c-MYC mRNA translation regulators and their use in cancer therapy

Abstract

The present invention relates to novel c-MYC mRNA translation regulators, compositions containing same, methods for their preparation, and their use in the treatment of cancer.

Description

[Technical field]

[0001] The present invention relates to novel c-MYC mRNA translation regulators, compositions containing same, methods for their preparation, and their use in the treatment of cancer. [Background technology]

[0002] Cancer is the second leading cause of death in the United States, after heart disease. In the United States, cancer is responsible for one in every four deaths. The 5-year relative survival rate for all cancer patients diagnosed between 1996 and 2003 was 66%, up from 50% between 1975 and 1977 (Cancer Facts & Figures American Cancer Society: Atlanta, GA (2008)). Between 2000 and 2009, the rate of new cancer cases in men decreased by an average of 0.6% per year, but remained stable in women. Between 2000 and 2009, the death rate from all cancers decreased by an average of 1.8% per year in men and 1.4% per year in women. This improvement in survival reflects advances in early diagnosis and improved treatment. Finding highly effective anticancer drugs with low toxicity is a major goal of cancer research.

[0003] The Myc family includes three major members, namely the proto-oncogene c-Myc (cellular myelocytomatosis, abbreviated as Myc), L-Myc, and N-Myc. These three Myc homologs are involved in the early stages of carcinogenesis and metastatic spread in most human cancers. In most types of tumors, the Myc gene does not have mutations or duplications, but its mRNA and / or protein levels are increased, indicating that Myc overexpression is induced in cancer at the transcriptional, mRNA steady-state, and translational levels. In fact, Myc gene expression is usually dependent on growth factor signaling, and the half-lives of both Myc RNA and Myc protein are very short (30 and 20 min, respectively) [Dang, CV (2012). MYC on the path to cancer. Cell 149, 22-35]. However, in tumor cells, the intracellular levels of Myc are independent of such signaling and regulation, resulting in exacerbated Myc function, driving intracellular and extracellular transcriptional programs that enable tumor growth and proliferation. However, Myc does not necessarily have to be overexpressed in order for cancer to be highly dependent on Myc activity. According to a study by Soucek et al. (Nature (2008) 455(7213):679-83), tumors expressing c-Myc at endogenous levels show tumor regression by Myc inhibition via a genetically engineered system. Therefore, treatment with Myc inhibitors is not necessarily limited to cancers that overexpress Myc. The compounds of the present invention can also be used to regulate the translation of Myc mRNA, in which case the direct target of the compound is the protein or RNA that regulates the translation of Myc mRNA, and such tumors that are Myc-dependent will benefit from the therapeutic utility of the compounds of the present invention.

[0004] Myc is an important anticancer drug target due to its broad pathogenic significance. Deregulation of the Myc gene has been found in a wide range of human hematological malignancies and solid tumors, particularly in breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin lymphoma, Burkitt lymphoma, diffuse large B-cell lymphoma, prostate cancer, colon cancer, gastric cancer, primary central nervous system lymphoma, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, germinal center-derived lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, and lung adenocarcinoma. Recent studies have also shown that deregulation of c-MYC is associated with the development of BRAFV600E thyroid cancer, choroid plexus cancer, and colitis-associated cancer. In addition, a significant number of cases of epithelial ovarian cancer have been found to have MYC gene amplification. In the TCGA dataset, Myc amplification occurs in several cancer types, including breast, colon, pancreatic, gastric, and uterine cancers.

[0005] Myc gene is a very important oncogene and is considered a driver of carcinogenesis, and MYC protein is an important transcription factor that broadly targets various genes, but it remains difficult to rationally design direct Myc inhibitors. This is mainly because MYC protein lacks a structural region suitable for therapeutic inhibition by small molecules and is considered a difficult target for drug discovery [BioDrugs (2019) 33:539-553].

[0006] Designing and developing MYC regulators is challenging, primarily because the MYC protein has a disordered structure that lacks pockets or grooves that could serve as binding sites for regulators. Inhibiting MYC transcription, blocking protein-protein interactions (PPIs) of MYC and its cofactors, or affecting signaling pathways associated with MYC have previously been used as potential regulatory targets but have not been developed as drug candidates. Myc PPI inhibitors have failed to demonstrate sufficient efficacy in cell-based assays or animal models because they require high target occupancy to promote efficacy. Regulators of signaling pathways upstream of Myc, such as mTOR regulators, have failed due to lack of target specificity.

[0007] Nevertheless, therapeutic approaches targeting c-Myc remain elusive. The lack of a clear ligand-binding domain is a major obstacle to direct inhibition, a challenging feature shared by many of the major transcriptional targets in cancer. Therefore, as outlined herein, there is a need for alternative means of targeting Myc, namely compounds that modulate the translation of Myc mRNA. Summary of the Invention [Means for solving the problem]

[0008] The present invention provides compounds represented by structural formulas I, II, and I(a)-I(h) as defined below, as well as compounds represented by structural formulas listed in Table 1, or pharma- ceutically acceptable salts, stereoisomers, tautomers, hydrates, N-oxides, reverse amide analogs, prodrugs, isotopic variants (e.g., deuterated analogs), PROTACs, pharmaceutical products, or any combination thereof. In various embodiments, the compounds of the present invention are c-MYC mRNA translation regulators. In various embodiments, the compounds of the present invention are c-MYC mRNA transcription regulators. In various embodiments, the compounds of the present invention are c-MYC inhibitors. In various embodiments, the compounds of the present invention are any combination of c-MYC mRNA transcription regulators, c-MYC mRNA transcription regulators, and c-MYC inhibitors.

[0009] The present invention also provides pharmaceutical compositions comprising compounds represented by structural formulas I, II, and I(a)-I(h), as defined below, as well as compounds represented by the structural formulas listed in Table 1, or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, prodrug, isotopic variant (e.g., deuterated analogue), PROTAC, pharmaceutical product, or any combination thereof.

[0010] The present invention also provides a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting cancer, comprising the step of administering to a subject suffering from cancer a compound represented by structural formulas I, II, and I(a)-I(h), as defined below, or a compound represented by a structural formula listed in Table 1, under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit cancer in the subject.

[0011] The invention also provides a method for suppressing, reducing, or inhibiting tumor growth, comprising administering to a subject having tumor growth a compound represented by structural formulas I, II, and I(a)-I(h), as defined below, and a compound represented by a structural formula listed in Table 1, under conditions effective to suppress, reduce, or inhibit tumor growth in the subject. In some embodiments, the tumor is cancer. In some embodiments, the subject is afflicted with cancer.

[0012] The present invention also provides a method for regulating c-MYC mRNA translation in a cell, comprising the step of contacting a cell with a compound represented by structural formulas I, II, and I(a)-I(h) as defined below, and a compound represented by a structural formula listed in Table 1, thereby regulating c-MYC mRNA translation in the cell.

[0013] The present invention also provides a method for regulating c-MYC mRNA transcription in a cell, comprising the step of contacting a cell with a compound represented by structural formulas I, II, and I(a)-I(h) as defined below, and a compound represented by a structural formula listed in Table 1, thereby regulating c-MYC mRNA transcription in the cell. [Brief description of the drawings]

[0014] This patent or application contains at least one color drawing. Copies of this patent or patent application publication with color drawing(s) will be provided by the Patent and Trademark Office upon request and payment of the necessary fee.

[0015] [Figure 1] FIG. 1 shows how protein synthesis monitoring (PSM) specifically monitors the synthesis of c-Myc. The assay system includes the human non-small cell lung cancer cell line A549, which expresses high levels of c-Myc. Two tRNAs (di-tRNAs) that decode one specific glycine codon and one specific proline codon were transfected with control RNAi or RNAi directed against c-Myc. The FRET signal in c-Myc siRNA-treated cells is inhibited, so the FRET signal specifically monitors c-Myc translation. In blue are cell nuclei stained with DAPI. In yellow are FRET signals from a tRNA pair that decodes the glutamine-serine dicodon. [Diagram 2] Figure 2 shows selective regulation of c-Myc translation. The figure shows metabolic labeling in A549 cells treated with vehicle, the general translation inhibitor cycloheximide, or anti-c-Myc compounds. Treatment with cycloheximide completely inhibited global protein synthesis, while treatment with the tested compounds had no significant effect. In grey are cell nuclei stained with DAPI. In yellow is L-azidohomoalanine (AHA) metabolic labeling. [Diagram 3] FIG. 3 shows that the compounds of the invention act at the level of mRNA processing / stability. A549 cells were exposed to vehicle, the general transcription inhibitor Actinomycin D, or anti-c-Myc compounds. The upper panel shows that a significant decrease in c-Myc protein levels was observed after treatment with Actinomycin D or the tested compounds. The lower panel shows that c-MYC mRNA levels and transcription sites were completely decreased after treatment with Actinomycin D. Treatment with the tested compounds reduced c-MYC mRNA levels by 30% without affecting the transcription sites. Grey indicates cell nuclei stained with DAPI. Red indicates c-Myc protein. Purple indicates c-MYC mRNA. Yellow indicates c-Myc transcription sites. [Figure 4] FIG. 4 shows the efficacy of compounds of the invention in A549 cells. [Diagram 5]Figure 5 shows in vivo data measured for compound 332. Compound 332 inhibited c-Myc-dependent tumor growth in vivo. Relative tumor volume of A549 xenografts in NMRI female nude mice after administration of 3 mg / kg of the compound of the invention twice weekly for 49 days. Error bars represent median ± SEM for mice (n=10) at each time point and analyzed by Prism one-tailed T-test (*p<0.05). DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0016] In various embodiments, the present invention relates to a compound represented by the following structural formula (I): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0017] [ka]

[0018] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10(For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0019] [ka]

[0020] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10, R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, ethoxy) (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0021] [ka]

[0022] During the ceremony, X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1-C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring;

[0023] [ka]

[0024] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0025] In various embodiments, the present invention relates to a compound represented by the following structural formula (Ia): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0026] [ka]

[0027] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X10 is N, CH, or C(R); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 ) 3- Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3)CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0028] [ka]

[0029] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 Cycloalkyl), CD 3 , OCD 3 , NO 2 , -CH 2 CN, -R 8 C.N., R. 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3, -OCH 2 Ph, NHCO-N(R 10 )(R 11 ), R 8 -C(O)-R 10 , S.O. 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 a straight or branched chain alkoxyalkyl, a substituted or unsubstituted 4- to 7-membered heterocycle (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), a substituted or unsubstituted aryl, a substituted or unsubstituted benzyl, or R 8 -(substituted or unsubstituted 3- to 8-membered monocyclic, fused or spiro heterocycle); Or, R 7 is represented by the following structural formula A:

[0030] [ka]

[0031] X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form C 3 -C 8 forming a carbocyclic (e.g., cyclopropyl) or heterocyclic ring of; R 3 and R 4are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R 20 is represented by the following structural formula:

[0032] [ka]

[0033] R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 2 -CH 2 -O-CH 3 , C.H. 2 -O-CH 2 -CH 2 -O-CH 3 ), C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 Straight or branched chain haloalkyl (e.g., CHF 2 , C.F. 3 , C.F. 2 CH 3 , C.H. 2 CF 3 , C.F. 2 CH 2 CH 3, C.H. 2 CH 2 CF 3 , C.F. 2 CH(CH 3 ) 2 , CF(CH 3 )-CH(CH 3 ) 2 ), R 8 -aryl (e.g., CH 2 -Ph), -R 8 -OR 8 -OR 10 (For example, (CH 2 ) 2 -O-(CH 2 ) 2 -O-CH 3 ), -R 8 -OR 10 (For example, (CH 2 ) 2 -O-CH 3 ), -R 8 -R 10 , substituted or unsubstituted aryl (e.g., phenyl), or substituted or unsubstituted heteroaryl (e.g., pyridine (2,3,4-pyridine)); R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 2 -CH 2 -O-CH 3 , C.H. 2 -O-CH 2 -CH 2 -O-CH 3 ), C 1 -C 5 Linear or branched alkoxy of C 1 -C 5Straight or branched chain haloalkyl (e.g., CHF 2 , C.F. 3 , C.F. 2 CH 3 , C.H. 2 CF 3 , C.F. 2 CH 2 CH 3 , C.H. 2 CH 2 CF 3 , C.F. 2 CH(CH 3 ) 2 , CF(CH 3 )-CH(CH 3 ) 2 ), R 8 -aryl (e.g., CH 2 -Ph), -R 8 -OR 8 -OR 10 (For example, (CH 2 ) 2 -O-(CH 2 ) 2 -O-CH 3 ), -R 8 -OR 10 , -R 8 -R 10 (For example, (CH 2 ) 2 -O-CH 3 ), substituted or unsubstituted aryl (e.g., phenyl), or substituted or unsubstituted heteroaryl (e.g., pyridine (2,3,4-pyridine)); Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2-O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0034] In various embodiments, the present invention relates to a compound represented by the following structural formula (Ib): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0035] [ka]

[0036] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 6 are F, Cl, Br, I, OH, SH, and R.8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), (CH 2 ) 3 -Piran, C.H. 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Methyl-THF, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane, CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10)(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 )2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -OCH 2 -CH 2 -O-CH 3 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 )2-O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C1-C5 straight or branched chain thioalkoxy, C1-C5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), substituted or unsubstituted 3-8 membered heterocycle (e.g., trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, 1-methylazepan-2-one, 3-azabicyclo[3.1.0]hexane), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0037] [ka]

[0038] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 are joined together to form a substituted or unsubstituted pyrrolidine ring, piperazine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, pyrazole, imidazole, 2,5-diazabicyclo[2.2.1]heptane, or diazabicyclo[2.2.1]heptane; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8-SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, pyrazole, piperazine, piperidine, dioxazole, triazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0039] [ka]

[0040] During the ceremony, X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3-C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R 20 is represented by the following structural formula:

[0041] [ka]

[0042] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0043] In various embodiments, the present invention relates to a compound represented by the following structural formula (Ic): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0044] [ka]

[0045] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3, (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2-Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0046] [ka]

[0047] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10, R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, ethoxy) (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0048] [ka]

[0049] During the ceremony, X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1-C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring;

[0050] [ka]

[0051] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0052] In various embodiments, the present invention relates to a compound represented by the following structural formula (Id): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0053] [ka]

[0054] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X10 is N, CH, or C(R); X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , X 9 , and X 10 at least one of is N; R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 )3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0055] [ka]

[0056] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, ethoxy) (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0057] [ka]

[0058] During the ceremony, X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R 20 is represented by the following structural formula:

[0059] [ka]

[0060] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0061] In various embodiments, the present invention relates to a compound represented by the following structural formula (Ie): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0062] [ka]

[0063] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 5 and R 6 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, ethoxy) (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0064] [ka]

[0065] During the ceremony, X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form =O or C 3 -C 8forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH)2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R 20 is represented by the following structural formula:

[0066] [ka]

[0067] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0068] In various embodiments, the present invention relates to a compound represented by the following structural formula (If): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0069] [ka]

[0070] During the ceremony, A' is a 3- to 8-membered monocyclic or fused saturated, unsaturated or aromatic heterocyclic ring; X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 10 is N, CH, or C(R); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2-Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2-CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8-aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0071] [ka]

[0072] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3, OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, ethoxy) (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0073] [ka]

[0074] During the ceremony, X 1 is N or O; R 1 and R 2are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R 20 is represented by the following structural formula:

[0075] [ka]

[0076] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0077] In various embodiments, the present invention relates to a compound represented by the following structural formula (Ig): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0078] [ka]

[0079] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 100 is C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methyl), R 8 -OH (e.g., (CH 2 ) 2 -OH), -R 8 -OR 10 (For example, (CH 2 ) 2 -O-CH 3 ), R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -NH(CH 3 ), (CH 2) 2 -NH 2 ), R 20 or a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., pyrrolidine, piperidine); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8-(substituted or unsubstituted 3-10 membered monocyclic, fused or spiro heterocyclic ring) (e.g., (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3-Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula C:

[0080] [ka]

[0081] During the ceremony, k, 1 to 4; R 12 and R 13 are, independently of each other, H, C 1 -C 5 or R 20 is; Or, R 12 and R 13 are joined together to form a substituted or unsubstituted 4- to 7-membered heterocycle (e.g., piperidine, piperazine, pyrrolidine, oxa-6-azaspiro[3.3]heptane); Or, R 6 is represented by the following structural formula Bi:

[0082] [ka]

[0083] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 20 is represented by the following structural formula:

[0084] [ka]

[0085] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0086] In some embodiments, R 100 is methyl and R 5 If H, then R 12 and R 13 and R are not both alkyl. 100 is methyl and R 5 If H, then R 12 and R 13 cannot combine with each other to form piperidine.

[0087] In various embodiments, the present invention relates to a compound represented by the following structural formula (Ih): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0088] [ka]

[0089] During the ceremony, Ring F is absent or is a substituted or unsubstituted, saturated or unsaturated 4- to 8-membered heterocycle (e.g., pyrrolidine, pyridine, imidazole, pyrimidine, triazole, oxadiazole, pyrazole); R 1 and R 2 are independently H, F, Cl, Br, I, OH, SH, and CF 3, substituted or unsubstituted C 1 -C 5 Alkyl, C 1 -C 5 Linear or branched chain or C 3 -C 8 or substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 is a cyclic alkoxy; Or, R 1 and R 2 are bonded together to form C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); Or, R 2 and R 4 are joined together to form a F ring as defined above (e.g., pyrrolidine, pyridine, pyrimidine, triazole, oxadiazole, pyrazole); However, when ring F is aromatic, R 1 and / or R 3 does not exist; R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R 8 -OR 10 (For example, (CH 2 ) 2 -O-CH 3 ), R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -NH(CH 3 )), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2, NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 3 -4-fluoropiperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0090] [ka]

[0091] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 ´ are, independently of each other, H, F, Cl, Br, I, OH, OR 20, S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O. 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 20 is represented by the following structural formula:

[0092] [ka]

[0093] R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 2 -CH 2 -O-CH 3 , C.H. 2 -O-CH 2 -CH 2 -O-CH 3 ), C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 Straight or branched chain haloalkyl (e.g., CHF 2 , C.F. 3 , C.F.2 CH 3 , C.H. 2 CF 3 , C.F. 2 CH 2 CH 3 , C.H. 2 CH 2 CF 3 , C.F. 2 CH(CH 3 ) 2 , CF(CH 3 )-CH(CH 3 ) 2 ), R 8 -aryl (e.g., CH 2 -Ph), -R 8 -OR 8 -OR 10 (For example, (CH 2 ) 2 -O-(CH 2 ) 2 -O-CH 3 ), -R 8 -OR 10 , -R 8 -R 10 (For example, (CH 2 ) 2 -O-CH 3 ), substituted or unsubstituted aryl (e.g., phenyl), or substituted or unsubstituted heteroaryl (e.g., pyridine (2,3,4-pyridine)); R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 2 -CH 2 -O-CH 3 , C.H. 2 -O-CH 2 -CH 2-O-CH 3 ), C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 Straight or branched chain haloalkyl (e.g., CHF 2 , C.F. 3 , C.F. 2 CH 3 , C.H. 2 CF 3 , C.F. 2 CH 2 CH 3 , C.H. 2 CH 2 CF 3 , C.F. 2 CH(CH 3 ) 2 , CF(CH 3 )-CH(CH 3 ) 2 ), R 8 -aryl (e.g., CH 2 -Ph), -R 8 -OR 8 -OR 10 (For example, (CH 2 ) 2 -O-(CH 2 ) 2 -O-CH 3 ), -R 8 -OR 10 , -R 8 -R 10 (For example, (CH 2 ) 2 -O-CH 3 ), substituted or unsubstituted aryl (e.g., phenyl), or substituted or unsubstituted heteroaryl (e.g., pyridine (2,3,4-pyridine)); Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, CH 2 CF 3 , C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0094] In various embodiments, the present invention relates to a compound represented by the following structural formula (II): or a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, pharmaceutical, or any combination thereof:

[0095] [ka]

[0096] During the ceremony, X 2 , X 3 , and X 4 are, independently of each other, a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are, independently of each other, a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 5 is H or C 1 -C 5 is a straight or branched chain alkyl (e.g., methyl); R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 3 ) 2 -O-CH(CH 3 ) 2 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) (e.g., CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle) (e.g., (CH 2 )3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CCH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 )), R 9 -R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -C(O)-piperidine), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -CH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3-C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 ) (Optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl) or substituted or unsubstituted benzyl; Or, R 6 and R 5 are linked together to form a substituted or unsubstituted 5- to 8-membered heterocycle (e.g., azepane, piperazine, 2-(piperazin-1-yl)acetamide); Or, R 6 is represented by the following structural formula B or structural formula Bi:

[0097] [ka]

[0098] During the ceremony, m is 0 or 1; R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 is; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 alkyl (e.g., ethyl, trifluoroethyl); Or, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 is; Or, R 12 and R 13 combine with each other to form the B ring; Or, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 is; or C1 and C3 are bonded together to form a ring D, and R 12 and R 13 are independent of each other and R 30 is; Or, R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 is; Or, R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine; C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, methylpiperidine); Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3-8 membered heterocycle (B: piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethylpyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine); Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutane, cyclohexane); R 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR (e.g., C(O)NH(CH 3 )), C(O)N(R 10 )(R 11 ) (e.g., C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), C(O)NH(CH 2 CH 2 OH)) and SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., methylimidazole, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8Cyclic alkoxy (e.g., methoxy, ethoxy) (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 4- to 7-membered heterocycles (e.g., morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, piperazine, piperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine), R 8 -(substituted or unsubstituted 3-8 membered monocyclic, fused or spirocyclic heterocycle), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 is represented by the following structural formula A:

[0099] [ka]

[0100] During the ceremony, X 1 is N or O; R 1 and R 2 are, independently of each other, H, F, or CF 3 is; Or, R 1 and R 2 are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 is; Or, R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); However, X 1 If is O, then R 4 does not exist; R 7 ´ is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 Cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OCH 2 Ph, COOH, C(O)H, -C(O)NH 2 , S.O.2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl (e.g., CHF 2 ), C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R 7 and R 7 ´ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring;

[0101] [ka]

[0102] R 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R 8 are independent of each other, [CH 2 ] p and p is 1 to 10; R 9 [CH] q , or [C] q and q is 2 to 10; R 10 and R 11 are, independently of each other, H, C 1 -C 5 Substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl (e.g., CH 2 CF 3 ), C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 Is R; Or, R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer of 0 to 4 (for example, 1, 2).

[0103] In some embodiments, X in formula I 2 is a nitrogen atom. 2 is CH.

[0104] In some embodiments, X in formula I 3 is a nitrogen atom. 3 is CH.

[0105] In some embodiments, X in formula I4 is a nitrogen atom. 4 is CH.

[0106] In some embodiments, X in formula I 5 is a nitrogen atom. 5 is a carbon atom.

[0107] In some embodiments, X in formula I 6 is a nitrogen atom. 6 is a carbon atom.

[0108] In some embodiments, X in formula I 7 is a nitrogen atom. 7 is a carbon atom.

[0109] In some embodiments, X in formula I 8 is a nitrogen atom. 8 is a carbon atom.

[0110] In some embodiments, X in formula I 9 is a nitrogen atom. 9 is a carbon atom.

[0111] In some embodiments, X in formula I 10 is a nitrogen atom. 10 is N. In other embodiments, X 10 is CH. In other embodiments, X 10 is C(R), where R is as defined below.

[0112] In some embodiments, X in structural formula I, II, and / or I(a)-I(h) 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , and X9 In some embodiments, at least one of X in Structural Formula I(d) is a nitrogen atom. 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , and X 9 In some embodiments, at least one of X in Structural Formula I(d) is a nitrogen atom. 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , X 9 , X 10 At least one of is a nitrogen atom.

[0113] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 5 is H. In other embodiments, R 5 is C 1 -C 5 In another embodiment, R 5 is methyl. In other embodiments, R 5 is methyl, ethyl, propyl, isopropyl, butyl, t-butyl, isobutyl, pentyl, and neopentyl, each of which represents a separate embodiment of the present invention.

[0114] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 5 and R 6 are bonded together to form a substituted or unsubstituted 5- to 8-membered heterocycle. In some embodiments, R 5 and R 6 are linked together to form a substituted 5-8 membered heterocycle. In some embodiments, R 5 and R 6are bonded together to form an unsubstituted 5-8 membered heterocycle. In some embodiments, the heterocycle is azepane, piperazine, or 2-(piperazin-1-yl)acetamide, each of which represents a separate embodiment of the present invention. In some embodiments, the heterocycle is F, Cl, Br, I, CF 3 , R 20 , C 1 -C 5 Straight or branched chain alkyl of C 1 -C 5 Straight or branched chain haloalkyl, OH, alkoxy, R 8 -OH (e.g., CH 2 -OH), OMe, Amide, C(O)N(R) 2 , C(O)N(R 10 )(R 11 ), R 8 -C(O)N(R 10 )(R 11 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 , NH(R 10 ), N(R 10 )(R 11 ), N(CH 3 ) 2 , N.H. 2 , C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3-8 membered heterocycles (e.g., saturated, unsaturated or aromatic monocyclic, fused or spirocyclic, pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention. In some embodiments, the heterocycle of formula I(e) is substituted with at least one substituent selected from unsubstituted CO 2 -R.

