereomeric salt. Separation and racemization of the separate enantiomers can be achieved using chiral chromatography (e.g., chiral HPLC columns), with or without conventional derivatization treatment of the separated chiral isomers prior to separation depending on the method used to achieve more efficient separation of chiral isomers. Enzymatic methods can also be used to separate derivatized or underivatized chiral isomers. Similarly, optically active starting materials can be used to obtain optically pure compounds of the present invention by chiral synthesis.

[0043] The compounds of the present invention may also exist in tautomeric forms: the present invention includes all possible tautomers of the compounds of the present invention, including the forms of single tautomers or any mixture of said tautomers in any proportion.

[0044] The compounds of the present invention may exist in the form of solvates (preferably hydrates), which contain polar solvents that are structural elements of the crystal lattice of said compounds, such as water, methanol or ethanol, in particular. The amount of polar solvent, in particular water, may be stoichiometric or non-stoichiometric.

[0045] The present invention further covers all possible crystalline forms or polymorphs of the compounds of the present invention, which may be a single polymorph or a mixture of one or more polymorphs in any proportion.

[0046] The present invention further includes all pharmaceutically acceptable isotopically labeled compounds, which have an atomic mass or mass number different from the atomic mass or mass number predominant in nature, but are identical to the compounds of the present invention except for the replacement of one or more atoms by atoms having the same atomic number.

[0047] The present invention also includes within its scope metabolites of the compounds of the present invention, i.e., substances formed in the body upon administration of the compounds of the present invention. Metabolites of the compounds can be identified using techniques known in the art, and their activity can be characterized by test methods. Such products can be produced, for example, by oxidation, reduction, hydrolysis, amidation, deamidation, esterification, enzymatic degradation, etc., of the administered compound. Thus, the present invention includes metabolites of the compounds of the present invention, including compounds obtained by contacting a compound of the present invention with a mammal for a time sufficient to produce a metabolic product thereof.

[0048] The present invention further includes within its scope prodrugs of the compounds of the present invention, which are derivatives of certain compounds of the present invention that have little or no pharmacological activity themselves and that, when administered to or on the body, can be converted to compounds of the present invention having the desired activity, for example, by hydrolytic cleavage. Generally, such prodrugs are functional derivatives of the compounds and are readily convertible in vivo to compounds with the desired therapeutic activity. For summaries of prodrugs and methods for their preparation, see, for example, J. Rautio et al., Nature Reviews Drug Discovery (2008) 7, 255-270 and Prodrugs: Challenges and Rewards (V. Stella et al. ed., Springer, 2007). Prodrugs of the present invention may be prepared, for example, by replacing appropriate functional groups of the compounds of the present invention with certain moieties known to those skilled in the art as "pro-moieties."

[0049] The term "polymorph" or "crystalline polymorph" refers to a single crystalline polymorph or a mixture of one or more crystalline polymorphs in any proportion.

[0050] The term "crystalline form" or "crystal" refers to any solid material that exhibits three-dimensional order and, in contrast to amorphous solid materials, produces a characteristic X-ray powder diffraction pattern of well-defined peaks.

[0051] The term "amorphous" refers to any solid material that is disordered in three dimensions.

[0052] The term "hydrate" describes a solvate containing the drug and a stoichiometric or non-stoichiometric amount of water.

[0053] The term "pharmaceutically acceptable carrier" refers to a substance that does not have a significant irritating effect on the living body and does not impair the biological activity and properties of the active compound. "Pharmaceutically acceptable carrier" includes, but is not limited to, glidants, sweeteners, diluents, preservatives, dyes / colorants, flavoring agents, surfactants, wetting agents, dispersants, disintegrants, stabilizers, solvents, or emulsifiers. Non-limiting examples of such carriers include calcium carbonate, calcium phosphate, various sugars and various starches, cellulose derivatives, gelatin, vegetable oils, and polyethylene glycols.

[0054] The terms "administration" or "dosing" and the like refer to methods that allow delivery of a compound or composition to a desired site of biological action. These methods include, but are not limited to, oral or parenteral administration (including intracerebroventricular, intravenous, subcutaneous, intraperitoneal, intramuscular, or intravascular injection or infusion), topical administration, and rectal administration. In particular, injection or oral administration.

[0055] As used herein, the term "treatment" includes alleviating, reducing, or ameliorating a disease or symptom, preventing other symptoms, improving or preventing underlying metabolic factors of a symptom, inhibiting a disease or symptom, e.g., arresting the progression of a disease or symptom, alleviating a disease or symptom, promoting the remission of a disease or symptom, or arresting the symptoms of a disease or symptom, and broadly includes prevention. "Treatment" also includes achieving therapeutic benefit and / or prophylactic benefit. Therapeutic benefit refers to the eradication or amelioration of the condition being treated. Therapeutic benefit may also be achieved by eradicating or ameliorating one or more physiological symptoms associated with an underlying disease, such that an improvement in the disease is observed in a patient even though the patient still suffers from the underlying disease. Prophylactic benefit refers to the ability of a composition to be administered to a patient at risk of developing a particular disease or who reports one or more physiological symptoms of the disease, even if the disease has not been diagnosed.

[0056] The terms "active ingredient," "therapeutic agent," "active substance," or "active agent" refer to a chemical entity that can effectively treat or prevent a disorder, disease, or condition in a targeted subject.

[0057] The terms "effective amount," "therapeutically effective amount," or "prophylactically effective amount" for a drug, drug unit, or active ingredient refer to a sufficient amount of drug or agent used to achieve the expected effect while allowing for tolerable side effects. The effective amount varies from person to person, depends on the age and general condition of the individual, and also on the specific active substance; in some cases, an appropriate effective amount can be determined by one skilled in the art based on routine testing.

[0058] As used herein, an "individual" includes a human or a non-human animal. Exemplary human individuals include human individuals (referred to as patients) suffering from a disease (e.g., a disease described herein) or normal individuals. "Non-human animals" in the present invention include all vertebrates, e.g., non-mammals (e.g., birds, amphibians, reptiles) and mammals, e.g., non-human primates, domestic animals and / or domesticated animals (e.g., sheep, dogs, cats, cows, pigs, etc.).

[0059] Lipid droplets (LDs) are intracellular storage organelles that store neutral lipids. The surface of lipid droplets is covered with a single layer of phospholipid membrane, into which lipid droplet proteins are embedded. In different tissues, the neutral lipids stored in lipid droplets may vary in composition, but are primarily triglycerides and sterol esters. Depending on the cell type, several other endogenous neutral lipids (e.g., retinyl esters, ether-based lipids, and free cholesterol) may also be stored in LDs. Major proteins on the surface of lipid droplets are Perilipin family proteins (PAT family proteins), including Perilipin1, Perilipin2 (PLIN2, also known as Adipophilin or ADRP), Perilipin3 (PLIN3, also known as TIP47), Perilipin4 (PLIN4, also known as S3-12), and Perilipin5 (PLIN5 or OXPAT / LSDP5).

[0060] The term "lipid" refers to an organic compound with lipophilic or amphiphilic properties. Herein, it particularly refers to lipophilic organic compounds present in living organisms. Lipid molecules having an acidic group, such as a carboxyl group, a phosphoric acid / phosphate ester group, or a sulfonic acid group, are acidic lipids, examples of which include, but are not limited to, fatty acids and phospholipids. Lipid molecules without an acidic group are neutral lipids, examples of which include, but are not limited to, triglycerides, steroids (e.g., sterols), steroid esters (e.g., sterol esters), ether-based lipids, and neutral glycolipids. Examples of sterols include, but are not limited to, cholesterol. Examples of ether-based lipids include, but are not limited to, alkylglycerol (AKG) and alkylphospholipids. Herein, neutral lipids particularly refer to those stored in lipid droplets.

[0061] The term "steroid," also known as a steride, is a derivative of cyclopentanoperhydrophenanthrene. The term "sterol" refers to a steride containing an alcoholic hydroxyl group, also known as a steroid alcohol. The sterol is preferably a steride containing a 3-OH group, such as cholesterol (also known as a cholesteroid alcohol).

[0062] The term "steroid ester" or "sterol ester" refers to an ester formed between a steride (a sterol, also called a steroid alcohol) containing an alcoholic hydroxyl group and an acid, particularly a fatty acid. Examples of steroid esters include, but are not limited to, cholesteryl esters such as cholesterol oleate and linoleate.

[0063] The term "lipid droplet probe" refers to a small molecule known to indicate lipid droplets. Some lipid droplet probes can be detected by an optical signal under appropriate conditions. The optical signal may be fluorescent, with a wavelength in the visible light range, or may be invisible to the naked eye, such as infrared or near-infrared. Preferably, the "lipid droplet probe" is likely to partition into lipids rather than into the aqueous phase. It should be understood that some environmentally sensitive probes emit stronger signals in a lipophilic environment, but this does not indicate that they are likely to partition into lipids.

[0064] The terms "lipid droplet-binding structure," "lipid droplet-binding compound," and "lipid droplet-binding moiety" refer to a structure, compound, or molecular moiety capable of binding to lipid droplets, preferably selectively binding to lipid droplets in cells. The lipid droplet-binding compound herein includes known lipid droplet probes, compounds capable of binding to lipid droplet marker proteins, or compounds capable of binding to neutral lipids in lipid droplets. Lipid droplet marker proteins include, but are not limited to, Perilipin2 (PLIN2, also known as Adipophilin or ADRP, PMID: 30351430) and Perilipin3 (PLIN3, also known as TIP47, PMID: 25961502). Compounds capable of binding to neutral lipids in lipid droplets include, but are not limited to, steroids and steroid esters. Lipid droplet probes include, but are not limited to, lipid droplet-specific probes and probes that preferentially target lipid droplets in cells, preferably lipid droplet-specific probes.Examples of lipid droplet probes include lipophilic dye molecules with affinity for lipid droplets, such as azo dyes with affinity for lipid droplets (e.g., Oil Red BB, also known as Sudan I, Sudan II, Sudan III, and Sudan IV, Oil Red O (also known as Sudan 5B), Sudan Red G, and Sudan Black B (also known as Solvent Black 3)), reported by Fam et al. ("Recent Advances in Fluorescent Probes for Lipid Droplets," Materials (2018), 11, 1768), Nile Red, BODIPY® 493 / 503, monodansylpentane (compatible in multicolor, MDH), PyrPy 10d, and PyrPy 11c, PITE (pyroindole-tetraphenylethylene hybrid), TPE-AmAl, TPA-BI, LipidGreen, LipidGreen2, LD540, AF8, AF10, AFN, NAP AIEgen dyes (e.g., NAP-Ph, NAP-Br, NAP-CF3, NAP-Py), LD-BTD1, LipiDye, Phos 2a, Phos 2b, Phos 3a, Phos 3b, SF44, SF58, FAS, DPAS, BTD-coumarin hybrids (e.g., BTD-Lip), IND-TPA, photoactivatable AIE probes (e.g., BZT 3a, BZT 4a), LD-TPZn, LQD, photoactivatable AIE probes (e.g., PhotoAFN 2a-c), TPE-AC, TPMN, TTMN, MeTTMN, MeOTTMN, DCMa, DCI, DCFu, NLV-1, StatoMerocynaine dyes (SMCy dyes such as SMCy 3, SMCy 5.5).

[0065] The LC3 protein refers to the microtubule-associated protein 1 light chain 3 (MAP1LC3, LC3) family in the Atg8 protein family. The LC3 protein particularly refers to members of the human LC3 family, such as human microtubule-associated protein 1 light chain 3 alpha (MAP1LC3A, LC3A; see, for example, Uniprot Accession: Q9H492-1 and Q9H492-2), human microtubule-associated protein 1 light chain 3 beta (MAP1LC3B, LC3B; see, for example, Uniprot Accession: Q9GZQ8), or human microtubule-associated protein 1 light chain 3 gamma (MAP1LC3C, LC3C; see, for example, Uniprot Accession: Q9BXW4), particularly LC3A and LC3B, and more particularly LC3B.

[0066] LC3 proteins, such as LC3A, LC3B, and LC3C, can be localized to the membranes of pre-autophagosomes and autophagosomes and are important proteins in the autophagy process.

[0067] Usable forms of LC3 protein include, but are not limited to, LC3-I and LC3-II. Specifically, usable LC3 proteins include, but are not limited to, LC3A-I, LC3A-II, LC3B-I, LC3B-II, LC3C-I, or LC3C-II, preferably LC3A-II, LC3B-I, LC3B-II, LC3C-I, or LC3C-II, particularly LC3A-II, LC3B-I, or LC3B-II, and more particularly LC3B-I or LC3B-II.

[0068] As used herein, homologs of the LC3 protein may be used in the methods of the present invention, for example, as long as they are able to interact with lipid droplets.

[0069] As used herein, LC3 protein homologs may be derived from eukaryotes such as yeast, or from other non-human animals such as insects (e.g., Drosophila), fish, rodents, artiodactyls, and primates. LC3 protein homologs may also be derived from other proteins with similar structure and function, such as, but not limited to, GABARAP and GABARAPL1. For example, reference may be made to, but is not limited to, GABARAP (Uniprot Accession: O95166) and GABARAPL1 (Uniprot Accession: Q9H0R8-1 and Q9H0R8-2).

[0070] As used herein, fragments of the LC3 protein or its homologs may be used in the methods of the present invention, as long as they are capable of interacting with, for example, lipid droplets. Such fragments may have, for example, 25% or more, 30% or more, 35% or more, 40% or more, 50% or more, 60% or more, 70% or more, 80% or more, 90% or more, 95% or more, or 100% identity with the LC3 protein or its homologs.

[0071] To achieve the objectives of the present invention, proteins or fragments thereof that are identical or homologous to the LC3 protein or its homologs may be used, as long as they can be used in the methods of the present invention. For example, proteins that interact with lipid droplets may have an identity of 25% or more, 30% or more, 35% or more, 40% or more, 50% or more, 60% or more, 70% or more, 80% or more, 90% or more, 95% or more, or 100%.

[0072] In exemplary embodiments, the LC3 protein or a homolog thereof or a fragment thereof has 25% or more, 30% or more, 35% or more, 40% or more, 50% or more, 60% or more, 70% or more, 80% or more, 90% or more, 95% or more, or 100% sequence identity to the amino acid sequence of any of SEQ ID NOs: 1 to 4. As should be understood by those skilled in the art, this may indicate that the LC3 protein or a homolog thereof or a fragment thereof used may comprise such a sequence.

[0073] Those skilled in the art will further appreciate that modified or mature forms of the LC3 protein, its homologs, or fragments thereof can be used. For example, in some cases, amino acids 121-125 at the C-terminus of the LC3 protein, such as LC3A (e.g., SEQ ID NO:1 or SEQ ID NO:2), LC3B (e.g., SEQ ID NO:3), or LC3C (e.g., SEQ ID NO:4), are truncated. For example, in some cases, after the C-terminal amino acids are cleaved, the LC3 protein is lipidated to a phosphatidylethanolamine (PE)-modified form. Such solutions are also within the scope of the LC3 protein described in the present invention.

[0074] Those skilled in the art should understand that the LC3 protein, its homologs, or fragments thereof used in the present invention may be modified or altered according to actual needs. Such solutions are also within the scope of the present invention. Such modifications or alterations include, but are not limited to, the addition or labeling of a tag (e.g., GST or HIS), or the substitution, deletion, addition, or substitution of some amino acids. For example, to facilitate tag cleavage, a small modification or alteration can be made to the end of the sequence of SEQ ID NO:3. For example, replacing M at the N-terminus of SEQ ID NO:3 with GG, and then adding a tag such as GST to the modified or unmodified sequence, which can then be used in the present invention. Solutions corresponding to such modified or altered sequences, or sequences having 25% or more, 30% or more, 35% or more, 40% or more, 50% or more, 60% or more, 70% or more, 80% or more, 90% or more, 95% or more, or 100% sequence identity thereto, are also within the scope of the present invention.

[0075] The term "affinity activity screening" refers to the process of detecting the affinity binding between a sample and a target. The detection method used in affinity activity screening may be, for example, absorbance, radiation (e.g., scintillation proximity assay), fluorescence (e.g., fluorescence resonance energy transfer, fluorescence polarization assay, particularly time-related fluorescence technology), chemiluminescence (e.g., chemically amplified luminescence proximity homogeneous assay, ALPHAScreen), surface plasmon resonance (SPR, for example, GE's Biacore series implementation can be used), isothermal titration calorimetry (ITC), microscale thermophoresis (MST), or grazing incidence differential reflectance.

[0076] As used herein, "sequence identity" between two amino acid sequences refers to the percentage of amino acids that are identical between the two sequences. "Sequence homology" refers to the percentage of amino acids that are identical or represent conservative amino acid substitutions. For sequence comparison, one sequence is generally used as a reference sequence, and a test sequence is compared with a reference sequence. When using a sequence comparison algorithm, the test sequence and the reference sequence are input into a computer, subsequence coordinates are designated, if necessary, and sequence algorithm program parameters are designated. The sequence comparison algorithm calculates the percent sequence identity of the test sequence relative to the reference sequence based on the designated program parameters. Examples of algorithms suitable for determining percentages of sequence identity and sequence similarity include, but are not limited to, the BLAST algorithm and the BLAST 2.0 algorithm. Software for performing BLAST analysis can be obtained from the National Center for Biotechnology Information (NCBI).

[0077] The terms "small molecule compound," "small organic molecule," or "low molecular weight compound" refer to molecules having a size comparable to that of organic molecules commonly used in drugs. This term excludes biological macromolecules (e.g., proteins, nucleic acids, etc.), but covers low molecular weight proteins or their derivatives, such as dipeptides, tripeptides, tetrapeptides, pentapeptides, etc.

[0078] As used herein, the term "binding" refers to a covalent or non-covalent interaction. Examples of covalent binding include, but are not limited to, covalent binding via orthogonal organic chemical reactions, such as the Click reaction. Preferably, "LC3 binding" refers to having affinity (also referred to as binding affinity) for LC3 protein, and "lipid droplet binding" refers to having a non-covalent interaction with lipid droplets or components that make up lipid droplets. Examples of non-covalent interactions include affinity interactions, ion pair interactions, dipole-dipole electrostatic interactions, hydrogen bonds, π effects, induced dipole-dipole interactions, and hydrophobic effects.

[0079] Affinity can be detected by any known method. For example, a parameter of binding strength between the target molecule and the LC3 protein, its homolog, or a fragment thereof is measured. The parameter may vary depending on the binding test performed, but may be, for example, absorbance value, radioactive signal and / or distribution in the sample, fluorescent signal intensity and / or distribution in the sample, heat change, reflected light intensity, reflected light phase change, etc.

[0080] Non-covalent interaction can be detected by any known method.For example, measure the parameter of the binding strength between the molecule to be measured and neutral lipid, for example, measure the distribution in sample.In order to predict or estimate the distribution of molecules in the sample that contains neutral lipid, some methods can be used, for example, measure the solubility of molecules in neutral lipid under appropriate conditions, or measure the distribution of molecules between aqueous phase and oil phase formed by neutral lipid under appropriate conditions.

[0081] The terms "LC3 binding structure", "LC3 binding compound" and "LC3 binding moiety" refer to a structure, compound or molecular moiety that is capable of binding to an LC3 protein or a homologue or fragment thereof.

[0082] The terms "conjugate" or "link," or "binding" an LC3 binding moiety to a lipid droplet binding moiety, refer to the binding of structures having a specific function by a covalent bond. For example, the phrase "an LC3 binding moiety is conjugated to a lipid droplet binding moiety" refers to the covalent binding of a structure capable of binding to LC3 to a structure capable of binding to lipid droplets to form an "LC3 binding moiety-lipid droplet binding moiety-conjugate" (also referred to herein as a "conjugate compound"). "Unconjugated" indicates that the LC3 binding compound is not covalently bound to the lipid droplet binding moiety, or that the lipid droplet binding compound is not covalently bound to the LC3 binding moiety.

[0083] The term "lipid metabolism-related disease" refers to a lipid metabolism disorder and / or a disease caused by lipid metabolism activity, particularly a disease caused by a lipid metabolism disorder (e.g., a neutral lipid metabolism disorder). Lipid metabolism-related diseases include, but are not limited to, diseases associated with abnormal accumulation of lipid droplets.

[0084] The term "diseases associated with abnormal lipid droplet accumulation" refers to diseases caused by abnormal lipid droplet accumulation in somatic cells or diseases in which abnormal lipid droplet concentration appears during the disease process. Detecting the triglyceride or sterol content in tissues can determine whether an individual suffers from or is at risk of suffering from a disease associated with abnormal lipid droplet accumulation. Triglycerides and sterols are stored in the lipid droplets described above. Tissues or cells separated from tissues can be detected by histochemical methods, for example, by Oil Red O staining / BODIPY (e.g., BODIPY® 493 / 503) staining or by using a triglyceride or sterol kit (e.g., a commercially available kit). In a mouse model of non-alcoholic fatty liver disease (NAFLD), DAG and ceramide levels are elevated in hepatocytes, heart, and muscle LDs. Examples of diseases associated with abnormal lipid droplet accumulation include, but are not limited to, neutral lipid storage disease (NLSD), mutated multiple acyl-CoA dehydrogenase deficiency (MADD) in lymphoblastoid cells, obesity, intrahepatic lipid deposition (hepatic steatosis, e.g., NAFLD, particularly nonalcoholic steatohepatitis (NASH)), type II diabetes, hepatocellular carcinoma, Alzheimer's disease, and atherosclerosis. Examples of NLSD include, but are not limited to, NLSD I (Chanarin-Dorfman syndrome) and neutral lipid storage disease with myopathy (NLSDM).

[0085] Examples of diseases associated with abnormal lipid droplet accumulation include cholesteryl ester storage disease (CESD), familial hypercholesterolemia, metabolic syndrome, and stroke. "Pathological conditions associated with abnormal lipid droplet accumulation" include symptoms of diseases associated with abnormal lipid droplet accumulation and other pathological conditions or symptoms caused by abnormal lipid accumulation. Secondary dyslipidemia or abnormal blood lipids caused by various diseases produce "lipotoxicity" to organs, cells, or tissues, and such situations are included in pathological conditions associated with abnormal lipid droplet accumulation.

[0086] The basic mechanism of autophagy is classified into three types: macroautophagy, molecular chaperone-mediated autophagy (CMA), and microautophagy. As used herein, "autophagy" is not limited to macroautophagy, CMA, or microautophagy. Preferably, "autophagy" refers to macroautophagy. Macroautophagy is not limited to selective macroautophagy or non-selective macroautophagy. Some literature refers to the lipid macroautophagy form as lipid autophagy, abbreviated as lipophagy. Some literature recognizes that lipophagy can selectively distinguish lipids. Lipophagy is included within the scope of "autophagy" described herein.

[0087] The following detailed description of the invention is intended to illustrate non-limiting embodiments so that those skilled in the art can more fully understand the technical solution, principles and practical applications of the present invention, and can modify and implement the present invention in many forms so that the present invention can optimally meet the requirements of specific applications.

[0088] Compounds of the Invention In one aspect, the present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite, or prodrug thereof: LCM-L-TM (I) (In the formula, LCM is the LC3 binding moiety; L is a linker moiety, TM is the lipid droplet-binding moiety.

[0089] In one embodiment, the LCM and TM moieties are each independently selected from small molecule compounds. In a specific embodiment, the molecular weight of the LCM and TM moieties is each independently about 100 to about 2000 Da, preferably about 200 to about 1000 Da, e.g., about 200 to about 900 Da, about 200 to about 800 Da, about 200 to about 700 Da, about 200 to about 600 Da, or about 200 to about 500 Da.

[0090] In an alternative embodiment, the TM moiety binds to a lipid droplet-associated target. The lipid droplet-associated target is a component of lipid droplets, preferably selected from neutral lipids and lipid droplet marker proteins. In one embodiment, the neutral lipid is selected from triglycerides and cholesteryl esters. In one embodiment, the lipid droplet marker protein is selected from Perilipin family proteins (e.g., Perilipin1, Perilipin2, and Perilipin3). In a further embodiment, the lipid droplet marker protein is one that can be detected by a commercially available anti-lipid droplet marker protein antibody.

[0091] In another alternative embodiment, in the compound of formula (I), the LCM moiety may be linked to one or more TM moieties, or vice versa. When one or more TM moieties are present, each TM moiety may be independently selected, and each TM moiety may be the same or different. In one embodiment, there are multiple TM moieties targeting the same target. It should be understood that multiple identical or different TM moieties may be used in one conjugate compound, even if they target the same target. When one or more TM moieties are used, each linker L used may be independently selected. The target targeted by the TM moiety is a target associated with lipid droplets.

[0092] In one embodiment, the LCM portion interacts with the LC3 protein, and the TM portion interacts with lipid droplets, increasing their recognition by autophagosomes and thereby localizing the lipid droplets in close proximity to the autophagosomes to promote lipid droplet degradation.

[0093] In a further embodiment, the TM moiety itself does not have affinity activity for autophagosomes or lysosomes within the cell.

[0094] LCM part In one embodiment, an LC3 binding moiety refers to a moiety that has affinity for the LC3 protein. In one embodiment, the LCM moiety has the structure of formula (1) below, or a pharmaceutically acceptable salt thereof: [ka] (In the formula, Ring A is a benzene ring, Ring B is a saturated or unsaturated 5- or 6-membered heterocycle, the heterocycle containing 1, 2, or 3 heteroatoms each independently selected from N, O, and S; The C ring is C 6-10 an aryl group and a 5- to 10-membered heteroaryl group, and each of the aryl groups or heteroaryl groups is independently R X1and optionally substituted with one or more groups selected from L 1 is a bond or a C1-C6 hydrocarbon chain, Alternatively, the C ring is absent and L 1 does not exist, R 1 is =Y (where Y is O or S), or OR 7 and R 2 are independently H, halogen, -NO2, -CN, C at each occurrence. 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 Alkynyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl groups, =O, =S, =NR a1 , -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 , -C(=S)OR a1 , -C(=S)NR a1 R b1 , -C(=S)R a1 , -P(=O)(OR a1 ) OR b1 , -C(=NR a1 )NR b1 R c1, -OCN, -SCN, -N=C=O, -NCS, and the alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group, or heteroaryl group is selected from halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 Alkynyl groups, ═O, ═S, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 , -S(=O)R a2 and -C(=NR a2 )NR b2 R c2 and optionally substituted with one or more substituents selected from R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from R X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 The alkyl, alkenyl or alkynyl group is selected from the group consisting of halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 Alkylene group - 3-membered to 7-membered heterocyclic group) 2, ═O, —COOH and C 1-6 optionally substituted with one or more substituents selected from alkyl groups; R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group or aryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1, -S(=O)2OR Y1 , -S(=O)2R Y1 , -S(=O)2NR Y1 R Y2 , -S(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, ═O, ═S, —OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 and optionally substituted with one or more substituents selected from R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-8 Alkyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 optionally substituted with one or more substituents selected from alkynyl groups, -OH, -SH, -NH2, =O, and -COOH; n is 1 or 2.

[0095] In one embodiment, R 1 is ═O. In another embodiment, R 1 is =S. In another embodiment, R 1is OR 7 is.

[0096] In one embodiment, Ring B is a saturated or unsaturated 5- or 6-membered heterocycle containing 1, 2, or 3 heteroatoms, each independently selected from N, O, and S. In one embodiment, Ring B is a saturated or unsaturated 5-membered heterocycle containing 1 or 2 heteroatoms, each independently selected from N and O. In another embodiment, Ring B is dihydropyrrole. In another embodiment, Ring B is selected from 2,3-dihydro-1H-pyrrole and 3,4-dihydro-1H-pyrrole, preferably 2,3-dihydro-1H-pyrrole. In a further embodiment, Ring B is pyrrolidine.

[0097] In a further preferred embodiment, the AB ring system is [ka] wherein Y is O or S, and the C ring is a 5- to 7-membered heteroaryl group, preferably a 5- to 6-membered heteroaryl group, and particularly a 5-membered heteroaryl group, and each of the heteroaryl groups is independently R X1 In a particular embodiment, the AB ring system is optionally substituted with 1, 2, 3, 4 or 5 groups selected from: [ka] and the ring C is a 5- to 7-membered heteroaryl group, preferably a 5- to 6-membered heteroaryl group, particularly a 5-membered heteroaryl group, and each of the heteroaryl groups is independently R X1In another embodiment, the C ring contains 1, 2, 3, or 4 heteroatoms, each independently selected from N, O, and S, preferably N and O. In a further embodiment, the C ring contains at least one N atom. In one embodiment, the C ring is a 5-membered heteroaryl group containing 1 or 2 N atoms, each independently selected from R X1 In another embodiment, Ring C is selected from pyrrole and imidazole.

[0098] In one embodiment, Ring B is a saturated or unsaturated 6-membered heterocycle containing 1 or 2 heteroatoms, each independently selected from N and O. In another embodiment, Ring B is a dihydropyrimidine. In a preferred embodiment, Ring B is selected from 1,6-dihydropyrimidine, 1,2-dihydropyrimidine, and 1,4-dihydropyrimidine.

[0099] In a further preferred embodiment, the AB ring system is [ka] and Y is O or S. In a particular embodiment, the AB ring system is [ka] is.

[0100] In a further embodiment, the B ring is a 2H-pyran or a 4H-pyran. In a preferred embodiment, the AB ring system is [ka] and Y is O or S. In a particular embodiment, the AB ring system is [ka] is.

[0101] In a further embodiment, Ring C is a phenyl group and each independently R X1 is optionally substituted with 1, 2, 3, 4 or 5 groups selected from:

[0102] In one embodiment, L 1 is a bond. In another embodiment, L 1 is a C1-C6 hydrocarbon chain. 1 is a C1-C2 hydrocarbon chain.

[0103] In one embodiment, the AB ring system is [ka] , there is no C ring and there is no L1.

[0104] In another embodiment, Ring A is a benzene ring, Ring B is a saturated or unsaturated 5- or 6-membered heterocycle containing 1, 2, or 3 heteroatoms each independently selected from N, O, and S; The C ring is C 6-10 an aryl group and a 5- to 10-membered heteroaryl group, and each of the aryl groups or heteroaryl groups is independently R X1 and optionally substituted with one or more groups selected from L 1 is a bond or a C1-C6 hydrocarbon chain, R 1 is =Y (where Y is O or S), or OR 7 and R 2 are independently H, halogen, -NO2, -CN, C at each occurrence. 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 Alkynyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl groups, =O, =S, =NR a1 , -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 , -C(=S)OR a1 , -C(=S)NR a1 R b1 , -C(=S)R a1 , -P(=O)(OR a1 ) OR b1 , -C(=NR a1 )NR b1 R c1 , -OCN, -SCN, -N=C=O, -NCS, and the alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group, or heteroaryl group is selected from halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 Alkynyl groups, ═O, ═S, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 , -S(=O)R a2 and -C(=NR a2 )NRb2 R c2 and optionally substituted with one or more substituents selected from R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from R X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 The alkyl, alkenyl or alkynyl group is selected from the group consisting of halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 Alkylene group - 3-membered to 7-membered heterocyclic group) 2, ═O, —COOH and C 1-6 optionally substituted with one or more substituents selected from alkyl groups; R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group or aryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6alkyl groups), R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 , -S(=O)2OR Y1 , -S(=O)2R Y1 , -S(=O)2NR Y1 R Y2 , -S(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, ═O, ═S, —OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 and optionally substituted with one or more substituents selected from R Y1 , R Y2 , R Y3 , R Y4are independently expressed as H, C 1-8 Alkyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 optionally substituted with one or more substituents selected from alkynyl groups, -OH, -SH, -NH2, =O, and -COOH; n is 1.

[0105] Thus, in one embodiment, Formula (I) has the structure of Formula (i) below, where the LCM moiety is the structure of Formula (1) above (see Formula (1) above and embodiments thereof) or a pharmaceutically acceptable salt thereof: [ka]

[0106] In one embodiment, L may be covalently attached to any suitable site in formula (1).

[0107] Within the scope of the structure described in formula (1) is the structure described in formula (2) below: In one embodiment, the LCM moiety has the structure of formula (2) below. [ka] (In the formula, Y is O or S; The C ring is C 6-10an aryl group and a 5- to 7-membered heteroaryl group, and each of the aryl groups or heteroaryl groups is independently R X1 and optionally substituted with one or more groups selected from R 2 is H, C 1-8 alkyl groups, L 1 is a bond or a C1-C6 hydrocarbon chain, R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from R X1 , R X2 is as defined in equation (1).

[0108] In one embodiment, Y is O. When Y is O, formula (2) becomes: [ka] is.

[0109] In one embodiment, Ring C is a 5- to 6-membered heteroaryl group, each of which is independently R X1 In a preferred embodiment, Ring C is a 5-membered heteroaryl group, each of which is independently selected from R X1 In another embodiment, the C ring contains 1, 2, 3, or 4 heteroatoms, each independently selected from N, O, and S, preferably N and O. In a further embodiment, the C ring contains at least one N atom. In one embodiment, the C ring is a 5-membered heteroaryl group containing 1 or 2 N atoms, each independently selected from R X1 In another embodiment, Ring C is selected from pyrrole and imidazole.

[0110] In one embodiment, L 1 is a bond. In another embodiment, L 1 is a C1-C6 hydrocarbon chain. 1 is a C1-C2 hydrocarbon chain. 1 is a methylene or methine group. 1 is a methine group. 1 teeth, [ka] is.

[0111] In another particular embodiment, the structure of formula (2) is selected from compounds A1, A2, and A3. [ka]

[0112] Thus, in one embodiment, formula (I) has the structure of formula (ii) below, where the LCM moiety has the structure of formula (2) above (see formula (2) above and embodiments thereof) or a pharmaceutically acceptable salt thereof: [ka]

[0113] In one embodiment, L may be covalently attached to any suitable site in formula (2), such as, for example, —OH, a suitable heterocyclic N atom, or the like.

[0114] In another particular embodiment, the structure of formula (2) is selected from compounds A1, A2, and A3. [ka]

[0115] Within the scope of the structure described in formula (1) is the structure described in formula (3) below: In one embodiment, the LCM moiety has the structure of formula (3) below. [ka] (In the formula, Ring B is a saturated or unsaturated 6-membered heterocycle, the heterocycle containing 1, 2 or 3 heteroatoms each independently selected from N, O and S; The C ring is C 6-10 aryl groups, each independently R X1 and optionally substituted with one or more groups selected from Alternatively, the C ring is absent and L 1 does not exist, A ring, L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R X1 , n is as defined in formula (1).

[0116] In one embodiment, Ring B is a saturated or unsaturated 6-membered heterocycle containing 1, 2, or 3 heteroatoms, each independently selected from N, O, and S. In one embodiment, Ring B is a saturated or unsaturated 6-membered heterocycle containing 1 or 2 heteroatoms, each independently selected from N and O. In another embodiment, Ring B is a dihydropyrimidine. In a preferred embodiment, Ring B is selected from 1,6-dihydropyrimidine, 1,2-dihydropyrimidine, and 1,4-dihydropyrimidine.

[0117] In a further preferred embodiment, the AB ring system is [ka] and Y is O or S. In a particular embodiment, the AB ring system is [ka] is.

[0118] In a further embodiment, the B ring is a 2H-pyran or a 4H-pyran. In a preferred embodiment, the AB ring system is [ka] and Y is O or S. In a particular embodiment, the AB ring system is [ka] is.

[0119] In a further embodiment, Ring C is a phenyl group and each independently R X1 is optionally substituted with 1, 2, 3, 4 or 5 groups selected from:

[0120] In one embodiment, L 1 is a bond. In another embodiment, L 1 is a C1-C6 hydrocarbon chain. 1 is a C1-C2 hydrocarbon chain.

[0121] In one embodiment, the AB ring system is [ka] , there is no C ring and there is no L1.

[0122] Thus, in one embodiment, Formula (I) has the structure of Formula (iii) below, where the LCM moiety has the structure of Formula (3) above (see Formula (3) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0123] In one embodiment, L may be covalently attached to any suitable site in formula (3).

[0124] In an alternative embodiment, the B and C rings of the compound of formula (3) may further comprise L 2 to obtain a variant of the compound of formula (3), which has the structure of formula (3'): [ka] (In the formula, The C ring is C 6-10 aryl groups, each independently R X1 and optionally substituted with one or more groups selected from R 1 is H, =O, or OR 7 and L 1 is a bond or a C1-C2 hydrocarbon chain, L 2 is a bond or a C1-C2 hydrocarbon chain, L 1 and L 2 is not a bond at the same time, R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from A ring, B ring, R 2 ,n,R X1 is as defined in equation (3).

[0125] In one embodiment, R 1 is H.