[0115] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 6is H. In other embodiments, R 6 are H, F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 , C.H. 2 -O-CH 3 , (CH 2 ) 2 -O-CH 3 (CH 2 ) 3 -O-CH 3 , (CH 2 ) 2 -O-CH(CH 3 ) 2 , R 8 -SR 10 , (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 , R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), CH 2 -Cyclopropyl, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -Cyclohexanol, R 8 -(substituted or unsubstituted 3- to 8-membered monocyclic, fused or spiro heterocyclic ring), (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Oxetane, CH2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3-Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane, CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 -CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2 ) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 )3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 ), R 8 -C(O)N(R 10 )(R 11 ), (CH 2 ) 2 -C(O)-piperidine, R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl, CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 )2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -OCH 2 -CH 2 -O-CH 3 , CH(CH 3 )C(O)N(CH 3 ) 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic alkoxymethoxy (optionally with at least one methylene group (CH 2) replaced with an oxygen atom), O-(CH 2 ) 2 -O-CH 3 , C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 Cycloalkyl, cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol, R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-di-one, azabicyclohexane), substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl (e.g., benzyl), or substituted or unsubstituted benzyl. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy, OMe, amide, C(O)N(R) 2 , C(O)-alkyl, C(O)-pyrrolidine, C(O)-piperidine, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), N(CH 3 ) 2 , N.H. 2 , C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3- to 8-membered heterocycles, pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole, halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention. In some embodiments, R 6 is H. In some embodiments, R 6 -R 8 -OR 10 In some embodiments, R 6 is CH 2 -O-CH 3 In some embodiments, R 6 is R 8 -SR 10 In some embodiments, R 6 is (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 In some embodiments, R 6 is R 8 -NHC(O)-R 10 In some embodiments, R 6 is (CH 2 ) 3 -NHC(O)-R 10 In some embodiments, R 6 is (CH 2 )-NHC(O)-R 10 In some embodiments, R 6 is R 8 -(substituted or unsubstituted C 3 -C 8 R 8 -(substituted or unsubstituted C 3 -C 8 Examples of cycloalkyl include, but are not limited to, CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2-Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2-Cyclopentanol and CH 2 -cyclohexanol, each of which represents a separate embodiment of the present invention. In some embodiments, R 6 is R 8 -(substituted or unsubstituted, saturated, unsaturated or aromatic, monocyclic, fused or spirocyclic, 3-8 membered heterocycle). In some embodiments, R 6 is R 8 -(substituted or unsubstituted saturated monocyclic 3- to 8-membered heterocycle). In some embodiments, R 6 is R 8 -(substituted or unsubstituted unsaturated monocyclic 3- to 8-membered heterocycle). In some embodiments, R 6 is R 8 -(substituted or unsubstituted aromatic 3- to 8-membered monocyclic ring). In some embodiments, R 6 is R 8 -(substituted or unsubstituted saturated fused 3- to 8-membered heterocycle). In some embodiments, R 6 is R 8 -(substituted or unsubstituted unsaturated fused 3- to 8-membered heterocycle). In some embodiments, R 6 is R 8 -(substituted or unsubstituted aromatic fused 3- to 8-membered heterocycle). In some embodiments, R 6 is R 8 -(substituted or unsubstituted fused 3- to 8-membered heterocycle). 8 -(substituted or unsubstituted saturated, Examples of saturated or aromatic monocyclic, fused or spiro-heterocyclic rings having 3 to 8 ring members include, but are not limited to, (CH 2 ) 3 - Piran, (CH 2 ) 2 -pyrazole, (CH 2 ) 2 -imidazole, CH 2 -Tetrahydrofuran, CH 2-Dioxane, CH 2 -Oxetane, CH 2 -Piperidine, CH 2 -Triazole, CH 2 -1-Oxa-8-azaspiro[4.5]decane, (CH 2 ) 3 -Diazabicyclo[2.2.1]heptane, CH 2 -Methyl-THF, CH 2 -Ethyl-piperidine, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -2-Oxo-methylpyrrolidine, CH 2 -Methyl-azetidine and CH 2 In some embodiments, R 6 NH 2 In some embodiments, R 6 is NHR. In some embodiments, R 6 is N(R) 2 In some embodiments, R 6 is NH(R 10 In some embodiments, R 6 is N(R 10 )(R 11 In some embodiments, R 6 is R 8 -N(R 10 )(R 11 In some embodiments, R 8 -N(R 10 )(R 11 Examples of ) include, but are not limited to, (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -N(CH(CH 3 ) 2 ) 2 , (CH 2) 3 -Piperidine, (CH 2 ) 4 -NH(CH 3 ), (CH 2 ) 3 -NH-CH 3 , (CH 2 ) 3 -NH-CH 2 CH 3 , (CH 2 ) 3 -N(CH 2 CH 3 ) 2 , (CH 2 ) 3 -NH 2 , and (CH 2 ) 3 -N(CH 2 CH 3 )(CH 2 CF 3 In some embodiments, R 6 is R 8 -C(O)N(R 10 )(R 11 ), e.g., (CH 2 ) 2 -C(O)-piperidine, and the like. In some embodiments, R 6 is C 1 -C 5 C is a straight or branched chain, substituted or unsubstituted alkyl. 1 -C 5 Examples of linear or branched substituted or unsubstituted alkyl are CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), CH(CH 3 )C(O)N(CH 3 ) 2 , benzyl, methyl, ethyl, and CH 2 -OCH 2 -CH 2 -O-CH 3 In some embodiments, R 6 is a substituted or unsubstituted C 3 -C 8 In some embodiments, substituted or unsubstituted C 3 -C 8 Examples of cycloalkyl include cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, and 2,3-dihydro-1H-indeno. 6 is R 8 -(substituted or unsubstituted C 3 -C 8 In some embodiments, R 6is a substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spiro 3-10 membered heterocycle. In some embodiments, the substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spiro 3 membered heterocycle is piperidine, azetidine, pyrrolidine, pyrrolidinone, quinuclidine, tetrahydropyran, azaspiro[3.3]heptane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-di-one, or azabicyclohexane. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is a substituted or unsubstituted R 8 -aryl, such as benzyl. In some embodiments, R 6 are F, Cl, Br, I, and CF 3 , R 20 , C 1 -C 5 Straight or branched chain alkyl of C 1 -C 5 Straight or branched chain haloalkyl, OH, alkoxy, R 8 -OH (e.g., CH 2 -OH), OMe, Amide, C(O)N(R) 2 , C(O)N(R 10 )(R 11 ), R 8 -C(O)N(R 10 )(R 11 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 , NH(R 10 ), N(R 10 )(R 11 ), N(CH 3 ) 2 , N.H. 2 , C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8cycloalkyl, cyclobutanol, substituted or unsubstituted 3- to 8-membered heterocycles (e.g., saturated, unsaturated or aromatic monocyclic, fused or spirocyclic pyrans, oxetanes, piperidines, pyrazoles, methyl-pyrazoles, triazoles, imidazoles), halophenyls, (benzyloxy)phenyls, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0116] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 6 and R 5 are joined together to form a substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spiro 5-8 membered heterocycle. In some embodiments, the substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spiro 5-8 membered heterocycle is azepane, piperazine, or 2-(piperazin-1-yl)acetamide. Each represents a separate embodiment of the present invention. In some embodiments, the ring is further selected from the group consisting of F, Cl, Br, I, C, and the like. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), CF 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2Each represents a separate embodiment of the present invention.

[0117] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 6 is represented by the following structural formula B.

[0118] [ka]

[0119] During the ceremony, m is 0 or 1; and R 12 is R 20 or C 1 -C 5 C(O)-alkyl, R 13 is R 30 or R 12 and R 13 are both H; or R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 or R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 or R 12 and R 13 are joined together to form a B ring; or R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 or C1 and C3 are bonded together to form a D ring, and R 12 and R 13 are independent of each other and R 30 or R 13and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 or R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C, and ring E are each independently a substituted or unsubstituted 3- to 8-membered monocyclic, spirocyclic, or fused heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; and The D ring is a substituted or unsubstituted C 3 -C 8 is a cycloalkyl group.

[0120] In some embodiments, structure B is represented by structure Bi.

[0121] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 6 is represented by the following structural formula Bi.

[0122] [ka]

[0123] During the ceremony, m is 0 or 1; and R 12 is R 20 or C 1 -C 5 C(O)-alkyl, R 13 is R 30 or R 12 and R 13 are both H; or R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5 or R12 and C3 are bonded to each other to form ring A, and R 13 is R 30 or R 12 and R 13 are joined together to form a B ring; or R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 or C1 and C3 are bonded together to form a D ring, and R 12 and R 13 are independent of each other and R 30 or R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 or R 12 and R 13 are joined together to form ring B, and C1 and C3 are joined together to form ring D; Ring A, ring C, and ring E are each independently a substituted or unsubstituted 3- to 8-membered monocyclic, spirocyclic, or fused heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; and The D ring is a substituted or unsubstituted C 3 -C 8 is a cycloalkyl group.

[0124] In some embodiments, R of structural formula B and / or Bi 12 is H. In some embodiments, R 12 is R 20 In another embodiment, R 12 is R 30 In some embodiments, R 12 is C 1 -C 5 In some embodiments, R 12 is a substituted or unsubstituted C 1 -C 5In some embodiments, R 12 is the unsubstituted C 1 -C 5 In some embodiments, the alkyl is ethyl. In some embodiments, R 12 is the replaced C 1 -C 5 In some embodiments, the alkyl is trifluoroethyl.

[0125] In some embodiments, R of structural formula B and / or Bi 13 is H. In other embodiments, R 13 is R 30 In some embodiments, R 13 is a substituted or unsubstituted C 1 -C 5 In some embodiments, R 13 is the unsubstituted C 1 -C 5 In some embodiments, the alkyl is ethyl. In some embodiments, R 13 is the replaced C 1 -C 5 In some embodiments, the alkyl is trifluoroethyl.

[0126] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 6 is represented by structural formula B. In some embodiments, R 12 is R 20 , or C 1 -C 5 and R 13 is R 30 In some embodiments, R of structural formula B is 12 and R 13 are both H. In some embodiments, R 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C 5In some embodiments, R of structural formula B is an alkyl (e.g., ethyl, trifluoroethyl). 12 and R 13 are each independently H or trifluoroethyl. In some embodiments, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 In some embodiments, R of structural formula B is 12 and R 13 are linked together to form ring B. In some embodiments, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 In some embodiments, C1 and C3 of formula B are linked together to form a D ring, and R of formula B is 12 and R 13 are independent of each other and R 30 In some embodiments, R of structural formula B is 13 and C2 are bonded to each other to form an E ring, m is 1, and R in structural formula B 12 is R 30 In some embodiments, R of structural formula B is 12 and R 13 are bonded to each other to form ring B, and C1 and C3 of structural formula B are bonded to each other to form ring D.

[0127] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 6 is represented by structural formula Bi. In some embodiments, R of structural formula Bi is 12 is R 20 , or C 1 -C 5 and R 13 is R 30 In some embodiments, R of formula Bi is 12 and R 13 are both H. In some embodiments, R of structural formula Bi 12 and R 13 are each independently H or substituted or unsubstituted C 1 -C5 In some embodiments, R of structural formula Bi is an alkyl (e.g., ethyl, trifluoroethyl). 12 and R 13 are each independently H or trifluoroethyl. In some embodiments, R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 In some embodiments, R of formula Bi is 12 and R 13 are bonded together to form ring B. In some embodiments, R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 In some embodiments, C1 and C3 of formula Bi are bonded together to form a D ring, and R of formula Bi is 12 and R 13 are independent of each other and R 30 In some embodiments, R of formula Bi is 13 and C2 are bonded to each other to form an E ring, m is 1, and R of the structural formula Bi 12 is R 30 In some embodiments, R of formula Bi is 12 and R 13 are bonded to each other to form a B ring, and C1 and C3 of structural formula Bi are bonded to each other to form a D ring.

[0128] In some embodiments, R of structural formula I(g) 6 is represented by the following structural formula C.

[0129] [ka]

[0130] During the ceremony, k is an integer from 1 to 4; R 12 and R 13 are independent of each other, H, C 1 -C 5or R 20 or R 12 and R 13 are bonded to each other to form a substituted or unsubstituted 4- to 7-membered heterocycle (e.g., piperidine, piperazine, pyrrolidine, oxa-6-azaspiro[3.3]heptane).

[0131] In some embodiments, k in Structural Formula C is 1. In some embodiments, k is 2. In some embodiments, k is 3. In some embodiments, k is 4.

[0132] In some embodiments, R of structural formula C 12 and R 13 are independent of each other, H, C 1 -C 5 or R 20 Each represents a separate embodiment of the present invention. In some embodiments, R of structural formula C is 12 and R 13 In some embodiments, R in Structural Formula C is 12 and R 13 In some embodiments, R in Structural Formula C is 12 and R 13 Both are alkyl.

[0133] In some embodiments, R of structural formula C 12 and R 13 are bonded together to form a substituted or unsubstituted 4- to 7-membered heterocycle. In some embodiments, R 12 and R 13are linked together to form piperidine, piperazine, pyrrolidine, or oxa-6-azaspiro[3.3]heptane. Each represents a separate embodiment of the present invention. In some embodiments, the heterocycle may be further substituted with at least one substituent as defined herein for heterocycles.

[0134] In some embodiments, R of structural formula I(b) 6 is represented by the structural formula Bi and / or B, R in structural formula Bi and / or B 12 is R 20 , or C 1 -C 5 and R of the structural formula Bi and / or B. 13 is R 30 or R 12 and R 13 are both H, or R 12 and R 13 are, independently of each other, H or trifluoroethyl; or R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 or R 12 and R 13 are joined together to form a substituted or unsubstituted pyrrolidine ring, piperazine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, pyrazole, imidazole, 2,5-diazabicyclo[2.2.1]heptane, or diazabicyclo[2.2.1]heptane; or R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 or C1 and C3 are bonded together to form a D ring, and R 12 and R 13 are independent of each other and R 30 or R 13and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 or R 12 and R 13 are bonded together to form a B ring, and C1 and C3 are bonded together to form a D ring.

[0135] In some embodiments, R of structural formula I(b) 6 is represented by the structural formula Bi and / or B, R in structural formula Bi and / or B 12 is R 20 , or C 1 -C 5 and R of the structural formula Bi and / or B. 13 is R 30 or R 12 and C3 are bonded to each other to form ring A, and R 13 is R 30 or R 12 and R 13 are joined together to form a substituted or unsubstituted pyrrolidine ring, piperazine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, pyrazole, imidazole, 2,5-diazabicyclo[2.2.1]heptane, or diazabicyclo[2.2.1]heptane; or R 12 and C1 are bonded to each other to form a C ring, and R 13 is R 30 or C1 and C3 are bonded together to form a D ring, and R 12 and R 13 are independent of each other and R 30 or R 13 and C2 are bonded together to form an E ring, m is 1, and R 12 is R 30 or R 12 and R 13are bonded together to form a B ring, and C1 and C3 are bonded together to form a D ring.

[0136] In some embodiments, the A ring of structural formula Bi is a substituted or unsubstituted monocyclic, spiro or fused 3- to 8-membered heterocycle. In some embodiments, the A ring is an unsubstituted monocyclic 3- to 8-membered heterocycle. In some embodiments, the A ring is an unsubstituted spiro 3- to 8-membered heterocycle. In some embodiments, the A ring is an unsubstituted fused 3- to 8-membered heterocycle. In some embodiments, the A ring is a substituted monocyclic 3- to 8-membered heterocycle. In some embodiments, the A ring is a substituted spiro 3- to 8-membered heterocycle. In some embodiments, the A ring is a substituted fused 3- to 8-membered heterocycle. In some embodiments, the A ring is pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, piperidine, methylpiperidine, methyl-2-oxopyrrolidine, pyran-azetidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane. Each represents a separate embodiment of the present invention. In some embodiments, the A ring is pyrrolidine, methylpyrrolidine, or ethylpyrrolidine. Each represents a separate embodiment of the present invention.

[0137] In some embodiments, the B ring of structural formula Bi is a substituted or unsubstituted monocyclic, spiro or fused 3-8 membered heterocycle. In some embodiments, the B ring is an unsubstituted monocyclic 3-8 membered heterocycle. In some embodiments, the B ring is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, the B ring is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, the B ring is a substituted monocyclic 3-8 membered heterocycle. In some embodiments, the B ring is a substituted spiro 3-8 membered heterocycle. In some embodiments, the B ring is a substituted fused 3-8 membered heterocycle. In some embodiments, the B ring is pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, hydroxymethyl-pyrrolidinepiperidine, methylpiperidine, fluoropiperidine, difluoropiperidine, piperazine, methyl-piperazine, dimethyl-pyrazole, methyl-2-oxopyrrolidine, pyran-, azetidine, methyl-azetidine, imidazole, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane, diazabicyclo[2.2.1]heptane, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, thiomorpholine, or 1,1-dioxido-2-oxa-6-azaspiro[3.3]heptane, each of which represents a separate embodiment of the present invention. In some embodiments, the B ring is piperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, 1,1-dioxido-2-oxa-6-azaspiro[3.3]heptane, hydroxymethyl-pyrrolidine, or diazabicyclo[2.2.1]heptane, each of which represents a separate embodiment of the present invention.

[0138] In some embodiments, the C ring of structural formula Bi is a substituted or unsubstituted monocyclic, spiro or fused 3-8 membered heterocycle. In some embodiments, the C ring is an unsubstituted monocyclic 3-8 membered heterocycle. In some embodiments, the C ring is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, the C ring is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, the C ring is a substituted monocyclic 3-8 membered heterocycle. In some embodiments, the C ring is a substituted spiro 3-8 membered heterocycle. In some embodiments, the C ring is a substituted fused 3-8 membered heterocycle. In some embodiments, the C ring is pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, piperidine, methylpiperidine, methyl-2-oxopyrrolidine, pyran-azetidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane. Each represents a separate embodiment of the present invention. In some embodiments, the C ring is piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane. Each represents a separate embodiment of the present invention.

[0139] In some embodiments, the D ring of formula Bi is a substituted or unsubstituted C 3 -C 8 In some embodiments, the D ring is a cycloalkyl of the formula: 3 -C 8 In some embodiments, the D ring is an unsubstituted C 3 -C 8 In some embodiments, the D ring is cyclopropane, cyclobutene, cyclopentane, cyclohexane, or cycloheptane. Each represents a separate embodiment of the present invention.

[0140] In some embodiments, the E ring of structural formula Bi is a substituted or unsubstituted monocyclic, spiro or fused 3-8 membered heterocycle. In some embodiments, the E ring is an unsubstituted monocyclic 3-8 membered heterocycle. In some embodiments, the E ring is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, the E ring is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, the E ring is a substituted monocyclic 3-8 membered heterocycle. In some embodiments, the E ring is a substituted spiro 3-8 membered heterocycle. In some embodiments, the E ring is a substituted fused 3-8 membered heterocycle. In some embodiments, the E ring is pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, piperidine, methylpiperidine, methyl-2-oxopyrrolidine, pyran-azetidine, methyl-azetidine, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane. Each represents a separate embodiment of the present invention. In some embodiments, the E ring is pyrrolidine, azetidine, ethylpyrrolidine, oxopyrrolidine, or methylpiperidine. Each represents a separate embodiment of the present invention.

[0141] In some embodiments, R of structural formula I(b) 6 are F, Cl, Br, I, OH, SH, and R. 8 -OH, R 8 -SH, -R 8 -OR 10 (For example, 2 -O-CH 3 ), R 8 -SR 10 (For example, (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 ), R 8 -NHC(O)-R 10 , -OR 8 -R 10 , R 8 - (e.g., CH 2 -Cyclobutanol, CH 2-Difluorocyclopropyl, CH 2 -Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -cyclohexanol), (CH 2 ) 3 -Piran, C.H. 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Methyl-THF, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -Methyl-azetidine, CH 2 -Azaspiroheptane, CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 -CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10)(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl (e.g., CH(CH 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH 3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), benzyl, methyl, ethyl, CH 2 -OCH 2 -CH 2 -O-CH 3 ), C 1 -C5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy (e.g., methoxy, O-(CH 2 ) 2 -O-CH 3 Optionally, at least one methylene group (CH 2 ) replaced with an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indenol), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, 1-methylazepan-2-one, 3-azabicyclo[3.1.0]hexane), substituted or unsubstituted aryl, or substituted or unsubstituted benzyl. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-alkyl, C(O)-pyrrolidine, C(O)-piperidine, N(R) 2 (For example, N(CH 3 ) 2 , N.H. 2 ), NH(R10 ), N(R 10 )(R 11 ), C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0142] In some embodiments, R of structural formula I(b) 6 -R 8 -OR 10 In some embodiments, -R 8 -OR 10 is CH 2 -O-CH 3 In some embodiments, R 6 is R 8 -SR 10 In some embodiments, R 8 -SR 10 is (CH 2 ) 3 -S-(CH 2 ) 2 CH 3 In some embodiments, R 6 is R 8 -NHC(O)-R 10 In some embodiments, R 6 is R 8 -(substituted or unsubstituted C 3 -C 8 In some embodiments, R 8 -(substituted or unsubstituted C 3 -C 8 Cycloalkyl) is CH 2 -Cyclobutanol, CH 2 -Difluorocyclopropyl, CH 2-Methylcyclopropyl, CH 2 -Dimethylamino-cyclohexyl, (CH 2 ) 2 -Cyclopentanol, CH 2 -Cyclohexanol, (CH 2 ) 3 -Piran, C.H. 2 -Tetrahydrofuran, CH 2 -Dioxane, CH 2 -Methyl-THF, CH 2 -Tetrahydrofuran, CH 2 -Oxa-azaspirodecane, CH 2 -Azaspiroheptane, (CH 2 ) 3 -Dimethylpyrazole, CH 2 -Methyl-azetidine, or CH 2 -azaspiroheptane. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is C 1 -C 5 In some embodiments, R 6 is C 1 -C 5 In some embodiments, the substituted alkyl is a straight or branched chain substituted alkyl of the formula: 3 )CH 2 OCH 3 , CH(CH 3 )CH 2 NH 2 , CH(CH 3 )C(O)N(CH 3 ) 2 , C.H. 2 -CH(OH)Ph, (CH 2 ) 3 N(H)CH 2 CH 3 , CH(CH 3 )(CH 2 ) 2 OH, CH(CH 2 OH)(CH 2 CH 3 ), (CH 2 ) 3 -OCH3 , (CH 2 ) 2 -OCH 3 , (CH 2 ) 2 -OCH(CH 3 ) 2 , CH(CH 2 OH)(CH 2 CH(CH 3 ) 2 ), C.H. 2 CH(CH 3 )(OCH 3 ), C.H. 2 CH(N(CH 3 ) 2 )(CH 2 CH 3 ), C.H. 2 -OCH 2 -CH 2 -O-CH 3 or benzyl, each of which represents a separate embodiment of the present invention. In some embodiments, R 6 is C 1 -C 5 In some embodiments, the unsubstituted alkyl is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, or neopentyl. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is a substituted or unsubstituted C 3 -C 8 In some embodiments, R 6 is the replaced C 3 -C 8 In some embodiments, the substituted cycloalkyl is methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, or 2,3-dihydro-1H-indenol. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is the unsubstituted C 3 -C 8In some embodiments, unsubstituted cycloalkyl is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl. Each represents a separate embodiment of the present invention. In some embodiments, R 6 is a substituted or unsubstituted 3-8 membered heterocycle. In some embodiments, the substituted heterocycle is trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, 1-methylazepan-2-one, or 3-azabicyclo[3.1.0]hexane. Each represents a separate embodiment of the present invention.