[0126] In another embodiment, R 2 is -OH.

[0127] In one embodiment, R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl groups).

[0128] Thus, in one embodiment, formula (I) has the structure of formula (iii') below, where the LCM moiety is the structure of formula (3') above (see formula (3') above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0129] In one embodiment, L may be covalently attached to any suitable site in formula (3').

[0130] Within the scope of the structures described in formula (1) and formula (3) is the structure described in formula (4) below: In one embodiment, the LCM moiety has the structure of formula (4) below. [ka] (In the formula, Y is O or S; X is O, R 9 H, halogen, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2, -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 and -S(=O)R a2 and R a1 , R b1 , R a2 , R b2 is as defined in equation (3), R 10 H, halogen, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 alkyl groups, R 3 H, halogen, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 4 H, halogen, -NO2, -CN, C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 Selected from R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R 5 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R 6 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(benzyl group), -SH, -S(C 1-6 alkyl group), -S (benzyl group), -NH2, -NH(C 1-6alkyl group), -N(C 1-6 alkyl group), -NH (benzyl group), and the alkyl group or benzyl group is selected from halogen, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2) optionally substituted with one or more substituents selected from

[0131] In one embodiment, Y is O. When Y is O, formula (4) becomes: [ka] is.

[0132] In one embodiment, R 9 H, halogen, C 1-6 Alkyl group, -OR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -S(=O)2NR a1 R b1 wherein the alkyl group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 In one embodiment, R 9 is H, halogen, -OR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 In one embodiment, R 9 -OR a1 or -NR a1 R b1 In another embodiment, R9 is -C(=O)OR a2 or -C(=O)NR a2 R b2 In particular embodiments, R 9 is -C(=O)O(C 1-6 In particular embodiments, R 9 is -COOH.

[0133] In one embodiment, R 10 is selected from H, halogen, or a methyl group. 10 is H.

[0134] In one embodiment, R a1 , R b1 are independently expressed as H, C 1-6 Alkyl group, -C(=O)R Y1 wherein the alkyl group is selected from halogen, -OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 R is optionally substituted with one or more substituents selected from Y1 , R Y3 , R Y4 is as defined in formula (3). In one embodiment, R a1 , R b1 are independently expressed as H, C 1-6 Alkyl group, -C(=O)(C 1-6 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 In one embodiment, R a1 , R b1 are independently H and C for each occurrence. 1-6 The alkyl group is selected from the group consisting of:

[0135] In one embodiment, R a2 , R b2 are independently H and C for each occurrence. 1-6 The alkyl group is selected from the group consisting of:

[0136] In one embodiment, R 3 are H, -OH, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, —OH, —SH, —NH2, —NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 In one embodiment, R is optionally substituted with one or more substituents selected from alkylene groups (3- to 7-membered heterocyclic groups) and —COOH. 3 is selected from H, halogen, methyl group, —OH, —NH2, —NHCH3, and the methyl group is selected from halogen, —OH, —NH2, —NH(C 1-2 In one embodiment, R 3is selected from H, halogen, methyl group, —OH, —NH, —NHCH, said methyl group being optionally substituted with a substituent selected from halogen, —OH, —OCH, —NH, —NHCH. In one embodiment, R 3 is selected from H, halogen, methyl, —OH, and —NH. In one embodiment, R 3 is selected from H, F, Cl, a methyl group, —OH, and —NH. In another embodiment, R 3 is selected from H, F, a methyl group, —OH, and —NH. In particular embodiments, R 3 is selected from H, a methyl group, and —OH. In another particular embodiment, R 3 is H. In a further particular embodiment, R 3 is —OH. In another embodiment, R 3 is a dimethylaminomethyl group.

[0137] In one embodiment, R 4 H, -OR 7 , -SR 7 , -NR 7 R 8 Selected from R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 In one embodiment, R 4 is C 1-6 The alkyl group is a halogen atom, -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6In particular embodiments, R 4 is —CHCOOH. In another embodiment, R 4 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In one embodiment, R 4 H, halogen, C 1-3 Alkyl groups, -OH, -O(C 1-3 alkyl group), -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2 and -COOH, wherein the alkyl group is selected from halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In another particular embodiment, R is optionally substituted with one or more substituents selected from alkyl groups and -COOH. 4 is -OH.

[0138] In one embodiment, R 5 is H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 In another embodiment, R is optionally substituted with one or more substituents selected from alkylene groups (3- to 7-membered heterocyclic groups) and —COOH. 5 H, halogen, C 1-3 Alkyl groups, -OH, -O(C 1-3 alkyl group), -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2 and -COOH, wherein the alkyl group is selected from halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R is optionally substituted with one or more substituents selected from alkyl groups and -COOH. 5 H, halogen, C 1-3 Alkyl groups, -OH, -O(C 1-3 alkyl group), -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 5 is a dimethylaminomethyl group. In one embodiment, R5 is -OH.

[0139] In one embodiment, R 6 H, halogen, C 1-6 In one embodiment, R is selected from an alkyl group, —OH, —NH, wherein the alkyl group is optionally substituted with one or more substituents selected from a halogen, —OH, —NH. 6 are H, F, Cl, Br, and C 1-6 In one embodiment, R is selected from an alkyl group, —OH, —NH, wherein the alkyl group is optionally substituted with one or more substituents selected from a halogen, —OH, —NH. 6 is selected from H, F, Cl, Br, a methyl group, —OH, and —NH. In one embodiment, R 6 is H or —OH.

[0140] In one embodiment, R 3 is a methyl group, and R 4 are -OH, -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R is substituted with one or more substituents selected from alkyl groups and -COOH. 3 is a methyl group, and R 4 -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 and -COOH.

[0141] In another embodiment, R 3is a methyl group, and R 5 are -OH, -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In another embodiment, R is substituted with one or more substituents selected from alkyl groups and -COOH. 3 is a methyl group, and R 5 -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 and -COOH.

[0142] Thus, in one embodiment, formula (I) has the structure of formula (iv) below, where the LCM moiety has the structure of formula (4) above (see formula (4) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0143] In one embodiment, L may be covalently attached to any suitable site in formula (4).

[0144] The structure according to formula (5) below falls within the scope of the structures according to formula (1), formula (3) and formula (4). In one embodiment, the LCM moiety has the structure according to formula (5) below. [ka] (In the formula, Y, R 9 , R 10 , R3 , R 4 , R 5 , R 6 is defined as in equation (4).

[0145] In one embodiment, Y is O. When Y is O, formula (5) becomes: [ka] is.

[0146] In particular embodiments, the structure of formula (5) is compound A4 [ka] The structure is as follows.

[0147] Thus, in one embodiment, formula (I) has the structure of formula (v) below, where the LCM moiety has the structure of formula (5) above (see formula (5) above and embodiments thereof) or a pharmaceutically acceptable salt thereof: [ka]

[0148] In one embodiment, L may be covalently attached to any suitable site in formula (5), such as, for example, -OH, -COOH, etc.

[0149] In particular embodiments, the structure of formula (v) is [ka] is.

[0150] Within the scope of the structures described in formula (1) and formula (3) is the structure described in formula (6) below: In one embodiment, the LCM moiety has the structure of formula (6) below. [ka] (In the formula, Ring B is a saturated or unsaturated 6-membered heterocycle, the heterocycle containing 1, 2 or 3 heteroatoms each independently selected from N, O and S; The C ring is C 6-10 aryl groups, each independently R X1 and optionally substituted with one or more groups selected from L 1 is a bond or a C1-C6 hydrocarbon chain, R 2 H, halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 Alkynyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl groups, =O, =S, =NR a1 , -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 , -C(=S)OR a1 , -C(=S)NR a1 R b1 , -C(=S)R a1 , -P(=O)(OR a1 ) OR b1 , -C(=NR a1 )NR b1 R c1, -OCN, -SCN, -N=C=O, -NCS, and the alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group, or heteroaryl group is selected from halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 Alkynyl groups, ═O, ═S, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 , -S(=O)R a2 and -C(=NR a2 )NR b2 R c2 and optionally substituted with one or more substituents selected from R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from R X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 The alkyl, alkenyl or alkynyl group is selected from the group consisting of halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 Alkylene group - 3-membered to 7-membered heterocyclic group) 2, ═O, —COOH and C 1-6 optionally substituted with one or more substituents selected from alkyl groups; R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 , -S(=O)2OR Y1 , -S(=O)2R Y1, -S(=O)2NR Y1 R Y2 , -S(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, ═O, ═S, —OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 and optionally substituted with one or more substituents selected from R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-8 Alkyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 optionally substituted with one or more substituents selected from alkynyl groups, -OH, -SH, -NH2, =O, and -COOH; A ring, R 1 is as defined in equation (3).

[0151] In one embodiment, Ring B is a saturated or unsaturated 6-membered heterocycle containing 1 or 2 heteroatoms, each independently selected from N and O. In another embodiment, Ring B is a dihydropyrimidine. In a preferred embodiment, Ring B is selected from 1,6-dihydropyrimidine, 1,2-dihydropyrimidine, and 1,4-dihydropyrimidine.

[0152] In a further preferred embodiment, the AB ring system is [ka] and Y is O or S. In a particular embodiment, the AB ring system is [ka] is.

[0153] In a further embodiment, the B ring is a 2H-pyran or a 4H-pyran. In a preferred embodiment, the AB ring system is [ka] and Y is O or S. In a particular embodiment, the AB ring system is [ka] is.

[0154] In a further embodiment, Ring C is a phenyl group and each independently R X1 is optionally substituted with 1, 2, 3, 4 or 5 groups selected from:

[0155] In one embodiment, L 1 is a bond. In another embodiment, L 1 is a C1-C6 hydrocarbon chain. 1 is a C1-C2 hydrocarbon chain.

[0156] In a further embodiment, R 2H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, =O, =S, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 and -S(=O)R a2 In another embodiment, R 2 is H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O)(3- to 7-membered heterocyclic group), -C(=O)(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 In a further embodiment, R is selected from the group consisting of alkylene, alkenyl, alkynyl, cyclic hydrocarbon, and heterocyclic groups, and is optionally substituted with one or more substituents selected from halogen, nitro, cyano, —OH, —SH, —NH, and —COOH. 2 H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 In a preferred embodiment, R 2 H, halogen, -NO2, -CN, C 1-6 alkyl group, -OH, wherein the alkyl group is selected from halogen, -NO2, -CN, C 1-6 Alkyl group, -NR a2 R b2 In a further preferred embodiment, R 2 H, halogen, C 1-6 alkyl group, -OH, wherein the alkyl group is selected from halogen, C 1-6 Alkyl groups and -NR a2 R b2 In a further embodiment, R 2 is H, C 1-4 an alkyl group, —OH, wherein the alkyl group is selected from —NR a2 R b2 In particular embodiments, R 2 is H, C 1-4 an alkyl group, —OH, wherein the alkyl group is —CH2[CH(CH3)2], and —NR a2 R b2 In another embodiment, R 2 is -NR a1 R b1 In particular embodiments, R 2 teeth, [ka] is.

[0157] In one embodiment, R X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 In a preferred embodiment, R is optionally substituted with one or more substituents selected from alkylene groups (3- to 7-membered heterocyclic groups), ═O, and —COOH. X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -NC(=O)R 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 In a preferred embodiment, R X1 and R X2are each independently a halogen, C 1-6 Alkyl group, -OR 7 , -NR 7 R 8 and more preferably, each independently selected from halogen, -OR 7 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In a further preferred embodiment, R X1 and R X2 are independently F, Cl, Br, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, optionally substituted C 1-6 alkyl groups, and the above-mentioned optionally substituted C 1-6 Alkyl groups are halogens, -NO2, -CN, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In particular embodiments, R X1 and R X2 is independently selected at each occurrence from F, Cl, Br, a methyl group, —OH, and a dimethylaminomethyl group.

[0158] R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 alkynyl groups, and the alkyl, alkenyl and alkynyl groups are selected from halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In a preferred embodiment, R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In particular embodiments, R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —N(C 1-6 In another particular embodiment, R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0159] In one embodiment, R a1 , R b1 , Rc1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, -OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 In a preferred embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)RY1 wherein the alkyl, aryl or heteroaryl group is selected from the group consisting of halogen, -OR Y3 and -NR Y3 R Y4 In another preferred embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, -OR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 wherein the alkyl group is selected from halogen, -OR Y3 and -NR Y3 R Y4 In a further preferred embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, -OR Y1 , -NR Y1 R Y2 , -C(=O)R Y1 wherein the alkyl group is selected from halogen, -OR Y3 and -NR Y3 R Y4 In a further embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, -OR Y1 , -NR Y1 R Y2 , -C(=O)R Y1wherein the alkyl group is selected from halogen, —NR Y3 R Y4 In particular embodiments, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-3 It is selected from an alkyl group, -OH, and a p-methylbenzoyl group, and said alkyl group is optionally substituted with one or more groups selected from a halogen and -NH2.

[0160] In another embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-8 Alkyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from halogen, -NO2, -CN, -OH, -SH, -NH2, -COOH and C 1-6 In a preferred embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, phenyl group, phenyl group-C1-4 Alkyl group, 5- to 6-membered heteroaryl group, 5- to 6-membered heteroaryl group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from halogen, -NO2, -CN, -OH, -SH, -NH2, -COOH and C 1-6 In a further preferred embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-6 Alkyl group, phenyl group, phenyl group-C 1-4 Alkyl group, 5- to 6-membered heteroaryl group, 5- to 6-membered heteroaryl group-C 1-4 alkyl groups, wherein the alkyl or phenyl groups are selected from halogen, -NO2, -CN, -OH, -SH, -NH2, -COOH and C 1-6 In a further preferred embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-6 Alkyl group, phenyl group, phenyl group-C 1-4 alkyl group, and the alkyl group or phenyl group is selected from halogen, C 1-6 In particular embodiments, R Y1 , R Y2 , R Y3 , R Y4 is independently selected at each occurrence from H and a p-methylphenyl group.

[0161] In another embodiment, R 2 is H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O)(3- to 7-membered heterocyclic group), -C(=O)(C1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 In a further embodiment, R is selected from the group consisting of alkylene, alkenyl, alkynyl, cyclic hydrocarbon, and heterocyclic groups, and is optionally substituted with one or more substituents selected from halogen, nitro, cyano, —OH, —SH, and —NH. 2 H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 In a preferred embodiment, R 2 H, halogen, -NO2, -CN, C 1-6 alkyl group, -OH, wherein the alkyl group is selected from halogen, -NO2, -CN, C 1-6 Alkyl group, -NR a2 R b2 In a further preferred embodiment, R 2 H, halogen, C 1-6 alkyl group, -OH, wherein the alkyl group is selected from halogen, C 1-6 Alkyl groups and -NR a2 R b2 In a further embodiment, R 2 is H, C 1-4 an alkyl group, —OH, wherein the alkyl group is selected from —NR a2 R b2 In particular embodiments, R 2 is H, C 1-4 an alkyl group, —OH, wherein the alkyl group is —CH2[CH(CH3)2], and —NR a2 R b2 In another embodiment, R 2 is -NR a1 R b1 In particular embodiments, R 2 teeth, [ka] is.

[0162] In one embodiment, R X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 In a preferred embodiment, R X1 and R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -NC(=O)R 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 In a preferred embodiment, R X1 and R X2are each independently a halogen, C 1-6 Alkyl group, -OR 7 , -NR 7 R 8 and more preferably, each independently selected from halogen, -OR 7 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In a further preferred embodiment, R X1 and R X2 are independently F, Cl, Br, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, optionally substituted C 1-6 alkyl groups, and the above-mentioned optionally substituted C 1-6 Alkyl groups are halogens, -NO2, -CN, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In particular embodiments, R X1 and R X2 is independently selected at each occurrence from F, Cl, Br, a methyl group, —OH, and a dimethylaminomethyl group.

[0163] R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 alkynyl groups, and the alkyl, alkenyl and alkynyl groups are selected from halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In a preferred embodiment, R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In particular embodiments, R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —N(C 1-6 In another particular embodiment, R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0164] In one embodiment, R a1 , R b1 , R c1 , R a2 , R b2, R c2 are independently expressed as H, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, -OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 In a preferred embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group -C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1wherein the alkyl, aryl or heteroaryl group is selected from the group consisting of halogen, -OR Y3 and -NR Y3 R Y4 In another preferred embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, -OR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 wherein the alkyl group is selected from halogen, -OR Y3 and -NR Y3 R Y4 In a further preferred embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, -OR Y1 , -NR Y1 R Y2 , -C(=O)R Y1 wherein the alkyl group is selected from halogen, -OR Y3 and -NR Y3 R Y4 In a further embodiment, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, -OR Y1 , -NR Y1 R Y2 , -C(=O)R Y1 wherein the alkyl group is selected from halogen, —NRY3 R Y4 In particular embodiments, R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-3 It is selected from an alkyl group, -OH, and a p-methylbenzoyl group, and said alkyl group is optionally substituted with one or more groups selected from a halogen and -NH2.

[0165] In another embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-8 Alkyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group, and the alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from halogen, -NO2, -CN, -OH, -SH, -NH2 and C 1-6 In a preferred embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, phenyl group, phenyl group-C 1-4Alkyl group, 5- to 6-membered heteroaryl group, 5- to 6-membered heteroaryl group-C 1-4 alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group, and the alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from halogen, -NO2, -CN, -OH, -SH, -NH2 and C 1-6 In a further preferred embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-6 Alkyl group, phenyl group, phenyl group-C 1-4 Alkyl group, 5- to 6-membered heteroaryl group, 5- to 6-membered heteroaryl group-C 1-4 alkyl group, wherein the alkyl group or phenyl group is selected from halogen, —NO2, —CN, —OH, —SH, —NH2 and C 1-6 In a further preferred embodiment, R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-6 Alkyl group, phenyl group, phenyl group-C 1-4 alkyl group, and the alkyl group or phenyl group is selected from halogen, C 1-6 In particular embodiments, R Y1 , R Y2 , R Y3 , R Y4 is independently selected at each occurrence from H and a p-methylphenyl group.

[0166] In one embodiment, R 3 , R 6 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 In a preferred embodiment, R 3 , R 6 are each independently selected from H, halogen, and —OH, and more preferably H or —OH.

[0167] In one embodiment, R 4 , R 5 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -NH(C 1-4 Alkylene group, 3- to 7-membered heterocyclic group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6In another embodiment, R 4 , R 5 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In a further embodiment, R 4 , R 5 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In another embodiment, R 4 , R5 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl group, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl group), and ═O.

[0168] Thus, in one embodiment, formula (I) has the structure of formula (vi) below, where the LCM moiety is the structure of formula (6) above (see formula (6) above and embodiments thereof) or a pharmaceutically acceptable salt thereof: [ka]

[0169] In one embodiment, L may be covalently attached to any suitable site in formula (6).

[0170] The structure according to formula (7) below falls within the scope of the structures according to formulas (1), (3) and (6). In one embodiment, the LCM moiety has the structure according to formula (7): [ka] (In the formula, X is O, Y is O or S; R 3 , R 4 , R 5, R 6 is as defined in equation (6), The C ring is [ka] and R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 Selected from R 7 , R 8 is as defined in equation (6), R 2 H, halogen, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2, -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 and -S(=O)R a2 and R a2 , R b2 is defined as in equation (6).

[0171] In one embodiment, Y is O. When Y is O, formula (7) becomes: [ka] is.

[0172] In one embodiment, R 2 H, halogen, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 and -S(=O)R a2 In one embodiment, R 2 -OR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 In another embodiment, R 2 H, halogen, C 1-6alkyl groups, said alkyl groups being optionally substituted with one or more substituents selected from halogen, -NO2, -CN, -OH, -NH2 and -COOH.

[0173] In one embodiment, R a2 , R b2 are independently expressed as H, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from the group consisting of halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 In a preferred embodiment, R a2 , R b2 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —OH, —NH, —NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2.

[0174] In one embodiment, R 3 H, halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In one embodiment, R 3 H, halogen, C 1-3 Alkyl groups, -OH, -O(C 1-3 alkyl group), -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 3 is selected from H, halogen, methyl group, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, and the methyl group is selected from halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 3 is selected from H, halogen, methyl, —OH, —OCH, —NH, —NHCH, —N(CH), and the methyl group is optionally substituted with a substituent selected from halogen, —OH, —OCH, —NH, —NHCH, and —N(CH). 3 is selected from H, halogen, methyl, —OH, —NH, —N(CH). In a further embodiment, R 3 H, halogen, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-4 alkyl group), -NH2, -NH(C 1-4In one embodiment, R 3 is selected from H, halogen, methyl group, —OH, —OCH3, —NH2, —NHCH3, and the methyl group is selected from halogen, —OH, —O(C 1-2 alkyl group), -NH2, -NH(C 1-2 In one embodiment, R 3 is selected from H, halogen, methyl, —OH, —OCH, —NH, —NHCH, said methyl group optionally substituted with a substituent selected from halogen, —OH, —OCH, —NH, —NHCH. In another embodiment, R 3 H, halogen, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), -NH2, wherein the alkyl group is selected from halogen, -OH, -O(C 1-4 In one embodiment, R 3 is selected from H, halogen, methyl group, —OH, —OCH3, —NH2, and the methyl group is selected from halogen, —OH, —O(C 1-2 In one embodiment, R 3 is selected from H, halogen, methyl, —OH, —OCH, —NH, wherein the methyl group is optionally substituted with a substituent selected from halogen, —OH, —OCH, —NH. In one embodiment, R 3 is selected from H, halogen, methyl, —OH, and —NH. In another embodiment, R 3 H, halogen, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-4 In one embodiment, R 3 is selected from H, halogen, methyl group, -OH, -OCH3, and the methyl group is selected from halogen, -OH, -O(C 1-2In one embodiment, R 3 is selected from H, halogen, methyl, —OH, —OCH, said methyl group optionally substituted with a substituent selected from halogen, —OH, —OCH. In one embodiment, R 3 is selected from H, halogen, methyl, and —OH. 3 is H, halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH3, —NH2, —NHCH3, —N(CH3)2, and substituted methyl groups, and the substituted methyl groups are selected from halogen, —OH, —O(C 1-2 alkyl group), -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH, —NH, —NHCH, —N(CH), and substituted methyl groups, wherein the substituted methyl groups are substituted with substituents selected from halogen, —OH, —OCH, —NHCH, and —N(CH). 3 is selected from H, halogen, —OH, —NH, and a methyl group, wherein the methyl group is substituted with —N(CH). 3 is H, halogen, -OH, -O(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH3, and substituted methyl groups, and the substituted methyl groups are selected from halogen, —OH, —O(C 1-2 alkyl group), -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH, and substituted methyl groups, wherein the substituted methyl groups are substituted with substituents selected from halogen, —OH, —OCH, —NHCH, and —N(CH). 3 is selected from H, halogen, —OH, and a methyl group, wherein the methyl group is substituted with —N(CH). 3 is H, halogen, -OH, -O(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 3 is H, halogen, -OH, C 1-2 alkyl groups, wherein the alkyl groups are selected from halogen, —NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, and methyl group, and the methyl group is selected from halogen, —NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 3is selected from H, halogen, —OH, and a methyl group, wherein the methyl group is substituted with a substituent selected from halogen, —NHCH, and —N(CH). 3 is selected from H, halogen, —OH, and a methyl group, wherein the methyl group is substituted with —N(CH3)2. 3 is H, halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH3, —NH2, —NHCH3, and substituted methyl groups, and the substituted methyl groups are selected from halogen, —OH, —O(C 1-2 alkyl group), -NH(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH3, —NH2, —NHCH3, and substituted methyl groups, wherein the substituted methyl groups are substituted with substituents selected from halogen, —OH, —OCH3, and —NHCH3. 3 is selected from H, halogen, —OH, —NH, and a methyl group, wherein the methyl group is substituted with —N(CH). 3 is H, halogen, -OH, -O(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 In one embodiment, R 3is selected from H, halogen, —OH, —OCH3, and substituted methyl groups, and the substituted methyl groups are selected from halogen, —OH, —O(C 1-2 alkyl group), -NH(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, —OCH, and a substituted methyl group, wherein the substituted methyl group is substituted with a substituent selected from halogen, —OH, —OCH, and —NHCH. 3 is selected from H, halogen, —OH, and a methyl group, wherein the methyl group is substituted with —N(CH). 3 is H, halogen, -OH, -O(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -NH2, -NH(C 1-4 In one embodiment, R 3 is H, halogen, -OH, C 1-2 alkyl groups, wherein the alkyl groups are selected from halogen, —NH(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, and methyl group, and the methyl group is selected from halogen, —NH(C 1-2 In one embodiment, R 3 is selected from H, halogen, —OH, and a methyl group, wherein the methyl group is substituted with a substituent selected from halogen and —NHCH. 3 is selected from H, F, Cl, a methyl group, —OH, and —NH. In another embodiment, R 3 is selected from H, F, a methyl group, —OH, and —NH. In one embodiment, R 3 is H. In one embodiment, R 3 is —OH. In one embodiment, R 3 is CH3.

[0175] In one embodiment, R 4 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In one embodiment, R 4 is H, halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 4 is H, halogen, -OH, -O(C 1-3 alkyl group), -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, substituted C 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl group is a halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R 4 is H, halogen, -OH, -NH2, -NH(C 1-4 alkyl group), substituted C 1-4 Alkyl groups, substituted -O(C 1-4 alkyl group), substituted -N(C 1-4alkyl group)2, and the above-mentioned substituted C 1-4 Alkyl groups, substituted -O(C 1-4 alkyl group) and substituted -N(C 1-4 alkyl group)2 is halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-4 In one embodiment, R 4 is H, halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), substituted C 1-2 Alkyl groups, substituted -O(C 1-2 alkyl group), and the above-mentioned substituted C 1-2 Alkyl groups and substituted -O(C 1-2 alkyl group) is halogen, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 In one embodiment, R 4 is H, halogen, -OH, -OCH3, -NH2, -NHCH3, substituted C 1-2 alkyl groups, and the above-mentioned substituted C 1-2 The alkyl group is substituted with one or more substituents selected from halogen, —OH, —OCH, —NH, and —NHCH. In one embodiment, R 4 is H, halogen, -OH, -NH2, -NH(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -OCH3, -NH2, -NH(C 1-4 In one embodiment, R 4 is H, halogen, -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 alkyl group)2, substituted C 1-2 alkyl groups, and the above-mentioned substituted C 1-2 The alkyl group is a halogen, -OH, -O(C 1-2alkyl group), -NH2, -NH(C 1-2 In one embodiment, R 4 is H, halogen, -OH, -NH2, -NHCH3, substituted C 1-2 alkyl groups, and the above-mentioned substituted C 1-2 The alkyl group is substituted with one or more substituents selected from halogen, —OH, —OCH, —NH, and —NHCH. In one embodiment, R 4 H, halogen, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 4 H, halogen, C 1-2 In one embodiment, R is selected from the group consisting of an alkyl group, —OH, —OCH, —NH, —NHCH, and —N(CH). 4 H, halogen, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-4 In one embodiment, R 4 H, halogen, C 1-2 In one embodiment, R is selected from alkyl groups, -OH, -OCH, -NH, -NHCH, and -N(CH), wherein the alkyl groups are optionally substituted with one or more substituents selected from halogen, -OH, and -OCH. 4 H, halogen, C 1-4 Alkyl groups, -OH, -O(C 1-4alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-4 In one embodiment, R 4 H, halogen, C 1-2 In one embodiment, R is selected from an alkyl group, —OH, —OCH, wherein the alkyl group is optionally substituted with one or more substituents selected from a halogen, —OH, —OCH. 4 is selected from H, —OH, —OCH. In one embodiment, R 4 is H. In one embodiment, R 4 is -OH.

[0176] In one embodiment, R 5 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 In one embodiment, R 5 H, halogen, C 1-4Alkyl groups, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 5 is H, halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, -C(=O)O(C 1-4 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-4 alkyl group), -C(=O)N(C 1-4 alkyl group)2, -OC(=O)(C 1-4 alkyl group), -NC(=O)(C 1-4 alkyl group)2, -C(=O)(C 1-4 alkyl group), substituted C 1-4 alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, -C(=O)O(C 1-4 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-4 alkyl group), -C(=O)N(C 1-4 alkyl group)2, -OC(=O)(C 1-4 alkyl group), -NC(=O)(C 1-4 alkyl group)2, -C(=O)(C 1-4 In one embodiment, R 5 is H, halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, substituted C 1-4alkyl groups, and the above-mentioned substituted C 1-4 The alkyl group is a halogen, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 5 is H, halogen, -O(C 1-4 alkyl group), -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, substituted C 1-2 alkyl groups, and the above-mentioned substituted C 1-2 The alkyl group is a halogen, -O(C 1-4 alkyl group), -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 5 is H, halogen, -O(C 1-4 alkyl group), -NH(C 1-4 alkyl group), -N(C 1-4 alkyl group)2, substituted C 1-2 alkyl groups, and the above-mentioned substituted C 1-2 The alkyl group is substituted with one or more substituents selected from halogen, —OCH, —NHCH, and —N(CH). In one embodiment, R 5 is H, halogen, -O(C 1-2 alkyl group), -NH(C 1-2 alkyl group), -N(C 1-2 alkyl group)2, substituted C 1-2 alkyl groups, and the above-mentioned substituted C 1-2 The alkyl group is substituted with one or more substituents selected from halogen, -OCH3, -NHCH3, -N(CH3)2.

[0177] In one embodiment, R 6 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In another embodiment, R 6 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In one embodiment, R is selected from the group consisting of alkyl groups, -C ... 6 H, halogen, -NO2, -CN, C 1-2 Alkyl groups, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In a further embodiment, R is selected from the group consisting of alkyl groups, -OH, -NH, and optionally substituted with one or more substituents selected from halogen, -OH, and -NH. 6 H, halogen, -NO2, -CN, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In another embodiment, R is selected from the group consisting of alkyl groups, optionally substituted with one or more halogens. 6 H, halogen, -NO2, -CN, C 1-2 Alkyl groups, -OH, -O(C 1-2 alkyl group), -NH2, -NH(C 1-4 alkyl group), -N(C 1-4 In one embodiment, R 6 are H, F, Cl, Br, and C 1-6 In another embodiment, R is selected from an alkyl group, —OH, —NH, wherein the alkyl group is optionally substituted with one or more substituents selected from a halogen, —OH, —NH.6 is selected from H, F, Cl, Br, a methyl group, —OH, and —NH. In particular embodiments, R 6 is H or —OH, in particular H.

[0178] In one embodiment, R 3 is a methyl group, and R 4 are -OH, -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In one embodiment, R is substituted with one or more substituents selected from alkyl groups and -COOH. 3 is a methyl group, and R 4 -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 and -COOH.

[0179] In another embodiment, R 3 is a methyl group, and R 5 are -OH, -NH2, -NH(C 1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 In another embodiment, R is substituted with one or more substituents selected from alkyl groups and -COOH. 3 is a methyl group, and R 5 -NH2, -NH(C1-3 alkyl group), -N(C 1-3 alkyl group)2, C substituted with -COOH 1-3 alkyl groups, and the above-mentioned substituted C 1-3 The alkyl groups are -OH, -NH2, -NH(C 1-2 alkyl group), -N(C 1-2 and -COOH.

[0180] In one embodiment, R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O)(3- to 7-membered heterocyclic group), -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 In one embodiment, R is selected from the group consisting of alkylene groups, 3- to 7-membered heterocyclic groups, and the alkyl, alkylene, alkenyl, alkynyl, cyclic hydrocarbon, and heterocyclic groups are optionally substituted with one or more substituents selected from H, halogen, nitro, cyano, —OH, —SH, —NH, ═O, and —COOH. 14 , R 15 , R 16 , R 17 , R 18are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl group, -OR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 In one embodiment, R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 In one embodiment, R 14 , R 15 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4Alkylene group -C 3-6 In one embodiment, R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 In one embodiment, R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 In one embodiment, R14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 In one embodiment, R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C =O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 In one embodiment, R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 In one embodiment, R 14 , R 15 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 In one embodiment, R 16 is H. In one embodiment, R 16 is -OCH3.

[0181] Thus, in one embodiment, formula (I) has the structure of formula (vii) below, where the LCM moiety is the structure of formula (7) above (see formula (7) above and embodiments thereof) or a pharmaceutically acceptable salt thereof: [ka]

[0182] In one embodiment, L may be covalently attached to any suitable site in formula (7).

[0183] The structure according to formula (8) below falls within the scope of the structures according to formula (1), formula (3), formula (6) and formula (7). In one embodiment, the LCM moiety has the structure according to formula (8) below. [ka] (In the formula, Y is O or S; C ring, R 2 , R 3 , R 4 , R 5 , R 6 is defined as in equation (7).

[0184] In one embodiment, Y is O. When Y is O, formula (8) becomes: [ka] is.

[0185] In particular embodiments, the structure of formula (8) is selected from compounds A5, A6, and A7. [ka]

[0186] Thus, in one embodiment, Formula (I) has the structure of Formula (viii) below, where the LCM moiety is the structure of Formula (8) above (see Formula (8) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0187] In one embodiment, L may be covalently attached to any suitable site in formula (8), such as, for example, —OH.

[0188] In one embodiment, formula (viii) is [ka] is.

[0189] In particular embodiments, the structure of formula (viii) is [ka] is selected from.

[0190] The structure according to formula (9) below falls within the scope of the structures according to formula (1), formula (3) and formula (6). In one embodiment, the LCM moiety has the structure according to formula (9) below. [ka] (In the formula, R 19 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, -COOH, m is 0, 1, 2, 3, 4 or 5; R 2 , R 3 , R 4 , R5 , R 6 is defined as in equation (6).

[0191] In one embodiment, R 2 H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 In a preferred embodiment, R 2 H, halogen, -NO2, -CN, C 1-6 alkyl group, -OH, wherein the alkyl group is selected from halogen, -NO2, -CN, C 1-6 Alkyl group, -NR a2 R b2 In a further preferred embodiment, R 2 H, halogen, C 1-6 alkyl group, -OH, wherein the alkyl group is selected from halogen, C 1-6Alkyl groups and -NR a2 R b2 In a further embodiment, R 2 is H, C 1-4 an alkyl group, —OH, wherein the alkyl group is selected from —NR a2 R b2 In particular embodiments, R 2 is H, C 1-4 an alkyl group, —OH, wherein the alkyl group is —CH2[CH(CH3)2], and —NR a2 R b2 In another embodiment, R 2 is -NR a1 R b1 is an alkyl group substituted with R a1 , R b1 , R a2 , R b2 is as defined in formula (6). In particular embodiments, R 2 teeth, [ka] is.

[0192] In one embodiment, R 19 are each independently a halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0193] In particular embodiments, the structure of formula (9) is the structure of compound A8 [ka] is.

[0194] Thus, in one embodiment, formula (I) has the structure of formula (ix) below, where the LCM moiety is the structure of formula (9) above (see formula (9) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0195] In one embodiment, L may be covalently attached to any suitable site in formula (9), such as, for example, —NH.

[0196] In particular embodiments, the structure of formula (ix) is [ka] is.

[0197] In one embodiment, the structure of the LCM moiety is the structure of formula (10) below, or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 20 is selected from bicycloheteroaryl groups having 9 to 10 ring atoms, the ring atoms containing 1 to 3 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, the remaining atoms being carbon atoms, and the heteroaryl group is unsubstituted or X3 and is substituted with at least one group selected from R 21 is C 1-8 alkyl groups, R 22 is R X3 is selected from R 23 is a phenyl group, unsubstituted or X3 and is substituted with at least one group selected from R X3are independently generated for each occurrence, C 1-8 Alkyl group, C 1-8 Alkenyl groups, halogens, -CN, -CF3, -CHF2, -CH2F, -NO2, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group), -COOH, -C(=O)O(C 1-8 alkyl group), -C(=O)NH(C 1-8 alkyl group), -C(=O)N(C 1-8 alkyl group), -S(=O)2OH, -S(=O)2(OC 1-8 alkyl group), -S(=O)2NH2, -S(=O)2NH(C 1-8 alkyl group), -S(=O)2N(C 1-8 alkyl group), wherein the alkyl group is selected from halogen, —NO, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group), optionally substituted with one or more substituents selected from =O and -COOH; p is 0, 1 or 2.

[0198] In one embodiment, R 20 is selected from the group consisting of bicycloheteroaryl groups such as benzofuryl, benzothienyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzotriazolyl, indazolyl, indolyl and isoindolyl groups, wherein the heteroaryl groups are unsubstituted or 1-8 It is substituted with at least one group selected from alkyl groups.