[0143] In some embodiments, R of structural formulas I, II, and / or I(a)-I(f) 7 is H, F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, SR 10 , -R 8 -OR 10 , -R 8 -SR 10 , R 8 -(C 3 -C 8 cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 -CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10, NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl, C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic alkoxy (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched thioalkyl of C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8cycloalkyl, substituted or unsubstituted 4-6 membered heterocycle, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl. Each represents a separate embodiment of the present invention. In some embodiments, R 7 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-alkyl, C(O)-pyrrolidine, C(O)-piperidine, N(R) 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), CF 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0144] In some embodiments, R of structural formula I, II, I(b), and / or I(d)-I(f) is 7 is H. In some embodiments, R 7 is F. In some embodiments, R 7 is Cl. In some embodiments, R 7 is Br. In some embodiments, R 7 is I. In some embodiments, R 7 is OH. In some embodiments, R 7 OR 20 In some embodiments, R 7 CF 3In some embodiments, R 7 is CN. In some embodiments, R 7 NH 2 In some embodiments, R 7 is NHR. In some embodiments, R 7 is N(R) 2 In some embodiments, R 7 is NH(R 10 In some embodiments, R 7 is N(R 10 )(R 11 In some embodiments, R 7 is NHC(O)-R 10 In some embodiments, R 7 is COOH. In some embodiments, R 7 is -C(O)Ph. In some embodiments, R 7 is C(O)OR 10 In some embodiments, R 7 is C(O)H. In some embodiments, R 7 is C(O)-R 10 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is -C(O)NH 2 In some embodiments, R 7 is C(O)NHR. In some embodiments, C(O)NHR is C(O)NH(CH 3 In some embodiments, R 7 is C(O)N(R 10 )(R 11 In some embodiments, C(O)N(R 10 )(R 11 ) is C(O)NH(CH 3 ), C(O)NH(CH 2 CH 2 OCH 3 ), or C(O)NH(CH 2 CH2 Each represents a separate embodiment of the present invention. In some embodiments, R 7 SO 2 R. In some embodiments, R 7 is C 1 -C 5 In some embodiments, alkyl is methylimidazole, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, neopentyl, or hexyl. Each represents a separate embodiment of the present invention. In some embodiments, R 7 is C 1 -C 5 Linear or branched chain or C 3 -C 8 In some embodiments, R 7 is C 1 -C 5 In some embodiments, the haloalkyl is a straight chain haloalkyl of CHF 2 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is C 3 -C 8 In some embodiments, R 7 is C 1 -C 5 Linear or branched chain or C 3 -C 8 and optionally, at least one methylene group (CH 2 ) is replaced with an oxygen atom. In some embodiments, R 7 is C 1 -C 5 In some embodiments, the alkoxy is a straight chain alkoxy of the formula: In some embodiments, the alkoxy is a methoxy. In some embodiments, the alkoxy is an ethoxy. In some embodiments, R 7 is C 1 -C 5In some embodiments, R 7 is C 3 -C 8 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is C 1 -C 5 In some embodiments, R 7 is a substituted or unsubstituted C 3 -C 8 In some embodiments, cycloalkyl is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl, each of which represents a separate embodiment of the present invention. In some embodiments, R 7 is a substituted or unsubstituted 4- to 7-membered heterocycle. In some embodiments, R 7 is an unsubstituted 4- to 7-membered heterocycle. In some embodiments, R 7 is a substituted 4-7 membered heterocycle. In some embodiments, the heterocycle is morpholine, tetrahydropyran, oxetane, pyrrolidine, pyrrolidinone, imidazole, pyrazole, piperazine, piperidine, oxadiazole, triazole, or 2-oxopyrrolidine. Each represents a separate embodiment of the present invention. In some embodiments, R 7 is R 8-(substituted or unsubstituted 3-8 membered monocyclic, fused or spiro heterocyclic ring). In some embodiments, R 7 is R 8 -(unsubstituted monocyclic 3- to 8-membered heterocycle). In some embodiments, R 7 is R 8 -(unsubstituted fused 3- to 8-membered heterocycle). In some embodiments, R 7 is R 8 -(unsubstituted spirocyclic 3-8 membered heterocycle). In some embodiments, R 7 is R 8 -(substituted monocyclic 3-8 membered heterocycle). In some embodiments, R 7 is R 8 -(substituted fused 3- to 8-membered heterocycle). In some embodiments, R 7 is R 8 -(substituted spirocyclic 3-8 membered heterocycle). In some embodiments, the heterocycle may be saturated. In some embodiments, the heterocycle may be unsaturated. In some embodiments, the heterocycle may be aromatic. In some embodiments, R 7 is substituted or unsubstituted aryl. In some embodiments, R 7 is phenyl. In some embodiments, R 7 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0145] In some embodiments, R of structural formula I(a) 7 OR 20 In some embodiments, R 7 is a substituted or unsubstituted 4- to 7-membered heterocycle. In some embodiments, R 7 is an unsubstituted 4- to 7-membered heterocycle. In some embodiments, R 7 is a substituted 4-7 membered heterocycle. In some embodiments, the heterocycle is morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, triazole, or 2-oxopyrrolidine. Each represents a separate embodiment of the present invention. In some embodiments, R 7 is substituted or unsubstituted aryl. In some embodiments, R 7 is phenyl. In some embodiments, R 7 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), CF 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0146] In some embodiments, R of structural formula I(c) 7 are H, F, Cl, and C. 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy, C 1 -C 5 or a straight or branched chain haloalkoxy of C 1 -C 5 It is not a straight or branched chain, substituted or unsubstituted alkyl.

[0147] In some embodiments, R of structural formulas I, II, and / or I(a)-I(f) 7 is represented by the following structural formula A.

[0148] [ka]

[0149] During the ceremony, X1 is N or O; R 1 and R 2 are independently H, F, or CF 3 or R 1 and R 2 are bonded together to form =O or C 3 -C 8 forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1-C 5 alkyl (e.g., methoxyethyl, methylaminoethyl, aminoethyl), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 6-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R 20 or R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, piperazine); However, X 1 If is O, then R 4 does not exist;

[0150] In some embodiments, X in formula A 1 is N. In other embodiments, X 1 is O.

[0151] In some embodiments, R of structural formula A 1 is H. In other embodiments, R 1 is F. In other embodiments, R 1 CF 3 It is.

[0152] In some embodiments, R of structural formula A 2 is H. In other embodiments, R 2 is F. In other embodiments, R 2 CF 3 It is.

[0153] In some embodiments, R of structural formula A 1 and R 2 are joined together to form =O. In another embodiment, R 1 and R 2 are bonded together to form C 3 -C 8 In another embodiment, R 1 and R 2are bonded together to form C 3 -C 8 In some embodiments, the carbocycle is cyclopropyl. In other embodiments, R 1 and R 2 are bonded to each other to form a 3- to 8-membered heterocycle.

[0154] In some embodiments, R of Structural Formula A in Structural Formula I(a) 1 and R 2 do not bond with each other to form =O.

[0155] In some embodiments, R of structural formula A 3 is H. In some embodiments, R 3 is methyl. In some embodiments, R 3 is a substituted or unsubstituted C 1 -C 5 In some embodiments, alkyl is methoxyethylene, methylaminoethylene, or aminoethylene. Each represents a separate embodiment of the present invention. In some embodiments, R 3 is a substituted or unsubstituted C 3 -C 8 In some embodiments, the cycloalkyl is cyclopropyl. In some embodiments, R 3 is a substituted or unsubstituted 5- to 7-membered heterocycle. In some embodiments, the heterocycle is pyrrolidine, methylpyrrolidine, or piperidine. Each represents a separate embodiment of the present invention. In some embodiments, R 3 is R defined as follows: 20 It is.

[0156] In some embodiments, R of structural formula A 4 is H. In some embodiments, R 4 is methyl. In some embodiments, R 4 is a substituted or unsubstituted C 1 -C 5In some embodiments, alkyl is methoxyethylene, methylaminoethylene, or aminoethylene. Each represents a separate embodiment of the present invention. In some embodiments, R 4 is a substituted or unsubstituted C 3 -C 8 In some embodiments, the cycloalkyl is cyclopropyl. In some embodiments, R 4 is a substituted or unsubstituted 5- to 7-membered heterocycle. In some embodiments, the heterocycle is pyrrolidine, methylpyrrolidine, or piperidine. Each represents a separate embodiment of the present invention. In some embodiments, R 4 is R as defined herein below 20 It is.

[0157] In some embodiments, R of structural formula A 3 and R 4 are linked together to form a 3-8 membered heterocycle. In some embodiments, the heterocycle is imidazole, pyrrolidine, 2-oxopyrrolidine, piperidine, morpholine, or piperazine. Each represents a separate embodiment of the present invention.

[0158] In some embodiments, X in formula A 1 If is O, then R 4 does not exist.

[0159] In some embodiments, R of structural formula I(a) 7 OR 20 , a substituted or unsubstituted 4-7 membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, triazole, 2-oxopyrrolidine), or a substituted or unsubstituted aryl. 7 is represented by structural formula A, where X 1 , R 1 , R 2 , R 3 and R 4is R 1 and R 2 are as defined above except that they cannot be combined with each other to form =O.

[0160] In some embodiments, R of structural formula I(c) 7 ´ is not H.

[0161] In some embodiments, R of structural formula I, II, I(a)-I(b), and / or I(d)-I(h) is 7 In some embodiments, R′ in structural formula I, II, and / or I(a)-I(h) is H. 7 ´ is F, Cl, Br, I, OH, OR 20 , S.H., R. 8 -OH, R 8 -SH, -R 8 -OR 10 , R 8 -(C 3 -C 8 cycloalkyl), R 8 -(3-8 membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 -CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)OR 10 , R 8 -C(O)-R 10, C(O)H, C(O)-R 10 , C 1 -C 5 Straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Straight or branched chain substituted or unsubstituted alkenyl of C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic haloalkyl, C 1 -C 5 Linear or branched chain or C 3 -C 8 cyclic alkoxy (optionally with at least one methylene group (CH 2 ) is replaced by an oxygen atom), C 1 -C 5 Straight or branched chain thioalkoxy of C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 Linear or branched alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, substituted or unsubstituted 3-8 membered heterocycle, substituted or unsubstituted aryl, and substituted or unsubstituted benzyl. Each represents a separate embodiment of the present invention. In some embodiments, R 7 ´Furthermore, F, Cl, Br, I, C 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), CF 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0162] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 7 In some embodiments, R 7 In some embodiments, R 7 In some embodiments, R 7 In some embodiments, R 7 In some embodiments, R 7 ´CF 3 In some embodiments, R 7 ´ is C 1 -C 5 In some embodiments, R 7 ´ is C 1 -C 5 In some embodiments, alkyl is isopropyl, methyl, or ethyl. Each represents a separate embodiment of the present invention. In some embodiments, R 7 ´ is C 1 -C 5In some embodiments, R 7 ´ is C 1 -C 5 Linear or branched chain or C 3 -C 8 In some embodiments, R 7 ´ is C 1 -C 5 In some embodiments, the haloalkyl is a straight or branched chain haloalkyl of CHF 2 In some embodiments, R 7 ´ is C 3 -C 8 In some embodiments, R 7 ´ is a substituted or unsubstituted C 3 -C 8 In some embodiments, the cycloalkyl is cyclopropyl.

[0163] In some embodiments, R of structural formulas I, II, and / or I(a)-I(f) 7 and R 7 and R′ are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring. 7 and R 7 In some embodiments, R 7 and R 7 In some embodiments, R 7 and R 7 In some embodiments, R 7 and R 7 In some embodiments, R 7 and R 7In some embodiments, R 7 and R 7 In some embodiments, R 7 and R 7 ' are joined together to form a 5- or 6-membered substituted or unsubstituted heterocyclic ring.

[0164] In some embodiments, R of structural formula I(c) 7 and R 7 In some embodiments, R 7 and R 7 ´ is H, F, Cl, C 1 -C 5 Linear or branched chain or C 3 -C 8 Cyclic alkoxy, C 1 -C 5 or a straight or branched chain haloalkoxy of C 1 -C 5 and n is an integer from 1 to 6. Each represents a separate embodiment of the present invention.

[0165] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 30 , H, R 20 , F, Cl, Br, I, OH, SH, OH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 Straight or branched chain substituted or unsubstituted alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8-OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. Each represents a separate embodiment of the present invention. In some embodiments, R 30 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention. In some embodiments, R 30 is H. In some embodiments, R 30 is R 20 It is.

[0166] In some embodiments, R in structural formulas I, II, and / or I(a)-I(h) is H, F, Cl, Br, I, OH, SH, OH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), C.F. 3 , CN, NO 2 , C 1 -C 5Straight or branched chain alkyl of C 1 -C 5 Linear or branched alkoxy of C 1 -C 5 R 8 -aryl, -R 8 -OR 8 -OR 10 , -R 8 -OR 10 , -R 8 -R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, each of which represents a separate embodiment of the present invention. In some embodiments, R is further selected from the group consisting of F, Cl, Br, I, C, 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention. In some embodiments, R is H.

[0167] In various embodiments, each R of the compounds of structural formulas I, II, and / or I(a)-I(h) 8 are independent of each other, CH 2In some embodiments, R 8 is CH 2 CH 2 In some embodiments, R 8 is CH 2 CH 2 CH 2 In some embodiments, R 8 is CH 2 CH 2 CH 2 CH 2 It is.

[0168] In some embodiments, p in Structural Formulae I, II, and / or I(a)-I(h) is 1. In other embodiments, p is 2. In other embodiments, p is 3. In some embodiments, p is 4. In some embodiments, p is 5. In some embodiments, p is 1-3. In some embodiments, p is 1-5. In some embodiments, p is 1-10.

[0169] In some embodiments, R9 in structural formulas I, II, and / or I(a)-I(h) is C≡C. In some embodiments, R 9 is C≡CC≡C. In some embodiments, R 9 is CH=CH. In some embodiments, R 9 is CH=CH-CH=CH.

[0170] In some embodiments, q in Structural Formulas I, II, and / or I(a)-I(h) is 2. In some embodiments, q is 4. In some embodiments, q is 6. In some embodiments, q is 8. In some embodiments, q is 2-6.

[0171] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 10 , H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl), CH2 -CH 2 -O-CH 3 , C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, CH 2 CF 3 , C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), R 20 , C(O)R, or S(O) 2 R. Each represents a separate embodiment of the present invention. In some embodiments, R 10 is H. In some embodiments, R 10 is C 1 -C 5 In some embodiments, R 10 is C 1 -C 5 In another embodiment, R 10 is CH 3 In another embodiment, R 10 is CH 2 CH 3 In another embodiment, R 10 is CH 2 CH 2 CH 3 In some embodiments, R 10 is isopropyl. In some embodiments, R 10 is butyl. In some embodiments, R 10 , isobutyl. In some embodiments, R 10 , t-butyl. In some embodiments, R 10 , pentyl. In some embodiments, R 10 , isopentyl. In some embodiments, R 10 , neopentyl. In some embodiments, R 10 , benzyl. In some embodiments, R 10 , C 1 -C 5In another embodiment, R 10 , C.H. 2 -CH 2 -O-CH 3 In another embodiment, R 10 , C.H. 2 CF 3 In another embodiment, R 10 , C 1 -C 5 In another embodiment, R 10 , C 1 -C 5 In another embodiment, R 10 , O-CH 3 In another embodiment, R 10 , R 20 In another embodiment, R 10 , C(O)R. In other embodiments, R 10 , S(O) 2 R. In some embodiments, R 10 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), CF 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2Each represents a separate embodiment of the present invention.

[0172] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 11 , H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl), CH 2 -CH 2 -O-CH 3 , C.H. 2 CF 3 , C 1 -C 5 Straight or branched chain alkoxy (e.g., O-CH 3 ), C(O)R, or S(O) 2 R. Each represents a separate embodiment of the present invention. In some embodiments, R 11 is H. In some embodiments, R 11 is C 1 -C 5 In some embodiments, R 11 is C 1 -C 5 In another embodiment, R 11 is CH 3 In another embodiment, R 11 is CH 2 CH 3 In another embodiment, R 11 is CH 2 CH 2 CH 3 In some embodiments, R 11 is isopropyl. In some embodiments, R 11 is butyl. In some embodiments, R 11 is isobutyl. In some embodiments, R 11 is t-butyl. In some embodiments, R 11 is pentyl. In some embodiments, R 11is isopentyl. In some embodiments, R 11 is neopentyl. In some embodiments, R 11 is benzyl. In some embodiments, R 11 is C 1 -C 5 In another embodiment, R 11 is CH 2 -CH 2 -O-CH 3 In another embodiment, R 11 is CH 2 CF 3 In another embodiment, R 11 is C 1 -C 5 In another embodiment, R 11 is C 1 -C 5 In another embodiment, R 11 is O-CH 3 In another embodiment, R 11 is R 20 In another embodiment, R 11 is C(O)R. In other embodiments, R 11 is S(O) 2 R. In some embodiments, R 11 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), CF 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0173] In some embodiments, R of structural formula I, II, and / or I(a)-I(h) 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle. 10 and R 11 are linked together to form a piperazine ring. 10 and R 11 They are linked together to form a piperidine ring. In some embodiments, the substituents include F, Cl, Br, I, C 1 -C 5 Straight or branched chain alkyl, OH, alkoxy, OMe, amide, C(O)N(R) 2 , C(O)-pyrrolidine, C(O)-piperidine, N(R 2 , NH(R 10 ), N(R 10 )(R 11 ), N(CH 3 ) 2 , N.H. 2 , C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3- to 8-membered heterocycles, pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole, halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0174] In some embodiments, n in structural formula I, II, I(a)-I(b), and / or I(d)-I(h) is an integer from 0 to 4. In some embodiments, n in structural formula I(c) is an integer from 1 to 4. In some embodiments, n in structural formula I, II, I(a)-I(b), and / or I(d)-I(h) is 0. In some embodiments, n in structural formula I, II, and / or I(a)-I(h) is 1. In some embodiments, n in structural formula I, II, and / or I(a)-I(h) is 2. In some embodiments, n in structural formula I, II, and / or I(a)-I(h) is 3. In some embodiments, n in structural formula I, II, and / or I(a)-I(h) is 4. In some embodiments, n in structural formula I, II, and / or I(a)-I(h) is 1 or 2.

[0175] In some embodiments, A' in structural formula I(f) is a 3-8 membered monocyclic or fused ring saturated, unsaturated, or aromatic heterocycle. In some embodiments, A' is a 3-8 membered monocyclic heterocycle. In some embodiments, A' is a fused ring heterocycle with 4-10 rings. In some embodiments, A' is a monocyclic aromatic 3-8 membered heterocycle. In some embodiments, A' is a fused ring aromatic 3-10 membered heterocycle. In some embodiments, A' is piperidine. In some embodiments, A' is piperazine. In some embodiments, A' is morpholine. In some embodiments, A' is pyridinyl. In other embodiments, A' is 2-pyridinyl. In other embodiments, A' is 3-pyridinyl. In other embodiments, A' is 4-pyridinyl. In other embodiments, A' is pyrimidine. In other embodiments, A' is pyridazine. In another embodiment, A' is pyrazine. In another embodiment, A' is pyrazole. In another embodiment, A' is benzothiazolyl. In another embodiment, A' is benzimidazolyl. In another embodiment, A' is quinolinyl. In another embodiment, A' is isoquinolinyl. In another embodiment, A' is indolyl. In another embodiment, A' is indenyl. In another embodiment, A' is benzofuran-2(3H)-one. In another embodiment, A' is benzo[d][1,3]dioxole. In another embodiment, A' is tetrahydrothiophene 1,1-dioxide. In another embodiment, A' is thiazole. In another embodiment, A' is benzimidazole. In another embodiment, A' is piperidine. In another embodiment, A' is imidazole. In another embodiment, A' is thiophene. In another embodiment, A' is isoquinoline. In another embodiment, A' is indole. In another embodiment, A' is 1,3-dihydroisobenzofuran. In another embodiment, A' is benzofuran. In another embodiment, A' is tetrahydro-2H-pyran. In another embodiment, A' is isothiazolyl. In another embodiment, A' is thiadiazolyl.In another embodiment, A' is triazolyl. In another embodiment, A' is thiazolyl. In another embodiment, A' is oxazolyl. In another embodiment, A' is isoxazolyl. In another embodiment, A' is pyrrolyl. In another embodiment, A' is furanyl. In another embodiment, A' is oxadiazolyl. In another embodiment, A' is oxadiazolyl. In another embodiment, A' is 1,2,3-, 1,2,4-, 1,2,5-, or 1,3,4-oxadiazolyl. Each represents a separate embodiment of the present invention. In another embodiment, A' is tetrahydrofuranyl. In another embodiment, A' is oxazolonyl. In another embodiment, A' is oxazolidonyl. In another embodiment, A' is thiazolonyl. In another embodiment, A' is isothiazolinonyl. In another embodiment, A' is isoxazolidinonyl. In another embodiment, A' is imidazolidinonyl. In another embodiment, A' is pyrazolonyl. In another embodiment, A' is 2H-pyrrol-2-onyl. In another embodiment, A' is furanonyl. In another embodiment, A' is thiophenonyl. In another embodiment, A' is thiane 1,1 dioxide. In another embodiment, A' is triazolopyrimidine. In other embodiments, A' is 3H-[1,2,3]triazolo[4,5-d]pyrimidine, 1H-[1,2,3]triazolo[4,5-d]pyrimidine, [1,2,4]triazolo[4,3-c]pyrimidine, [1,2,4]triazolo[4,3-a]pyrimidine, [1,2,3]triazolo[1,5-a]pyrimidine, [1,2,3]triazolo[1,5-c]pyrimidine, [1,2,4]triazolo[1,5-a]pyrimidine, or [1,2,4]triazolo[1,5-c]pyrimidine. Each represents a separate embodiment of the present invention. In other embodiments, A' is 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine.

[0176] In some embodiments, R of structural formula I(g) 100 , H, C 1 -C 5substituted or unsubstituted linear or branched alkyl (e.g., methyl), R 8 -OH (e.g., (CH 2 ) 2 -OH), -R 8 -OR 10 (For example, (CH 2 ) 2 -O-CH 3 ), R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 -NH(CH 3 ), (CH 2 ) 2 -NH 2 ), R 20 or a substituted or unsubstituted 3-8 membered heterocycle (e.g., pyrrolidine, piperidine). Each represents a separate embodiment of the present invention. In some embodiments, R 100 is H. In some embodiments, R 100 is C 1 -C 5 In some embodiments, R 100 is C 1 -C 5 In another embodiment, R 100 is CH 3 In another embodiment, R 100 is CH 2 CH 3 In another embodiment, R 100 is CH 2 CH 2 CH 3 In some embodiments, R 100 is isopropyl. In some embodiments, R 100 is butyl. In some embodiments, R 100 is isobutyl. In some embodiments, R 100 is t-butyl. In some embodiments, R 100 is pentyl. In some embodiments, R 100is isopentyl. In some embodiments, R 100 is neopentyl. In some embodiments, R 100 is benzyl. In some embodiments, R 100 is C 1 -C 5 In another embodiment, R 100 is CH 2 -CH 2 -O-CH 3 In another embodiment, R 100 is CH 2 -CH 2 In another embodiment, R 100 is R 8 In another embodiment, R 100 is (CH 2 ) 2 In another embodiment, R 100 -R 8 -OR 10 In another embodiment, R 100 is (CH 2 ) 2 -O-CH 3 In another embodiment, R 100 is R 8 -N(R 10 )(R 11 In another embodiment, R 100 is (CH 2 ) 2 -NH(CH 3 In another embodiment, R 100 is (CH 2 ) 2 -NH 2 In another embodiment, R 100 is the R defined above. 20 In another embodiment, R 100 is a substituted or unsubstituted 3- to 8-membered heterocycle. 100 is pyrrolidine. In another embodiment, R 100 is piperidine. In another embodiment, R 100 is C 1 -C5 In another embodiment, R 100 is C 1 -C 5 In another embodiment, R 100 is O-CH 3 In another embodiment, R 100 is C(O)R. In other embodiments, R 100 is S(O) 2 R. In some embodiments, R 100 is further divided into F, Cl, Br, I, and C. 1 -C 5 Straight or branched chain alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 NH(R 10 ), N(R 10 )(R 11 ), (e.g., N(CH 3 ) 2 , N.H. 2 ), C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3- to 8-membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0177] In some embodiments, R of structural formula I(h) 1 is H. In other embodiments, R 1 is F. In other embodiments, R 1 CF 3 In another embodiment, R 1 is Cl. In other embodiments, R 1is Br. In another embodiment, R 1 is I. In other embodiments, R 1 is OH. In other embodiments, R 1 is SH. In other embodiments, R 1 is a substituted or unsubstituted C 1 -C 5 In another embodiment, R 1 is C 1 -C 5 Linear or branched chain or C 3 -C 8 In another embodiment, R 1 is a substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8 is a cyclic alkoxy.

[0178] In some embodiments, R of structural formula I(h) 2 is H. In other embodiments, R 2 is F. In other embodiments, R 2 CF 3 In another embodiment, R 2 is Cl. In other embodiments, R 2 is Br. In another embodiment, R 2 is I. In other embodiments, R 2 is OH. In other embodiments, R 2 is SH. In other embodiments, R 2 is a substituted or unsubstituted C 1 -C 5 In another embodiment, R 2 is C 1 -C 5 Linear or branched chain or C 3 -C 8 In another embodiment, R 2 is a substituted or unsubstituted C 1 -C 5 Linear or branched chain or C 3 -C 8is a cyclic alkoxy.

[0179] In some embodiments, R of structural formula I(h) 1 and R 2 are bonded together to form a 3- to 8-membered carbocyclic or heterocyclic ring. 1 and R 2 are linked together to form a 3-8 membered carbocyclic ring. In some embodiments, the carbocyclic ring is cyclopropyl. In other embodiments, R 1 and R 2 are bonded to each other to form a 3- to 8-membered heterocycle.

[0180] In some embodiments, R of structural formula I(h) 3 is H. In some embodiments, R 3 is methyl. In some embodiments, R 3 is a substituted or unsubstituted C 1 -C 5 In some embodiments, alkyl is methoxyethylene, methylaminoethylene, or aminoethylene. Each represents a separate embodiment of the present invention. In some embodiments, R 3 -R 8 -OR 10 In some embodiments, R 3 is (CH 2 ) 2 -O-CH 3 In some embodiments, R 3 is R 8 -N(R 10 )(R 11 In some embodiments, R 3 is (CH 2 ) 2 -NH(CH 3 In some embodiments, R 3 is a substituted or unsubstituted C 3 -C 8 In some embodiments, the cycloalkyl is cyclopropyl. In some embodiments, R 3is a substituted or unsubstituted 5- to 7-membered heterocycle. In some embodiments, R 3 is pyrrolidine. In some embodiments, R 3 is methylpyrrolidine. In some embodiments, R 3 is piperidine. In some embodiments, R 3 is R defined as follows: 20 It is.

[0181] In some embodiments, R of structural formula I(h) 4 is H. In some embodiments, R 4 is methyl. In some embodiments, R 4 is a substituted or unsubstituted C 1 -C 5 In some embodiments, alkyl is methoxyethylene, methylaminoethylene, or aminoethylene. Each represents a separate embodiment of the present invention. In some embodiments, R 4 -R 8 -OR 10 In some embodiments, R 4 is (CH 2 ) 2 -O-CH 3 In some embodiments, R 4 is R 8 -N(R 10 )(R 11 In some embodiments, R 4 is (CH 2 ) 2 -NH(CH 3 In some embodiments, R 4 is a substituted or unsubstituted C 3 -C 8 In some embodiments, the cycloalkyl is cyclopropyl. In some embodiments, R 4 is a substituted or unsubstituted 5- to 7-membered heterocycle. In some embodiments, R 4 is pyrrolidine. In some embodiments, R 4is methylpyrrolidine. In some embodiments, R 4 is piperidine. In some embodiments, R 4 is R defined as follows: 20 It is.