[0199] In one embodiment, R 22 is C 1-8 It is selected from alkyl groups, halogens and -CN.

[0200] In one embodiment, p is 0.

[0201] In a particular embodiment, the structure of formula (10) is the structure of compound A9 or A9'. [ka]

[0202] Thus, in one embodiment, formula (I) has the structure of formula (x) below, where the LCM moiety is the structure of formula (10) above (see formula (10) above and embodiments thereof) or a pharmaceutically acceptable salt thereof: [ka]

[0203] In one embodiment, L may be covalently attached to any suitable site in formula (10), such as, for example, —S(O)OH.

[0204] In particular embodiments, the structure of formula (x) is [ka] The structure is as follows.

[0205] In one embodiment, the structure of the LCM moiety is the structure of formula (11) below, or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 24 is selected from 3- to 7-membered heterocyclic groups, and the heterocyclic groups are unsubstituted or X3 and is substituted with at least one group selected from L 3 is one C 1-8 Alkylene group and one C 3-6 cycloalkylene groups; R 25 is H, C 1-8alkyl groups, R 26 are halogens, -NO2, -CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, L 4 is C 1-8 Alkylene group and C 1-8 alkoxyylidene groups, R 27 is a phenyl group, unsubstituted or X3 and is substituted with at least one group selected from q is 0, 1 or 2; R X3 is defined as in equation (10).

[0206] In one embodiment, R 24 is selected from 5- to 6-membered heterocyclic groups, preferably a pyrrolidinyl group, and the heterocyclic group is unsubstituted or 1-8 It is substituted with at least one group selected from alkyl groups.

[0207] In one embodiment, L 3 teeth, [ka] is.

[0208] In one embodiment, q is 1.

[0209] In a particular embodiment, the structure of formula (11) is the structure of compound A10. [ka]

[0210] Thus, in one embodiment, formula (I) has the structure of formula (xi) below, where the LCM moiety is the structure of formula (11) above (see formula (11) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0211] In one embodiment, L may be covalently attached to any suitable site in formula (11), such as, for example, -NH2.

[0212] In particular embodiments, the structure of formula (xi) is [ka] is.

[0213] In one embodiment, the structure of the LCM moiety is the structure of formula (12) below, or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 28 is C 1-8 an alkenyl group, wherein the alkenyl group is at least one C 1-8 substituted with an alkyl group, the alkyl group being R X4 and optionally substituted with one or more groups selected from R 29 is H, C 1-8 alkyl groups, R 30 are halogens, -NO2, -CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, L 5 is -O-, C 1-8 Alkylene group and C 1-8alkoxyylidene groups, R 31 is selected from a 6-membered heteroaryl group having 6 ring atoms, the ring atoms containing 1 to 2 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, and the remaining ring atoms being carbon atoms, the heteroaryl group being unsubstituted or X3 and is substituted with at least one group selected from r is 0, 1, 2, 3 or 4; s is 0, 1, 2, 3 or 4; R X4 are independently generated for each occurrence, C 1-8 Alkyl group, C 1-8 Alkenyl groups, halogens, -CN, -CF3, -CHF2, -CH2F, -NO2, -O(C 1-8 alkyl group), -S(C 1-8 alkyl group), -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, -OC(=O)(C 1-8 alkyl group), -NHC(=O)(C 1-8 alkyl group), -NC(=O)(C 1-8 alkyl group)2, -OS(=O)2(C 1-6 alkyl group), -NHS(=O)2(C 1-8 alkyl group), -N(C 1-8 alkyl group)S(=O)2(C 1-8 alkyl group), wherein the alkyl group is selected from halogen, —NO2, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group), optionally substituted with one or more substituents selected from =O and -COOH; R X3 is defined as in equation (10).

[0214] In one embodiment, R 29 is H.

[0215] In one embodiment, R 31 is a pyridyl group, preferably pyridyl-3-yl, said pyridyl group being unsubstituted or 1-8 It is substituted with at least one substituent selected from alkyl groups.

[0216] In one embodiment, R X4 is -O(C 1-8 alkyl group), preferably -O(C 1-3 alkyl groups), especially methoxy groups.

[0217] In one embodiment, R 28 teeth, [ka] is.

[0218] In one embodiment, r is 1.

[0219] In a particular embodiment, the structure of formula (12) is the structure of compound A11. [ka]

[0220] Thus, in one embodiment, formula (I) has the structure of formula (xii) below, where the LCM moiety is the structure of formula (12) above (see formula (12) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0221] In one embodiment, L may be covalently attached to any suitable site in formula (12).

[0222] In particular embodiments, the structure of formula (xii) is [ka] is.

[0223] In one embodiment, the structure of the LCM moiety is the structure of formula (13) below, or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 32 is selected from 3- to 7-membered heterocyclic groups, and the heterocyclic groups are unsubstituted or X3 and is substituted with at least one group selected from L 6 is -O-, C 1-8 Alkylene group and C 1-8 alkoxyylidene groups, R 33 , R 34 is a halogen, C 1-8 alkyl groups, R 35 are halogens, -NO2, -CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, R 36 is selected from a 5-membered heteroaryl group having 5 ring atoms, the ring atoms containing 1 to 3 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or X3 and is substituted with at least one group selected from t is 0, 1, 2 or 3; u is 0, 1, 2, 3 or 4; R X3 is defined as in equation (10).

[0224] In one embodiment, R 32is selected from 5- to 6-membered heterocyclic groups, and the heterocyclic group is preferably a pyrrolidinyl group, an imidazolidinyl group, a pyrazolidinyl group, a tetrahydropyranyl group, a piperidinyl group, a morpholinyl group, a thiomorpholinyl group, or a piperazinyl group, and the heterocyclic group is unsubstituted or substituted with a halogen, C 1-8 It is substituted with at least one group selected from alkyl groups.

[0225] In one embodiment, R 36 is selected from the group consisting of 5-membered heteroaryl groups such as pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl and isothiazolyl groups, said heteroaryl groups being unsubstituted or 1-8 It is substituted with at least one group selected from alkyl groups.

[0226] In one embodiment, t is 0. In another embodiment, u is 0.

[0227] In a particular embodiment, the structure of formula (13) is the structure of compound A12. [ka]

[0228] Thus, in one embodiment, Formula (I) has the structure of Formula (xiii) below, where the LCM moiety is the structure of Formula (13) above (see Formula (13) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0229] In one embodiment, L may be covalently attached to any suitable site in formula (13).

[0230] In particular embodiments, the structure of formula (xiii) is [ka] is.

[0231] In one embodiment, the structure of the LCM moiety is the structure of formula (14) below, or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 37 is selected from 6-membered heteroaryl groups having 6 ring atoms, the ring atoms containing 1 to 2 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, and the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or substituted with halogen, —NO, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, R 38 , R 39 , R 40 are each independently R X3 is selected from R 41 is selected from a 5-membered heteroaryl group having 5 ring atoms, the ring atoms containing 1 to 3 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or X3 and is substituted with at least one group selected from v is 0, 1, 2 or 3; w is 0, 1, 2, 3 or 4; x is 0, 1, 2, 3 or 4; R X3 is defined as in equation (10).

[0232] In one embodiment, R 37is selected from the group consisting of 6-membered heteroaryl groups such as pyridyl, pyrimidyl, and pyridazyl, preferably pyrimidyl, and more preferably pyrimidyl-4-yl, and the 6-membered heteroaryl group is unsubstituted or substituted with halogen, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2.

[0233] In one embodiment, R 41 is selected from the group consisting of 5-membered heteroaryl groups such as thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, and the like, preferably thienyl or furyl, more preferably thienyl, especially thienyl-2-yl, and the 5-membered heteroaryl group is unsubstituted or substituted with halogen, -CN, and C 1-8 It is substituted with at least one group selected from alkyl groups.

[0234] In one embodiment, v is 0. In another embodiment, w is 0. In one embodiment, x is 0.

[0235] In a particular embodiment, the structure of formula (14) is the structure of compound A13. [ka]

[0236] Thus, in one embodiment, Formula (I) has the structure of Formula (xiv) below, where the LCM moiety is the structure of Formula (14) above (see Formula (14) above and embodiments thereof) or a pharmaceutically acceptable salt thereof. [ka]

[0237] In one embodiment, L may be covalently attached to any suitable site in formula (14), such as, for example, -NH.

[0238] In particular embodiments, the structure of formula (xiv) is [ka] is.

[0239] L Linker L is a chemical bond or group connecting the LCM moiety and the TM moiety. In one embodiment, L is rigid or flexible. In a preferred embodiment, L is flexible. In one embodiment, L is a chemical bond. In another embodiment, L is a linear or branched hydrocarbon chain comprising 1 to 60, preferably 1 to 30, more preferably 2 to 16 (e.g., 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 16) carbon atoms, each of which may be optionally substituted with one or more, for example, 1 to 3, preferably 1 to 2, especially 1 heteroatom, selected from oxygen, sulfur, nitrogen, and phosphorus, preferably oxygen, sulfur, or nitrogen, more preferably oxygen or nitrogen, especially oxygen, and the carbon atom or heteroatom is selected from R L1 , R L2 , R L3 , R L4 and R L5 and optionally substituted with one or more groups selected from

[0240] R L1 , R L2 , R L3 , R L4 and R L5 are each independently H, a halogen group, or C 1-6 Alkyl group, -O(C 1-6 alkyl group), -S(C 1-6 alkyl group), -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, C 3-6 Cycloalkyl groups, C 6-10Aryl group, 5- to 7-membered heteroaryl group, 3- to 7-membered heterocyclic group, -O(C 3-6 cycloalkyl group), -S(C 3-6 cycloalkyl group), -NH(C 3-6 cycloalkyl group), -N(C 3-6 cycloalkyl group)2, -N(C 3-6 Cycloalkyl group)(C 1-6 alkyl group), -OH, -NH2, -SH, -S(=O)2(C 1-6 alkyl group), -P(=O)(OC 1-6 alkyl group)(C 1-6 alkyl group), -P(=O)(OC 1-6 alkyl group)2, -C≡CC 1-6 Alkyl groups, -C≡CH, -CH=CH(C 1-6 alkyl group), -C(C 1-6 alkyl group)=CH(C 1-6 alkyl group), -C(C 1-6 alkyl group)=C(C 1-6 alkyl group), -Si(OH), -Si(C 1-6 alkyl group)3, -Si(OH)(C 1-6 alkyl group)2, -C(=O)(C 1-6 alkyl group), -COOH, halogen, -CN, -CF3, -CHF2, -CH2F, -NO2, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -N(C 1-6 alkyl group)C(=O)NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)C(=O)N(C 1-6 alkyl group)2, -NHC(=O)NH(C 1-6 alkyl group), -NHC(=O)N(C 1-6 alkyl group), -NHC(=O)NH, -N(C 1-6 alkyl group)S(=O)2NH(C1-6 alkyl group), -N(C 1-6 alkyl group)S(=O)2N(C 1-6 alkyl group), -NHS(=O)2NH(C 1-6 alkyl group), -NHS(=O)2N(C 1-6 The heteroatom may be located in the middle of the chain, at one end of the chain, or at both ends of the chain. When the heteroatom is located at the end, the linker is attached to the LCM moiety and / or the TM moiety through the heteroatom. In one embodiment, L is a linear group.

[0241] In another embodiment, L is the structure of formula (a): or a pharmaceutically acceptable salt thereof: -Dy- (a) (wherein y is an integer greater than 1, Each D independently represents a bond, -CR L1 R L2 -, -O-, -S-, -S(=O)-, S(=O)2-, -NR L3 -, -S(=O)2NR L3 -, -S(=O)NR L3 -, -C(=O)NR L3 -, -NR L3 C(=O)NR L4 -, -NR L3 S(=O)NR L4 -, -C(=O)-, -CR L1 =CR L2 -, -C≡C-, -SiR L1 R L2 -, -P(=O)R L1 -, -P(=O)OR L1 -, 0 to 6 R L1 and / or R L2 C optionally substituted with a group 3-6 Cycloalkyl group, 0 to 6 R L1 and / or R L2 a 3- to 7-membered heterocyclic group optionally substituted with a group, 0 to 6 R L1 and / or R L2 an aryl group optionally substituted with a group, 0 to 6 R L1 and / or R L2heteroaryl groups optionally substituted with a group; If y is greater than 1, R L1 or R L2 are each independently 0 to 4 R L5 ) y is an integer of 30 or less. In one embodiment, y is an integer of 20 or less, preferably 16 or less, e.g., 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 16. In one embodiment, y is an integer of 12 or less.

[0242] In one embodiment, each D is independently -CR L1 R L2 -, -O- and -NR L3 In one embodiment, R L1 , R L2 and R L3 is H. In particular embodiments, the structure of L is: [ka] In one embodiment, each D is independently -CR L1 R L2 In particular embodiments, the structure of L is [ka] In particular embodiments, y is 12 and D is -CR L1 R L2 In one embodiment, R L1 and R L2 is H. In another particular embodiment, the structure of L is: [ka] is.

[0243] In particular embodiments, each D is independently —C(═O)—, 0 to 6 R L1 and / or RL2 Heteroaryl groups optionally substituted with -O-, -CR L1 R L2 -, 0 to 6 R L1 and / or R L2 a 3- to 7-membered heterocyclic group optionally substituted with a -NR L3 In one embodiment, R L1 , R L2 and R L3 are each H. In another particular embodiment, the structure of L is [ka] is.

[0244] TM part In one embodiment, the lipid droplet binding moiety is a moiety capable of non-covalently interacting with lipid droplets.

[0245] In one embodiment, the lipid droplet-binding moiety is a neutral lipid that binds to lipid droplets. In a specific embodiment, the neutral lipid that binds to lipid droplets is selected from steroids and steroid esters. It should be understood that the neutral lipid that binds to lipid droplets may also be an analog of a neutral lipid stored in lipid droplets. In another embodiment, the neutral lipid that binds to the lipid droplets is an analog of a neutral lipid stored in lipid droplets. In a specific embodiment, the neutral lipid analog is selected from a cholesteryl ester analog that is stored in lipid droplets.

[0246] In one embodiment, the TM moiety comprises a known lipid droplet probe, a compound capable of binding to a lipid droplet marker protein, or a compound capable of binding to neutral lipids in lipid droplets. In one embodiment, the lipid droplet probe is selected from a lipid droplet-specific probe or a probe that preferentially targets lipid droplets in cells, preferably a lipid droplet-specific probe. In another embodiment, the lipid droplet probe is selected from a dye molecule having affinity for lipid droplets. In one embodiment, the lipid droplet probe is lipophilic or amphiphilic. In a further embodiment, the lipid droplet probe is selected from a lipophilic dye molecule having affinity for neutral lipids. In a specific embodiment, the TM moiety is an azo dye having affinity for lipid droplets. In a particular embodiment, the azo dye having affinity for lipid droplets is selected from Sudan I, Sudan II, Sudan III, Oil Red BB, Oil Red O, Sudan Red G, and Sudan Black B, preferably selected from Sudan III, Oil Red O, and Oil Red BB. In a further specific embodiment, the azo dye having affinity for lipid droplets is Oil Red BB. In specific embodiments, the lipid droplet probe is selected from the group consisting of Sudan I, Sudan II, Sudan III, Oil Red BB, Oil Red O, Sudan Red G, Sudan Black B, Nile Red, BODIPY® 493 / 503, monodansylpentane, PyrPy 10d, PyrPy 11c, PITE, TPE-AmAl, TPA-BI, LipidGreen, LipidGreen2, LD540, AF8, AF10, AFN, NAP AIEgen dyes, LD-BTD1, LipiDye, Phos 2a, Phos 2b, Phos 3a, Phos 3b, SF44, SF58, FAS, DPAS, BTD-coumarin hybrid, IND-TPA, photoactivatable AIE probe, LD-TPZn, LQD, photoactivatable AIEgen probe (e.g., PhotoAFN 2a-c), TPE-AC, TPMN, TTMN, MeTTMN, MeOTTMN, DCMa, DCI, DCFu, NLV-1, StatoMerocynaine dyes (SMCy dyes). In a particular embodiment, the NAP AIEgen dye is selected from NAP-Ph, NAP-Br, NAP-CF3, and NAP-Py.In particular embodiments, the BTD-coumarin hybrid is BTD-Lip. In particular embodiments, the photoactivatable AIE probe is BZT 3a. In particular embodiments, the photoactivatable AIE probe is BZT 4a. In particular embodiments, the photoactivatable AIEgen probe is PhotoAFN 2a-c. In particular embodiments, the SMCy dye is selected from SMCy 3 and SMCy 5.5. In a preferred embodiment, the lipid droplet probe has a selective affinity for lipid droplets. In another preferred embodiment, the lipid droplet probe has a selective affinity for neutral lipids stored in lipid droplets.

[0247] Some exemplary lipid droplet probes are selected from the structures shown in the figures below. [ka] [ka] [ka] In the formula, LQD is a lipophilic quantum dot reported by Mandal et al. ("Quantum Dot-Based Designed Nanoprobe for Imaging Lipid Droplet", J. Phys. Chem. C 2017, 121, 42, 23727-23735). LQD TPMN, LQD TTMN, LQD MeTTMN, and LQD MeOTTMN are quantum dot-based fluorescent probes.

[0248] In a specific embodiment, the lipid droplet probe comprises: [ka] is.

[0249] In specific embodiments, the lipid droplet probe is selected from cholesterol having a visualization group, a cholesteryl ester having a visualization group, and a triglyceride having a visualization group. The visualization group may be a fluorescent group. In specific embodiments, the lipid droplet probe is selected from cholesterol having a luminescent group, a cholesteryl ester having a luminescent group, and a triglyceride having a luminescent group. The luminescent group may be a fluorescent group.

[0250] In another specific embodiment, the lipid droplet probe is selected from the following molecules (commercially available from Invitrogen): [ka] [ka] [ka]

[0251] In another specific embodiment, the lipid droplet probe is selected from the following molecules (commercially available from Invitrogen): [ka]

[0252] In a preferred embodiment, the lipid droplet probe comprises: [ka] [ka] [ka] is selected from.

[0253] In one embodiment, the TM moiety has the structure of formula (II): [ka] (In the formula, The E ring and the F ring are each independently selected from a benzene ring and a naphthalene ring, and the E ring is R E and the F ring is optionally substituted with one or more groups selected from R F and the G ring is optionally substituted with one or more groups selected from R G and optionally substituted with one or more groups selected from Ring G is absent or selected from a benzene ring and a naphthalene ring; Z 1 is an azo group, Z 2 is absent or an azo group, R E , R F and R G are independently H, halogen, -NO2, -CN, =O, =S, C at each occurrence. 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O) (3- to 7-membered heterocyclic group), -N(C 1-6 alkyl group)-(C=O)(3- to 7-membered heterocyclic group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, The Two R's E , two R F or two R's G between them bond to each other and the atoms to which they are bonded. 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 Z is optionally substituted with one or more substituents selected from alkyl groups. 2 is absent, rings G and F are connected by a bond.

[0254] Thus, in one embodiment, Formula (I) has the structure of Formula (xv) below, where the TM moiety is the structure of Formula (II) above (see Formula (II) and its embodiments above), or a pharmaceutically acceptable salt thereof. [ka]

[0255] In one embodiment, L may be covalently attached to any suitable site in formula (II).

[0256] Within the scope of the structure described in formula (II) is the structure described in formula (III) below: In one embodiment, the TM moiety has the structure of formula (III) below. [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are each independently H, halogen, -NO2, -CN, =O, =S, C 1-6Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O) (3- to 7-membered heterocyclic group), -N(C 1-6 alkyl group)-(C=O)(3- to 7-membered heterocyclic group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6alkyl group), -S(=O)2N(C 1-6 alkyl group)2) optionally substituted with one or more substituents selected from

[0257] In one embodiment, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are each independently H, halogen, or C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cycloalkyl group), -O(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cycloalkyl group), -O(C=O)(C 1-4 Alkylene group -C 3-6 Cycloalkyl group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cycloalkyl group), -S(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cycloalkyl group), -N(C 3-6 cycloalkyl group)2, -NH(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -N(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cycloalkyl group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 The alkyl group, alkylene group, cycloalkyl group, or heterocyclic group is selected from the group consisting of halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53, R 54 , R 55 , R 56 and R 57 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0258] In another embodiment, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 are each independently H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O)(3- to 7-membered heterocyclic group), -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0259] In a further embodiment, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 are each independently H, halogen, or C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cycloalkyl group), -O(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cycloalkyl group), -O(C=O)(C 1-4 Alkylene group -C 3-6Cycloalkyl group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cycloalkyl group), -S(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cycloalkyl group), -N(C 3-6 cycloalkyl group)2, -NH(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -N(C 1-4 Alkylene group -C 3-6 cycloalkyl group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cycloalkyl group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 The alkyl group, alkylene group, cycloalkyl group, or heterocyclic group is selected from the group consisting of halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C1-6 optionally substituted with one or more substituents selected from alkyl groups, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0260] In one embodiment, R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are each independently H, halogen, or C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group, cycloalkyl group or heterocyclic group is selected from halogen, nitro group, cyano group, —OH, —O(C1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0261] In specific embodiments, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 are each independently H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), or R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or the heterocyclic ring is not substituted with halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from -S(=O)OH, -COOH, -S(=O)OH, and R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are each independently H, halogen, or C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 alkyl group, and the alkyl group, cycloalkyl group or heterocyclic group is selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups, -S(=O)2, -COOH, and -S(=O)2OH.

[0262] In further specific embodiments, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 At least one of the following is -Cl, -Br, -I, -NO2, -CN, =O, =S, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group) or -S(=O)N(C 1-6 alkyl group), and the remaining groups are each independently H, halogen, —NO, —CN, ═O, ═S, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from: -S(=O)2, -COOH, -S(=O)2OH; or R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or the heterocyclic ring is not substituted with halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups, -S(=O)2, -COOH, and -S(=O)2OH.

[0263] In particular embodiments, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 At least one of -Cl, -Br, -I, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group) or -N(C 1-6alkyl group), preferably -OH, -SH or -NH, more preferably -OH or -NH, particularly preferably -OH, and the remaining groups are each independently H, halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from: -S(=O)2, -COOH, -S(=O)2OH; or R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or the heterocyclic ring is not substituted with halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups, -S(=O)2, -COOH, and -S(=O)2OH.

[0264] In another specific embodiment, R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 is H, or R 49 , R50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 1 to 4, particularly preferably 1, 2 or 4 of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 The alkyl group is particularly preferably a methoxy group, and the remaining groups are each independently H, halogen, C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group is preferably selected from H and halogen, particularly preferably H, and the alkyl group is preferably selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0265] In further specific embodiments, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 At least one of the following is -Cl, -Br, -I, -NO2, -CN, =O, =S, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group) or -S(=O)N(C 1-6 alkyl group), and the remaining groups are each independently H, halogen, —NO, —CN, ═O, ═S, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from: -S(=O)2, -COOH, -S(=O)2OH; or R 42, R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or the heterocyclic ring is not substituted with halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from -S(=O)OH, -COOH, -S(=O)OH, and R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 is H, or R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 1 to 4, particularly preferably 1, 2 or 4 of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 The alkyl group is particularly preferably a methoxy group, and the remaining groups are each independently H, halogen, C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group is selected from the group consisting of alkyl groups, preferably H and halogen, particularly preferably H, and the alkyl group is selected from the group consisting of halogen, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, In further specific embodiments, R 49 and R 52 At least one of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 alkyl group) is particularly preferably a methoxy group, and / or R 50 and R 51 At least one of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 alkyl group) is particularly preferably a methoxy group, and / or R 53 and R 56 At least one of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 alkyl group) is particularly preferably a methoxy group, and / or R 54 and R 57 At least one of the1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 alkyl group) is particularly preferably a methoxy group, and R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 The remaining groups are each independently H, halogen, C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group is selected from the group consisting of alkyl groups, preferably H and halogen, particularly preferably H, and the alkyl group is selected from the group consisting of halogen, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 and optionally substituted with one or more substituents selected from alkyl groups).

[0266] In particular embodiments, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 is -OH, -SH or -NH, more preferably -OH or -NH, and particularly preferably -OH, and the remaining groups are H, and R 49, R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 is H, or R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 2 to 4, particularly preferably 2 or 4 of the 1-3 is an alkyl group, preferably C 1-3 alkyl groups, more preferably methyl groups, and the remaining groups are each independently selected from H; or R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 1 to 4, particularly preferably 1 or 2 of the groups represented by the formula (I) is -O(C 1-6 alkyl group), preferably -O(C 1-3 alkyl group), more preferably a methoxy group, and the remaining groups are each independently selected from H.

[0267] In another particular embodiment, R 42 is -OH, -SH or -NH, more preferably -OH or -NH, particularly preferably -OH; R 43 , R 44 , R 45 , R 46 , R 47 and R 48 are each independently selected from H, —OH, —SH, or —NH, more preferably H, —OH, or —NH, particularly preferably H or —OH, and especially preferably H; R 49, R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 is H, or R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 2 to 4, particularly preferably 2 or 4 of the 1-3 is an alkyl group, preferably C 1-3 alkyl groups, more preferably methyl groups, and the remaining groups are each independently selected from H; or R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 1 to 4, particularly preferably 1 or 2 of the groups represented by the formula (I) is -O(C 1-6 alkyl group), preferably -O(C 1-3 alkyl group), more preferably a methoxy group, and the remaining groups are each independently selected from H.

[0268] In a further particular embodiment, the structure of formula (III) is [ka] is selected from Preferably, [ka] Selected from, in particular [ka] is.

[0269] Thus, in one embodiment, Formula (I) has the structure of Formula (xvi) below, where the TM moiety is the structure of Formula (III) above (see Formula (III) and its embodiments above), or a pharmaceutically acceptable salt thereof. [ka]

[0270] In one embodiment, L may be covalently attached to any suitable site in formula (III).

[0271] In particular embodiments, the structure of formula (xvi) is [ka] is selected from Preferably, [ka] Selected from, in particular [ka] is.

[0272] Within the scope of the structure described in formula (II) is the structure described in formula (IV) below: In one embodiment, the TM moiety has the structure of formula (IV) below. [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 53 , R 54 , R 55 , R 56 and R 57 is as defined in formula (III).

[0273] In particular embodiments, the structure of formula (IV) is [ka] is selected from.

[0274] Thus, in one embodiment, Formula (I) has the structure of Formula (xvii) below, where the TM moiety is the structure of Formula (IV) above (see Formula (IV) and its embodiments above), or a pharmaceutically acceptable salt thereof. [ka]

[0275] In one embodiment, L may be covalently attached to any suitable site in formula (IV).

[0276] In particular embodiments, the structure of formula (xvii) is [ka] is selected from.

[0277] Within the scope of the structure set forth in formula (II) is the structure set forth in formula (V) below: In one embodiment, the TM moiety has the structure of formula (V) below. [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 53 , R 54 , R 55 , R 56 and R 57 is as defined in formula (III), R 58 , R 59 , R 60 , R 61 , R 62 and R 63are each independently H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O) (3- to 7-membered heterocyclic group), -N(C 1-6 alkyl group)-(C=O)(3- to 7-membered heterocyclic group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C1-6 alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2) optionally substituted with one or more substituents selected from

[0278] In specific embodiments, R 58 , R 59 , R 60 , R 61 , R 62 and R 63 is H, or R 58 , R 59 , R 60 , R 61 , R 62 and R 63 At least one, preferably 1 to 6, more preferably 1 to 4, particularly preferably 1, 2 or 4 of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C 1-3 The alkyl group is particularly preferably a methoxy group, and the remaining groups are each independently H, halogen, C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group is preferably selected from H and halogen, particularly preferably H, and the alkyl group is preferably selected from halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 In particular embodiments, R 58 , R 59 , R 60 , R 61 , R 62 and R 63 is H.

[0279] In particular embodiments, the structure of formula (V) is [ka] is.

[0280] Thus, in one embodiment, Formula (I) has the structure of Formula (xviii) below, where the TM moiety is the structure of Formula (V) above (see Formula (V) and its embodiments above), or a pharmaceutically acceptable salt thereof. [ka]

[0281] In one embodiment, L may be covalently attached to any suitable site in formula (V).

[0282] In particular embodiments, the structure of formula (xviii) is [ka] is.

[0283] Within the scope of the structure set forth in formula (II) is the structure set forth in formula (VI) below: In one embodiment, the TM moiety has the structure of formula (VI) below. [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 53 , R 54 , R 55 , R 56 and R 57 is as defined in formula (III).

[0284] In another particular embodiment, the structure of formula (VI) is: [ka] is.

[0285] Thus, in one embodiment, Formula (I) has the structure of Formula (xix) below, where the TM moiety is the structure of Formula (VI) above (see Formula (VI) and embodiments thereof above), or a pharmaceutically acceptable salt thereof. [ka]

[0286] In one embodiment, L may be covalently attached to any suitable site in formula (VI).

[0287] In another particular embodiment, the structure of formula (xix) is [ka] is.

[0288] In alternative embodiments, two or more structures of formula (II) are linked together to form a conjugate or hybrid, and such structures are also included within the scope of the TM moiety of the compounds of the invention. In particular embodiments, the TM moiety of the compounds of the invention is [ka] is.

[0289] Thus, in one embodiment, formula (I) has the following structure: [ka]

[0290] In one embodiment, L may be covalently attached to any suitable site in formula (II).

[0291] In one embodiment, the TM moiety has the structure of formula (VII): [ka] (In the formula, [ka] represents a single bond or a double bond, [ka] If represents a double bond, R a does not exist, [ka] If represents a single bond, R a are H, OH, -O(C 1-8 alkyl group), -O(C 1-8 silyl group), -C(=O)O(C 1-26 alkyl group), -C(=O)O(C 1-26 alkenyl groups), wherein the alkenyl groups contain 1 to 8 double bonds; R b , R c , R d are independently H, C 1-8 Alkyl group, C 1-8 Alkenyl groups, -OH, -O(C 1-8 alkyl group), -O(C 1-8 silyl groups), Re , R f , R g are independently H, C 1-4 Alkyl groups, -OH, -O(C 1-4 alkyl group), L 7 is a chemical bond, C 1-8 alkylene groups, R h is H, C 1-20 Alkyl group, C 1-20 Alkenyl groups, -OH, -O(C 1-20 alkyl group), -O(C 1-20 silyl groups), and the alkyl and alkenyl groups are selected from -OH, C 1-8 Alkyl group, C 1-8 Alkenyl group, C 1-8 Alkynyl group, -O(C 1-20 alkyl group), -O(C 1-20 silyl groups), k is 0, 1, or 2.

[0292] In one embodiment, [ka] represents a single bond, and R a are H, OH, -O(C 1-8 alkyl group), -C(=O)O(C 1-22 alkyl group), -C(=O)O(C 1-22 alkenyl groups), and the alkenyl groups contain 1 to 8, preferably 2 to 6, and more preferably 3 to 6 double bonds.

[0293] In one embodiment, R b , R c , R d is H. In another embodiment, R e , R f is a methyl group. In a further embodiment, R g is a methyl group. In a further embodiment, R h is C 3-10 is an alkyl group, preferably C5-8 alkyl group, more preferably C 6-7 It is an alkyl group, particularly a C6 alkyl group.

[0294] In particular embodiments, the structure of formula (VII) is [ka] is selected from.

[0295] Thus, in one embodiment, Formula (I) has the structure of Formula (xx) below, where the TM moiety is the structure of Formula (VII) above (see Formula (VII) and embodiments thereof above), or a pharmaceutically acceptable salt thereof. [ka]

[0296] In one embodiment, L may be covalently attached to any suitable site in formula (VII).

[0297] In particular embodiments, the structure of formula (xx) is

[0298] [ka] is selected from.

[0299] In one embodiment, the TM moiety comprises an alkynyl group or an azido group. In a particular embodiment, the TM moiety is [ka] Or -N3.

[0300] Thus, in one embodiment, formula (I) has the structure of formula (xxi) or formula (xxii) below, where the TM moiety is: [ka] Or -N3.) [ka]

[0301] Conjugate Compounds Some examples of conjugate compounds are as follows: Formula (i) to Formula (xxii).

[0302] The LCM moiety and L, and the TM moiety and L are covalently bonded, and the site of the covalent bond may be any suitable site. In one embodiment, a carbon atom of the LCM moiety is covalently bonded to L. In another embodiment, a heteroatom of the LCM moiety is covalently bonded to L. Those skilled in the art can select an appropriate reaction for bonding based on the structures of the LCM moiety, L, and TM moiety, and conversely, can adjust the substituents of the LCM moiety, L, and TM moiety based on the type of reaction. It should be understood that when a covalent bond is formed between the LCM moiety and L, or between the TM moiety and L, the structure of the product (conjugate compound) can be easily determined based on the structures of the LCM moiety, L, and TM moiety prior to covalent bonding, and conversely, the structure of the LCM moiety, L, and TM moiety prior to covalent bonding can be easily determined based on the structure of the product (conjugate compound). In a particular embodiment, both the LCM moiety and L contain a hydroxy group, and the hydroxy group of the LCM moiety and the hydroxy group of L are covalently bonded, resulting in the elimination of one molecule of water. In another particular embodiment, both the TM moiety and L contain a hydroxy group, and the hydroxy group of the TM moiety and the hydroxy group of L are covalently bonded, resulting in the elimination of one molecule of water. In another particular embodiment, L contains a nucleophilic reactive site, and the LCM moiety contains a nucleophilically active O- or N-containing structure that forms a covalent bond with the nucleophilic reactive site of L. In another particular embodiment, L contains a nucleophilic reactive site, and the TM moiety contains a nucleophilically active O- or N-containing structure that forms a covalent bond with the nucleophilic reactive site of L.

[0303] In one embodiment, the compound of formula (I) is [ka] [ka] [ka] is selected from.

[0304] In one embodiment, the compound of formula (I) is selected from compounds 1A, 1B, 2A, 2B, 3A, 3B, 4A, 4B, 5A, 6, 7, 8, 9, 10A, 10B, and 11A, and preferably selected from compounds 1A, 1B, 2A, 2B, 3A, 3B, 4A, 4B, 5A, 6, 7, 8, 9, 10A, and 11A. In one embodiment, the compound of formula (I) is selected from compounds 1A, 1B, 2A, 2B, 3A, 3B, 4A, 4B, 5A, 5B, 6, 7, 8, and 9.

[0305] Compound manufacturing method In another aspect, the present invention provides a method for producing a compound of the present invention, comprising covalently linking a structure capable of binding to an LC3 protein with a structure capable of binding to lipid droplets to form an "LC3 binding moiety-lipid droplet binding moiety conjugate" ("conjugate compound"). Each moiety of the conjugate compound is as described above.

[0306] In one embodiment, a structure capable of binding to an LC3 protein is screened or identified by the following method. (I) contacting a candidate compound with a measurement system containing an LC3 protein or a homologue thereof or a fragment thereof; and (II) A compound that binds with affinity to the LC3 protein or its homolog or a fragment thereof is selected.

[0307] In one embodiment, structures capable of binding to lipid droplets are screened or identified in the following manner. (I') contacting a candidate compound with a measurement system containing a target that is a lipid droplet, a lipid droplet marker protein, or a known neutral lipid present in the target lipid droplet; and (II') A compound that non-covalently interacts with the target described in (I') is selected.

[0308] Pharmaceutical compositions and pharmaceutical preparations Another object of the present invention is to provide pharmaceutical compositions comprising a prophylactically or therapeutically effective amount of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite, or prodrug thereof, and one or more pharmaceutically acceptable carriers.

[0309] As used herein, a "pharmaceutically acceptable carrier" refers to a diluent, adjuvant, excipient, or vehicle with which a therapeutic agent is administered that is, within the scope of reasonable medical judgment, suitable for contact with the tissues of humans and / or other animals without undue toxicity, irritation, allergic response, or other problem or complication commensurate with a reasonable benefit / risk ratio.

[0310] In one embodiment, the present invention provides a capsule containing a compound of the present invention but no other carrier.

[0311] The pharmaceutical compositions of the present invention may be in the form of tablets, chewable tablets, capsules, liquids, parenteral solutions, lozenges, suppositories, suspensions, etc. The compositions may be formulated to contain a daily dose or an appropriate fraction of a daily dose in a dosage unit, which may be a single tablet or capsule or an appropriate volume of a liquid.

[0312] In one embodiment, the liquid formulation is prepared with a water-soluble salt such as hydrochloride. Generally, all compositions are prepared according to methods known in pharmaceutical chemistry. Capsules can be prepared by mixing the compound with a suitable carrier or diluent and filling an appropriate amount of the mixture into capsules. Common carriers and diluents include, but are not limited to, inert powdered substances such as many different types of starch, powdered cellulose, especially crystalline and microcrystalline cellulose, sugars such as fructose, mannitol and sucrose, grain flours and similar edible powders.