[0182] In some embodiments, R of structural formula I(h) 2 and R 4 are linked together to form a ring F, as defined below. In some embodiments, R 2 and R 4 are bonded together to form a substituted or unsubstituted, saturated or unsaturated 4- to 8-membered heterocycle. 2 and R 4 are bonded together to form a substituted or unsubstituted unsaturated 4- to 8-membered heterocycle. 2 and R 4 are linked together to form a pyrrolidine, pyridine, pyrimidine, triazole, oxadiazole, or pyrazole. Each represents a separate embodiment of the present invention. In some embodiments, when the F ring is aromatic, R 1 is absent. In some embodiments, when the F ring is aromatic, R 3 is absent. In some embodiments, when the F ring is aromatic, R 1 and / or R 3 does not exist.

[0183] In some embodiments, R of structural formula I(h) 3 and R 4 are linked together to form a 3-8 membered heterocycle. In some embodiments, the heterocycle is pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, or imidazole. Each represents a separate embodiment of the present invention.

[0184] In some embodiments, the F ring of structural formula I(h) is absent. In some embodiments, the F ring is a substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycle. In some embodiments, the F ring is a substituted, saturated 4-8 membered heterocycle. In some embodiments, the F ring is a substituted, unsaturated 4-8 membered heterocycle. In some embodiments, the F ring is an unsubstituted, saturated 4-8 membered heterocycle. In some embodiments, the F ring is an unsubstituted, unsaturated 4-8 membered heterocycle. In some embodiments, the F ring is an unsubstituted, unsaturated 4-8 membered heterocycle. In some embodiments, the F ring is a piperidine. In some embodiments, the F ring is piperazine. In some embodiments, the F ring is morpholine. In some embodiments, the F ring is pyridinyl. In other embodiments, the F ring is 2-pyridinyl. In other embodiments, the F ring is pyrimidine. In other embodiments, the F ring is imidazole. In other embodiments, the F ring is pyridazine. In other embodiments, the F ring is pyrazine. In another embodiment, the F ring is pyrazole. In another embodiment, the F ring is thiazole. In another embodiment, the F ring is isothiazolyl. In another embodiment, the F ring is thiadiazolyl. In another embodiment, the F ring is triazolyl. In another embodiment, the F ring is thiazolyl. In another embodiment, the F ring is oxazolyl. In another embodiment, the F ring is isoxazolyl. In another embodiment, the F ring is pyrrolyl. In another embodiment, the F ring is oxadiazolyl. In another embodiment, the F ring is 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, or 1,3,4-oxadiazolyl. Each represents a separate embodiment of the present invention. In another embodiment, the F ring is oxazolonyl. In another embodiment, the F ring is oxazolidonyl. In another embodiment, the F ring is thiazolonyl. In another embodiment, the F ring is isothiazolinonyl. In another embodiment, the F ring is isoxazolidinonyl. In another embodiment, the F ring is imidazolidinonyl. In another embodiment, the F ring is pyrazolonyl. In another embodiment, the F ring is 2H-pyrrol-2-onyl.In another embodiment, the F ring is a triazolopyrimidine. In another embodiment, the F ring is a 3H-[1,2,3]triazolo[4,5-d]pyrimidine, a 1H-[1,2,3]triazolo[4,5-d]pyrimidine, a [1,2,4]triazolo[4,3-c]pyrimidine, a [1,2,4]triazolo[4,3-a]pyrimidine, a [1,2,3]triazolo[1,5-a]pyrimidine, a [1,2,3]triazolo[1,5-c]pyrimidine, a [1,2,4]triazolo[1,5-a]pyrimidine, or a [1,2,4]triazolo[1,5-c]pyrimidine. Each represents a separate embodiment of the invention. In another embodiment, the F ring is a 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine.

[0185] In various embodiments, the present invention relates to the compounds, pharmaceutical compositions, and / or methods of use thereof as set forth in Table 1 below, each of which represents a separate embodiment of the present invention.

[0186] [Table 1-1]

[0187] [Table 1-2]

[0188] [Table 1-3]

[0189] [Table 1-4]

[0190] [Table 1-5]

[0191] [Table 1-6]

[0192] [Table 1-7]

[0193] [Table 1-8]

[0194] [Table 1-9]

[0195] [Table 1-10]

[0196] [Table 1-11]

[0197] [Table 1-12]

[0198] [Table 1-13]

[0199] It is well understood that in structures of the present invention where a carbon atom has fewer than four bonds, H atoms are present to complete the carbon valence. It is well understood that in structures of the present invention where a nitrogen atom has fewer than three bonds, H atoms are present to complete the nitrogen valence.

[0200] In some embodiments, the present invention relates to the compounds, pharmaceutical compositions, and / or methods of use thereof listed above, where the compound includes its pharma- ceutically acceptable salts, stereoisomers, tautomers, hydrates, N-oxides, reverse amide analogs, prodrugs, isotopic variants (deuterated analogs), PROTACs, pharmaceutical products, or any combination thereof. In some embodiments, the compound is a c-MYC mRNA translation regulator. In some embodiments, the compound is a c-MYC mRNA translation inhibitor. In some embodiments, the compound is a c-MYC inhibitor. In various embodiments, the compound is a c-MYC mRNA transcription regulator. In various embodiments, the compound is any combination of a c-MYC mRNA transcription regulator, a c-MYC mRNA transcription regulator, and a c-MYC inhibitor.

[0201] As used herein, unless otherwise specified, the term "alkyl" can be a straight or branched chain alkyl group containing up to about 30 carbons. In various embodiments, alkyl can be any of the following: 1 -C 5 In some embodiments, alkyl is C 1 -C 6 In some embodiments, alkyl is C 1 -C 8 In some embodiments, alkyl is C 1 -C 10 In some embodiments, alkyl is C 1 -C 12 In some embodiments, alkyl is C 1 -C 20 In some embodiments, the branched alkyl is an alkyl substituted with an alkyl side chain of 1 to 5 carbons. In various embodiments, the alkyl group can be unsubstituted. In some embodiments, the alkyl group can be halogen, haloalkyl, hydroxyl, alkoxy, carbonyl, amido, alkylamido, dialkylamido, cyano, nitro, CO 2 H, amino, alkylamino, dialkylamino, carboxyl, thio, thioalkyl, C1 -C 5 Straight or branched chain haloalkoxy, CF 3 , phenyl, halophenyl, (benzyloxy)phenyl, -CH 2 CN, NH 2 , NH-alkyl, N(alkyl) 2 , -OC(O)CF 3 , -OCH 2 Ph, -NHCO-alkyl, -C(O)Ph, C(O)O-alkyl, C(O)H, -C(O)NH 2 or any combination thereof.

[0202] An alkyl group may be the sole substituent or may be part of a larger substituent such as alkoxy, alkoxyalkyl, haloalkyl, arylalkyl, alkylamino, dialkylamino, alkylamide, alkylurea, etc. Preferred alkyl groups are methyl, ethyl, and propyl, and thus include halomethyl, dihalomethyl, trihalomethyl, haloethyl, dihaloethyl, trihaloethyl, halopropyl, dihalopropyl, trihalopropyl, methoxy, ethoxy, propoxy, arylmethyl, arylethyl, arylpropyl, methylamino, ethylamino, propylamino, dimethylamino, diethylamino, methylamide, acetamide, propylamide, halomethylamide, haloethylamide, halopropylamide, methyl-urea, ethyl-urea, propyl-urea, 2,3,4-CH 2 -C 6 H 4 -Cl, C(OH)(CH 3 )(Ph), etc.

[0203] As used herein, the term "aryl" refers to any aromatic ring that is directly bonded to another group and can be either substituted or unsubstituted. An aryl group can be the only substituent or a component part of a larger substituent such as arylalkyl, arylamino, arylamide, etc. Exemplary aryl groups include, but are not limited to, phenyl, tolyl, xylyl, furanyl, naphthyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, thiazolyl, oxazolyl, isoxazolyl, pyrazolyl, imidazolyl, thiophen-yl, pyrrolyl, indolyl, phenylmethyl, phenylethyl, phenylamino, phenylamido, 3-methyl-4H-1,2,4-triazolyl, 5-methyl-1,2,4-oxadiazolyl. Substituents include, but are not limited to, F, Cl, Br, I, C, 1 -C 5 Straight or branched chain alkyl, C 1 -C 5 Straight or branched chain haloalkyl, C 1 -C 5 Linear or branched alkoxy, C 1 -C 5 Straight or branched chain haloalkoxy, CF 3 , phenyl, halophenyl, (benzyloxy)phenyl, CN, NO 2 , -CH 2 CN, NH 2 , NH-alkyl, N(alkyl) 2 , hydroxyl, -OC(O)CF 3 , -OCH 2 Ph, -NHCO-alkyl, COOH, -C(O)Ph, C(O)O-alkyl, C(O)H, -C(O)NH 2 or a combination thereof.

[0204] As used herein, the term "alkoxy" refers to an ether group substituted with an alkyl group as defined above. Alkoxy refers to both straight and branched chain alkoxy groups. Non-limiting examples of alkoxy groups include, but are not limited to, methoxy, ethoxy, propoxy, iso-propoxy, and tert-butoxy.

[0205] As used herein, the term "aminoalkyl" refers to an amine group substituted with an alkyl group as defined above. Aminoalkyl refers to a mono-, di-, or trialkylamine. Non-limiting examples of aminoalkyl groups include -N(Me) 2 , -NHMe, -NH 3 Examples include:

[0206] A "haloalkyl" group refers, in some embodiments, to an alkyl group as defined above that is substituted with one or more halogen atoms, such as F, Cl, Br, or I. The term "haloalkyl" includes, but is not limited to, fluoroalkyl, i.e., an alkyl group having at least one fluorine atom. Non-limiting examples of haloalkyl groups include CF 3 , C.F. 2 CF 3 , C.F. 2 CH 3 , C.H. 2 CF 3 , C.F. 2 CH 2 CH 3 , C.H. 2 CH 2 CF 3 , C.F. 2 CH(CH 3 ) 2 , CF(CH 3 )-CH(CH 3 ) 2 Examples include:

[0207] A "halophenyl" group, in some embodiments, refers to a phenyl substituent substituted with one or more halogen atoms, such as F, Cl, Br, or I. In one embodiment, the halophenyl is 4-chlorophenyl.

[0208] An "alkoxyalkyl" group refers, in some embodiments, to an alkyl group as defined above that is substituted with an alkoxy group as defined above, e.g., methoxy, ethoxy, propoxy, i-propoxy, t-butoxy, etc. Non-limiting examples of alkoxyalkyl groups include -CH 2 -O-CH 3 , -CH 2 -O-CH(CH 3 ) 2 , -CH 2 -OC(CH 3 ) 3 , -CH 2 -CH 2 -O-CH 3 , -CH 2 -CH 2 -O-CH(CH 3 ) 2 , -CH 2 -CH 2 -OC(CH 3 ) 3 Examples include:

[0209] A "cycloalkyl" or "carbocyclic" group, in various embodiments, refers to a ring structure that includes carbon atoms as ring atoms, and may be saturated or unsaturated, substituted or unsubstituted, and either monocyclic or fused. In some embodiments, a cycloalkyl is a 3- to 10-membered ring. In some embodiments, a cycloalkyl is a 3- to 12-membered ring. In some embodiments, a cycloalkyl is a 6-membered ring. In some embodiments, a cycloalkyl is a 5- to 7-membered ring. In some embodiments, a cycloalkyl is a 3- to 8-membered ring. In some embodiments, a cycloalkyl group can be unsubstituted or substituted with halogen, alkyl, haloalkyl, hydroxyl, alkoxy, carbonyl, amido, alkylamido, dialkylamido, cyano, nitro, CO 2H, amino, alkylamino, dialkylamino, carboxyl, thio, thioalkyl, C 1 -C 5 Straight or branched chain haloalkoxy, CF 3 , phenyl, halophenyl, (benzyloxy)phenyl, -CH 2 CN, NH 2 , NH-alkyl, N(alkyl) 2 , -OC(O)CF 3 , -OCH 2 Ph, -NHCO-alkyl, -C(O)Ph, C(O)O-alkyl, C(O)H, -C(O)NH 2 , or any combination thereof. In some embodiments, the cycloalkyl ring may be fused to another saturated or unsaturated cycloalkyl or heterocyclic 3-8 membered ring. In some embodiments, the cycloalkyl ring is a saturated ring. In some embodiments, the cycloalkyl ring is an unsaturated ring. Non-limiting examples of cycloalkyl groups include cyclohexyl, cyclohexenyl, cyclopropyl, cyclopropenyl, cyclopentyl, cyclopentenyl, cyclobutyl, cyclobutenyl, cyclooctyl, cyclooctadienyl (COD), and cyclooctaene (COE).

[0210] A "heterocycle" or "heterocyclic" group, in various embodiments, refers to a ring structure that, in addition to carbon atoms, includes sulfur, oxygen, nitrogen, or any combination thereof as part of the ring. An "aromatic heterocycle", in various embodiments, refers to an aromatic ring structure that, in addition to carbon atoms, includes sulfur, oxygen, nitrogen, or any combination thereof as part of the ring. In some embodiments, the heterocycle or aromatic heterocycle is a 3- to 10-membered ring. In some embodiments, the heterocycle or aromatic heterocycle is a 3- to 12-membered ring. In some embodiments, the heterocycle or aromatic heterocycle is a 6-membered ring. In some embodiments, the heterocycle or aromatic heterocycle is a 5- to 7-membered ring. In some embodiments, the heterocycle or aromatic heterocycle is a 3- to 8-membered ring. In some embodiments, the heterocycle or aromatic heterocycle can be unsubstituted or substituted with a halogen, alkyl, haloalkyl, hydroxyl, alkoxy, carbonyl, amido, alkylamido, dialkylamido, cyano, nitro, CO 2 H, amino, alkylamino, dialkylamino, carboxyl, thio, thioalkyl, C 1 -C 5 Straight or branched chain haloalkoxy, CF 3 , phenyl, halophenyl, (benzyloxy)phenyl, -CH 2 CN, NH 2 , NH-alkyl, N(alkyl) 2 , -OC(O)CF 3 , -OCH 2 Ph, -NHCO-alkyl, -C(O)Ph, C(O)O-alkyl, C(O)H, -C(O)NH 2or any combination thereof. In some embodiments, the heterocycle or aromatic heterocycle may be fused to another saturated or unsaturated cycloalkyl or heterocyclic 3-8 membered ring. In some embodiments, the heterocycle is a saturated ring. In some embodiments, the heterocycle is an unsaturated ring. Non-limiting examples of heterocycles or heteroaromatic ring systems include pyridine, piperidine, morpholine, piperazine, thiophene, pyrrole, benzodioxole, benzofuran-2(3H)-one, benzo[d][1,3]dioxole, indole, oxazole, isoxazole, imidazole and 1-methylimidazole, furan, triazole, pyrimidine, pyrazine, oxacyclobutane (1 or 2-oxacyclobutane), naphthalene, tetrahydrothiophene 1,1-dioxide, thiazole, benzimidazole, piperidine, 1-methylpiperidine, isoquinoline, 1,3-dihydroisobenzofuran, benzofuran, 3-methyl-4H-1,2,4-triazole, 5-methyl-1,2,4-oxadiazole, indole.

[0211] In some embodiments, a "heterocycle" according to the present invention refers to a substituted or unsubstituted, 3-8 membered, saturated, unsaturated, or aromatic, monocyclic, fused, or spiro ring, which contains at least one heteroatom selected from N, O, and S. In some embodiments, the heterocycle can be a substituted or unsubstituted, saturated, unsaturated, or aromatic, monocyclic, fused, or spiro ring, each of which represents a separate embodiment of the present invention. The heterocycle can be a 3-10 membered ring, a 3-9 membered ring, a 3-8 membered ring, a 3-7 membered ring, a 3-6 membered ring, a 3-5 membered ring, a 4-6 membered ring, a 4-7 membered ring, a 4-8 membered ring, a 4-9 membered ring, a 5-6 membered ring, a 5-7 membered ring, a 5-8 membered ring, a 5-10 membered ring, or a 5-9 membered ring, each of which represents a separate embodiment of the present invention. Examples of heterocycles include, but are not limited to, pyran, tetrahydropyran, pyrazole, imidazole, furan, tetrahydrofuran, dioxane, oxetane, azetidine, pyridine, pyridine, pyrimidine, piperidine, triazole, oxadiazole, tetrahydrofuran (THF), piperidine, tetrahydrofuran, morpholine, thiomorpholine 1,1-dioxide, oxa-azaspirodecane, azaspiroheptane, 5-azaspiro[2.4]heptane, 2-azaspiro[3.3]heptane, oxa-azaspirodecane, 5-azaspiro[2.4]heptane, 2-azaspiro[3.3]heptane, 5-azaspiro[2.4 ... The heterocycle may further include azapiroheptane, 2-oxa-6-azaspiro[3.3]heptane, pyrrole, pyrrolidine, pyrrolidin-2-one, 2-oxo-pyrrolidine, pyrrolidinone, quinuclidine, oxetane, azepane, azepan-2-one, azabicyclohexane, 2-azabicyclo[2.1.1]hexane, 3-azabicyclo[3.1.0]hexane, 1-oxa-8-azaspiro[4.5]decane, diazabicyclo[2.2.1]heptane, 2,5-diazabicyclo[2.2.1]heptane, and thiomorpholine 1,1-dioxide. In some embodiments, the heterocycle may further include F, Cl, Br, I, CF 3 , and R 20 , e.g., C 1 -C 5 Straight or branched chain alkyl (e.g., methyl, ethyl, propyl), alkylene amine (e.g., CH 2 -NH 2 ), C 1 -C5 Straight or branched chain haloalkyl, OH, alkoxy (e.g., OCH 3 ), alkylene-OH (e.g., CH 2 -OH), amides, alkylene amides (e.g., CH 2 -C(O)NH 2 ), C(O)-heterocycles, amines (e.g., NH 2 ), alkylamines (e.g., NH(CH 3 )), dialkylamines (e.g., N(CH 3 ) 2 ), CF 3 , aryl, phenyl, halophenyl, heteroaryl, C 3 -C 8 Cycloalkyl (e.g., cyclopropyl), saturated, unsaturated, or aromatic 3- to 8-membered monocyclic, fused, or spirocyclic heterocycles, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0212] In some embodiments, a "monocyclic or fused-ring saturated, unsaturated, or aromatic heterocycle" or a "saturated, unsaturated, or aromatic monocyclic, fused-ring, or spirocyclic heterocycle" is any ring that contains at least one heteroatom selected from N, O, and S, including, but not limited to, pyridinyl, (2-, 3-, and 4-pyridinyl), quinolinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, tetrazinyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, imidazolyl, 1-methylpyridinyl ... Chilimidazole, pyrazolyl, pyrrolyl, furanyl, thiophene-yl, quinolinyl, isoquinolinyl, 2,3-dihydroindenyl, indenyl, tetrahydronaphthyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepin, benzodioxolyl, benzo[d][1,3]dioxole, tetrahydronaphthyl, indolyl, 1H-indole, isoindolyl, anthracenyl, benzimidazolyl, 2,3-dihydro-1H-benzo[d]imidazolyl, indazolyl, 2H-indazole, triazolyl, 4,5,6,7-tetrahydroindenyl, tetrahydro-2H-indazole, 3H-indol-3-one, purinyl, benzoxazolyl, 1,3-benzoxazolyl, benzisoxazolyl, benzothiazolyl, 1,3-benzothiazole, 4,5,6,7-tetrahydro-1,3-benzothiazole, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxaline, 1-(pyridin-1(2H)-yl)ethanone, cinnolinyl, phthalazinyl, quinolinyl, isoquinolinyl, acridinyl, benzofuranyl, 1-benzofuran, isobenzofuranyl, benzofuran -2(3H)-one, benzothiophenyl, benzoxadiazole, benzo[c][1,2,5]oxadiazolyl, 1,2,3-, 1,2,4-, 1,2,5-, or 1,3,4-oxadiazolyl, imidazo[2,1-b][1,3,]thiazole, 4H,5H,6H-cyclopenta[d][1,3]thiazole, 5H,6H,7H,8H-imidazo[1,2-a]pyridine, 7-oxo-6H,7H-[1,3]thiazolo[4,5-d]pyrimidine, [1,3]thiazolo[5,4-b]pyridine, 2H,3H-imidazo[2,1-b][1,3]thiazole, thieno[3,2-d]pyrimidin-4(3H)-one, 4-oxo-4H-thieno[3,2-d][1,3]thiazine, imidazo[1,2-a]pyridine, 1H-imidazo[4,5-b]pyridine, 1H-imidazo[4,5-c]pyridine, 3H-imidazo[4,5-c]pyridine, pyrazolo[1,5-a]pyridine, imidazo[1,2-a]pyrazine, imidazo[1,2-a]pyrimidine, 1H-pyrrolo[2,3-b]pyridine, pyrido [2,3-b]pyrazine, pyrido[2,3-b]pyrazin-3(4H)-one, 4H-thieno[3,2-b]pyrrole, quinoxalin-2(1H)-one, 1H-pyrrolo[3,2-b]pyridine, 7H-pyrrolo[2,3-d]pyrimidine, oxazolo[5,4-b]pyridine, thiazolo[5,4-b]pyridine, thieno[3,2-c]pyridine, 3-methyl-4H-1,2,4-triazole, 5-methyl-1,2,4-oxadiazole, etc. In some embodiments, the heterocycle according to the present invention is selected from the group consisting of pyran, tetrahydropyran, pyrazole, imidazole, furan, tetrahydrofuran, dioxane, oxetane, azetidine, pyridine, pyridine, pyrimidine, piperidine, triazole, oxadiazole, tetrahydrofuran (THF), piperidine, tetrahydrofuran, morpholine, thiomorpholine 1,1-dioxide, oxa-azaspirodecane, azaspiroheptane, 5-azaspirodec ... azaspiro[2.4]heptane, 2-azaspiro[3.3]heptane, oxa-azaspiroheptane, pyrrole, pyrrolidine, pyrrolidin-2-one, 2-oxo-pyrrolidine, pyrrolidinone, quinuclidine, oxetane, azepane, azepan-2-one, azabicyclohexane, 2-azabicyclo[2.1.1]hexane, 3-azabicyclo[3.1.0]hexane, 1-oxa-8-azaspiro[4.5]decane, and diazabicyclo[2.2.1]heptane. Each represents a separate embodiment of the present invention. In some embodiments, the heterocycle may further comprise F, Cl, Br, I, CF, 3 , and R 20 , e.g., C 1 -C 5 Linear or branched chain alkyl (e.g., methyl, ethyl, propyl), alkylene amine (e.g., CH2 -NH 2 ), C 1 -C 5 Straight or branched chain haloalkyl, OH, alkoxy (e.g., OCH 3 ), alkylene-OH (e.g., CH 2 -OH), amides, alkylene amides (e.g., CH 2 -C(O)NH 2 ), C(O)-heterocycles, amines (e.g., NH 2 ), alkylamines (e.g., NH(CH 3 )), dialkylamines (e.g., N(CH 3 ) 2 ), C.F. 3 , aryl, phenyl, halophenyl, heteroaryl, C 3 -C 8 Cycloalkyl (e.g., cyclopropyl), saturated, unsaturated, or aromatic 3- to 8-membered monocyclic, fused, or spirocyclic heterocycles, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0213] In various embodiments, the present invention provides a compound of the present invention, or an isomer, metabolite, pharma- ceutically acceptable salt, pharmaceutical product, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, polymorph, crystal, or any combination thereof. In some embodiments, the present invention provides an isomer of a compound of the present invention. In some embodiments, the present invention provides a metabolite of a compound of the present invention. In some embodiments, the present invention provides a pharma- ceutical product of a compound of the present invention. In some embodiments, the present invention provides a tautomer of a compound of the present invention. In some embodiments, the present invention provides a hydrate of a compound of the present invention. In some embodiments, the present invention provides an N-oxide of a compound of the present invention. In some embodiments, the present invention provides a reverse amide analog of a compound of the present invention. In some embodiments, the present invention provides a prodrug of a compound of the present invention. In some embodiments, the present invention provides an isotopic variant of a compound of the present invention (e.g., but not limited to, a deuterated analog). In some embodiments, the present invention provides a PROTAC (proteolysis-inducing chimera) of a compound of the present invention. In some embodiments, the present invention provides polymorphs of the compounds of the present invention. In some embodiments, the present invention provides crystals of the compounds of the present invention. In some embodiments, the present invention provides compositions comprising the compounds of the present invention described herein, or isomers, metabolites, pharma- ceutically acceptable salts, pharmaceutical products, tautomers, hydrates, N-oxides, reverse amide analogs, prodrugs, isotopic variants (e.g., deuterated analogs), PROTACs, polymorphs, crystals, or any combination thereof of the compounds of the present invention.

[0214] In various embodiments, the term "isomer" includes, but is not limited to, a stereoisomer or analog thereof, an optical isomer or analog thereof, a structural isomer or analog thereof, a conformational isomer or analog thereof, etc. In some embodiments, an isomer is a stereoisomer. In some embodiments, an isomer is an optical isomer.

[0215] Certain compounds of the present invention may exist in specific geometric or stereoisomeric forms.All such compounds, including cis isomers, trans isomers, R enantiomers, S enantiomers, diastereomers, racemic mixtures thereof, and any combinations thereof, are intended to be included within the scope of the present invention.Substituents such as alkyl groups may further have asymmetric carbon atoms.Such isomers and their combinations are also included in the present invention.