[0313] Tablets can be prepared by direct compression, wet granulation, or dry granulation. These preparations generally incorporate diluents, binders, lubricants, and disintegrants, as well as the compound. Typical diluents include, for example, various types of starch, lactose, mannitol, kaolin, calcium phosphate or sulfate, inorganic salts (e.g., sodium chloride), and powdered sugar. Powdered cellulose derivatives are also useful. Typical tablet binders include, for example, starch, gelatin, and sugars (e.g., lactose, fructose, glucose, etc.). Natural and synthetic gums are also suitable, including gum arabic, alginates, methylcellulose, polyvinylpyrrolidone, and the like. Polyethylene glycol, ethylcellulose, and waxes can serve as binders.

[0314] Lubricants can be selected from slippery solids such as talc, magnesium stearate, calcium stearate, stearic acid, and hydrogenated vegetable oils. Tablet disintegrants are substances that swell when wet, causing the tablet to disintegrate and release the compound. Tablet disintegrants include starch, clay, cellulose, algin, and gum. More specifically, for example, corn starch and potato starch, methylcellulose, agar, bentonite, wood cellulose, powdered natural sponge, anion exchange resin, alginic acid, guar gum, citrus pulp, and carboxymethylcellulose, and sodium lauryl sulfate may be used. Tablets can be coated with sugar, which is a flavoring and sealant, or coated with a film-forming protective agent to optimize the tablet's dissolution characteristics. The composition can also be formulated as a chewable tablet, for example, by adding a substance such as mannitol to the formulation.

[0315] When it is desired to administer as a suppository, a typical base can be used. Cocoa butter is a traditional suppository base, which can be modified by adding waxes to slightly raise its melting point. In particular, water-miscible suppository bases containing polyethylene glycols of various molecular weights are widely used.

[0316] The effect of the compound can be delayed or prolonged by appropriate formulation.For example, the compound can be prepared as slowly dissolving pellets and incorporated into tablets or capsules, or as a sustained-release implantable device.Also, this technique involves preparing pellets with several different dissolution rates and filling capsules with a mixture of the pellets.Tablets or capsules can be coated with a film that resists dissolution for a predictable period of time.Non-oral formulations can also be prepared to be long-acting by dissolving or suspending the compound in an oily or emulsified solvent that can be gradually dispersed in serum.

[0317] In one embodiment, the pharmaceutical composition of the invention and / or the pharmaceutical formulation of the invention is provided in the form of a kit.

[0318] Treatment Methods and Uses In one aspect, the present invention provides a method for reducing intracellular lipid droplets, comprising contacting a conjugated compound of the present invention with a cell or tissue containing lipid droplets, wherein the lipid droplets are contained in the cell under physiological or pathological conditions and / or are induced to be produced by the cell.

[0319] The lipid droplet-containing cells or tissues may be derived, for example, from normal cells or tissues, biological models associated with lipid droplet accumulation, or cells or tissues from clinical patients. In one embodiment, the lipid droplets are lipid droplets contained in cells under normal physiological conditions. In another embodiment, the lipid droplets are lipid droplets contained in cells in a pathological state of a lipid metabolism-related disease. In a further embodiment, the lipid droplets are lipid droplets produced when cells are induced with an exogenous substance (e.g., sodium oleate).

[0320] In one aspect, the present invention provides use of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotopic compound, metabolite or prodrug thereof, or a pharmaceutical composition of the present invention in the manufacture of a medicament for reducing intracellular lipid droplets.

[0321] In a further aspect, the present invention provides the use of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotopic compound, metabolite or prodrug thereof, or a pharmaceutical composition of the present invention, in reducing intracellular lipid droplets.

[0322] In a still further aspect, the present invention provides a method for reducing intracellular lipid droplets, comprising administering to an individual in need thereof an effective amount of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof, or a pharmaceutical composition of the present invention.

[0323] In one aspect, the present invention provides the use of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotopic compound, metabolite, or prodrug thereof, or a pharmaceutical composition of the present invention, in the manufacture of a medicament for the treatment or prevention of a lipid metabolism-related disorder.

[0324] In a further aspect, the present invention provides the use of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotopic compound, metabolite or prodrug thereof, or a pharmaceutical composition of the present invention, in the treatment or prevention of a lipid metabolism-related disease.

[0325] In a still further aspect, the present invention provides a method for treating or preventing a lipid metabolism-related disease, comprising administering to an individual in need thereof an effective amount of a compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof, or a pharmaceutical composition of the present invention.

[0326] The compounds of the present invention can be administered to patients orally or parenterally in common formulations, such as capsules, microcapsules, tablets, granules, powders, troches, pills, suppositories, injections, suspensions, syrups, patches, creams, lotions, ointments, gels, sprays, liquids, and emulsions. Suitable formulations may contain common organic or inorganic additives, such as excipients (e.g., sucrose, starch, mannitol, sorbitol, lactose, glucose, cellulose, talc, calcium phosphate, or calcium carbonate), binders (e.g., cellulose, methylcellulose, hydroxymethylcellulose, polypropylpyrrolidone, polyvinylpyrrolidone, gelatin, gum arabic, polyethylene glycol, sucrose, or starch), disintegrants (e.g., starch, carboxymethylcellulose, hydroxypropyl starch, low-substituted hydroxypropyl cellulose, sodium bicarbonate, calcium phosphate, or calcium citrate), lubricants (e.g., sucrose, hydroxypropyl starch, low-substituted hydroxypropyl cellulose, sodium bicarbonate, calcium phosphate, or calcium citrate), or the like. The formulations can be manufactured by a commonly used method using additives such as hydroxypropyl cellulose, magnesium tearic acid, light anhydrous silicic acid, talc, or sodium lauryl sulfate, flavoring agents (e.g., citric acid, menthol, glycine, or orange powder), preservatives (e.g., sodium benzoate, sodium hydrogen sulfite, methylparaben, or propylparaben), stabilizers (e.g., citric acid, sodium citrate, or acetic acid), suspending agents (e.g., methylcellulose, polyvinylpyrrolidone, or aluminum stearate), dispersing agents (e.g., hydroxypropylmethylcellulose), diluents (e.g., water), and base waxes (e.g., cocoa butter, white petrolatum, or polyethylene glycol).

[0327] Dosage regimens may be adjusted to provide the optimum desired response. For example, when administered in the form of an injection, they may be administered as a single bolus, a bolus, and / or continuous infusions. For example, several divided doses may be administered over time, and the dose may be proportionally reduced or increased as indicated by the exigencies of the therapeutic situation. It should be noted that dosage values ​​vary depending on the type and severity of the condition to be improved and may include single or multiple doses. Generally, treatment dosages will depend on considerations such as the age, sex, and general health of the patient being treated, the frequency of treatment and the nature of the desired effect, the extent of tissue damage, the duration of symptoms, and other variables adjusted by each physician. Furthermore, it should be understood that the specific dosage regimen for any particular individual should be adjusted over time according to the individual's needs and the professional judgment of the person administering or supervising the administration of the composition. The dosage and administration regimen of the above-mentioned pharmaceutical compositions can be readily determined by those skilled in the clinical arts. For example, the compositions or compounds of the present invention can be administered in divided doses, ranging from four times daily to one dose every three days, at dosages of, for example, 0.01 to 1000 mg per administration. The desired dose can be administered in one or more applications to achieve the desired results. The pharmaceutical compositions of the present invention can be provided in unit dosage forms.

[0328] Concomitant medication The compound of the present invention or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite, or prodrug thereof, or the pharmaceutical composition of the present invention or the pharmaceutical formulation of the present invention according to the present invention can be used in combination with other therapeutic agents for the treatment or prevention of lipid metabolism-related diseases. In one embodiment, the other therapeutic agent is selected from substances that treat or prevent insulin resistance, substances that reduce the level of free fatty acids, and substances that reduce the level of cholesterol.

[0329] Exemplary embodiments of the present invention may include the following.

[0330] <1> A compound having a structure comprising Formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite, or prodrug thereof. LCM-L-TM (I) (In the formula, LCM is the LC3 binding moiety; L is a linker moiety, TM is the lipid droplet-binding moiety.

[0331] <2> In formula (I), the LCM portion is a portion having affinity for LC3 protein, and the TM portion is a portion capable of non-covalently interacting with lipid droplets. <1> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0332] <3> The above formula (1) has the structure of the following formula (2): [ka] (In the formula, Y is O or S; The C ring is C 6-10 an aryl group and a 5- to 7-membered heteroaryl group, and each of the aryl groups or heteroaryl groups is independently R X1 and optionally substituted with one or more groups selected from R 2 is H, C 1-8 alkyl groups, L 1 is a bond or a C1-C6 hydrocarbon chain, R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from R X1 , R X2 is the above <3> as defined by R X1 and R X2are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 The alkyl, alkenyl or alkynyl group is selected from the group consisting of halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 Alkylene group - 3-membered to 7-membered heterocyclic group) 2, ═O, —COOH and C 1-6 optionally substituted with one or more substituents selected from alkyl groups; R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group -C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group or aryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 , -S(=O)2OR Y1 , -S(=O)2R Y1 , -S(=O)2NR Y1 R Y2 , -S(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, ═O, ═S, —OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 and optionally substituted with one or more substituents selected from R Y1 , R Y2 , R Y3 , R Y4 are independently expressed as H, C 1-8 Alkyl group, C 3-10 Cyclic hydrocarbon group, C 3-10 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 10-membered heterocyclic group, 3- to 10-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, -NO2, -CN, C 1-8 Alkyl group, C 2-8 Alkenyl group, C 2-8 alkynyl groups, optionally substituted with one or more substituents selected from -OH, -SH, -NH2, =O, and -COOH. In particular, the structure of formula (2) [ka] The above is selected from <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0333] <4> The above formula (1) has the structure of the following formula (5): [ka] (In the formula, Y is O or S; R 9 H, halogen, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2 , -S(=O)2NR a2 R b2 and -S(=O)R a2 and R a1 , R b1 , R a2 , R b2 is the above <3> as defined by R 10 H, halogen, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 alkyl groups, R 3 H, halogen, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 4 H, halogen, -NO2, -CN, C 1-6 Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 Selected from R 7 , R 8 are independently expressed as H, C 1-6alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), and R 7 , R 8 is the above <3> as defined by R 5 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl group), wherein the alkyl group is selected from halogen, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R 6 H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(benzyl group), -SH, -S(C 1-6 alkyl group), -S (benzyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -NH (benzyl group), and the alkyl group or benzyl group is selected from halogen, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2) optionally substituted with one or more substituents selected from In particular, the structure of formula (5) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0334] <5> The above formula (6) has the structure of the following formula (8): [ka] (In the formula, Y is O or S; The C ring is [ka] and R 14 , R 15 , R 16 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 Selected from R 7 , R 8 is the above <6> and preferably R 14 , R 15 , R 17 , R 18 are each independently H, halogen, -NO2, -CN, C 1-6 Alkyl groups, -OH, -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), and R 16 is H or -OCH3, R 2 H, halogen, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 , -S(=O)2OR a2 , -S(=O)2R a2, -S(=O)2NR a2 R b2 and -S(=O)R a2 and R a2 , R b2 , R c2 is the above <6> and preferably R 2 H, halogen, C 1-6 alkyl groups, said alkyl groups being optionally substituted with one or more substituents selected from halogen, —NO2, —CN, —OH, —NH2 and —COOH; R 3 are H, -OH, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, —OH, —SH, —NH2, —NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 optionally substituted with one or more substituents selected from alkylene group-3- to 7-membered heterocyclic group)2 and -COOH; R 4 H, -OR 7 , -SR 7 , -NR 7 R 8 Selected from R 7 , R 8 are independently expressed as H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 5 is H, C 1-6 alkyl groups, wherein the alkyl groups are selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 optionally substituted with one or more substituents selected from alkylene group-3- to 7-membered heterocyclic group)2 and -COOH; R 6 H, halogen, C 1-6 an alkyl group, —OH, —NH2, said alkyl group being optionally substituted with one or more substituents selected from halogen, —OH, —NH2. In particular, the structure of formula (8) [ka] The above is selected from <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0335] <6> The above formula (6) has the structure of the following formula (9): [ka] (In the formula, R 2 H, halogen, -NO2, -CN, C 1-6 Alkyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, -OR a1 , -SR a1 , -NR a1 R b1 , -C(=O)OR a1 , -C(=O)NR a1 R b1 , -C(=O)R a1 , -S(=O)2OR a1 , -S(=O)2R a1 , -S(=O)2NR a1 R b1 , -S(=O)R a1 The alkyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl group, -OR a2 , -SR a2 , -NR a2 R b2 , -C(=O)OR a2 , -C(=O)NR a2 R b2 , -C(=O)R a2 and optionally substituted with one or more substituents selected from R 19 are each independently a halogen, -NO2, -CN, or C 1-6Alkyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7 , -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 wherein the alkyl group is selected from halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, -COOH, m is 0, 1, 2, 3, 4 or 5; R 3 , R 4 , R 5 , R 6 are each independently H and R X2 is selected from R X2 are each independently a halogen, -NO2, -CN, or C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, -OR 7 , -SR 7 , -NR 7 R 8 , -C(=O)OR 7 , -C(=O)NR 7 R 8 , -OC(=O)R 7 , -NC(=O)R 7 R 8 , -C(=O)R 7 , -S(=O)2OR 7, -S(=O)2R 7 , -S(=O)2NR 7 R 8 , -OS(=O)2R 7 , -NS(=O)2R 7 R 8 , -S(=O)R 7 The alkyl, alkenyl or alkynyl group is selected from the group consisting of halogen, —NO2, —CN, —OH, —O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 Alkylene group - 3-membered to 7-membered heterocyclic group) 2, ═O, —COOH and C 1-6 optionally substituted with one or more substituents selected from alkyl groups; R 7 , R 8 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, —NO2, —CN, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)O(C 1-6 alkyl group), -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -OC(=O)(C 1-6 alkyl group), -NHC(=O)(C 1-6 alkyl group), -C(=O)(C 1-6 alkyl groups), R a1 , R b1 , R c1 , R a2 , R b2 , R c2 are independently expressed as H, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl group, C 6-10 Aryl group, C 6-10 Aryl group -C 1-4 Alkyl group, 5- to 10-membered heteroaryl group, 5- to 10-membered heteroaryl group-C 1-4 Alkyl group, -OR Y1 , -SR Y1 , -NR Y1 R Y2 , -C(=O)OR Y1 , -C(=O)NR Y1 R Y2 , -C(=O)R Y1 , -S(=O)2ORY1 , -S(=O)2R Y1 , -S(=O)2NR Y1 R Y2 , -S(=O)R Y1 The alkyl group, alkenyl group, alkynyl group, cyclic hydrocarbon group, heterocyclic group, aryl group or heteroaryl group is selected from the group consisting of halogen, ═O, ═S, —OR Y3 , -SR Y3 , -NR Y3 R Y4 , -C(=O)R Y3 , -C(=O)OR Y3 and -C(=O)NR Y3 R Y4 and optionally substituted with one or more substituents selected from R Y1 , R Y2 , R Y3 , R Y4 is the above <1> or <2> ) In particular, the structure of formula (9) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0336] <7> The structure of the LCM moiety is the structure of the following formula (10) or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 20 is selected from bicycloheteroaryl groups having 9 to 10 ring atoms, the ring atoms containing 1 to 3 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, the remaining atoms being carbon atoms, and the heteroaryl group is unsubstituted or X3 and is substituted with at least one group selected from R 21 is C 1-8 alkyl groups, R 22 is RX3 is selected from R 23 is a phenyl group, unsubstituted or X3 and is substituted with at least one group selected from R X3 are independently generated for each occurrence, C 1-8 Alkyl group, C 1-8 Alkenyl groups, halogens, -CN, -CF3, -CHF2, -CH2F, -NO2, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group), -COOH, -C(=O)O(C 1-8 alkyl group), -C(=O)NH(C 1-8 alkyl group), -C(=O)N(C 1-8 alkyl group), -S(=O)2OH, -S(=O)2(OC 1-8 alkyl group), -S(=O)2NH2, -S(=O)2NH(C 1-8 alkyl group), -S(=O)2N(C 1-8 alkyl group), wherein the alkyl group is selected from halogen, —NO, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group), optionally substituted with one or more substituents selected from =O and -COOH; p is 0, 1 or 2. In particular, the structure of formula (10) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0337] <8> The structure of the LCM moiety is the structure of the following formula (11) or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 24 is selected from 3- to 7-membered heterocyclic groups, and the heterocyclic groups are unsubstituted or X3 and is substituted with at least one group selected from L 3 is one C 1-8 Alkylene group and one C 3-6 cycloalkylene groups; R 25 is H, C 1-8 alkyl groups, R 26 are halogens, -NO2, -CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, L 4 is C 1-8 Alkylene group and C 1-8 alkoxyylidene groups, R 27 is a phenyl group, unsubstituted or X3 and is substituted with at least one group selected from q is 0, 1 or 2; R X3 is the above <7> ) In particular, the structure of formula (11) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0338] <9> The structure of the LCM moiety is the structure of the following formula (12) or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 28 is C 1-8 an alkenyl group, wherein the alkenyl group is at least one C 1-8 substituted with an alkyl group, the alkyl group being R X4 and optionally substituted with one or more groups selected from R 29 is H, C 1-8 alkyl groups, R 30 are halogens, -NO2, -CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, L 5 is -O-, C 1-8 Alkylene group and C 1-8 alkoxyylidene groups, R 31 is selected from a 6-membered heteroaryl group having 6 ring atoms, the ring atoms containing 1 to 2 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, and the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or X3 and is substituted with at least one group selected from r is 0, 1, 2, 3 or 4; s is 0, 1, 2, 3 or 4; R X4 are independently generated for each occurrence, C 1-8 Alkyl group, C 1-8 Alkenyl groups, halogens, -CN, -CF3, -CHF2, -CH2F, -NO2, -O(C 1-8 alkyl group), -S(C 1-8 alkyl group), -NH(C 1-8 alkyl group), -N(C 1-8alkyl group)2, -OC(=O)(C 1-8 alkyl group), -NHC(=O)(C 1-8 alkyl group), -NC(=O)(C 1-8 alkyl group)2, -OS(=O)2(C 1-6 alkyl group), -NHS(=O)2(C 1-8 alkyl group), -N(C 1-8 alkyl group)S(=O)2(C 1-8 alkyl group), wherein the alkyl group is selected from halogen, —NO2, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group), optionally substituted with one or more substituents selected from =O and -COOH; R X3 is the above <7> ) In particular, the structure of formula (12) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0339] <10> The structure of the LCM moiety is the structure of the following formula (13) or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 32 is selected from 3- to 7-membered heterocyclic groups, and the heterocyclic groups are unsubstituted or X3 and is substituted with at least one group selected from L 6 is -O-, C 1-8 Alkylene group and C 1-8 alkoxyylidene groups, R 33 , R 34 is a halogen, C1-8 alkyl groups, R 35 are halogens, -NO2, -CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C 1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, R 36 is selected from a 5-membered heteroaryl group having 5 ring atoms, the ring atoms containing 1 to 3 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or X3 and is substituted with at least one group selected from t is 0, 1, 2 or 3; u is 0, 1, 2, 3 or 4; R X3 is the above <7> ) In particular, the structure of formula (13) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0340] <11> The structure of the LCM moiety is the structure of the following formula (14) or a pharmaceutically acceptable salt thereof: [ka] (In the formula, R 37 is selected from 6-membered heteroaryl groups having 6 ring atoms, the ring atoms containing 1 to 2 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, and the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or substituted with halogen, —NO, —CN, C 1-8 Alkyl groups, -OH, -O(C 1-8 alkyl group), -SH, -S(C1-8 alkyl group), -NH2, -NH(C 1-8 alkyl group), -N(C 1-8 alkyl group)2, R 38 , R 39 , R 40 are each independently R X3 is selected from R 41 is selected from a 5-membered heteroaryl group having 5 ring atoms, the ring atoms containing 1 to 3 heteroatoms each independently selected from oxygen, sulfur, and nitrogen, the remaining atoms being carbon atoms, the heteroaryl group being unsubstituted or X3 and is substituted with at least one group selected from v is 0, 1, 2 or 3; w is 0, 1, 2, 3 or 4; x is 0, 1, 2, 3 or 4; R X3 is the above <7> ) In particular, the structure of formula (14) [ka] The above <1> or <2> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0341] <12> In formula (I), L is a chemical bond or a linear or branched hydrocarbon group containing 1 to 60, preferably 1 to 30, more preferably 2 to 16 carbon atoms, each carbon atom being optionally substituted with one or more, for example 1 to 3, preferably 1 to 2, in particular 1 heteroatom, selected from oxygen, sulfur, nitrogen, phosphorus, preferably oxygen, sulfur or nitrogen, more preferably oxygen or nitrogen, in particular oxygen, and the carbon atom or heteroatom is selected from R L1 , R L2 , R L3 , R L4 and RL5 and optionally substituted with one or more groups selected from R L1 , R L2 , R L3 , R L4 and R L5 are each independently H, a halogen group, or C 1-6 Alkyl group, -O(C 1-6 alkyl group), -S(C 1-6 alkyl group), -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, C 3-6 Cycloalkyl groups, C 6-10 Aryl group, 5- to 7-membered heteroaryl group, 3- to 7-membered heterocyclic group, -O(C 3-6 cycloalkyl group), -S(C 3-6 cycloalkyl group), -NH(C 3-6 cycloalkyl group), -N(C 3-6 cycloalkyl group)2, -N(C 3-6 Cycloalkyl group)(C 1-6 alkyl group), -OH, -NH2, -SH, -S(=O)2(C 1-6 alkyl group), -P(=O)(OC 1-6 alkyl group)(C 1-6 alkyl group), -P(=O)(OC 1-6 alkyl group)2, -C≡CC 1-6 Alkyl groups, -C≡CH, -CH=CH(C 1-6 alkyl group), -C(C 1-6 alkyl group)=CH(C 1-6 alkyl group), -C(C 1-6 alkyl group)=C(C 1-6 alkyl group), -Si(OH), -Si(C 1-6 alkyl group)3, -Si(OH)(C 1-6 alkyl group)2, -C(=O)(C 1-6 alkyl group), -COOH, halogen, -CN, -CF3, -CHF2, -CH2F, -NO2, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C1-6 alkyl group)2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -N(C 1-6 alkyl group)C(=O)NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)C(=O)N(C 1-6 alkyl group)2, -NHC(=O)NH(C 1-6 alkyl group), -NHC(=O)N(C 1-6 alkyl group), -NHC(=O)NH, -N(C 1-6 alkyl group)S(=O)2NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)S(=O)2N(C 1-6 alkyl group), -NHS(=O)2NH(C 1-6 alkyl group), -NHS(=O)2N(C 1-6 alkyl group)2 and NHS(=O)2NH2; Preferably, L is a straight-chain group. <1> ~ <11> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0342] <13> The TM portion is selected from a lipid droplet probe, a compound capable of binding to a lipid droplet marker protein, and a compound capable of binding to a neutral fatty acid in a lipid droplet; Preferably, the lipid droplet probe is selected from the group consisting of Sudan I, Sudan II, Sudan III, Oil Red BB, Oil Red O, Sudan Red G, Sudan Black B, Nile Red, BODIPY® 493 / 503, monodansylpentane, PyrPy10d, PyrPy11c, PITE, TPE-AmAl, TPA-BI, LipidGreen, LipidGreen2, LD540, AF8, AF10, AFN, NAP AIEgen dyes, LD-BTD1, LipiDye, Phos 2a, Phos 2b, Phos 3a, Phos 3b, SF44, SF58, FAS, DPAS, BTD-coumarin hybrid, IND-TPA, photoactivatable AIE probe, LD-TPZn, LQD, photoactivatable AIEgen probe, TPE-AC, TPMN, TTMN, MeTTMN, MeOTTMN, DCMa, DCI, DCFu, NLV-1, StatoMerocynaine dye (SMCy dye), The NAP AIEgen dye is preferably selected from NAP-Ph, NAP-Br, NAP-CF3, NAP-Py, The BTD-coumarin hybrid is preferably BTD-Lip; The photoactivatable AIE probe is preferably BZT 3a; The photoactivatable AIEgen probe is preferably PhotoAFN 2a-c; The SMCy dyes are preferably selected from SMCy 3 and SMCy 5.5, In particular, the TM moiety is selected from Sudan I, Sudan II, Sudan III, Oil Red BB, Oil Red O, Sudan Red G, Sudan Black B, preferably Oil Red O and Oil Red BB, in particular Oil Red BB. <1> ~ <12> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0343] <14> The TM moiety is a structure of formula (II) below or a conjugate or hybrid formed by interconnecting two or more structures of formula (II): <1> ~ <13> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof. [ka] (In the formula, The E ring and the F ring are each independently selected from a benzene ring and a naphthalene ring, and the E ring is R E and the F ring is optionally substituted with one or more groups selected from R F and the G ring is optionally substituted with one or more groups selected from R G and optionally substituted with one or more groups selected from Ring G is absent or selected from a benzene ring and a naphthalene ring; Z 1 is an azo group, Z 2 is absent or an azo group, R E , R F and R G are independently H, halogen, -NO2, -CN, =O, =S, C at each occurrence. 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O) (3- to 7-membered heterocyclic group), -N(C 1-6 alkyl group)-(C=O)(3- to 7-membered heterocyclic group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, The Two R's E, two R F or two R's G between them bond to each other and the atoms to which they are bonded. 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2) optionally substituted with one or more substituents selected from