[0216] In various embodiments, the present invention encompasses the use of various stereoisomers of the compounds of the present invention.It will be understood by those skilled in the art that the compounds of the present invention may contain at least one chiral center.Therefore, the compounds used in the method of the present invention can exist and be isolated in optically active or racemic form. Thus, the compounds of the present invention may exist as stereoisomers or optically active isomers (e.g., enantiomers such as (R) or (S)), enantiomerically enriched mixtures, racemic mixtures, single diastereomers, diastereomeric mixtures, or any other stereoisomers, including, but not limited to, the (R)(R), (R)(S), (S)(S), (S)(R), (R)(R)(R), (R)(R)(S), (R)(S)(R), (S)(R)(S), (S)(R)(S), or (S)(S)(S) stereoisomers. Some compounds may also exhibit polymorphism. It is to be understood that the present invention encompasses any racemic, optically active, polymorphic, or stereoisomeric forms, or any combination thereof, which forms have properties useful in the treatment of the various diseases (conditions) described herein.

[0217] It is well known in the art how to obtain optically active forms, such as resolution of racemic forms by recrystallization techniques, synthesis from optically active starting materials, chiral synthesis, or chromatographic separation using chiral stationary phases.

[0218] The compounds of the present invention can also exist in the form of racemic mixtures containing substantially equal amounts of stereoisomers. In some embodiments, the compounds of the present invention can be produced or otherwise isolated using known techniques to obtain stereoisomers that are substantially free of their corresponding stereoisomers (i.e., substantially pure). By substantially pure, it is intended that the purity of stereoisomers is at least about 95%, more preferably at least about 98%, and most preferably at least about 99%.

[0219] The compounds of the present invention can also be in the form of hydrates, which means that the compounds further contain stoichiometric or non-stoichiometric amounts of water bound by non-covalent intermolecular forces.

[0220] As used herein, when a chemical functional group (e.g., alkyl or aryl) is said to be "substituted," it is defined that one or more substitutions are possible. In some embodiments, these substitutions include, but are not limited to, halogen, C 1 -C 5 Straight or branched chain alkyl, OH, C 1 -C 5 Linear or branched alkyl-OH (e.g., C(CH 3 ) 2 CH 2 -OH, CH 2 CH 2 -OH), alkoxy (e.g., OMe), amide (e.g., C(O)N(R) 2 ), C(O)-pyrrolidine, C(O)-piperidine, N(R 2 , NH(R 10 ), N(R 10 )(R 11 ) (e.g., N(CH 3 ) 2 , N.H. 2 ), C.F. 3 , aryl, phenyl, heteroaryl, substituted or unsubstituted C 3 -C 8Cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3-8 membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN, and NO 2 Each represents a separate embodiment of the present invention.

[0221] The compounds of the present invention may exist in one or more of the possible tautomers, and depending on the conditions, it is possible to separate some or all of the tautomers into separate entities. It is understood that all possible tautomers are encompassed by the present invention, including all additional enol and keto tautomers and / or isomers. For example, but not limited to, the following tautomers are included:

[0222] [ka]

[0223] The present invention includes "agronomically acceptable salts" of the compounds of the present invention, which are formed by reaction of the compounds of the present invention with an acid or base. Certain compounds, particularly those having acidic or basic groups, can be in the form of salts, preferably agronomically acceptable salts. The term "pharmaceutical acceptable salts" refers to salts that retain the biological effectiveness and properties of the free base or free acid, but are not biologically or otherwise undesirable. Salts are formed from inorganic acids, such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like, or organic acids, such as acetic acid, propionic acid, glycolic acid, pyruvic acid, oxylic acid, maleic acid, malonic acid, succinic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, p-toluenesulfonic acid, salicylic acid, N-acetylcysteine, and the like. Other salts are known to those skilled in the art and can be readily adapted for use in accordance with the present invention.

[0224] Suitable pharma- ceutically acceptable salts of the amines of the compounds of the present invention can be generated from inorganic or organic acids.In various embodiments, examples of inorganic salts of amines include hydrogen sulfate, borate, bromide, chloride, hemisulfate, hydrobromide, hydrochloride, 2-hydroxyethylsulfonate (hydroxyethanesulfonate), iodate, iodide, isothionate, nitrate, persulfate, phosphate, sulfate, sulfamate, sulfanilate, sulfonic acid (alkylsulfonate, arylsulfonate, halogen-substituted alkylsulfonate, halogen-substituted arylsulfonate), sulfonate, and thiocyanate.

[0225] In various embodiments, examples of organic salts of amines can be selected from the aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic, carboxyl, and sulfonic classes of organic acids, examples of which include acetate, arginine, aspartate, ascorbate, adipate, anthranilate, algenate, alkanecarboxylate, substituted alkanecarboxylate, alginate, benzenesulfonate, benzoate, bisulfate, butyrate, bicarbonate, bitartrate, citrate, camphorate, camphorsulfonate, cyclohexylsulfamate, Cyclopentanepropionate, Calcium edetate, Camsylate, Carbonate, Clavulanate, Cinnamate, Dicarboxylate, Digluconate, Dodecylsulfonate, Dihydrochloride, Decanoate, Enanthate, Ethanesulfonate, Edetate, Edisylate, Estholate, Esylate, Fumarate, Formate, Fluoride, Galacturonate, Gluconate, Glutamate, Glycolate, Glucorate, Glucoheptanoate, Glycerophosphate, Gluceptate, Glycolylarsanilate, Glutarate, Glutamate, Heptanoate, Hex ... Xanthate, Hydroxymaleate, Hydroxycarboxylate, Hexylresorcinate, Hydroxybenzoate, Hydroxynaphthoate, Hydrofluoride, Lactate, Lactobionate, Laurate, Malate, Maleate, Methylenebis(beta-oxynaphthoate), Malonate, Mandelate, Mesylate, Methanesulfonate, Methylbromide, Methylnitrate, Methanesulfonate, Monopotassium maleate, Mucate, Monocarboxylate, Naphthalenesulfonate, 2-Naphthalenesulfonate, Nicotinate, Nitrate, Napsylate, N -Methylglucamine, oxalate, octanoate, oleate, pamoate, phenylacetate, picrate, phenylbenzoate, pivalate, propionate, phthalate, phenylacetate, pectinate, phenylpropionate, palmitate, pantothenate, polygalacturonate, pyruvate, quinate, salicylate, succinate, stearate, sulfanilate, acetate, tartrate, theophylline acetate, p-toluenesulfonate (tosylate), trifluoroacetate, terephthalate, tannate, theoclate,Trihaloacetates, triethiodides, tricarboxylates, undecanoates, and valerates.

[0226] In various embodiments, examples of inorganic salts of carboxylic acids or hydroxyls may be selected from alkali metals such as ammonium, lithium, sodium, potassium, cesium, etc.; alkaline earth metals such as calcium, magnesium, aluminum, etc.; zinc, barium, choline, quaternary ammonium.

[0227] In some embodiments, examples of organic salts of carboxylic acids or hydroxyls may be selected from arginine, organic amines (including aliphatic organic amines, cycloaliphatic organic amines, aromatic organic amines, benzathine, t-butylamine, betamin (N-benzylphenethylamine), dicyclohexylamine, dimethylamine, diethanolamine, ethanolamine, ethylenediamine, hydrabamine, imidazole, lysine, methylamine, meglamine, N-methyl-D-glucamine, N,N'-dibenzylethylenediamine, nicotinamide, organic amines, ornithine, pyridine, picoline, piperazine, procaine, tris(hydroxymethyl)methylamine, triethylamine, triethanolamine, trimethylamine, tromethamine), and urea.

[0228] In various embodiments, the salts may be produced by conventional means, for example, by reacting the product in free base or free acid form with one or more equivalents of the appropriate acid or base in a solvent or medium in which the salt is insoluble or in a solvent such as water, which is then removed under vacuum or by lyophilization, or by exchanging an ion of an existing salt with another ion or with a suitable ion exchange resin.

[0229] Pharmaceutical Compositions

[0230] Another aspect of the present invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to an aspect of the present invention. The pharmaceutical composition of the present invention may contain one or more of the compounds of the present invention described above. In general, the pharmaceutical composition of the present invention may comprise a compound of the present invention or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier. The term "pharmaceutically acceptable carrier" refers to any suitable adjuvant, carrier, excipient, or stabilizer, and may take the form of solid or liquid, such as tablet, capsule, powder, solution, suspension, or emulsion.

[0231] Generally, the compositions of the present invention may contain about 0.01 to 99 percent, preferably about 20 to 75 percent, of active compound together with adjuvants, carriers, and / or excipients. Although individual needs may vary, determining the optimal range of effective amounts of each component is within the skill of one of ordinary skill in the art. A typical dosage is about 0.01 to 100 mg / kg body weight. A preferred dosage is about 0.1 to 100 mg / kg body weight. A most preferred dosage is about 1 to 100 mg / kg body weight. Additionally, treatment regimens for administration of the compounds of the present invention can be readily determined by one of ordinary skill in the art. That is, the frequency of administration and the dosage can be established by routine optimization, preferably while minimizing side effects.

[0232] The solid unit dosage form can be of the usual type. The solid form dosage form can be, for example, a capsule of the usual gelatin type, which contains the compound of the present invention and a carrier such as a lubricant or an inert filler (e.g., lactose, sucrose, or cornstarch). In some embodiments, these compounds are tableted in combination with a conventional tablet base such as lactose, sucrose, or cornstarch, a binder such as acacia, cornstarch, or gelatin, a disintegrant such as cornstarch, potato starch, or alginic acid, and a lubricant such as stearic acid or magnesium stearate.

[0233] Tablets, capsules, and the like may also contain binders such as tragacanth, acacia, corn starch, or gelatin, excipients such as dicalcium phosphate, disintegrating agents such as corn starch, potato starch, or alginic acid, lubricants such as magnesium stearate, and sweeteners such as sucrose, lactose, or saccharin. When the dosage unit form is a capsule, it may contain, in addition to materials of the above type, a liquid carrier such as a fatty oil.

[0234] Various other materials can be used as coatings or to modify the physical form of the dosage unit. For example, tablets can be coated with shellac, sugar, or both. A syrup can contain, in addition to the active ingredient, sucrose as a sweetening agent, methyl and propyl parabens as preservatives, a dye, and a flavoring, such as cherry or orange flavor.

[0235] For oral therapeutic administration, these active compounds may be incorporated with excipients and used in the form of tablets, capsules, elixirs, suspensions, syrups, and the like. Such compositions and preparations should contain at least 0.1% of active compound. The percentage of the compound in these compositions may, of course, be varied and may conveniently be about 2-60% of the weight of the unit. The amount of active compound in such therapeutically useful compositions is such that a suitable dosage will be obtained. Preferred compositions according to the invention are prepared so that an oral dosage unit contains about 1-800 mg of active compound.

[0236] The active compounds of the present invention may, for example, be administered orally with an inert diluent or an assimilable edible carrier, enclosed in a hard or soft capsule, compressed into tablets, or incorporated directly into the food of the diet.

[0237] Pharmaceutical forms suitable for injection include sterile aqueous solutions or dispersions and sterile powders for the extemporaneous preparation of sterile injectable solutions or dispersions. In any case, the pharmaceutical forms must be sterile and have a fluidity to allow easy injection with a syringe. They must also be stable under the conditions of manufacture and storage and protected against the contaminating action of microorganisms such as bacteria and fungi. The carrier can be, for example, a solvent or dispersion medium containing water, ethanol, polyol (for example, glycerol, propylene glycol, and liquid polyethylene glycol), a suitable mixture thereof, or vegetable oil.

[0238] The compounds or pharmaceutical compositions of the present invention may also be administered in injectable doses as a solution or suspension in a physiologically acceptable diluent with a pharmaceutical adjuvant, carrier, or excipient. Such adjuvants, carriers, and / or excipients include sterile liquids such as water and oils, with or without the addition of surfactants or other pharma- ceutical and physiologically acceptable ingredients, but are not limited to such. Exemplary oils are oils of petroleum, animal, vegetable, or synthetic origin, such as peanut oil, soybean oil, or mineral oil. In general, water, saline, aqueous dextrose or related sugar solutions, and glycols, such as propylene glycol and polyethylene glycol, are preferred liquid carriers, particularly for injectable solutions.

[0239] These active compounds may also be administered parenterally. Solutions or suspensions of these active compounds may be prepared in water, suitably mixed with a surfactant such as hydroxypropylcellulose. Dispersions may also be prepared in glycerol, liquid polyethylene glycols, and mixtures thereof in oil. Exemplary oils are oils of petroleum, animal, vegetable, or synthetic origin, for example, peanut oil, soybean oil, or mineral oil. In general, water, saline, aqueous dextrose or related sugar solutions, and glycols, such as propylene glycol and polyethylene glycol, are preferred liquid carriers, particularly for injectable solutions. Under normal conditions of storage and use, these preparations contain a preservative to prevent the growth of microorganisms.

[0240] When used as an aerosol, the compounds of the invention in solution or suspension can be packaged in a pressurized aerosol container with a suitable propellant, e.g., a conventional adjuvant and a hydrocarbon propellant, such as propane, butane, or isobutane. The materials of the invention can also be administered in non-pressurized forms, such as in a nebulizer or atomizer.

[0241] In various embodiments, the compounds of the present invention are administered in combination with anti-cancer therapies. Examples of anti-cancer therapies include, but are not limited to, chemotherapy, immunotherapy, radiation therapy, biological therapy, surgical intervention, and any combination thereof. In various embodiments, the compounds of the present invention are administered in combination with anti-cancer agents by administering the compounds described herein alone or in combination with other agents.

[0242] When administering the compound of the present invention, the compound of the present invention may be administered systemically or directly to the specific site where cancer cells or precancerous cells are present.Therefore, administration can be achieved by any method that is effective for delivering the compound or pharmaceutical composition of the present invention to cancer cells.Exemplary methods of administration of the compound or pharmaceutical composition of the present invention include, but are not limited to, oral, topical, transdermal, parenteral, subcutaneous, intravenous, intramuscular, intraperitoneal, intranasal, intracavity, intravesical, intraocular, intraarterial, intralesional, or administration or application to mucous membranes such as nose, throat, or bronchus.

[0243] biological activity

[0244] In various embodiments, the present invention provides compounds and compositions, including any of the embodiments described herein, for use in any of the methods of the present invention. In various embodiments, the use of the compounds of the present invention or compositions comprising same will have utility in inhibiting, suppressing, enhancing, or stimulating a desired response in a subject, as will be understood by those skilled in the art. In some embodiments, the compositions of the present invention may further comprise additional active ingredients having activity useful in the particular application in which the compounds of the present invention are administered.

[0245] The present invention relates to the use of the compounds of the present invention or pharma- ceutically acceptable salts thereof for the treatment, inhibition, and reduction of cancer. Thus, in various embodiments, the present invention relates to a method for the treatment, inhibition, reduction of severity, reduction of risk of developing, or inhibition of cancer, comprising administering to a subject suffering from cancer a compound of the present invention under conditions effective for the treatment, inhibition, reduction of severity, reduction of risk of developing, or inhibition of cancer in the subject. In some embodiments, the compounds of the present invention are c-MYC mRNA translation regulators. In some embodiments, the compounds of the present invention are c-MYC mRNA translation inhibitors. In some embodiments, the compounds of the present invention are c-MYC inhibitors. In some embodiments, the compounds of the present invention are c-MYC mRNA transcription regulators. In some embodiments, the compounds of the present invention are any combination of c-MYC mRNA transcription regulators, c-MYC mRNA transcription regulators, and c-MYC inhibitors. In some embodiments, the compounds of the present invention are any of the compounds listed in Table 1; each compound represents a separate embodiment of the present invention. In some embodiments, the cancer is an early stage cancer. In some embodiments, the cancer is an advanced stage cancer. In some embodiments, the cancer is an invasive cancer. In some embodiments, the cancer is a metastatic cancer. In some embodiments, the cancer is a drug-resistant cancer.

[0246] In some embodiments, the cancer is bladder cancer (urothelial carcinoma), myelodysplasia, breast cancer, cervical cancer, endometrial cancer, esophageal cancer, head and neck cancer (squamous cell carcinoma), kidney cancer (e.g., renal cell carcinoma, clear cell renal cell carcinoma), liver cancer (hepatocellular carcinoma), lung cancer (e.g., metastatic cancer, non-small cell lung cancer, NSCLC, squamous cell carcinoma, small cell lung cancer (SCLC)), metastatic cancer (e.g., to the brain), nasopharyngeal carcinoma, solid tumors, gastric cancer, adrenocortical carcinoma, glioblastoma multiforme, acute myeloid leukemia, chronic lymphocytic leukemia, lymphoma. (e.g., Hodgkin's lymphoma, diffuse large B cell, primary central nervous system), malignant melanoma, uveal melanoma, meningioma, multiple myeloma, breast cancer, metastatic breast cancer, anal cancer (e.g., squamous cell carcinoma), bile duct cancer, bladder cancer, muscle invasive urothelial carcinoma, colorectal cancer, metastatic colorectal cancer, fallopian tube cancer, gastroesophageal junction cancer (e.g., adenocarcinoma), laryngeal cancer (e.g., squamous cell carcinoma), Merkel cell carcinoma, oral cancer, ovarian cancer (e.g., epithelial), pancreatic cancer (e.g., adenocarcinoma, metastatic carcinoma), penile cancer (e.g., For example, squamous cell carcinoma), peritoneal cancer, prostate cancer (e.g., castration-resistant prostate cancer, metastatic prostate cancer), rectal cancer, skin cancer (e.g., basal cell carcinoma, squamous cell carcinoma), small intestine cancer (e.g., adenocarcinoma), testicular cancer, thymic cancer, anaplastic thyroid cancer, bile duct cancer, chordoma, cutaneous T-cell lymphoma, gastrointestinal cancer, familial pheochromocytoma-paraganglioma, glioma, HTLV-1-associated adult T-cell leukemia-lymphoma, blood cancer, hepatitis C (HCV), papillomavirus respiratory infection, foetal The cancer is selected from the group consisting of uterine leiomyosarcoma, acute lymphocytic leukemia, chronic myelogenous leukemia, T-cell lymphoma, follicular lymphoma, primary mediastinal large B-cell lymphoma, diffuse large B-cell testicular lymphoma, melanoma, malignant mesothelioma, pleural mesothelioma, mycosis fungoides, neuroendocrine carcinoma, oral epithelial dysplasia, sarcoma, severe sepsis, Sezary syndrome, smoldering myeloma, soft tissue sarcoma, nasal natural killer (NK) cell T-cell lymphoma, and peripheral T-cell lymphoma.

[0247] In some embodiments, the cancer is selected from the group consisting of, but not limited to, breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's lymphoma, Burkitt's lymphoma, diffuse large B-cell lymphoma, prostate cancer, colon cancer, gastric cancer, primary central nervous system lymphoma, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, germinal center-derived lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, lung adenocarcinoma, BRAFV600E thyroid cancer, choroid plexus carcinoma, colitis-associated cancer, epithelial ovarian cancer, colon cancer, pancreatic cancer, and uterine cancer.

[0248] In some embodiments, the cancer is selected from a solid tumor and a non-solid tumor.

[0249] In various embodiments, the invention relates to a method for suppressing, reducing, or inhibiting tumor growth comprising administering to a subject having tumor growth a compound of the invention under conditions effective to suppress, reduce, or inhibit tumor growth in the subject.

[0250] In some embodiments, the tumor may be a solid tumor or a non-solid tumor.

[0251] In some embodiments, the solid tumor cancer is selected from the group consisting of, but not limited to, breast cancer, ovarian cancer, prostate cancer, colon cancer, gastric cancer, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, lung adenocarcinoma, BRAFV600E thyroid cancer, choroid plexus carcinoma, colitis-associated cancer, epithelial ovarian cancer, colorectal cancer, pancreatic cancer, and uterine cancer.

[0252] In some embodiments, non-solid tumors include, but are not limited to, hematological malignancies, such as leukemia, lymphoma, myeloma, and inherited cancers, such as retinoblastoma and Wilm's tumor.

[0253] In some embodiments, the non-solid tumor cancer is selected from the group consisting of, but not limited to, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's lymphoma, Burkitt's lymphoma, diffuse large B-cell lymphoma, primary central nervous system lymphoma, glioblastoma, medulloblastoma, germinal center-derived lymphoma, myeloma, retinoblastoma, and Wilm's tumor.

[0254] Thus, in various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting cancer, comprising administering to a subject suffering from cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit cancer in the subject. In some embodiments, the cancer is an early stage cancer. In some embodiments, the cancer is an advanced cancer. In some embodiments, the cancer is an invasive cancer. In some embodiments, the cancer is a metastatic cancer. In some embodiments, the cancer is a drug resistant cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0255] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting breast cancer, comprising administering to a subject suffering from breast cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit breast cancer in the subject. In some embodiments, the breast cancer is early stage breast cancer. In some embodiments, the breast cancer is advanced breast cancer. In some embodiments, the breast cancer is invasive breast cancer. In some embodiments, the breast cancer is metastatic breast cancer. In some embodiments, the breast cancer is drug resistant breast cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0256] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting ovarian cancer, comprising administering to a subject suffering from ovarian cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit ovarian cancer in the subject. In some embodiments, the ovarian cancer is early stage ovarian cancer. In some embodiments, the ovarian cancer is advanced ovarian cancer. In some embodiments, the ovarian cancer is invasive ovarian cancer. In some embodiments, the ovarian cancer is metastatic ovarian cancer. In some embodiments, the ovarian cancer is drug resistant ovarian cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0257] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting acute myeloid leukemia, comprising administering to a subject suffering from acute myeloid leukemia a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit acute myeloid leukemia in the subject. In some embodiments, the acute myeloid leukemia is early stage acute myeloid leukemia. In some embodiments, the acute myeloid leukemia is advanced acute myeloid leukemia. In some embodiments, the acute myeloid leukemia is aggressive acute myeloid leukemia. In some embodiments, the acute myeloid leukemia is metastatic acute myeloid leukemia. In some embodiments, the acute myeloid leukemia is drug resistant acute myeloid leukemia. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0258] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting chronic myeloid leukemia, comprising administering to a subject suffering from chronic myeloid leukemia a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit chronic myeloid leukemia in the subject. In some embodiments, the chronic myeloid leukemia is early stage chronic myeloid leukemia. In some embodiments, the chronic myeloid leukemia is advanced chronic myeloid leukemia. In some embodiments, the chronic myeloid leukemia is aggressive chronic myeloid leukemia. In some embodiments, the chronic myeloid leukemia is metastatic chronic myeloid leukemia. In some embodiments, the chronic myeloid leukemia is drug-resistant chronic myeloid leukemia. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0259] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting Hodgkin's lymphoma and / or Burkitt's lymphoma, comprising administering to a subject suffering from Hodgkin's lymphoma and / or Burkitt's lymphoma a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit Hodgkin's lymphoma and / or Burkitt's lymphoma in the subject. In some embodiments, the Hodgkin's lymphoma and / or Burkitt's lymphoma is early stage Hodgkin's lymphoma and / or Burkitt's lymphoma. In some embodiments, the Hodgkin's lymphoma and / or Burkitt's lymphoma is advanced Hodgkin's lymphoma and / or Burkitt's lymphoma. In some embodiments, the Hodgkin's lymphoma and / or Burkitt's lymphoma is aggressive Hodgkin's lymphoma and / or Burkitt's lymphoma. In some embodiments, the Hodgkin's lymphoma and / or Burkitt's lymphoma is metastatic Hodgkin's lymphoma and / or Burkitt's lymphoma. In some embodiments, the Hodgkin's lymphoma and / or Burkitt's lymphoma is drug-resistant Hodgkin's lymphoma and / or Burkitt's lymphoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0260] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting diffuse large B-cell lymphoma, comprising administering to a subject suffering from diffuse large B-cell lymphoma a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit diffuse large B-cell lymphoma in the subject. In some embodiments, the diffuse large B-cell lymphoma is early stage diffuse large B-cell lymphoma. In some embodiments, the diffuse large B-cell lymphoma is advanced diffuse large B-cell lymphoma. In some embodiments, the diffuse large B-cell lymphoma is invasive diffuse large B-cell lymphoma. In some embodiments, the diffuse large B-cell lymphoma is metastatic diffuse large B-cell lymphoma. In some embodiments, the diffuse large B-cell lymphoma is drug-resistant diffuse large B-cell lymphoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in the cell. In some embodiments, the compound of the present invention is any of the compounds listed in Table 1; each compound represents a separate embodiment of the present invention.