[0344] <15> Formula (II) has the structure of formula (III): [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are each independently H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O) (3- to 7-membered heterocyclic group), -N(C 1-6 alkyl group)-(C=O)(3- to 7-membered heterocyclic group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is not a halogen atom, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or heterocyclic ring is not substituted with halogen, a nitro group, a cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 optionally substituted with one or more substituents selected from alkyl groups, Preferably, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48At least one of the following is -Cl, -Br, -I, -NO2, -CN, =O, =S, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group) or -S(=O)N(C 1-6 alkyl group), and the remaining groups are each independently H, halogen, —NO, —CN, ═O, ═S, C 1-6 Alkyl groups, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group)2, wherein the alkyl group is selected from halogen, —OH, —O(C 1-6alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from: -S(=O)2, -COOH, -S(=O)2OH; or R 42 , R 43 , R 44 , R 45 , R 46 , R 47 and R 48 From, preferably R 44 and R 45 Two adjacent groups selected from are bonded to each other and together with the atoms to which they are attached form a C 3-10 A hydrocarbon ring or a 3- to 7-membered heterocyclic ring is formed, and the hydrocarbon ring or the heterocyclic ring is not substituted with halogen, —OH, —O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 optionally substituted with one or more substituents selected from -S(=O)OH, -COOH, -S(=O)OH, and R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 is H, or R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 At least one, preferably 1 to 6, more preferably 1 to 4, particularly preferably 1, 2 or 4 of the 1-6 Alkyl group or -O(C 1-6 alkyl group), preferably C 1-3 Alkyl group or -O(C 1-3 alkyl group), and C 1-3 The alkyl group is particularly preferably a methyl group, and —O(C1-3 The alkyl group is particularly preferably a methoxy group, and the remaining groups are each independently H, halogen, C 1-6 Alkyl group, C 3-6 Cycloalkyl groups, C 3-6 Cycloalkyl group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 The alkyl group is selected from the group consisting of alkyl groups, preferably H and halogen, particularly preferably H, and the alkyl group is selected from the group consisting of halogen, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2) optionally substituted with one or more substituents selected from In particular, formula (III) [ka] is selected from, preferably [ka] Selected from, in particular [ka] The above <14> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0345] <16> Formula (II) has the structure of formula (IV): [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 53 , R 54 , R 55 , R 56 and R57 is the above <11> ) In particular, formula (IV) [ka] The above is selected from <14> or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope, metabolite or prodrug thereof.

[0346] <17> Formula (II) has the structure of formula (V): [ka] (In the formula, R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 53 , R 54 , R 55 , R 56 and R 57 is the above <11> as defined by R 58 , R 59 , R 60 , R 61 , R 62 and R 63 are each independently H, halogen, -NO2, -CN, =O, =S, C 1-6 Alkyl group, C 2-6 Alkenyl group, C 2-6 Alkynyl group, C 3-6 Cyclic hydrocarbon group, C 3-6 Cyclic hydrocarbon group-C 1-4 Alkyl group, 3- to 7-membered heterocyclic group, 3- to 7-membered heterocyclic group-C 1-4 Alkyl groups, -OH, -O(C 1-6 alkyl group), -O(C 3-6 cyclic hydrocarbon group), -O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(3- to 7-membered heterocyclic group), -O(C 1-4alkylene group)-(3- to 7-membered heterocyclic group), -O(C=O)(C 1-6 alkyl group), -O(C=O)(C 3-6 cyclic hydrocarbon group), -O(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -O(C=O)(3- to 7-membered heterocyclic group), -O(C=O)(C 1-4 Alkylene group)-(3- to 7-membered heterocyclic group), -SH, -S(C 1-6 alkyl group), -S(C 3-6 cyclic hydrocarbon group), -S(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -S(3- to 7-membered heterocyclic group), -S(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group)2, -NH(C 3-6 cyclic hydrocarbon group), -N(C 3-6 Cyclic hydrocarbon group)2, -NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -NH(3- to 7-membered heterocyclic group), -N(3- to 7-membered heterocyclic group), -NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group)2, -NH(C=O)(C 1-6 alkyl group), -N(C 1-6 alkyl group)-(C=O)(C 1-6 alkyl group), -NH(C=O)(C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 3-6 cyclic hydrocarbon group), -NH(C=O)(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -N(C 1-6 alkyl group)-(C=O)(C 1-4 Alkylene group -C 3-6 -cyclic hydrocarbon group), -NH(C=O) (3- to 7-membered heterocyclic group), -N(C 1-6alkyl group)-(C=O)(3- to 7-membered heterocyclic group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)O(C 1-6 alkyl group), -C(=O)O(C 3-6 cyclic hydrocarbon group), -C(=O)O(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)O(3- to 7-membered heterocyclic group), -C(=O)O(C 1-4 alkylene group)-(3- to 7-membered heterocyclic group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group)2, -C(=O)NH(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)N(C 1-4 Alkylene group -C 3-6 cyclic hydrocarbon group), -C(=O)NH(3- to 7-membered heterocyclic group), -C(=O)N(3- to 7-membered heterocyclic group), -C(=O)NH(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -C(=O)N(C 1-4 alkylene group, 3- to 7-membered heterocyclic group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C 1-6 alkyl group)2, -S(=O)NH(C 1-6 alkyl group), -S(=O)N(C 1-6 alkyl group), and the alkyl group, alkylene group, alkenyl group, alkynyl group, cyclic hydrocarbon group or heterocyclic group is selected from halogen, nitro group, cyano group, -OH, -O(C 1-6 alkyl group), -SH, -S(C 1-6 alkyl group), -NH2, -NH(C 1-6 alkyl group), -N(C 1-6 alkyl group), -COOH, -C(=O)(C 1-6 alkyl group), -C(=O)NH2, -C(=O)NH(C 1-6 alkyl group), -C(=O)N(C 1-6 alkyl group), -S(=O)2OH, -S(=O)2NH(C 1-6 alkyl group), -S(=O)2N(C1-6 optionally substituted with ...

Claims

1. A compound having a structure comprising formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotopic compound thereof. LCM-L-TM (I) (In the formula, LCM is an LC3 binding moiety, and LCM has the structure of the corresponding moiety of formula (ii): 【Chemical 1】 (In the formula, Y is O or S; Ring C is selected from the group consisting of C 6-10 aryl groups, said aryl groups being optionally substituted with one or more groups each independently selected from the group consisting of R X1 ; R 2 is selected from the group consisting of H, C 1-8 alkyl groups; L 1 is a C 1 -C 6 hydrocarbon chain; R 3 , R 4 , R 5 , and R 6 are each independently selected from the group consisting of H and R X2 ; R X1 and R X2 at each occurrence are each independently selected from the group consisting of halogen, —NO 2 , —CN, —OR 7 , —SR 7 , and —NR 7 R 8 ; R 7 and R 8 are each independently selected from the group consisting of H. and L is a linker moiety, and L has the structure of formula (a) or a pharmaceutically acceptable salt thereof: -Dy- (a) wherein y is an integer greater than 1; y is an integer of 30 or less, Each D is independently selected from the group consisting of —CR L1 R L2 —, where R L1 and R L2 are H. and TM is a lipid droplet binding moiety, and TM has the structure of the corresponding moiety of formula (xvi): 【Chemistry 2】 (wherein R 42 , R 43 , R 44 , R 45 , R 46 , R 47 , R 48 , R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are each independently selected from the group consisting of H, halogen, —NO 2 , —CN, a C 1-6 alkyl group, —OH, —SH and —NH 2 ). (having

2. In formula (I), the LCM portion is a portion having affinity for the LC3 protein; The TM portion is a portion capable of non-covalently interacting with lipid droplets.

2. The compound of claim 1 or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotopic compound thereof.

3. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein y is an integer of 20 or less.

4. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein y is an integer of 16 or less.

5. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein y is an integer of 12 or less.

6. L is 【Chemistry 3】 2. The compound of claim 1, having the structure: or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer, or isotopic compound thereof.

7. Formula (ii) is 【Chemistry 4】 2. The compound of claim 1, having the structure: or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer, or isotopic compound thereof.

8. the TM portion is selected from the group consisting of lipid droplet probes; The lipid droplet probe is selected from the group consisting of Sudan III and Sudan IV; 2. The compound of claim 1 or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotopic compound thereof.

9. R ４２ , R ４３ , R ４４ , R ４５ , R ４６ , R ４７ and R ４８ At least one of the following is —Cl, —Br, —I, or —NO ２ , —CN, —OH, —SH, or —NH2, and the remaining groups are each independently H, halogen, or —NO ２ , -CN,C １－６ alkyl group, —OH, —SH, —NH2; R ４９ , R ５０ , R ５１ , R ５２ , R ５３ , R ５４ , R ５５ , R ５６ and R ５７ is H, or R ４９ , R ５０ , R ５１ , R ５２ , R ５３ , R ５４ , R ５５ , R ５６ and R ５７ At least one of １－６ 2. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer, or isotopic compound thereof, wherein: R is an alkyl group; and R is an alkyl group; and the remaining groups are each independently selected from the group consisting of H and halogen.

10. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein one to six of R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are a C 1-6 alkyl group.

11. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein one to four of R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are C 1-6 alkyl groups.

12. The compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein one, two or four of R 49 , R 50 , R 51 , R 52 , R 53 , R 54 , R 55 , R 56 and R 57 are a C 1-6 alkyl group.

13. The compound according to any one of claims 10 to 12, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein the C 1-6 alkyl group is selected from the group consisting of C 1-3 alkyl groups.

14. The compound according to claim 13, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein the C 1-3 alkyl group is a methyl group.

15. The compound of claim 9 or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, wherein R 49, R 50, R 51, R 52, R 53, R 54, R 55, R 56 and R 57 are H, or at least one of R 49, R 50, R 51, R 52, R 53, R 54, R 55, R 56 and R 57 is a C 1-6 alkyl group and the remaining groups are H.

16. Formula (xvi) is 【Chemistry 5】 2. The compound of claim 1, having the structure: or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer, or isotopic compound thereof.

17. Formula (xvi) is 【Chemistry 6】 2. The compound of claim 1, having the structure: or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer, or isotopic compound thereof.

18. The compound is 【Chemistry 7】 18. The compound according to any one of claims 1 to 17, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotopic compound thereof, selected from:

19. 20. A pharmaceutical composition comprising a prophylactically or therapeutically effective amount of a compound according to any one of claims 1 to 18, or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotopic compound thereof, and one or more pharmaceutically acceptable carriers.

20. A drug for treating a lipid metabolism-related disease, comprising the compound according to any one of claims 1 to 18 or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer or isotope thereof, or the pharmaceutical composition according to claim 19.

21. The drug described in claim 20, wherein the lipid metabolism-related disease is selected from the group consisting of MADD, obesity, NAFLD, type II diabetes, hepatocellular carcinoma, Alzheimer's disease and atherosclerosis.

22. A composition for reducing intracellular lipid droplets, comprising the compound according to any one of claims 1 to 18 or a pharmaceutically acceptable salt, stereoisomer, solvate, tautomer, or isotope thereof, The lipid droplets are contained in cells under physiological or pathological conditions and / or are induced to be produced by cells. composition.

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