[0261] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting prostate cancer, comprising administering to a subject suffering from prostate cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit prostate cancer in the subject. In some embodiments, the prostate cancer is early stage prostate cancer. In some embodiments, the prostate cancer is advanced prostate cancer. In some embodiments, the prostate cancer is invasive prostate cancer. In some embodiments, the prostate cancer is metastatic prostate cancer. In some embodiments, the prostate cancer is drug resistant prostate cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in cells. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0262] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting colon cancer, comprising administering to a subject suffering from colon cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit colon cancer in the subject. In some embodiments, the colon cancer is early stage colon cancer. In some embodiments, the colon cancer is advanced colon cancer. In some embodiments, the colon cancer is invasive colon cancer. In some embodiments, the colon cancer is metastatic colon cancer. In some embodiments, the colon cancer is drug resistant colon cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in cells. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0263] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting gastric cancer, comprising administering to a subject suffering from gastric cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit gastric cancer in the subject. In some embodiments, the gastric cancer is early gastric cancer. In some embodiments, the gastric cancer is advanced gastric cancer. In some embodiments, the gastric cancer is invasive gastric cancer. In some embodiments, the gastric cancer is metastatic gastric cancer. In some embodiments, the gastric cancer is drug-resistant gastric cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in cells. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0264] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting lymphoma, comprising administering to a subject suffering from lymphoma a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit lymphoma in the subject. In some embodiments, the lymphoma is an early stage lymphoma. In some embodiments, the lymphoma is an advanced lymphoma. In some embodiments, the lymphoma is an invasive lymphoma. In some embodiments, the lymphoma is a metastatic lymphoma. In some embodiments, the lymphoma is a drug-resistant lymphoma. In some embodiments, the lymphoma is a primary central nervous system lymphoma. In some embodiments, the lymphoma is a germinal center-derived lymphoma. In some embodiments, the lymphoma is a Hodgkin's lymphoma. In some embodiments, the lymphoma is a Burkitt's lymphoma. In some embodiments, the lymphoma is a diffuse large B-cell lymphoma. In some embodiments, the compounds of the invention are c-MYC mRNA translation regulators. In some embodiments, the compounds of the invention are c-MYC mRNA translation inhibitors. In some embodiments, the compounds of the invention are c-MYC mRNA transcription regulators. In some embodiments, the compounds of the invention are selective for c-MYC. In some embodiments, the compounds of the invention reduce the amount of c-Myc protein in cells. In some embodiments, the compounds of the invention are any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0265] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting glioblastoma, comprising administering to a subject suffering from glioblastoma a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit glioblastoma in the subject. In some embodiments, the glioblastoma is an early stage glioblastoma. In some embodiments, the glioblastoma is an advanced glioblastoma. In some embodiments, the glioblastoma is an invasive glioblastoma. In some embodiments, the glioblastoma is a metastatic glioblastoma. In some embodiments, the glioblastoma is a drug-resistant glioblastoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0266] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting medulloblastoma, comprising administering to a subject suffering from medulloblastoma a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit medulloblastoma in the subject. In some embodiments, the medulloblastoma is early stage medulloblastoma. In some embodiments, the medulloblastoma is advanced medulloblastoma. In some embodiments, the medulloblastoma is invasive medulloblastoma. In some embodiments, the medulloblastoma is metastatic medulloblastoma. In some embodiments, the medulloblastoma is drug resistant medulloblastoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0267] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting melanoma, comprising administering to a subject afflicted with melanoma a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit melanoma in the subject. In some embodiments, the melanoma is early stage melanoma. In some embodiments, the melanoma is advanced melanoma. In some embodiments, the melanoma is invasive melanoma. In some embodiments, the melanoma is metastatic melanoma. In some embodiments, the melanoma is drug resistant melanoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0268] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting non-small cell lung cancer, comprising administering to a subject suffering from non-small cell lung cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit non-small cell lung cancer in the subject. In some embodiments, the non-small cell lung cancer is early stage non-small cell lung cancer. In some embodiments, the non-small cell lung cancer is advanced non-small cell lung cancer. In some embodiments, the non-small cell lung cancer is invasive non-small cell lung cancer. In some embodiments, the non-small cell lung cancer is metastatic non-small cell lung cancer. In some embodiments, the non-small cell lung cancer is drug resistant non-small cell lung cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0269] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting esophageal squamous cell carcinoma, comprising administering to a subject suffering from esophageal squamous cell carcinoma a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit esophageal squamous cell carcinoma in the subject. In some embodiments, the esophageal squamous cell carcinoma is early stage esophageal squamous cell carcinoma. In some embodiments, the esophageal squamous cell carcinoma is advanced esophageal squamous cell carcinoma. In some embodiments, the esophageal squamous cell carcinoma is invasive esophageal squamous cell carcinoma. In some embodiments, the esophageal squamous cell carcinoma is metastatic esophageal squamous cell carcinoma. In some embodiments, the esophageal squamous cell carcinoma is drug resistant esophageal squamous cell carcinoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0270] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting osteosarcoma, comprising administering to a subject suffering from osteosarcoma a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit osteosarcoma in the subject. In some embodiments, the osteosarcoma is early stage osteosarcoma. In some embodiments, the osteosarcoma is advanced osteosarcoma. In some embodiments, the osteosarcoma is invasive osteosarcoma. In some embodiments, the osteosarcoma is metastatic osteosarcoma. In some embodiments, the osteosarcoma is drug resistant osteosarcoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0271] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting bladder cancer, comprising administering to a subject suffering from bladder cancer a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit bladder cancer in the subject. In some embodiments, the bladder cancer is early stage bladder cancer. In some embodiments, the bladder cancer is advanced bladder cancer. In some embodiments, the bladder cancer is invasive bladder cancer. In some embodiments, the bladder cancer is metastatic bladder cancer. In some embodiments, the bladder cancer is drug resistant bladder cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0272] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting pancreatic cancer, comprising administering to a subject suffering from pancreatic cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit pancreatic cancer in the subject. In some embodiments, the pancreatic cancer is early stage pancreatic cancer. In some embodiments, the pancreatic cancer is advanced pancreatic cancer. In some embodiments, the pancreatic cancer is invasive pancreatic cancer. In some embodiments, the pancreatic cancer is metastatic pancreatic cancer. In some embodiments, the pancreatic cancer is drug resistant pancreatic cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0273] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting lung adenocarcinoma, comprising administering to a subject suffering from lung adenocarcinoma a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit lung adenocarcinoma in the subject. In some embodiments, the lung adenocarcinoma is early stage lung adenocarcinoma. In some embodiments, the lung adenocarcinoma is advanced lung adenocarcinoma. In some embodiments, the lung adenocarcinoma is invasive lung adenocarcinoma. In some embodiments, the lung adenocarcinoma is metastatic lung adenocarcinoma. In some embodiments, the lung adenocarcinoma is drug resistant lung adenocarcinoma. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0274] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting thyroid cancer, comprising administering to a subject suffering from thyroid cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit thyroid cancer in the subject. In some embodiments, the thyroid cancer is early stage thyroid cancer. In some embodiments, the thyroid cancer is advanced thyroid cancer. In some embodiments, the thyroid cancer is invasive thyroid cancer. In some embodiments, the thyroid cancer is metastatic thyroid cancer. In some embodiments, the thyroid cancer is drug resistant thyroid cancer. In some embodiments, the thyroid cancer is BRAFV600E thyroid cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0275] In various embodiments, the present invention relates to a method for treating, inhibiting, reducing the severity of, reducing the risk of developing, or inhibiting choroid plexus cancer, comprising administering to a subject suffering from choroid plexus cancer a compound of the present invention under conditions effective to treat, inhibit, reduce the severity of, reduce the risk of developing, or inhibit choroid plexus cancer in the subject. In some embodiments, the choroid plexus cancer is early stage choroid plexus cancer. In some embodiments, the choroid plexus cancer is advanced choroid plexus cancer. In some embodiments, the choroid plexus cancer is invasive choroid plexus cancer. In some embodiments, the choroid plexus cancer is metastatic choroid plexus cancer. In some embodiments, the choroid plexus cancer is drug resistant choroid plexus cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0276] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting colitis-associated cancer, comprising administering to a subject suffering from colitis-associated cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit colitis-associated cancer in the subject. In some embodiments, the colitis-associated cancer is early colitis-associated cancer. In some embodiments, the colitis-associated cancer is advanced colitis-associated cancer. In some embodiments, the colitis-associated cancer is invasive colitis-associated cancer. In some embodiments, the colitis-associated cancer is metastatic colitis-associated cancer. In some embodiments, the colitis-associated cancer is drug-resistant colitis-associated cancer. In some embodiments, the compounds of the present invention are c-MYC mRNA translation regulators. In some embodiments, the compounds of the present invention are c-MYC mRNA translation inhibitors. In some embodiments, the compounds of the present invention are c-MYC mRNA transcription regulators. In some embodiments, the compounds of the present invention are selective for c-MYC. In some embodiments, the compound of the invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0277] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting ovarian cancer, comprising administering to a subject suffering from ovarian cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit ovarian cancer in the subject. In some embodiments, the ovarian cancer is early stage ovarian cancer. In some embodiments, the ovarian cancer is advanced ovarian cancer. In some embodiments, the ovarian cancer is invasive ovarian cancer. In some embodiments, the ovarian cancer is metastatic ovarian cancer. In some embodiments, the ovarian cancer is drug resistant ovarian cancer. In some embodiments, the ovarian cancer is epithelial ovarian cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0278] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting colorectal cancer, comprising administering to a subject suffering from colorectal cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit colorectal cancer in the subject. In some embodiments, the colorectal cancer is early stage colorectal cancer. In some embodiments, the colorectal cancer is advanced colorectal cancer. In some embodiments, the colorectal cancer is invasive colorectal cancer. In some embodiments, the colorectal cancer is metastatic colorectal cancer. In some embodiments, the colorectal cancer is drug resistant colorectal cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the invention.

[0279] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting uterine cancer, comprising administering to a subject suffering from uterine cancer a compound of the present invention under conditions effective to treat, suppress, reduce the severity of, reduce the risk of developing, or inhibit uterine cancer in the subject. In some embodiments, the uterine cancer is early stage uterine cancer. In some embodiments, the uterine cancer is advanced uterine cancer. In some embodiments, the uterine cancer is invasive uterine cancer. In some embodiments, the uterine cancer is metastatic uterine cancer. In some embodiments, the uterine cancer is drug resistant uterine cancer. In some embodiments, the compound of the present invention is a c-MYC mRNA translation regulator. In some embodiments, the compound of the present invention is a c-MYC mRNA translation inhibitor. In some embodiments, the compound of the present invention is a c-MYC mRNA transcription regulator. In some embodiments, the compound of the present invention is selective for c-MYC. In some embodiments, the compound of the present invention reduces the amount of c-Myc protein in a cell. In some embodiments, the compound of the present invention is any of the compounds set forth in Table 1; each compound represents a separate embodiment of the present invention.

[0280] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting metastatic cancer, comprising administering to a subject suffering from metastatic cancer a compound of the present invention, and / or an isomer, metabolite, pharma- ceutically acceptable salt, pharmaceutical product, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, polymorph, crystal, or any combination thereof. The compounds of the present invention are c-MYC mRNA translation regulators. In some embodiments, the compounds of the present invention are c-MYC mRNA translation inhibitors. In some embodiments, the compounds of the present invention are c-MYC mRNA transcription regulators. In some embodiments, the compounds of the present invention are selective for c-MYC. In some embodiments, the compounds of the present invention reduce the amount of c-Myc protein in a cell. In some embodiments, the cancer is breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's lymphoma, Burkitt's lymphoma, diffuse large B-cell lymphoma, prostate cancer, colon cancer, gastric cancer, primary central nervous system lymphoma, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, germinal center-derived lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, lung adenocarcinoma, thyroid cancer, choroid plexus cancer, colitis-associated cancer, colon cancer, or uterine cancer, each of which represents a separate embodiment of the present invention.

[0281] In various embodiments, the present invention relates to a method for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting advanced cancer, comprising administering to a subject suffering from advanced cancer a compound of the present invention, and / or an isomer, metabolite, pharma- ceutically acceptable salt, pharmaceutical product, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), PROTAC, polymorph, crystal, or any combination thereof. The compounds of the present invention are c-MYC mRNA translation regulators. In some embodiments, the compounds of the present invention are c-MYC mRNA translation inhibitors. In some embodiments, the compounds of the present invention are c-MYC mRNA transcription regulators. In some embodiments, the compounds of the present invention are selective for c-MYC. In some embodiments, the compounds of the present invention reduce the amount of c-Myc protein in a cell. In some embodiments, the cancer is breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's lymphoma, Burkitt's lymphoma, diffuse large B-cell lymphoma, prostate cancer, colon cancer, gastric cancer, primary central nervous system lymphoma, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, germinal center-derived lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, lung adenocarcinoma, thyroid cancer, choroid plexus cancer, colitis-associated cancer, colon cancer, or uterine cancer, each of which represents a separate embodiment of the present invention.

[0282] The compounds of the present invention are useful for treating, reducing the severity, reducing the risk of developing, or inhibiting cancer, metastatic cancer, advanced cancer, drug-resistant cancer, and various forms of cancer. In a preferred embodiment, the cancer is breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's lymphoma, Burkitt's lymphoma, diffuse large B-cell lymphoma, prostate cancer, colon cancer, gastric cancer, primary central nervous system lymphoma, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, germinal center-derived lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, lung adenocarcinoma, thyroid cancer, choroid plexus cancer, colitis-associated cancer, colon cancer, or uterine cancer. Each represents a separate embodiment of the present invention. Based on its mechanism of action, it is believed that other forms of cancer can be treated or prevented as well by administering the compounds or compositions of the present invention to a patient. The preferred compounds of the present invention are preferably selectively destructive to cancer cells and not to normal cells, causing the elimination of cancer cells. Importantly, because cancer cells are susceptible to destruction at much lower concentrations of the compounds of the present invention, harm to normal cells is minimized.

[0283] In various embodiments, other types of cancer that can be treated with the c-MYC mRNA translation regulators of the present invention include adrenocortical carcinoma, anal carcinoma, bladder carcinoma, brain tumor, brain stem tumor, breast cancer, glioma, cerebellar astrocytoma, cerebral astrocytoma, ependymoma, medulloblastoma, supratentorial primitive neuroectodermal, pineal tumor, hypothalamic glioma, carcinoid tumor, epithelial carcinoma, cervical cancer, colon cancer, central nervous system (CNS) cancer, endometrial cancer, esophageal cancer, extrahepatic bile duct cancer, and uterine cancer. ,Pnet,Extracranial Germ Cell Tumor,Eye Cancer,Intraocular Melanoma,Gallbladder Cancer,Gastric Cancer,Germ Cell Tumor,Extragonadal Tumor,Gestational Trophoblastic Neoplasm,Head and Neck Cancer,Hypopharyngeal Cancer,Pancreatic Islet Cell Carcinoma,Laryngeal Cancer,Leukemia,Acute Lymphoblastic,Leukemia,Oral Cancer,Hepatocellular Carcinoma,Lung Cancer,Non-Small Cell Lung Cancer,Small Cell,Lymphoma,AIDS-Related Lymphoma,Central Nervous System (Primary),Lymphoma,Cutaneous T Cell,Lymphoma,Hodgkin's Disease,Non-Small Cell,Lymphoma Hodgkin's disease, malignant mesothelioma, melanoma, Merkel cell carcinoma, metastatic squamous cell carcinoma, multiple myeloma, plasma cell neoplasms, mycosis fungoides, myelodysplastic syndromes, myeloproliferative disorders, nasopharyngeal carcinoma, neuroblastoma, oropharyngeal carcinoma, osteosarcoma, ovarian cancer, ovarian epithelial cancer, ovarian germ cell tumors, ovarian low malignant potential tumors, pancreatic cancer, exocrine carcinoma, pancreatic cancer, islet cell carcinoma, paranasal sinus and nasal cancer, parathyroid cancer, penile cancer, pheochromocytoma cancer, pituitary cancer , plasma cell neoplasms, prostate cancer, rhabdomyosarcoma, rectal cancer, renal cancer, renal cell carcinoma, salivary gland cancer, Sezary syndrome, skin cancer, cutaneous T-cell lymphoma, skin cancer, Kaposi's sarcoma, melanoma, small intestine cancer, soft tissue sarcoma, testicular tumor, thymoma, malignant tumor, thyroid cancer, urethral cancer, uterine cancer, sarcoma, rare cancer of childhood, vaginal cancer, vulvar cancer, Wilms' tumor, hepatocellular carcinoma, blood cancer, and any combination thereof. In some embodiments, the cancer is an invasive cancer. In some embodiments, the cancer is a metastatic cancer. In some embodiments, the cancer is an advanced cancer. In some embodiments, the cancer is a drug resistant cancer.

[0284] In various embodiments, "metastatic cancer" refers to a cancer that has spread (metastasized) from its original site to another area of ​​the body. Virtually all cancers can metastasize. Whether metastasis occurs depends on a complex interplay of various tumor cell factors, including the type of cancer, the maturity (degree of differentiation) of the tumor cells, the location and duration the cancer has been present, and other factors that are not fully understood. Metastasis spreads in three ways: local extension from the tumor to the surrounding tissue, metastasis via the bloodstream to a distant site, or metastasis via the lymphatic system to adjacent or distant lymph nodes. There are typical metastatic pathways for each type of cancer. Tumors are referred to by their primary site (e.g., breast cancer that has spread to the brain is referred to as brain metastatic breast cancer).

[0285] In various embodiments, "drug-resistant cancer" refers to cancer cells that have acquired resistance to chemotherapy. Cancer cells can acquire resistance to chemotherapy by various mechanisms, including mutation or overexpression of drug targets, inactivation of drugs, or elimination of drugs from the cells. Tumors that recur after an initial response to chemotherapy may exhibit resistance to multiple drugs (multidrug resistance). The traditional view of drug resistance is that one or more cells in a tumor population acquire genetic changes that confer drug resistance. Thus, the reasons for drug resistance are, among others, the following: (a) A portion of cells that are not killed by chemotherapy mutate (change) and acquire drug resistance. As they proliferate, there are more cells that are resistant to chemotherapy than cells that are sensitive to chemotherapy. (b) Gene amplification. Cancer cells make hundreds of copies of a particular gene. This gene causes the overproduction of a protein that renders anticancer drugs ineffective. (c) Cancer cells use a molecule called p-glycoprotein to pump drugs out of the cell as fast as the drugs enter the cell. (d) Cancer cells stop taking up drugs because proteins that transport drugs across the cell wall stop functioning. (e) Cancer cells learn how to repair DNA breaks caused by certain anticancer drugs. (f) Cancer cells develop mechanisms to inactivate drugs. One of the main causes of multidrug resistance is overexpression of P-glycoprotein (P-gp). This protein is a clinically important transport protein that belongs to the ATP-binding cassette family of cell membrane transporters. It can export substrates, including anticancer drugs, from tumor cells via an ATP-dependent mechanism. (g) Cells and tumors with activating RAS mutations are relatively resistant to most anticancer drugs. Thus, resistance to anticancer drugs used in chemotherapy is the main cause of treatment failure in malignant diseases and leads to tumor resistance. Drug resistance is the main cause of chemotherapy failure in cancer.

[0286] In various embodiments, "resistant cancer" refers to drug-resistant cancer as described above. In some embodiments, "resistant cancer" refers to cancer cells that have acquired resistance to treatments, such as chemotherapy, radiation therapy, or biological therapy.

[0287] In various embodiments, the invention relates to treating, suppressing, reducing the severity, reducing the risk of developing, or inhibiting cancer in subjects who have previously undergone chemotherapy, radiation therapy, or biological therapy.

[0288] In various embodiments, "chemotherapy" refers to the treatment of cancer, such as with drugs that directly kill cancer cells. Such drugs are referred to as "anti-cancer" or "anti-tumor" drugs. Today, chemotherapy includes over 100 drugs used to treat cancer. Chemotherapy is used to cure certain cancers, to control tumor growth when a cure is not possible, to shrink tumors before surgery or radiation therapy, to relieve symptoms (such as pain), or to destroy tiny cancer cells that may be present after surgical removal of a known tumor (called adjuvant therapy). Adjuvant therapy is also used to prevent cancer from recurring.

[0289] In various embodiments, "radiation therapy" (also referred to herein as "radiotherapy") refers to the treatment of cancer with high-energy x-rays or similar radiation (such as electrons). Many cancer patients undergo radiation therapy as part of their treatment. Radiation therapy can be external radiation therapy, where x-rays are applied from outside the body, or internal radiation therapy, where x-rays are applied from inside the body. Radiation therapy works by destroying cancer cells in the treatment area. Normal cells can also be damaged by radiation therapy, but normal cells can usually repair themselves. Radiation therapy can cure some cancers and can also reduce the chance of cancer recurrence after surgery. Radiation therapy can also be used to relieve symptoms of cancer.

[0290] In various embodiments, "biological therapy" refers to the treatment of cancer with substances that occur naturally in the body and destroy cancer cells. There are several types of biological therapy, such as treatment with monoclonal antibodies, cancer growth inhibitors, or vaccines, or gene therapy. Biological therapy is also called immunotherapy.

[0291] When the compounds or pharmaceutical compositions of the present invention are administered to treat, suppress, reduce the severity, reduce the risk, or inhibit a cancerous condition, the pharmaceutical composition may also include or be administered in combination with other therapeutic agents or treatment regimens now known or hereafter developed for the treatment of various types of cancer, including, but not limited to, radiation therapy, immunotherapy, chemotherapy, surgical intervention, and any combination thereof.

[0292] Thus, in various embodiments, the compounds of the invention are administered in combination with an anti-cancer therapy, examples of which include, but are not limited to, chemotherapy, immunotherapy, radiation therapy, biological therapy, surgical intervention, and any combination thereof.

[0293] In various embodiments, the compounds of the invention are administered in combination with anti-cancer agents, including compounds described herein alone or in combination with other agents.

[0294] In various embodiments, the composition for cancer treatment of the present invention may be used in combination with existing chemotherapy drugs or may be prepared as a mixture with them. Such chemotherapy drugs include, for example, alkylating agents, nitrosoureas, metabolic antagonists, antitumor antibiotics, alkaloids derived from plants, topoisomerase inhibitors, hormone therapy drugs, hormone antagonists, aromatase inhibitors, P-glycoprotein inhibitors, platinum complex derivatives, other immunotherapy drugs, and other anticancer drugs. Furthermore, the composition for cancer treatment of the present invention may be used in combination with cancer treatment adjuvant drugs for leukopenia (neutrophils), thrombocytopenia, antiemetics, and cancer pain drugs or may be prepared as a mixture with them to restore the patient's QOL.

[0295] In various embodiments, the invention provides methods of modulating c-MYC mRNA translation in a cell, comprising contacting the cell with a compound represented by structural formula I, II, and / or I(a)-I(f) and / or a compound represented by a structural formula listed in Table 1 above, thereby modulating c-MYC mRNA translation in the cell. In some embodiments, the methods of the invention are performed by modulating splicing of c-MYC mRNA. In some embodiments, the methods of the invention are performed by inclusion or exclusion of untranslated regions or alternative use of exons. In some embodiments, the methods of the invention are performed by modulating c-MYC mRNA modification. In some embodiments, the methods of the invention are performed by modulating the interaction of an RNA binding protein with c-MYC mRNA, thereby altering the localization of the mRNA. In some embodiments, the methods of the invention are performed by modulating the localization of c-MYC mRNA in the cytoplasm. In some embodiments, the methods of the invention are performed by modulating ribosomes or ribosomal accessory factors to c-MYC mRNA. In some embodiments, the methods of the invention are performed by decreasing the amount of c-MYC protein in the cell.

[0296] The invention provides a method of modulating c-MYC mRNA transcription in a cell, comprising contacting the cell with a compound represented by structural formula I, II, and / or I(a)-I(f) and / or a compound represented by a structural formula listed in Table 1 above, thereby modulating c-MYC mRNA transcription in the cell. In some embodiments, the method of the invention is performed by modulating splicing of c-MYC mRNA. In some embodiments, the method of the invention is performed by inclusion or exclusion of untranslated regions or alternative use of exons. In some embodiments, the method of the invention is performed by modulating c-MYC mRNA modification. In some embodiments, the method of the invention is performed by modulating the interaction of an RNA binding protein with c-MYC mRNA, thereby altering the localization of the mRNA. In some embodiments, the method of the invention is performed by modulating the localization of c-MYC mRNA in the cytoplasm. In some embodiments, the method of the invention is performed by modulating ribosomes or ribosomal accessory factors to c-MYC mRNA. In some embodiments, the method of the invention is performed by decreasing the amount of c-MYC protein in the cell.

[0297] In various embodiments, the present invention relates to a method of destroying cancer cells, comprising providing a compound of the present invention and contacting the compound of the present invention with cancer cells under conditions effective to destroy the cancer cells. According to various embodiments of destroying cancer cells, the cells can be destroyed in vivo or ex vivo (i.e., in culture).

[0298] A further aspect of the invention relates to a method of treating or preventing a cancerous condition, comprising the steps of providing a compound of the invention and administering an effective amount of a compound of the invention to a patient under conditions effective to treat or prevent the cancerous condition.

[0299] In one embodiment, the patient being treated is characterized by the presence of a pre-cancerous condition, and administration of the compounds of the invention is effective to prevent the progression of the pre-cancerous condition to a cancerous condition, which can be achieved by destroying the pre-cancerous cells prior to or concomitantly with their further progression to a cancerous condition.

[0300] In other embodiments, the patient being treated is characterized by the presence of a cancerous condition and administration of the compounds of the invention is effective to cause regression of the cancerous condition or inhibit the growth of the cancerous condition, i.e., to stop its growth altogether or to slow its rate of growth. This can be accomplished by preferably destroying the cancer cells regardless of their location in the patient's body, i.e., whether the cancer cells are located at the site of a primary tumor or whether the cancer cells have metastasized to form secondary tumors in the patient's body.

[0301] As used herein, subject or patient refers to any mammalian patient or subject, including, but not limited to, humans or other primates, dogs, cats, horses, cows, sheep, pigs, rats, mice, and other rodents. In some embodiments, the subject is male. In some embodiments, the subject is female. In some embodiments, the methods of the invention described herein may be useful for treating either males or females.

[0302] When administering the compound of the present invention, the compound of the present invention may be administered systemically or directly to a specific site where cancer cells or precancerous cells are present.Accordingly, administration can be achieved by any method that is effective for delivering the compound or pharmaceutical composition of the present invention to cancer cells or precancerous cells.Exemplary administration modes of the compound or composition of the present invention include, but are not limited to, oral, topical, transdermal, parenteral, subcutaneous, intravenous, intramuscular, intraperitoneal, intranasal, intracavity, intravesical, intraocular, intraarterial, intralesional, or administration or application to mucous membranes such as no...

Claims

1. A compound represented by structural formula (Ih) below, or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, Ring F is absent or a substituted or unsubstituted, saturated or unsaturated 4- to 8-membered heterocycle (e.g., pyrrolidine, pyridine, imidazole, pyrimidine, triazole, oxadiazole, pyrazole); R １ and R ２ are independently H, F, Cl, Br, I, OH, SH, CF ３ , substituted or unsubstituted C １ -C ５ Alkyl, C １ -C ５ or C ３ -C ８ or a cyclic haloalkyl of substituted or unsubstituted C １ -C ５ or C ３ -C ８ is a cyclic alkoxy; Or, R １ and R ２ are bonded to each other to form C ３ -C ８ forming a carbocyclic or heterocyclic ring (e.g., cyclopropyl); Or, R ２ and R ４ are joined together to form a ring F as defined above (e.g., pyrrolidine, pyridine, pyrimidine, triazole, oxadiazole, pyrazole); However, when the F ring is aromatic, R １ and / or R ３ does not exist; R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), —R ８ -O-R １０ (For example, (CH ２ ) ２ -O-CH ３ ), R ８ -N(R １０ ) (R １１ ) (e.g., (CH ２ ) ２ -NH(CH ３ )), substituted or unsubstituted C ３ -C ８ cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 5- to 7-membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine), or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X ５ , X ６ , X ８ , and X ９ are, independently of each other, a nitrogen atom or a carbon atom; X １０ is N, CH, or C(R); R ５ is H or C １ -C ５ is a straight or branched chain alkyl (e.g., methyl); R ６ is R ８ -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocyclic ring) (e.g., (CH ２ ) ３ -piperidine, (CH ２ ) ３ -4-fluoro-piperidine), or R ８ -N(R １０ ) (R １１ ) (e.g., (CH ２ ) ３ -N(CH ２ CH ３ ) ２ ) is; R ７ ' are each independently H, F, Cl, Br, I, OH, O—R ２０ , S.H., R. ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(3- to 8-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl (e.g., CHF ２ ), C １ -C ５ or C ３ -C ８ Cyclic alkoxy (e.g., methoxy) (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl (e.g., cyclopropyl), a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; R ２０ is represented by the following structural formula: R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ straight or branched chain substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH ２ -CH ２ -O-CH ２ -CH ２ -O-CH ３ , C.H. ２ -O-CH ２ -CH ２ -O-CH ３ ), C １ -C ５ linear or branched alkoxy of C １ -C ５ straight or branched chain haloalkyl (e.g., CHF ２ , C.F. ３ , C.F. ２ CH ３ , C.H. ２ CF ３ , C.F. ２ CH ２ CH ３ , C.H. ２ CH ２ CF ３ , C.F. ２ CH (CH ３ ) ２ , CF(CH ３ )-CH(CH ３ ) ２ ), R ８ -aryl (e.g., CH ２ -Ph), -R ８ -O-R ８ -O-R １０ (For example, (CH ２ ) ２ -O-(CH ２ ) ２ -O-CH ３ ), -R ８ -O-R １０ , -R ８ -R １０ (For example, (CH ２ ) ２ -O-CH ３ ), substituted or unsubstituted aryl (e.g., phenyl), or substituted or unsubstituted heteroaryl (e.g., pyridine (2,3,4-pyridine)); Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH ２ -CH ２ -O-CH ３ , C.H. ２ CF ３ ), C １ -C ５ substituted or unsubstituted straight or branched chain haloalkyl of CH ２ CF ３ , C １ -C ５ straight or branched chain alkoxy (e.g., O—CH ３ ), R ２０ , C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer from 0 to 4 (for example, 1, 2).

2. A compound represented by the following structural formula (Ih): or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical product, or any combination thereof: During the ceremony, Ring F is absent or a substituted or unsubstituted, saturated or unsaturated 4- to 8-membered heterocycle (e.g., pyrrolidine, pyridine, imidazole, pyrimidine, triazole, oxadiazole, pyrazole); R 1 and R 2 are, independently of each other, H, F, Cl, Br, I, OH, SH, or CF 3 ; or R 1 and R 2 are joined together to form a C 3 -C 8 carbocyclic ring (e.g., cyclopropyl); or R 2 and R 4 are joined together to form a ring F as defined above (e.g., pyrrolidine, pyridine, pyrimidine, triazole, oxadiazole, pyrazole); provided that when ring F is aromatic, R 1 and / or R 3 are absent; R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), —R 8 —O—R 10 (e.g., (CH 2 ) 2 —O—CH 3 ), R 8 —N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 —NH(CH 3 )), or substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl); or R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (eg, pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); X 2 , X 3 , and X 4 are each independently a nitrogen atom or CH; X 5 , X 6 , X 8 , and X 9 are each independently a nitrogen atom or a carbon atom; X 10 is N or CH; R 5 is H; R 6 is R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3-10 membered heterocycle) (e.g., (CH 2 ) 3 -piperidine, (CH 2 ) 3 -4-fluoro-piperidine) or R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 ); R 7 ' are each independently H, F, Cl, Br, I, OH, CF 3 , CD 3 , OCD 3 , CN, NO 2 , C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 linear or branched or C 3 -C 8 cyclic haloalkyl (e.g., CHF 2 ), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), or substituted or unsubstituted aryl; each R 8 is independently [CH 2 ] p , where p is 1 to 10; R 10 and R 11 are each independently H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 —CH 2 —O—CH 3 , CH 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, CH 2 CF 3 , C 1 -C 5 straight or branched chain alkoxy (e.g., O—CH 3 ), R 20 , C(O)R, or S(O) 2 R; or R 10 and R 11 are joined together to form a substituted or unsubstituted 3- to 8-membered heterocycle (eg, piperazine, piperidine); In the formula, n is an integer from 0 to 4 (for example, 1, 2).

3. A compound represented by the following structural formula (Ih): or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical product, or any combination thereof: During the ceremony, Ring F is a substituted or unsubstituted, saturated or unsaturated 4- to 8-membered heterocycle (e.g., pyrrolidine, pyridine, imidazole, pyrimidine, triazole, oxadiazole, pyrazole); R 1 is H, F, Cl, Br, I, OH, SH, or CF 3 ; or R 1 and R 2 are joined together to form a C 3 -C 8 carbocyclic ring (e.g., cyclopropyl); or R 2 and R 4 are joined together to form a ring F as defined above (e.g., pyrrolidine, pyridine, pyrimidine, triazole, oxadiazole, pyrazole); provided that when ring F is aromatic, R 1 and / or R 3 are absent; R 3 is H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), —R 8 —O—R 10 (e.g., (CH 2 ) 2 —O—CH 3 ), R 8 —N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 —NH(CH 3 )), or substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl); X 2 , X 3 , and X 4 are each independently a nitrogen atom or CH; X 5 , X 6 , X 8 , and X 9 are each independently a nitrogen atom or a carbon atom; X 10 is N or CH; R 5 is H; R 6 is R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3-10 membered heterocycle) (e.g., (CH 2 ) 3 -piperidine, (CH 2 ) 3 -4-fluoro-piperidine) or R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 ); R 7 ' are each independently H, F, Cl, Br, I, OH, CF 3 , CD 3 , OCD 3 , CN, NO 2 , C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 linear or branched or C 3 -C 8 cyclic haloalkyl (e.g., CHF 2 ), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), or substituted or unsubstituted aryl; each R 8 is independently [CH 2 ] p , where p is 1 to 10; R 10 and R 11 are each independently H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 —CH 2 —O—CH 3 , CH 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, CH 2 CF 3 , C 1 -C 5 straight or branched chain alkoxy (e.g., O—CH 3 ), R 20 , C(O)R, or S(O) 2 R; or R 10 and R 11 are joined together to form a substituted or unsubstituted 3- to 8-membered heterocycle (eg, piperazine, piperidine); In the formula, n is an integer from 0 to 4 (for example, 1, 2).

4. A compound according to any one of claims 1 to 3, R 1 is H; R 3 is H; R 2 and R 4 are joined together to form a pyrrolidine; R 7 ' is H, F, Cl, or CHF 2 ; R 6 is (CH 2 ) 3 -piperidine, (CH 2 ) 3 -4-fluoro-piperidine, or (CH 2 ) 3 -N(CH 2 CH 3 ) 2 ; or any combination thereof.

5. A compound represented by the following structural formula (Ih): or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical, or any combination thereof: During the ceremony, The F ring is absent; R 1 and R 2 are, independently of each other, H, F, Cl, Br, I, OH, SH, or CF 3 ; or R 1 and R 2 are joined together to form a C 3 -C 8 carbocyclic ring (e.g., cyclopropyl); R 3 and R 4 are each independently H, Me, substituted or unsubstituted C 1 -C 5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), —R 8 —O—R 10 (e.g., (CH 2 ) 2 —O—CH 3 ), R 8 —N(R 10 )(R 11 ) (e.g., (CH 2 ) 2 —NH(CH 3 )), or substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl); or R 3 and R 4 are bonded to each other to form a 3- to 8-membered heterocycle (eg, pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); X 2 , X 3 , and X 4 are each independently a nitrogen atom or CH; X 5 , X 6 , X 8 , and X 9 are each independently a nitrogen atom or a carbon atom; X 10 is N or CH; R 5 is H; R 6 is R 8 -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3-10 membered heterocycle) (e.g., (CH 2 ) 3 -piperidine, (CH 2 ) 3 -4-fluoro-piperidine) or R 8 -N(R 10 )(R 11 ) (e.g., (CH 2 ) 3 -N(CH 2 CH 3 ) 2 ); R 7 ' are each independently H, F, Cl, Br, I, OH, CF 3 , CD 3 , OCD 3 , CN, NO 2 , C 1 -C 5 linear or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C 1 -C 5 linear or branched or C 3 -C 8 cyclic haloalkyl (e.g., CHF 2 ), substituted or unsubstituted C 3 -C 8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 3- to 8-membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, imidazole, piperazine, piperidine, dioxazole, 2-oxopyrrolidine), or substituted or unsubstituted aryl; each R 8 is independently [CH 2 ] p , where p is 1 to 10; R 10 and R 11 are each independently H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl (e.g., methyl, ethyl, CH 2 —CH 2 —O—CH 3 , CH 2 CF 3 ), C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, CH 2 CF 3 , C 1 -C 5 straight or branched chain alkoxy (e.g., O—CH 3 ), R 20 , C(O)R, or S(O) 2 R; or R 10 and R 11 are joined together to form a substituted or unsubstituted 3- to 8-membered heterocycle (eg, piperazine, piperidine); In the formula, n is an integer from 0 to 4 (for example, 1, 2).

6. 10. A compound according to claim 1, 2 or 5, R １ is H; R ３ is H; R ２ is H and R ４ is H or cyclopropyl; R ７ ' is H, F, Cl, or CHF ２ is; R ６ is (CH ２ ) ３ -piperidine, (CH ２ ) ３ -4-fluoro-piperidine, or (CH ２ ) ３ -N(CH ２ CH ３ ) ２ is; or any combination thereof.

7. A compound according to any one of claims 1 to 6, The compound is a substantially pure single stereoisomer.

8. The compound of claim 1 or 2, A compound represented by any of the structural formulas in the table below.

9. A compound represented by the following structural formula (Ig): or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), pharmaceutical, or any combination thereof: During the ceremony, X 2 , X 3 , and X 4 are each independently a nitrogen atom or CH; X 5 , X 6 , X 8 , and X 9 are each independently a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 100 is a C 1 -C 5 linear or branched substituted or unsubstituted alkyl, R 8 —OH, —R 8 —O—R 10 , R 8 —N(R 10 )(R 11 ), R 20 , or a substituted or unsubstituted 3- to 8-membered heterocycle; R 5 is H or C 1 -C 5 straight or branched chain alkyl; R 6 is F, Cl, Br, I, OH, SH, R 8 —OH, R 8 —SH, —R 8 —O—R 10 , R 8 —NHC(O)—R 10 , —O—R 8 —R 10 , R 8 —(substituted or unsubstituted C 3 -C 8 cycloalkyl), R 8 —(substituted or unsubstituted 3- to 8-membered monocyclic or spiro heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , —CH 2 CN, —R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 —N(R 10 )(R 11 ), R 8 -C(O)N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)O-R 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 linear or branched C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11), CH(CF 3 )(NH—R 10 ), C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain substituted or unsubstituted alkenyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic alkoxy (optionally at least one methylene group (CH 2 ) in the alkoxy is replaced with an oxygen atom), C 1 -C 5 straight or branched chain thioalkoxy, C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 straight or branched chain alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, a substituted or unsubstituted 3- to 8-membered heterocycle, a substituted or unsubstituted aryl, a substituted or unsubstituted R 8 -aryl, or a substituted or unsubstituted benzyl; or R 6 and R 5 are joined together to form a substituted or unsubstituted 5- to 8-membered heterocycle; Alternatively, R 6 is represented by the following structural formula C: During the ceremony, k, 1 to 4; R 12 and R 13 are each independently H, C 1 -C 5 linear or branched, substituted or unsubstituted alkyl, or R 20 ; or R 12 and R 13 are bonded to each other to form a substituted or unsubstituted 4- to 7-membered heterocycle; Alternatively, R 6 is represented by the following structural formula Bi: m is 0 or 1; R 12 is R 20 or C 1 -C 5 C(O)-alkyl and R 13 is R 30 ; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are, independently of each other, H or substituted or unsubstituted C 1 -C 5 alkyl; Or, R 12 and C3 are bonded together to form ring A, and R 13 is R 30 ; Or, R 12 and R 13 are bonded together to form ring B; Or, R 12 and C1 are bonded together to form a C ring, and R 13 is R 30 ; Or, C1 and C3 are joined together to form a D ring, and R 12 and R 13 are each independently R 30 ; or R 13 and C2 are joined together to form an E ring, m is 1, and R 12 is R 30 ; or R 12 and R 13 are bonded together to form ring B, and C1 and C3 are bonded together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl; R 7 ' is H, F, Cl, Br, I, OH, O-R 20 , SH, R 8 -OH, R 8 -SH, -R 8 -O-R 10 , R 8 -(C 3 -C 8 cycloalkyl), R 8 -(3- to 8-membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)O-R 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 linear or branched C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain substituted or unsubstituted alkenyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic haloalkyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic alkoxy (optionally, at least one methylene group (CH 2 ) in the alkoxy is replaced with an oxygen atom), C 1 -C 5 straight or branched chain thioalkoxy, C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 straight or branched chain alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 20 is represented by the following structural formula: R 30 is H, R 20 , F, Cl, Br, I, OH, SH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain alkoxy, C 1 -C 5 straight or branched chain haloalkyl, R 8 -aryl, -R 8 -O-R 8 -O-R 10 , -R 8 -O-R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain alkoxy, C 1 -C 5 straight or branched chain haloalkyl, R 8 -aryl, -R 8 -O-R 8 -O-R 10 , -R 8 -O-R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; each R 8 is independently [CH 2 ] p , where p is 1 to 10; R 9 is [CH] q or [C] q , where q is 2 to 10; R 10 and R 11 are each independently H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl, C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, C 1 -C 5 straight or branched chain alkoxy, R 20 , C(O)R, or S(O) 2 R; or R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle; wherein n is an integer from 0 to 4; At least one of X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , and X 9 is N; or A compound represented by structural formula (Ig) below, or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X 2 , X 3 , and X 4 are each independently a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are each independently a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 100 is a C 1 -C 5 linear or branched substituted or unsubstituted alkyl, R 8 —OH, —R 8 —O—R 10 , R 8 —N(R 10 )(R 11 ), R 20 , or a substituted or unsubstituted 3- to 8-membered heterocycle; R 5 is H or C 1 -C 5 straight or branched chain alkyl; R 6 is F, Cl, Br, I, OH, SH, R 8 —OH, R 8 —SH, —R 8 —O—R 10 , R 8 —NHC(O)—R 10 , —O—R 8 —R 10 , R 8 —(substituted or unsubstituted C 3 -C 8 cycloalkyl), R 8 —(substituted or unsubstituted 3- to 8-membered monocyclic or spiro heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , —CH 2 CN, —R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 —N(R 10 )(R 11 ), R 8 -C(O)N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)O-R 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 linear or branched C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11), CH(CF 3 )(NH—R 10 ), C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain substituted or unsubstituted alkenyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic alkoxy (optionally at least one methylene group (CH 2 ) in the alkoxy is replaced with an oxygen atom), C 1 -C 5 straight or branched chain thioalkoxy, C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 straight or branched chain alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl, or substituted or unsubstituted benzyl; or R 6 and R 5 are joined together to form a substituted or unsubstituted 5- to 8-membered heterocycle; Alternatively, R 6 is represented by the following structural formula C: During the ceremony, k, 1 to 4; R 12 and R 13 are each independently H, C 1 -C 5 linear or branched, substituted or unsubstituted alkyl, or R 20 ; or R 12 and R 13 are bonded to each other to form a substituted or unsubstituted 4- to 7-membered heterocycle; Alternatively, R 6 is represented by the following structural formula Bi: m is 0 or 1; R 12 is R 20 or C 1 -C 5 C(O)-alkyl and R 13 is R 30 ; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are, independently of each other, H or substituted or unsubstituted C 1 -C 5 alkyl; Or, R 12 and C3 are bonded together to form ring A, and R 13 is R 30 ; Or, R 12 and R 13 are bonded together to form ring B; Or, R 12 and C1 are bonded together to form a C ring, and R 13 is R 30 ; Or, C1 and C3 are joined together to form a D ring, and R 12 and R 13 are each independently R 30 ; or R 13 and C2 are joined together to form an E ring, m is 1, and R 12 is R 30 ; or R 12 and R 13 are bonded together to form ring B, and C1 and C3 are bonded together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl; R 7 ' is F, Cl, Br, I, OH, O-R 20 , SH, R 8 -OH, R 8 -SH, -R 8 -O-R 10 , R 8 -(C 3 -C 8 cycloalkyl), R 8 -(3- to 8-membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)O-R 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 straight or branched chain C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain substituted or unsubstituted alkenyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic haloalkyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic alkoxy (optionally, at least one methylene group (CH 2 ) in the alkoxy is replaced with an oxygen atom), C 1 -C 5 straight or branched chain thioalkoxy, C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 straight or branched chain alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 20 is represented by the following structural formula: R 30 is H, R 20 , F, Cl, Br, I, OH, SH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain alkoxy, C 1 -C 5 straight or branched chain haloalkyl, R 8 -aryl, -R 8 -O-R 8 -O-R 10 , -R 8 -O-R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain alkoxy, C 1 -C 5 straight or branched chain haloalkyl, R 8 -aryl, -R 8 -O-R 8 -O-R 10 , -R 8 -O-R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; each R 8 is independently [CH 2 ] p , where p is 1 to 10; R 9 is [CH] q or [C] q , where q is 2 to 10; R 10 and R 11 are each independently H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl, C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, C 1 -C 5 straight or branched chain alkoxy, R 20 , C(O)R, or S(O) 2 R; or R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle; wherein n is an integer from 0 to 4; or A compound represented by structural formula (Ig) below, or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X 2 , X 3 , and X 4 are each independently a nitrogen atom or CH; X 5 , X 6 , X 7 , X 8 , and X 9 are each independently a nitrogen atom or a carbon atom; X 10 is N, CH, or C(R); R 100 is R 8 —OH, —R 8 —O—R 10 , R 8 —N(R 10 )(R 11 ), R 20 , or a substituted or unsubstituted 3- to 8-membered heterocycle; R 5 is H or C 1 -C 5 straight or branched chain alkyl; R 6 is F, Cl, Br, I, OH, SH, R 8 —OH, R 8 —SH, —R 8 —O—R 10 , R 8 —NHC(O)—R 10 , —O—R 8 —R 10 , R 8 —(substituted or unsubstituted C 3 -C 8 cycloalkyl), R 8 —(substituted or unsubstituted 3- to 8-membered monocyclic or spiro heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , —CH 2 CN, —R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 —N(R 10 )(R 11 ), R 8 -C(O)N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)O-R 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 linear or branched C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11), CH(CF 3 )(NH—R 10 ), C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain substituted or unsubstituted alkenyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic haloalkyl, substituted or unsubstituted C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic alkoxy (optionally at least one methylene group (CH 2 ) in the alkoxy is replaced with an oxygen atom), C 1 -C 5 straight or branched chain thioalkoxy, C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 straight or branched chain alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, substituted or unsubstituted R 8 -aryl, or substituted or unsubstituted benzyl; or R 6 and R 5 are joined together to form a substituted or unsubstituted 5- to 8-membered heterocycle; Alternatively, R 6 is represented by the following structural formula C: During the ceremony, k, 1 to 4; R 12 and R 13 are each independently H, C 1 -C 5 linear or branched, substituted or unsubstituted alkyl, or R 20 ; or R 12 and R 13 are bonded to each other to form a substituted or unsubstituted 4- to 7-membered heterocycle; Alternatively, R 6 is represented by the following structural formula Bi: m is 0 or 1; R 12 is R 20 or C 1 -C 5 C(O)-alkyl and R 13 is R 30 ; Or, R 12 and R 13 are both H; Or, R 12 and R 13 are, independently of each other, H or substituted or unsubstituted C 1 -C 5 alkyl; Or, R 12 and C3 are bonded together to form ring A, and R 13 is R 30 ; Or, R 12 and R 13 are bonded together to form ring B; Or, R 12 and C1 are bonded together to form a C ring, and R 13 is R 30 ; Or, C1 and C3 are joined together to form a D ring, and R 12 and R 13 are each independently R 30 ; or R 13 and C2 are joined together to form an E ring, m is 1, and R 12 is R 30 ; or R 12 and R 13 are bonded together to form ring B, and C1 and C3 are bonded together to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring D is a substituted or unsubstituted C 3 -C 8 cycloalkyl; R 7 ' is H, F, Cl, Br, I, OH, O-R 20 , SH, R 8 -OH, R 8 -SH, -R 8 -O-R 10 , R 8 -(C 3 -C 8 cycloalkyl), R 8 -(3- to 8-membered heterocycle), CF 3 , CD 3 , OCD 3 , CN, NO 2 , -CH 2 CN, -R 8 CN, NH 2 , NHR, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), R 8 -N(R 10 )(R 11 ), R 9 -R 8 -N(R 10 )(R 11 ), B(OH) 2 , -OC(O)CF 3 , -OCH 2 Ph, NHC(O)-R 10 , NHCO-N(R 10 )(R 11 ), COOH, -C(O)Ph, C(O)O-R 10 , R 8 -C(O)-R 10 , C(O)H, C(O)-R 10 , C 1 -C 5 linear or branched C(O)-haloalkyl, -C(O)NH 2 , C(O)NHR, C(O)N(R 10 )(R 11 ), SO 2 R, SO 2 N(R 10 )(R 11 ), CH(CF 3 )(NH-R 10 ), C 1 -C 5 linear or branched substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain substituted or unsubstituted alkenyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic haloalkyl, C 1 -C 5 straight or branched chain or C 3 -C 8 cyclic alkoxy (optionally, at least one methylene group (CH 2 ) in the alkoxy is replaced with an oxygen atom), C 1 -C 5 straight or branched chain thioalkoxy, C 1 -C 5 straight or branched chain haloalkoxy, C 1 -C 5 straight or branched chain alkoxyalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 20 is represented by the following structural formula: R 30 is H, R 20 , F, Cl, Br, I, OH, SH, alkoxy, N(R) 2 , NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain alkoxy, C 1 -C 5 straight or branched chain haloalkyl, R 8 -aryl, -R 8 -O-R 8 -O-R 10 , -R 8 -O-R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R 10 ), N(R 10 )(R 11 ), CF 3 , CN, NO 2 , C 1 -C 5 straight or branched chain substituted or unsubstituted alkyl, C 1 -C 5 straight or branched chain alkoxy, C 1 -C 5 straight or branched chain haloalkyl, R 8 -aryl, -R 8 -O-R 8 -O-R 10 , -R 8 -O-R 10 , -R 8 -R 10 , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; each R 8 is independently [CH 2 ] p , where p is 1 to 10; R 9 is [CH] q or [C] q , where q is 2 to 10; R 10 and R 11 are each independently H, C 1 -C 5 substituted or unsubstituted straight or branched chain alkyl, C 1 -C 5 substituted or unsubstituted straight or branched chain haloalkyl, C 1 -C 5 straight or branched chain alkoxy, R 20 , C(O)R, or S(O) 2 R; or R 10 and R 11 are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle; In the formula, n is an integer of 0 to 4.

10. The compound of claim 9, R 100 is methyl; R 5 is H; R 6 is a substituted or unsubstituted 3- to 8-membered monocyclic, fused, or spiro-heterocycle, R 8 -(substituted or unsubstituted 3- to 8-membered monocyclic, fused, or spiro-heterocycle), substituted or unsubstituted C 3 -C 8 cycloalkyl, R 8 -(substituted or unsubstituted C 3 -C 8 cycloalkyl), or R 8 -N(R 10 )(R 11 ); R 7 ' is H or F; or any combination thereof.

11. The compound of claim 9, A compound represented by any of the structural formulas in the table below.

12. A compound represented by the following structural formula (Ia): or a pharmaceutically acceptable salt, optical isomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X ５ , X ６ , X ７ , X ８ , and X ９ are, independently of each other, a nitrogen atom or a carbon atom; X １０ is N, CH, or C(R); R ５ is H or C １ -C ５ is a straight or branched chain alkyl; R ６ are H, F, Cl, Br, I, OH, SH, and R ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -S-R １０ , (CH ２ ) ３ -S-(CH ２ ) ２ CH ３ , R ８ -NHC(O)-R １０ , -O-R ８ -R １０ , R ８ -(substituted or unsubstituted C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), (CH ２ ) ３ -N(CH ２ CH ３ ) ２ , (CH ２ ) ３ -NH ２ , (CH ２ ) ３ -N(CH ２ CH ３ ) (CH ２ CF ３ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of the formula C １ -C ５ or C ３ -C ８ cyclic haloalkyl, substituted or unsubstituted C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, substituted or unsubstituted R ８ -aryl or substituted or unsubstituted benzyl; Or, R ６ is represented by the following structural formula Bi: During the ceremony, m is 0 or 1; R １２ is R ２０ , or C １ -C ５ and R １３ is R ３０ is; Or, R １２ and R １３ are both H; Or, R １２ and R １３ are each independently H or substituted or unsubstituted C １ -C ５ is an alkyl of Or, R １２ and C3 are bonded to each other to form ring A, and R １３ is R ３０ is; Or, R １２ and R １３ are bonded together to form ring B; Or, R １２ and C1 are bonded to each other to form a C ring, and R １３ is R ３０ is; Alternatively, C1 and C3 are bonded together to form a D ring, and R １２ and R １３ are each independently R ３０ is; Or, R １３ and C2 are bonded to each other to form an E ring, m is 1, and R １２ is R ３０ is; Or, R １２ and R １３ are bonded to each other to form ring B, and C1 and C3 are bonded to each other to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; The D ring is a substituted or unsubstituted C ３ -C ８ is a cycloalkyl of the formula: Or, R ６ and R ５ are bonded to each other to form a substituted or unsubstituted 5- to 8-membered heterocycle; R ７ is O-R ２０ , a substituted or unsubstituted 4- to 7-membered heterocycle (pyrrolidine), a substituted or unsubstituted aryl, or R ８ -(substituted or unsubstituted saturated monocyclic, fused or spirocyclic 3- to 8-membered heterocycle); Or, R ７ is represented by the following structural formula A: During the ceremony, X １ is N or O; R １ and R ２ are, independently of one another, H, F, or CF ３ is; Or, R １ and R ２ are bonded to each other to form C ３ -C ８ forming a carbocyclic or heterocyclic ring of the formula: R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, cyclopropyl, substituted or unsubstituted 5- to 7-membered heterocycle, or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle; However, X １ is O, then R ４ does not exist; R ７ ' is H, F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(3- to 8-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , -OCH ２ Ph, COOH, C(O)H, -C(O)NH ２ , S.O. ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched chain substituted or unsubstituted alkyl, methyl, C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl, CHF ２ , C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, cyclopropyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; Or, R ７ and R ７ ' are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R ２０ is represented by the following structural formula: R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R ３０ is H, R ２０ , F, Cl, Br, I, OH, SH, alkoxy, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched alkyl, methyl, C １ -C ５ substituted or unsubstituted straight or branched chain haloalkyl of CH ２ CF ３ , C １ -C ５ linear or branched alkoxy of R ２０ , C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle; where n is an integer from 0 to 4 (e.g., 1, 2), or A compound represented by the following structural formula (Ib): or a pharmaceutically acceptable salt, optical isomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X ５ , X ６ , X ７ , X ８ , and X ９ are, independently of each other, a nitrogen atom or a carbon atom; X １０ is N, CH, or C(R); R ６ is -R ８ -O-R １０ , R ８ -S-R １０ , R ８ -(substituted or unsubstituted C ３ -C ８ cycloalkyl), (CH ２ ) ３ -Piran, CH ２ -Tetrahydrofuran, CH ２ -Dioxane, CH ２ -methyl-THF, CH ２ -oxa-azaspirodecane, CH ２ -Azaspiroheptane, (CH ２ ) ３ -dimethylpyrazole, CH ２ -methyl-azetidine, benzyl, or C １ -C ５ is a straight or branched chain alkoxyalkyl; Or, R ６ is represented by the following structural formula Bi: During the ceremony, m is 0 or 1; R １２ is R ２０ , or C １ -C ５ and R １３ is R ３０ is; Or, R １２ and R １３ are both H; Or, R １２ and C3 are bonded to each other to form ring A, and R １３ is R ３０ is; Or, R １２ and R １３ are joined together to form a substituted or unsubstituted pyrrolidine ring, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, pyrazole, imidazole, 2,5-diazabicyclo[2.2.1]heptane, or diazabicyclo[2.2.1]heptane; Or, R １２ and C1 are bonded to each other to form a C ring, and R １３ is R ３０ is; Alternatively, C1 and C3 are bonded together to form a D ring, and R １２ and R １３ are each independently R ３０ is; Or, R １３ and C2 are bonded to each other to form an E ring, m is 1, and R １２ is R ３０ is; Or, R １２ and R １３ are bonded to each other to form ring B, ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring, and C1 and C3 are bonded to each other to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; The D ring is a substituted or unsubstituted C ３ -C ８ is a cycloalkyl of the formula: R ７ is F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH,SR １０ , -R ８ -O-R １０ , -R ８ -S-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted monocyclic, fused or spirocyclic 3- to 8-membered heterocyclic ring), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , -OCH ２ Ph, COOH, C(O)H, -C(O)NH ２ , S.O. ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C ２ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkyl of C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 4- to 7-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ is represented by the following structural formula A: During the ceremony, X １ is N or O; R １ and R ２ are, independently of one another, H, F, or CF ３ is; Or, R １ and R ２ are bonded to each other to form C ３ -C ８ forming a carbocyclic or heterocyclic ring of the formula: R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl, substituted or unsubstituted C ３ -C ８ a cycloalkyl, a substituted or unsubstituted 5- to 7-membered heterocycle, or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle; However, X １ is O, then R ４ does not exist; R ７ ' is H, F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(3- to 8-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , -OCH ２ Ph, COOH, C(O)H, -C(O)NH ２ , S.O. ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 3- to 8-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ and R ７ ' are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R ２０ is represented by the following structural formula: R ３０ is H, R ２０ , F, Cl, Br, I, OH, SH, alkoxy, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ straight or branched chain haloalkyl of -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched alkyl, methyl, CH ２ CF ３ , C １ -C ５ straight or branched chain alkoxy, C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle; where n is an integer from 0 to 4 (e.g., 1, 2), or A compound represented by the following structural formula (Ic): or a pharmaceutically acceptable salt, optical isomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X ５ , X ６ , X ７ , X ８ , and X ９ are, independently of each other, a nitrogen atom or a carbon atom; X １０ is N, CH, or C(R); R ５ is H or C １ -C ５ is a straight or branched chain alkyl (e.g., methyl); R ６ are H, F, Cl, Br, I, OH, SH, and R ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -S-R １０ , (CH ２ ) ３ -S-(CH ２ ) ２ CH ３ , R ８ -NHC(O)-R １０ , -O-R ８ -R １０ , R ８ -(substituted or unsubstituted C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), (CH ２ ) ３ -N(CH ２ CH ３ ) ２ , (CH ２ ) ３ -NH ２ , (CH ２ ) ３ -N(CH ２ CH ３ ) (CH ２ CF ３ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of the formula C １ -C ５ or C ３ -C ８ cyclic haloalkyl, substituted or unsubstituted C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, substituted or unsubstituted R ８ -aryl or substituted or unsubstituted benzyl; Or, R ６ is represented by the following structural formula B: During the ceremony, m is 0 or 1; R １２ is R ２０ , or C １ -C ５ and R １３ is R ３０ is; Or, R １２ and R １３ are both H; Or, R １２ and R １３ are each independently H or substituted or unsubstituted C １ -C ５ is an alkyl of Or, R １２ and C3 are bonded to each other to form ring A, and R １３ is R ３０ is; Or, R １２ and R １３ are bonded together to form ring B; Or, R １２ and C1 are bonded to each other to form a C ring, and R １３ is R ３０ is; Alternatively, C1 and C3 are bonded together to form a D ring, and R １２ and R １３ are each independently R ３０ is; Or, R １３ and C2 are bonded to each other to form an E ring, m is 1, and R １２ is R ３０ is; Or, R １２ and R １３ are bonded to each other to form ring B, and C1 and C3 are bonded to each other to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; The D ring is a substituted or unsubstituted C ３ -C ８ is a cycloalkyl of the formula: Or, R ６ and R ５ are bonded to each other to form a substituted or unsubstituted 5- to 8-membered heterocycle; R ７ is Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH,SR １０ , -R ８ -O-R １０ , -R ８ -S-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted monocyclic, fused or spirocyclic 3- to 8-membered heterocyclic ring), CF ３ , CDs ３ , OCD ３ , CN, -CH ２ CN, -R ８ CN, NHR, N(R) ２ , R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , -OCH ２ Ph, COOH, C(O)H, -C(O)NH ２ , S.O. ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ a straight or branched chain thioalkyl of C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 4- to 7-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ is represented by the following structural formula A: During the ceremony, X １ is N or O; R １ and R ２ are, independently of one another, H, F, or CF ３ is; Or, R １ and R ２ are bonded to each other to form C ３ -C ８ forming a carbocyclic or heterocyclic ring of the formula: R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl, substituted or unsubstituted C ３ -C ８ a cycloalkyl, a substituted or unsubstituted 5- to 7-membered heterocycle, or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle; However, X １ is O, then R ４ does not exist; R ７ ' is F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(3- to 8-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , -OCH ２ Ph, COOH, C(O)H, -C(O)NH ２ , S.O. ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 3- to 8-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ and R ７ ' are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; However, R ７ ´ is R ７ is different from; R ２０ is represented by the following structural formula: R ３０ is H, R ２０ , F, Cl, Br, I, OH, SH, alkoxy, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched alkyl, methyl, CH ２ CF ３ , C １ -C ５ straight or branched chain alkoxy, C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle; where n is an integer from 0 to 4 (e.g., 1, 2), or A compound represented by the following structural formula (Id): or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X ５ , X ６ , X ７ , X ８ , and X ９ are, independently of each other, a nitrogen atom or a carbon atom; X １０ is N, CH, or C(R); X ２ , X ３ , X ４ , X ５ , X ６ , X ７ , X ８ , X ９ , and X １０ at least one of is N; R ５ is H or C １ -C ５ is a straight or branched chain alkyl (e.g., methyl); R ６ are H, F, Cl, Br, I, OH, SH, and R ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -S-R １０ , (CH ２ ) ３ -S-(CH ２ ) ２ CH ３ , R ８ -NHC(O)-R １０ , -O-R ８ -R １０ , R 8 —(substituted or unsubstituted C 3 -C 8 cycloalkyl), R ８ -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), (CH ２ ) ３ -N(CH ２ CH ３ ) ２ , (CH ２ ) ３ -NH ２ , (CH ２ ) ３ -N(CH ２ CH ３ ) (CH ２ CF ３ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of the formula C １ -C ５ or C ３ -C ８ cyclic haloalkyl, substituted or unsubstituted C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, substituted or unsubstituted R ８ -aryl or substituted or unsubstituted benzyl; Or, R ６ is represented by the following structural formula Bi: During the ceremony, m is 0 or 1; R １２ is R ２０ , or C １ -C ５ and R １３ is R ３０ is; Or, R １２ and R １３ are both H; Or, R １２ and R １３ are each independently H or substituted or unsubstituted C １ -C ５ is an alkyl of Or, R １２ and C3 are bonded to each other to form ring A, and R １３ is R ３０ is; Or, R １２ and R １３ are bonded together to form ring B; Or, R １２ and C1 are bonded to each other to form a C ring, and R １３ is R ３０ is; Alternatively, C1 and C3 are bonded together to form a D ring, and R １２ and R １３ are each independently R ３０ is; Or, R １３ and C2 are bonded to each other to form an E ring, m is 1, and R １２ is R ３０ is; Or, R １２ and R １３ are bonded to each other to form ring B, and C1 and C3 are bonded to each other to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; The D ring is a substituted or unsubstituted C ３ -C ８ is a cycloalkyl of the formula: Or, R ６ and R ５ are bonded to each other to form a substituted or unsubstituted 5- to 8-membered heterocycle; R ７ is H, F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH,SR １０ , -R ８ -O-R １０ , -R ８ -S-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted monocyclic, fused or spirocyclic 3- to 8-membered heterocyclic ring), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkyl of C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 4- to 7-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ is represented by the following structural formula A: During the ceremony, X １ is N or O; R １ and R ２ are, independently of one another, H, F, or CF ３ is; Or, R １ and R ２ are bonded to each other to form ═O or C ３ -C ８ forming a carbocyclic or heterocyclic ring of the formula: R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl, substituted or unsubstituted C ３ -C ８ a cycloalkyl, a substituted or unsubstituted 5- to 7-membered heterocycle, or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle; However, X １ is O, then R ４ does not exist; R ７ ' is H, F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(3- to 8-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 3- to 8-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ and R ７ ' are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R ２０ is represented by the following structural formula: R ３０ is H, R ２０ , F, Cl, Br, I, OH, SH, alkoxy, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched alkyl, methyl, CH ２ CF ３ , C １ -C ５ straight or branched chain alkoxy, C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); where n is an integer from 0 to 4 (e.g., 1, 2), or A compound represented by structural formula (Ie): or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X ５ , X ６ , X ７ , X ８ , and X ９ are, independently of each other, a nitrogen atom or a carbon atom; X １０ is N, CH, or C(R); R ５ and R ６ are bonded to each other to form a substituted or unsubstituted 5- to 7-membered heterocycle; R ７ is H, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH,SR １０ , -R ８ -O-R １０ , -R ８ -S-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted monocyclic, fused or spirocyclic 3- to 8-membered heterocyclic ring), CF ３ , CDs ３ , OCD ３ , CN, -CH ２ CN, -R ８ C.N., R. ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , -OCH ２ Ph, COOH, C(O)H, -C(O)NH ２ , S.O. ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C ２ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ Branched chain or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkyl of C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 4- to 7-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ is represented by the following structural formula A: During the ceremony, X １ is N or O; R １ and R ２ are, independently of one another, H, F, or CF ３ is; Or, R １ and R ２ are bonded to each other to form C ３ -C ８ forming a carbocyclic or heterocyclic ring of the formula: R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl, substituted or unsubstituted C ３ -C ８ a cycloalkyl, a substituted or unsubstituted 5- to 7-membered heterocycle, or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle; However, X １ is O, then R ４ does not exist; R ７ ' is H; Or, R ７ and R ７ ' are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R ２０ is represented by the following structural formula: R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched alkyl, methyl, CH ２ CF ３ , C １ -C ５ straight or branched chain alkoxy, C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer from 0 to 4 (for example, 1, 2).

13. 13. The compound of claim 12, A compound represented by any of the structural formulas in the table below.

14. A compound represented by the following structural formula (If): or a pharmaceutically acceptable salt, optical isomer, tautomer, hydrate, N-oxide, reverse amide analog, isotopic variant (e.g., deuterated analog), pharmaceutical agent, or any combination thereof: During the ceremony, A' is a 3- to 8-membered monocyclic or fused saturated, unsaturated or aromatic heterocyclic ring; X ２ , X ３ , and X ４ are, independently of each other, a nitrogen atom or CH; X １０ is N, CH, or C(R); R ５ is H or C １ -C ５ is a straight or branched chain alkyl; R ６ are H, F, Cl, Br, I, OH, SH, and R ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -S-R １０ , (CH ２ ) ３ -S-(CH ２ ) ２ CH ３ , R ８ -NHC(O)-R １０ , -O-R ８ -R １０ , R ８ -(substituted or unsubstituted C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted saturated, unsaturated or aromatic monocyclic, fused or spirocyclic 3- to 10-membered heterocycle), CF ３ , CDs ３ , OCD ３ , C.N., N.O. ２ , -CH ２ CN, -R ８ C.N., N.H. ２ , NHR, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), R ８ -N(R １０ ) (R １１ ), (CH ２ ) ３ -N(CH ２ CH ３ ) ２ , (CH ２ ) ３ -NH ２ , (CH ２ ) ３ -N(CH ２ CH ３ ) (CH ２ CF ３ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl, substituted or unsubstituted C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, substituted or unsubstituted 3- to 8-membered heterocycle, substituted or unsubstituted aryl, substituted or unsubstituted R ８ -aryl or substituted or unsubstituted benzyl; Or, R ６ is represented by the following structural formula B: During the ceremony, m is 0 or 1; R １２ is R ２０ , or C １ -C ５ and R １３ is R ３０ is; Or, R １２ and R １３ are both H; Or, R １２ and R １３ are each independently H or substituted or unsubstituted C １ -C ５ is an alkyl of Or, R １２ and C3 are bonded to each other to form ring A, and R １３ is R ３０ is; Or, R １２ and R １３ are bonded together to form ring B; Or, R １２ and C1 are bonded to each other to form a C ring, and R １３ is R ３０ is; Alternatively, C1 and C3 are bonded together to form a D ring, and R １２ and R １３ are each independently R ３０ is; Or, R １３ and C2 are bonded to each other to form an E ring, m is 1, and R １２ is R ３０ is; Or, R １２ and R １３ are bonded to each other to form ring B, and C1 and C3 are bonded to each other to form ring D; Ring A, ring C and ring E are each independently a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; Ring B is a substituted or unsubstituted monocyclic, spirocyclic or fused 3- to 8-membered heterocyclic ring; The D ring is a substituted or unsubstituted C ３ -C ８ is a cycloalkyl of the formula: Or, R ６ and R ５ are bonded to each other to form a substituted or unsubstituted 5- to 8-membered heterocycle; R ７ is H, F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH,SR １０ , -R ８ -O-R １０ , -R ８ -S-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(substituted or unsubstituted monocyclic, fused or spirocyclic 3- to 8-membered heterocyclic ring), CF ３ , CDs ３ , OCD ３ , CN, -CH ２ CN, -R ８ C.N., R. ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkyl of C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 4- to 7-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ is represented by the following structural formula A: During the ceremony, X １ is N or O; R １ and R ２ are, independently of one another, H, F, or CF ３ is; Or, R １ and R ２ are bonded to each other to form ═O or C ３ -C ８ forming a carbocyclic or heterocyclic ring of the formula: R ３ and R ４ are each independently H, Me, substituted or unsubstituted C １ -C ５ alkyl, substituted or unsubstituted C ３ -C ８ a cycloalkyl, a substituted or unsubstituted 5- to 7-membered heterocycle, or R ２０ is; Or, R ３ and R ４ are bonded to each other to form a 3- to 8-membered heterocycle; However, X １ is O, then R ４ does not exist; R ７ ' is H, F, Cl, Br, I, OH, O-R ２０ , S.H., R. ８ -OH, R ８ -SH, -R ８ -O-R １０ , R ８ -(C ３ -C ８ cycloalkyl), R ８ -(3- to 8-membered heterocycle), CF ３ , CDs ３ , OCD ３ , CN, -CH ２ CN, -R ８ C.N., R. ８ -N(R １０ ) (R １１ ), R ９ -R ８ -N(R １０ ) (R １１ ), B(OH) ２ , —OC(O)CF ３ , -OCH ２ Ph, NHC(O)-R １０ , NHCO-N(R １０ ) (R １１ ), COOH, -C(O)Ph, C(O)OR １０ , R ８ -C(O)-R １０ , C(O)H, C(O)-R １０ , C １ -C ５ straight or branched chain C(O)-haloalkyl, —C(O)NH ２ , C(O)NHR, C(O)N(R １０ ) (R １１ ), SO ２ R, SO ２ N (R １０ ) (R １１ ), CH(CF ３ ) (NH-R １０ ), C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ a straight or branched chain substituted or unsubstituted alkenyl of C １ -C ５ or C ３ -C ８ cyclic haloalkyl of C １ -C ５ or C ３ -C ８ cyclic alkoxy (optionally, at least one methylene group (CH ２ ) is substituted with an oxygen atom), C １ -C ５ a straight or branched chain thioalkoxy of C １ -C ５ straight or branched chain haloalkoxy of C １ -C ５ linear or branched alkoxyalkyl, substituted or unsubstituted C ３ -C ８ cycloalkyl, a substituted or unsubstituted 3- to 8-membered heterocycle, a substituted or unsubstituted aryl, or a substituted or unsubstituted benzyl; Or, R ７ and R ７ ' are joined together to form a 5- or 6-membered, substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring; R ２０ is represented by the following structural formula: R ３０ is H, R ２０ , F, Cl, Br, I, OH, SH, alkoxy, N(R) ２ , NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R １０ ), N(R １０ ) (R １１ ), CF ３ , C.N., N.O. ２ , C １ -C ５ linear or branched, substituted or unsubstituted alkyl of C １ -C ５ linear or branched alkoxy of C １ -C ５ a straight or branched chain haloalkyl of R ８ -aryl, -R ８ -O-R ８ -O-R １０ , -R ８ -O-R １０ , -R ８ -R １０ , substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Each R ８ are each independently [CH ２ ] ｐ and p is 1 to 10; R ９ is [CH] ｑ , or [C] ｑ and q is 2 to 10; R １０ and R １１ are, independently of each other, H, C １ -C ５ substituted or unsubstituted straight or branched alkyl, methyl, CH ２ CF ３ , C １ -C ５ straight or branched chain alkoxy, C(O)R, or S(O) ２ It is R; Or, R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle (e.g., piperazine, piperidine); In the formula, n is an integer from 0 to 4 (for example, 1, 2).

15. 13. The compound of claim 12, R ６ is a compound represented by the structural formula Bi.

16. 16. The compound of claim 15, R １２ and R １３ are bonded to each other to form a pyrrolidine ring or a substituted or unsubstituted piperidine ring; C ３ and R １２ are linked together to form a pyrrolidine (A ring); or C ２ and R １３ are bonded to each other to form a piperidine (E ring).

17. A compound according to any one of claims 12 and 14 to 16, R ７ is a compound represented by structural formula A.

18. 18. The compound of claim 17, R １ is H; R ２ is H or CF ３ or R １ and R ２ are joined together to form a cyclopropyl; X １ is N; R ３ is H; R ４ is H or cycloalkyl.

19. 13. The compound of claim 12, R ７ If there is a ７ is C(O)N(R １０ ) (R １１ ), preferably C(O)N(H)(CH ３ ) a compound.

20. 19. A compound according to any one of claims 12, 14, 15, 17, and 18, R ７ is CH ２ -NH ２ A compound.

21. A compound according to any one of claims 1 to 20, R ７ ' is H or F.

22. A compound according to any one of claims 1 to 6, 12, 14, and 17 to 21, R ５ is H and R ６ is R ８ -N(R １０ ) (R １１ ) is; Preferably, R ８ is (CH ２ CH ２ CH ２ ) and R １０ and R １１ are bonded to each other to form a substituted or unsubstituted 3- to 8-membered heterocycle, preferably piperidine, or C １ -C ５ The compound forms an unsubstituted straight chain alkyl, preferably ethyl, of the formula:

23. 15. The compound of claim 14, A compound represented by any of the structural formulas in the table below.

24. A compound represented by any of the structural formulas in the table below.

25. A compound according to any one of claims 1 to 24, The compound is a c-MYC mRNA translation regulator, a c-MYC mRNA transcription regulator, a c-MYC inhibitor, or any combination thereof.

26. A compound according to any one of claims 1 to 25; and a pharmaceutically acceptable carrier.

27. Use of a compound according to any one of claims 1 to 25 or a pharmaceutical composition according to claim 26 for the manufacture of a medicament for treating, suppressing, reducing the severity of, reducing the risk of developing, or inhibiting cancer.

28. 28. The use according to claim 27, The cancer is selected from the group consisting of breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's lymphoma, Burkitt's lymphoma, diffuse large B-cell lymphoma, prostate cancer, colon cancer, gastric cancer, primary central nervous system lymphoma, glioblastoma, medulloblastoma, melanoma, non-small cell lung cancer, germinal center-derived lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, lung adenocarcinoma, BRAFV600E thyroid cancer, choroid plexus carcinoma, colitis-associated cancer, epithelial ovarian cancer, colorectal cancer, pancreatic cancer, and uterine cancer.

29. 29. The use according to claim 27 or 28, The use, wherein the cancer is early stage cancer, advanced cancer, invasive cancer, metastatic cancer, drug-resistant cancer, or any combination thereof.

30. Use according to any one of claims 27 to 29, The use, wherein the subject has previously been treated with chemotherapy, immunotherapy, radiation therapy, biological therapy, surgical intervention, or any combination thereof.

31. Use according to any one of claims 27 to 30, The compound is administered in combination with an anti-cancer therapy.

32. 32. The use according to claim 31 , The use, wherein the anti-cancer therapy is chemotherapy, immunotherapy, radiation therapy, biological therapy, surgical intervention, or any combination thereof.

33. Use of a compound according to any one of claims 1 to 25 or a pharmaceutical composition according to claim 26 for the manufacture of a medicament for suppressing, reducing or inhibiting tumor growth.

34. 1. A method for modulating c-MYC mRNA translation in a cell, comprising:

26. A method comprising contacting a cell with a compound according to any one of claims 1 to 25, thereby modulating c-MYC mRNA translation in said cell.

35. 1. A method for modulating c-MYC mRNA transcription in a cell, comprising:

26. A method comprising contacting a cell with a compound according to any one of claims 1 to 25, thereby modulating c-MYC mRNA transcription in the cell.

36. 36. The method of claim 34 or 35, The method comprises: by modulating c-MYC mRNA splicing (inclusion or exclusion of untranslated regions or alternative exon usage); This is done by regulating c-MYC mRNA modification; This is done by modulating the interaction of RNA-binding proteins with c-MYC mRNA, thereby altering mRNA localization; This is done by regulating the localization of c-MYC mRNA in the cytoplasm; by regulating ribosomes and ribosomal cofactors on c-MYC mRNA; This is done by reducing the amount of c-MYC protein in the cell; Or any combination thereof.

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